FormualtionHandbook 12-2007

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A Guide for R+D

FORMULATIONHANDBOOK

Rev. December/2007


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FORMULATIONHANDBOOK

Table of Contents

JRS PHARMA LP

Customer Service:

JRS PHARMAGMBH+CO.KG2981 Route 22, Suite 1Patterson, NY 12563-2359

Toll-Free: (800) 431-2457Phone: +1 (845) 878-3414Fax: +1 (845) 878-3484E-mail: [email protected]

Holzmhle 1D-73494 Rosenberg (Germany)Phone: + 49 (0) 79 67 / 1 52-0Fax: + 49 (0) 79 67 / 1 52-345E-mail: [email protected]

WORLDWIDE HEADQUARTERS

Customer Service: +49 (0) 7967 / 152-312

USA + CANADA

+1 (845) 878-3414

Page 1/2

Table of Contents Page 02

Introduction Page 04

Excipients Page 05

Table of Contents Guide Formulations Page 08

Acetylsalicylic Acid (High Dosage) [No. 4282-001] Page 11

Acetylsalicylic Acid (Effervescent) [No. 4282-023] Page 13

Acetylsalicylic Acid (OD Tablets) [No. 4282-029] Page 15

Allopurinol [No. 4282-002] Page 16

Ambroxol Hcl [No. 4282-003] Page 18

Amoxicillin [No. 4282-024] Page 20

Atenolol [No. 4282-030] Page 22

Azitrhomycin 1000 mg Direct Compression [No. 4282-033] Page 24

Boswellia Serrata [No. 4282-004] Page 25

Calcium + Vitamin D3 [No. 4282-034] Page 26

Cefalexin [No. 4282-040] Page 28

Chromium Picoliante [No. 4282-005] Page 29

Cimetidin [No. 4282-025] Page 30

Ciprofloxacin Hcl [No. 4282-006] Page 32

Citramon Chewable Tablet [No. 4282-041] Page 34

Citramon Direct Compression [No. 4282-042] Page 35

Creatine Monohydrate [No. 4282-028] Page 36

Diazepam [No. 4282-022] Page 37Enalapril [No. 4282-007] Page 39

Enalapril Hydrochlorothiazide [No. 4282-043] Page 40

Extract of Cartilage [4282-008] Page 41

Ginkgo Biloba [No. 4282-009] Page 42

Glucosamine [No. 4282-010] Page 43

Glucosamine-Chondroitin [No. 4282-035] Page 44

Guafenesin [No. 4282-011] Page 45

Ibuprofen (Direct Compression) [No. 4282-012] Page 47

Ibuprofen (Direct Compression) [No. 4282-013] Page 49

Ibuprofen (Wet Granulation) [No. 4282-014] Page 50

Lecithin [No. 4282-031] Page 51

Liuweidihuang TCM Fluid Bed Drying + Direct Compression [No. 4282-027] Page 52

Metformin [No. 4282-015] Page 54

Metformin [No. 4282-026] Page 56

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FORMULATIONHANDBOOK

Table of Contents

JRS PHARMA LP

Customer Service:






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Page 2/2

Metoprolol (Direct Compression) [No. 4282-016] Page 58

Metoprolol (Direct Compression) [No. 4282-017] Page 60

Multivitamin Chewable Tablets [No. 4282-032] Page 62

Multivitamin Effervescent Tablet [4282-039] Page 63

Natural Herbal Laxative Cassia Senna + Melissa off. [No. 4282-018] Page 64

Paracetamol 500 mg [No. 4282-038] Page 66

Peppermint Oil (Direct Compression) [No. 4282-037] Page 68

Piroxicam [No. 4282-019] Page 69

Ranitidine Hcl [No. 4282-020] Page 71

Silymarin [No. 4282-036] Page 73

Simethicone [No. 4282-021] Page 74

Simethicone Direct Compression [No. 4282-045] Page 75

Vitamin C + Zink [No. 4282-044] Page 76

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Dear Customer,

-

summarizes our commitment to the full range of technical services and support that

we provide for formulation development.

Take advantage of the experience and application know-how available from our

JRS PHARMA's Technical Competence Centers in all questions relating to solid

dosage forms.

This Formulation Handbook provides you with practical examples and ideas together

with an understanding of, and guides for diverse applications.

Use our suggestions and examples as the first steps (creative ideas) for your own

solutions.

Further technical details and product information can be found on the Internet under

www.jrspharma.com.

Our experts will be happy to answer any questions. We look forward to a co-operative

discussion with you.

JRS PHARMA

Technical Competence and Service Centers

"LEADING THE WORLD IN EXCIPIENTS"

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

FORMULATIONHANDBOOK

Introduction

JRS PHARMA LPJRS PHARMA GMBH+CO.KG

Patterson, NY 12563-2359D-73494 Rosenberg (Germany)

WORLDWIDE HEADQUARTERS USA + CANADA

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FORMULATIONHANDBOOK

PROSOLV SMCCSilicified Microcrystalline Cellulose (Microcrystalline

Cellulose, Ph.Eur., NF, JP & Silica, Colloidal Anhydrous,

Ph.Eur. & Colloidal Silicon Dioxide NF & Light

AnhydrousSilicic Acid JP)

PROSOLV SMCC is the most significant innovation in high

functionality excipients today. Used with simple direct com-

pression, it emulates the outcome of alternative granula-

tions while significantly reducing the number and quantity

of excipients.

PROSOLV SMCC is the high functionality ingredient that

offers significant benefits in terms of tablet size, production

yield and overall cost. Early use in formulation development

can result in early market entry, direct compression formulas

and smaller tablets that consumers prefer.

PROSOLV SMCC s characteristics are high compactibility,

high intrinsic flow, enhanced lubrication efficiency and im-

proved blending properties. Its benefits are proven in formu-

lation, manufacturing, marketing and regulatory approval.

Regulatory approvals have been simplified by the recognitionthat PROSOLV SMCC is comprised of compendial excipients.

Submissions have been approved in the USA, Europe and

Japan. It is listed in the Inactive Ingredients Guide (IIG) of the

US Food and Drug Administration (FDA) website.

VIVAPUR and EMCOCEL

EMCOMPRESS

Microcrystalline Cellulose, Ph.Eur., NF, JP

These brands of MCC are preferred excipients in tablet manu-

facturing due to their high compactibility, inherent flow and

ability to initiate disintegration. JRS Pharma has the benefit

of multiple manufacturing plants for worldwide availability.

Calcium Hydrogen Phosphate Dihydrate, Ph.Eur.,

Dibasic Calcium Phosphate, Dihydrate, USP

The first direct compression excipient. Its particles are of a

size, shape, and density to maximize flow in high-speed

tablet production and to reduce tablet weight variation.

ANHYDROUS EMCOMPRESS : In addition to excellent flow

enhancement in direct compression. It does not containwater of crystallization and can be used with moisture

sensitive actives. It is very often used in capsule formulations

and to accelerate formulation development.

Insoluble Tablet Binders:

EMDEXDextrates, NF

Ideal for chewable products, it is the only compendial

spherical dextrate available for direct compression that

delivers the required flow, compaction and flavor carrying

capacity for consumer products.

EMDEX has a great taste masking effect.

Soluble Tablet Binders:

The High Functionality Excipient

JRS Excipients

A synergistic co-processing platform resulting in a co-processed

API which becomes directly compressible, becomes a highly

effective binder/carrier, has maximized flow and contentuniformity, stabilizes hygroscopic actives. PROSOLV SMCC

co-processing provides the ultimate deaggregation and

dispersion of the API.

PROSOLV TECHNOLOGY:

Product Overview

Page 1/3

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ARBOCEL

VIVAPRESS

Powdered Cellulose, Ph.Eur., NF, JP

Plant derived unique functional filler for capsules and tablets

that shows excellent synergistic effect in hardness when used

in combination with lactose and starch.

Calcium Carbonate, Ph.Eur., USP

Precipitated Calcium Carbonate, JP

A direct compressible, calcium containing filler.VIVAPRESS

meets Proposition 65 for lead content.

FORMULATIONHANDBOOK

Functional Fillers:

CANDEX

SUGARTAB

COMPACTROL

Dextrates

A plant sourced tablet and capsule dextrate.

Compressible Sucrose

Excellent for chewable products, particularly vitamin formu-

lations. It offers good flow, excellent compressibility and flavor

masking.

Calcium Sulfate Dihydrate, Ph.Eur., NF

A non-hygroscopic and free-flowing product that offers

excellent and long-term stability. It can be used as a binder

inwet granulation, especially in combination with starch or

powdered cellulose. Due to its high bulk density and flowing

characteristics, it imparts a high degree of fluidity which is

essential for high-speed compaction and capsule filling.

JRS Excipients

Disintegrants:

EXPLOTAB

VIVASTAR

VIVASOL

EMCOSOY

SATIALGINE

Sodium Starch Glycolate, Type (A) Ph.Eur., NF

Sodium Carboxymethyl Starch, JPE

The classical Super Disintegrant based on starch. The

material shows excellent swelling properties and gives fast

disintegration times in combination with water insolubleexcipients. EXPLOTAB corresponds to type A (Ph.Eur.),

other types are available as well.

Sodium Starch Glycolate, Type (A) Ph.Eur., NF

Sodium Carboxymethyl Starch, JPE

Super disintegrant having great disintegration power and

cost savings.

VIVASTAR PSF is innovative in improving stability of certaindrugs by removing residual solvents.

Croscarmellose Sodium, Ph.Eur., NF, JPE

Starch-free super disintegrant that adds excellent results at

low use levels.

Soy Polysaccharides

An all natural super disintegrant, which does not contain

starch or sugar. Being a dietary fiber, it has excellent appli-

cation in nutritional products.

Alginic Acid, NF

A pharmaceutical grade alginic acid that offers rapid swelling

in an aqueous medium. It can be moistened and dried

without significant loss in disintegration and combines both

a wicking and swelling mechanism to promote

disintegration in either wet or dry granulations.

Product Overview

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FORMULATIONHANDBOOK

Coating and Sustained Release:

VIVAPHARMHydroxylpropyl Methylcellulose,Hypromellose,

Ph.Eur., USP

Low viscosity types - the economical coating polymer for

protecting tablets against moisture, light oxydation, and

increased patients compliance.

PRUV

LUBRITAB

Sodium Stearyl Fumarate, Ph.Eur., NF, JPE

PRUV is a unique tablet lubricant that is more hydrophilic

than traditional lubricants, less sensitive to blending and rela-

tively inert. This results in tablets with improved disintegration

and dissolution, harder tablets and better drug stability. It

can be used in all tablet formulations including chewables

and effervescent tablets.

Hydrogenated Vegetable Oil, NF, BP

Hydrogenated Oil, JP

Less chemically reactive than most common lubricants, it

can also be used as an auxiliary dry binder and controlled

release matrix.

VIVAPUR MCGMicrocrystalline Cellulose and Carboxymethylcellulose

Sodium, NF

An excellent thixotropic gelling agent to stabilize suspensions

and emulsions. It is pH stable and could be used in hot

and cold medium.

Thickener and Stabilizer:Lubricants and Modified Release:

Carriers:

Disclaimer:The information provided is based on thorough

research and is believed to be completely reliable. Appli-

cation suggestions are given to assist our customers, but

are for guidance only. Circumstances in which our material

is used vary and are beyond our control. Therefore, we cannot

assume any responsibility for risks or liabilities, which may

result from the use of this technical advice.

JRS Excipients

NON-PAREIL SEEDSSugar Spheres, NF

Sugar spheres are used in multiple drug units for improved

content uniformity, consistent and controlled drug release

and high drug stability.

Product Overview

Page 3/3

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AR

BOCEL

EM

COMPRESS

EM

COSOY

EM

DEX

EX

PLOTAB

PR

OSOLVSMCC

PR

UV

VIVAPRESS

VIVAPUR

VIVASOL

VIVASTAR

Po

wderedCellulose

Ca

lciumH

ydrogenPhosphate

So

yPolysaccharides

De

xtrates

So

diumS

tarchGlycolate

SilicifiedMicrocrystallineCellulose

So

diumS

tearylFumarate

Ca

lciumC

arbonate

MicrocrystallineCellulose

CroscarmelloseSodium

So

diumS

tarchGlycolate

FORMULATIONHANDBOOK

No.

Acetylsalicylic Acid (Effervescent) 4282-001

Acetylsalicylic Acid (High Dosage) 4282-023

Acetylsalicylic Acid (OD Tablets) 4282-029

Allopurinol 4282-002

Ambroxol HCl 4282-003

Amoxicillin 4282-024

Atenolol 4282-030

Azitrhomycin 4282-033

Boswellia Serrata 4282-004

Calcium + Vitamin D3 4282-034

Cefalexin 4282-040

Chromium Picoliante 4282-005

Cimetidin 4282-025

Ciprofloxacin HCl 4282-006

Citramon Chewable Tablet 4282-041

Citramon Direct Compression 4282-042

Creatine Monohydrate 4282-028

Diazepam 4282-022

Enalapril 4282-007

Enalapril Hydrochlorothiazide 4282-043

Extract of Cartilage 4282-008

Table of ContentsGuide Formulations

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

Page 1/3

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AR

BOCEL

EM

COMPRESS

EM

COSOY

EM

DEX

EX

PLOTAB

PR

OSOLVSMCC

PR

UV

VIVAPRESS

VIVAPUR

VIVASOL

VIVASTAR

Po

wderedCellulose

Ca

lciumH

ydrogenPhosphate

So

yPolysaccharides

De

xtrates

So

diumS

tarchGlycolate


So

diumS

tearylFumarate

Ca

lciumC

arbonate



So

diumS

tarchGlycolate

FORMULATIONHANDBOOK

Ginkgo Biloba 4282-009

Glucosamine 4282-010

Glucosamine-Chondroitin 4282-035

Guafenesin 4282-011

Ibuprofen (Direct Compression) 4282-012

Ibuprofen (Direct Compression) 4282-013

Ibuprofen (Wet Granulation) 4282-014

Lecithin 4282-031

Liuweidihuang TCM Fluid Bed Drying + Direct Compression 4282-027

Metformin 4282-015

Metformin 4282-026

Metoprolol (Direct Compression) 4282-016

Metoprolol (Direct Compression) 4282-017

Multivitamin Chewable Tablet V1 4282-032

Multivitamin Chewable Tablet V2 4282-039

Natural Herbal Laxative Cassia Senna + Melissa off. 4282-018

Paracetamol 500 mg 4282-038

Peppermint Oil (Direct Compression) 4282-037

Piroxicam 4282-019


Page 2/3

JRS PHARMA LP

Customer Service:






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No.

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AR

BOCEL

EM

COMPRESS

EM

COSOY

EM

DEX

EX

PLOTAB

PR

OSOLVSMCC

PR

UV

VIVAPRESS

VIVAPUR

VIVASOL

VIVASTAR

Po

wderedCellulose

Ca

lciumH

ydrogenPhosphate

So

yPolysaccharides

De

xtrates

So

diumS

tarchGlycolate


So

diumS

tearylFumarate

Ca

lciumC

arbonate



So

diumS

tarchGlycolate

FORMULATIONHANDBOOK

Ranitidine HCl 4282-020

Simethicone 4282-021

Simethicone (Direct Compression) 4282-045

Silymarin 4282-036

Vitamin C + Zink 4282-044

Disclaimer:The information provided is based on thorough research and is believed to be completely reliable. Application suggestions aregiven to assist our customers, but are for guidance only. Circumstances in which our material is used vary and are beyond our control.Therefore, we cannot assume any responsibility for risks or liabilities, which may result from the use of this technical advice.


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JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

No.


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Acetylsalicylic AcidDirect Compression

Key Words: High Dosage, Direct Compression

JRS Products:VIVAPUR 102, VIVASTAR P

FORMULATIONHANDBOOK

Comments:

Formulation

Procedure

Tablet Weight: 670 mg

Tablet Diameter: 13 mm

Compaction Force: 27 - 28 kN

Hardness: 79.1 NDisintegration Time: 40 sec

Acetylsalicylic Acid (ASA),VIVAPUR 102 andVIVASTAR P were blended to homogeneity for 15 minutes. Then a sievedmixture of magnesium stearate and Aerosil were added and mixed for another 5 minutes. The powder mix is ready for

direct compression.

Active content (mg) mg/tablet Contribution (%)Acetylsalicylic Acid (ASA) 500.0 500.0 74.6

VIVAPUR 102 (Microcrystalline Cellulose) 140.0 20.9VIVASTAR P(Sodium Starch Glycolate) 23.4 3.5

Magnesium Stearate 3.3 0.5Fumed Silica (Aerosil ) 3.3 0.5

Blending:

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Tablet Characteristics

# 4282-001

Page 1/2

JRS PHARMA LP

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Acetylsalicylic acid (ASA) is an old, very well known active

substance with analgesic and antipyretic properties. It is a

non-steroidal anti-inflammatory drug which also inhibits

platelet aggregation.

The common acetylsalicylic acid (ASA) dosage is 500 mg. Inthe following formulationVIVAPUR 102 is used as filler and

binder, andVIVASTAR P as disintegrant.

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Dissolution Medium: 900 ml 0.1 N HCl, 37C, n=6

Samples are taken after 5, 10, 20, 30, 45 and 60 minutes. The sample volume is 3 ml.

The determination of the active ingredient is done by an UV-spectrophotometer at = 280 nm.

DissolutionTest:

Diagram 1:

Typical Dissolution Profile Diagram of an Acetylsalicylic Acid 500 mg Tablet, Produced According to the Above Given

Formulation.

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Time (min)

120

110

100

90

80

70

60

50

40

30

20

10

0

5

DissolvedActiveIngredient(%)

0

Tablet Press: Korsch EK 0, instrumented

Turbula Mixer: Type T2A

Hardness Tester: Pharmatest PTB 311, n=6

Friability Tester: ERWEKA TAP

Disintegration Tester: ERWEKA ZT 3

Dissolution Tester: Pharmatest PTW II, with 6 vessels, flat blade paddle

Spectrophotometer: Shimadzu UV-2101 PC

Equipment:

1510 30 45 60



# 4282-001

Page 2/2

Acetylsalicylic AcidDirect Compression

JRS PHARMA LP

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Acetylsalicylic AcidEffervescent TabletDirect Compression

Key Words: Acetylsalicylic Acid, Direct

Compression, Effervescent Tablet JRS Products: EMDEX , PRUV

FORMULATIONHANDBOOK

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# 4282-023

JRS PHARMA LP

Customer Service:






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The acetylsalicylic acid is an old and very well known active with

analgesic, antipyretic, antiinflammatory and antiaggregant


Procedure

Compression Force 20 kNHardness 10.0 kp

Diameter 25 mm

Disintegration Time 176 sec.

All ingredients except were blended for 15 minutes. The was added and the tabletting powder was mixed for

another 3 min. Ready for direct compression.

PRUV PRUV

Blending:

Equipment:

properties. Its lipophility and low water solubility make the

development of an effervescent formulation a big challenge.


Tablet Diameter: 25 mm, biplane,

Hardness Tester: Schleuniger 2E

Disintegration Tester: Pharmatest Standard PTZ

Dissolution Tester: Pharmatest PTW 2

Spectrophotometer: Cecil Spektralphotometer, Series 1000

Comments:

Formulation

mg/Tablet Contribution (%)

Acetylsalicylic Acid (ASA) 500.0 12.5

PRUV (Sodium Stearyl Fumarate) 12.0 0.3Citric Acid 348.0 8.7

NaHCO 400.0 10.03

Glycine HCl 128.0 3.2

Aspartame 76.0 1.9

Flavour 36.0 0.9EMDEX (Dextrates) 2500.0 62.5

Total 4000.0 100.0



14/76

Dissolutuion Medium: 900 ml 0.1 N HCl, 37 C, n=6

Samples are taken after 5, 10, 15, 30, 60, 120, 180 and 300 minutes. The sample volume is 3 ml. The probes were

diluted if necessary. The determination of the acetylsalicylic acid was done by an UV-spectrophotometer at = 232.0 nm.

DissolutionTest:

Diagram 1:

Dissolution Profile of Acetylsalicylic Acid Effervescent Tablet, Produced According to the Above Given Formulation.

FORMULATIONHANDBOOK

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Compression, Effervescent Tablet JRS Products: EMDEX , PRUV

Page 2/2

# 4282-023

Time (min)

120

110

100

90

80

70

60

50

40

30

20

10

0

DissolvedActive(%)

0 32030020 40 60 80 100 120 140 160 180 200 220 240 260 280

Acetylsalicylic AcidEffervescent TabletDirect Compression

Back to Table of ContentsBack to Table of Contents


15/76

Acetylsalicylic AcidOD Tablets;DC Formulations


Compression, Fast Disintegration

JRS Products: PROSOLV SMCC 90, PURV , EXPLOTAB , VIVASOL , EMCOMPRESS

FORMULATIONHANDBOOK

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# 4282-029

JRS PHARMA LP

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The acetylsalicylic acid is an old and very well known active with

analgesic, antipyretic, antiinflammatory and antiaggregant

properties. The permanently growing interest on ODT (Orally

Disintegrating Tablets) in the last few years stimulate us to

create these formulations.

Formulation

Substance (%)

Formulation 1 2 3 4

Acetylsalicylic Acid 71.43 70.43 70.43 70.43PROSOLV SMCC 90 (Silicified Microcrystalline Cellulose) 20.00 20.00 14.00 14.00

Adipic Acid 4.00 4.00 - -

Citric Acid - - 4.00 7.50

Sodium Hydrogencarbonate 2.86 2.86 2.86 6.36EMCOMPRESS (CalciumHydrogen Phosphate) - - 1.00 -

EXPLOTAB (Sodium Starch Glycolate) - - 5.00 -VIVASOL ( ) 1.00 2.00 2.00 1.00

PRUV (Sodium Stearyl Fumarate) 0.71 0.71 0.71 0.71

Total 100 100 100 100

Croscarmellose Sodium

Procedure

All ingredients except PRUV were blended for 15 minutes. ThePRUV was added and the tabletting powder was mixed for

another 3 min. Ready for direct compression.

Note: The mentioned above formulations do not contain

taste masking substances!


Disintegration Time (sec) 29 27 28 40

Friability (%) 0.68 0.61 0.87 1.18

Compression Force (kN) 13.40 14.30 20.00 22.10

Hardness (kp) 7.10 6.80 7.10 8.10

Comments:




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AllopurinolDirect Compression

Key Words: Poor Flowability, Direct Compression


FORMULATIONHANDBOOK

Allopurinol is used to treat chronic gout (gouty arthritis). This

condition is caused by too much uric acid in the blood.It is also

used to prevent or treat other medical problems that may

occur if too much uric acid is present in the body.

Comments:


Formulation

Procedure




Hardness: 91.3 NDisintegrationTime: 11 sec

Allopurinol,VIVAPUR 102andVIVASTAR P were mixed in a Turbula mixer for 15 minutes. Then a sieved mixture ofmagnesium stearate and Aerosil were added and mixed for another 3 minutes. The powder mixwas ready fordirect

compression.

Blending:

These include certain kinds of kidney stones or other kidney

problems.Allopurinol can be directly compressed usingVIVAPUR

Microcrystalline Cellulose as a binder.

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Tablet Press: Korsch EK 0 eccentric press, 9 mm punch,biplane


Hardness Tester: Pharmatest PTB 311, n=6

FriabilityTester: Erweka TAP

DisintegrationTester: Erweka ZT 3

DissolutionTester: Pharmatest PTW II, with 6 vessels, flat blade paddle

Spectrophotometer: Shimadzu UV-2101 PC

Equipment:

Active content (mg) mg/tablet Contribution (%)

Allopurinol 100.0 100.0 55.5

72.0 40.0(Sodium Starch Glycolate) 6.2 3.5

Magnesium Stearate 0.9 0.5

Fumed Silica (Aerosil 200) 0.9 0.5

VIVAPUR 102(Microcrystalline Cellulose)VIVASTAR P

# 4282-002

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FORMULATIONHANDBOOK

120

100

90

80

70

60

50

40

30

20

10

0

0 5 10 15 20 25 30 35 40 45 50 55 60 65

Time (min)

DissolvedActiveIngredient(%)

Diagram 1:Typical Dissolution Profile Diagram of a AllopurinolTablet, ProducedAccording to theAbove Given Formulation.

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Samples are taken after 5, 10, 20, 30, 45 and 60 minutes. The sample volume is 3 ml. Samples were diluted if necessa-

ry.The determination of the active ingredient is done by an UV-spectrophotometer at = 248.8 nm.

DissolutionTest:

AllopurinolDirect Compression

# 4282-002

Page 2/2

Key Words: Poor Flowability, Direct Compression


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Ambroxol HClDirect Compression

Key Words: PoorlySoluble, LowDosage,

Direct Compression

JRS Products:VIVAPUR 12, ARBOCEL A 300,VIVASOL

FORMULATIONHANDBOOK

Ambroxol Hydrochloride is an example for a poorly soluble

active substance used in low concentrations. It can be com-pressed directly by usingVIVAPUR Microcrystalline Cellulose

as a dry binder andARBOCEL Powdered Cellulose as a plant-

derived filler.

Comments:

Formulation

Procedure


Tablet Diameter: 8 mmCompaction Force: 12.5 kN

Hardness: 64.0 N

DisintegrationTime: 13 sec

Friability:


19/76


Samples are taken after 1, 5, 10, 15, 20, 30, 45, 60, 75 and 90 minutes. The sample volume is 3 ml. Samples were

diluted if necessary.The determination of the active ingredient is done by an UV-spectrophotometer at = 223 nm.

DissolutionTest:

Diagram 1:Typical Dissolution Profile Diagram of a AmbroxolTablet, ProducedAccording to theAbove Given Formulation.

120

110

100

90

80

70

60

50

40

30

20

10

0

0 5 10 15 20 25 30 35 40 45 50 55 60 65 70 75 80 85 90

Time (min)

Disso

lvedActiveIngredient(%)

FORMULATIONHANDBOOK

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Ambroxol HClDirect Compression

Key Words: PoorlySoluble, LowDosage,

Direct Compression

JRS Products:VIVAPUR 12, ARBOCEL A 300,VIVASOL

# 4282-003

Page 2/2

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414



20/76

AmoxicillinDirect Compression

Key Words: High Dosage, Crystalline Active

Ingredient, Direct Compression

JRS Products:VIVAPUR , VIVASTAR , PRUV

FORMULATIONHANDBOOK

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024.GB0.0

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Page 1/2

# 4282-024

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

Amoxicillin is a bactericidal antibiotic with a relatively broad

spectrum of activity. It belongs to the penicillin group. Amoxicillin

mainly acts against infections caused by amoxicillin-sensitive


Formulation

Procedure

Diameter of Tablet: 20 mm


Compression Force: 25 - 26 kN

Hardness: 8.8 kp

Friability: 2.02 %Disintegration Time (in 200 ml Water): 98 sec

Mixing of all ingredients (10 min), compressing at a compaction force of approx. 25 kN

Blending:

Equipment:

micro organisms, i.e. respiratory tract infections, urogenital

infections or gastrointestinal infections. It is an example for

an easy to compress crystalline substance.


Amoxicillin Trihydrate 574.0 58.6VIVAPUR 12 (Microcrystalline Cellulose) 361.0 36.8

VIVASTAR P (Sodium Starch Glycolate) 36.0 3.8

Magnesium Stearate 4.5 0.4


Tablet Press: Korsch EKO, Nr. 6087/64 , 20 mm punch

Hardness Tester: Schleuniger, Type 2 E

Dissolution Tester: Pharmatest, Type PTW 2 , Nr. 6276

Disintegration Tester: Pharmatest Standard, Type PTZ , Nr. 6454

Friability Tester: Pharmatest, Typ PTF 1, Nr. 6453

Spectrophotometer: Cecil Spektralphotometer, Series 1000 (CE 1021)

Comments:



21/76


FORMULATIONHANDBOOK

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AmoxicillinDirect Compression

Key Words: High Dosage, Crystallin Active

Ingredient, Direct Compression

JRS Products:VIVAPUR , VIVASTAR , PRUV

Page 2/2

# 4282-024

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

Dissolution Medium: 900 ml 0,1 N HCl, 37C, n=3.

Samples were taken after 1, 5, 10, 20, 30, 60, 90 and 120 minutes.

The determination of the active ingredient was done by an U.V. spektrophotometer at Lambda =230 nm.

Dissolution Test:

120

110

100

90

80

70

60

50

40

30

20

10

0

0 20 40 60 80 100 120 140

Time (min)

Disso




22/76

AtenololDirect Compression

Key Words: Atenolol, Direct Compression,

Dissolution Profile

JRS Products:VIVAPUR 102, PURV , EXPLOTAB

FORMULATIONHANDBOOK

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Page 1/2

# 4282-030

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

Atenolol is a drug belonging to the group of beta blockers, a

class of drugs used primarily in cardiovascular diseases.

Atenolol (trade name Tenormin) can be used to treat

cardiovascular diseases such as hypertension, coronary heart

Comments:

disease, arrhythmias, and treatment of myocardial infarction

after the acute event. The drug is also used to treat other

conditions, including dysautonomia, anxiety and

hyperthyroidism (overfunction of the thyroid gland).

Formulation

active content/tablet (mg) Contribution (%)

VIVAPUR 102 (Microcrystalline Cellulose)EXPLOTAB (Sodium Starch Glycolate)

PRUV (Sodium Stearyl Fumarate)

Atenolol 50.0 16.7

238.0 79.3

9.0 3.0

3.0 1.0

Total 300.0 100.0


Tablet Weight: 300.0 mgTablet Diameter: 10 mm

Tablet Height: 3.4 mm

Compaction Force: 4.7-4.9 kN

Hardness: 7.1 kp

Disintegration 14 sec

Friability 0.22 %

Procedure

The Atenolol,VIVAPUR 102 and the EXPLOTAB were blendedfor 15 minutes. The

PRUVwas added and the tabletting

powder was mixed for another 3 min. Ready for direct

compression.



23/76


FORMULATIONHANDBOOK

4282_

029.

GB0.

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pdf

AtenololDirect Compression

Key Words: Atenolol, Direct Compression,

Dissolution Profile

JRS Products:VIVAPUR 102, PURV , EXPLOTAB

Page 2/2

# 4282-030

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

Dissolution Medium: 900 ml 0.1 N HCl, 37 C, n=6

Samples are taken after 5, 10, 15, 30, 60 and 120 minutes. The sample volume is 3 ml. The probes were dilueted if

necessary. The determination of the atenolol was done by an UV-spectrophotometer at l = 220 nm.

Dissolution Test:

120

110

100

90

80

70

60

50

40

30

20

10

0

0 10 20 30 40 50 60 70 80 90 100 110

Time (min)

Disso


Diagram 1:

Dissolution Profile of Atenolol Tablet, Produced According to the Above Given Formulation.



24/76

Azithromycin 1000 mgDirect Compression

Key Words: Azithromycin, Direct Compression

JRS Products: PROSOLV SMCC 50, PRUV , VIVASOL

FORMULATIONHANDBOOK

Azithromycin is an antibiotic acting API, which belongs to the

class of macrolides. Chemical it is similar to erythromycin.

Today, Azithromycin is one of the best selling antibiotics world-

wide. It is used against certain bacterial infections, mainly

bronchitis, pneumonia, rhinitis and some throat infections.


Formulation

Procedure

Tablet Weight: 1295.0 mg

Tablet Diameter: 14 mm, oblong

Tablet Height: 6.0 mmCompaction Force: 16-18 kN

Hardness: 10.3 kp

Disintegration Time: 41 sec

Friability: 2.3 %

The Azithromycin, and the were blended intensive for 15 minutes. The was added

and the tabletting powder was mixed for another 3 min. Press with compression force 16-18 kN!!A higher compression

forces may cause capping.

PROSOLV SMCC 5o VIVASOL PRUV


Azithromycin 1000 1000.0 77.22PROSOLV SMCC 5o (Silicified Microcrystalline Cellulose) 256.0 19.77

VIVASOL (Croscarmellose Sodium) 16.0 1.24PRUV (Sodium Stearyl Fumarate) 23.0 1.77

Total 1295.0 100

Blending:

The formulation of 1.000 mg Azithromycin per tablet is a

major challenge. The substance is very good flowing but poor

compressible. The monohydrate gives better compression

results than the dihydrate.

4282_

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Page 1/1

# 4282-033

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

Comments:

Tablet Press: Kilian Pressima, 14 mm punch oblong


DisintegrationTester: Pharmatest Standard PTZ

FriabilityTester: Pharmatest PTF

Equipment:



25/76

Boswellia SerrataDirect Compression

Key Words: Botanical Extract, Sticky Active,

High Dosage, Direct Compression

JRS Products: PROSOLV SMCC HD 90, PRUV

FORMULATIONHANDBOOK

Boswellia has been used historically for various conditions, in-

cluding arthritis and other inflammation. It is a gum resin, co-

hesive in nature and, consequently, poorly flowing. Since

Boswellia extract is a gum resin, it is also very poorly compac-

table. Due to its physical characteristics, Boswellia is gene-

rally granulated prior to tablet manufacture.

Comments:


Formulation

Procedure

PROSOLV SMCC HD 90

V-blender. Boswellia was

minutes.

and PRUV were dispensed to the correct masses and transferred to aPatterson-Kelly twin-shell

sieved through a twenty mesh and transferred into the V-blender. The powders were blended for five


Boswellia extract 200.0 200.0 49.75PROSOLV SMCC HD 90(Silicified Microcrystalline Cellulose) 200.0 49.75

PRUV (Sodium Stearyl Fumarate) 2.0 0.50

Blending:

Blender: Patterson-Kelly twin-shell V-blender

Flowability Apparatus: Hanson Research FlodexTablet Press: Korsch PH-106 instrumented rotary tablet press

Hardness Tester: Erweka TBH-30

Disintegration Tester: Erweka ZT-62

Friability Tester: Erweka TA-3

Equipment:

UsingPROSOLV SMCC HD 90, Boswellia was formulated into

a directly compressible tablet.PROSOLV SMCC HD 90 not only provided the necessary bin-

ding properties required for direct compression tableting, but

also served as the tablet disintegrant.

4282_

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Tablet Mass: 402 mg

Hardness: 14. kp

Compaction Force: 15.2 kN

Tablet Weight Variation: 2.3%Tablet Disintegration Time: 225 sec

4


Page 1/1

# 4282-004

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414



26/76

Calcium+Vit. D3 EffervescentDirect Compression

Key Words: Calcium, Vitamin D3,

Effervescent Tablet, Direct Compression

JRS Products: EMDEX ,VIVAPRESS , PRUV

FORMULATIONHANDBOOK

Vitamin D is a group of fat-soluble prohormones, the two major

forms of which are vitamin D2 (ergocalciferol) and vitamin D3

(cholecalciferol). Vitamin D regulates the calcium and phosphorus

levels in the blood by promoting their absorption from food in

the intestines, and by promoting re-absorption of calcium in

the kidneys. It promotes bone formation and mineralization

and is essential in the development of an intact and strong

skeleton. The combination of calcium supplement and

vitamin D3 ist very popular for the prevention and treatment

of osteoporosis.

4282_

034.GB0.0

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Page 1/2

# 4282-034

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

Comments:

Formulation

Active content (mg) mg/tablet Contribution (%)VIVAPRESS (CaCO ) (Calcium Carbonate) 670 670 16.753

Vitamin C 500 500 12.50

Vitamin D3 400 IU (10 mcg) 0.00025

Vitamin B6 10 10 0.25

Sodium Hydrogenphosphate 650 16.25

Citric Acid 575 14.37

Aspartam 70 1.75

Flavour (orange) 100 2.50

Beta Carotine 1 % CWS 25 0.63

Sodium Chloride 10 0.251310 32.75

PEG 6000 40 1.00 (Sodium Stearyl Fumarate) 40 1.00

Total 4000 100

CA 800

EMDEX (Dextrate)

PRUV




Compaction Force: 18 kN

Hardness: 7.5 kp

Disintegration < 2 min



27/76

Calcium+Vit. D3 EffervescentDirect Compression

Key Words: Calcium, Vitamin D3,

Effervescent Tablet, Direct Compression

JRS Products: EMDEX ,VIVAPRESS , PRUV

FORMULATIONHANDBOOK

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034.GB0.0

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Page 2/2

# 4282-034

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

Procedure

The vitamin mixture was preblended. All substances without the lubricant were mixed for 20 min. Than PRUVSodiumStearyl Fumarate was added and the powder was mixed for another 3 min. DC ready.

Blending:


Tablet Press: Korsch EK 0 eccentric press, 25 mm punch


DisintegrationTester: Pharmatest Standard PTZFriabilityTester: Pharmatest PTF

Equipment:



28/76

Cefalexin 1000 mgDirect Compression

Key Words : Cefalexin, High Dosage,

Direct Compression

JRS Products: PROSOLV SMCC 90, PRUV

FORMULATIONHANDBOOK

Cefalexin (INN) belolongs to the group of cephalosporins,

member of the big family of the -lactam antibiotics. It shows

bactericidal activity caused by disruption the synthesis of the

peptidoglycan layer of the bacterial cell walls. Cefalexin is so

called first generation cephalosporin antibiotic with

Comments:


Formulation

Procedure

The Cefalexin and the were blended for 15 minutes. The was added and the powder was mixed

for another 3 min. Ready for direct compression.

PROSOLV SMCC 90 PRUV


Cefalexin 1000.0 1000.0 73.26PROSOLV SMCC 50(Silicified Microcrystalline Cellulose) 345.0 25.27


Total 1365.0 100.00

Blending:

Tablet Press Korsch EK 0, instrumented

Hardness Tester Schleuniger 6D

Disintegration Tester Pharmatest Standard PTZ

Equipment:

predominantly activity against Gram-positive bacterias. Its

stability toward hydrochloric acid make this -lactam

antibiotic suitable for oral administration. We developed adirect compression formulation with PROSOLV as a binder

and PRUV as a lubricant.

4282_

040.GB0.0

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Tablet Weight 1365.0 mg

Tablet Diameter 20 mm

Compaction Force 9.5-10.5 kN

Tablet Hardness 8.5-9.0 kpDisintegration Time 123 sec

Page 1/1

# 4282-040

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414



29/76

Chromium PicolinateDirect Compression

Key Words : Sticky Active, Low Dosage,

Direct Compression

JRS Products: PROSOLV SMCC , PRUV

FORMULATIONHANDBOOK

Chromium Picolinate is a poorly flowing, low dose substance.

Chromium is an essential trace element. It is reported to play

an important role in blood sugar regulation and acts as a

cofactor to anumber of enzymes involved in energy produc-

Comments:


Formulation

Procedure

Chromium Picolinate,PRUV was added to the blender and blended for additional three minutes.

PROSOLV SMCC 90andPROSOLV SMCC 50added to the V-blender and blended for 30 minutes.


Chromium Picolinate 0.4 0.4 0.27PROSOLV SMCC 50(Silicified Microcrystalline Cellulose) 15.0 9.95PROSOLV SMCC 90(Silicified Microcrystalline Cellulose) 135.0 89.58


Blending:

Blender: Patterson-Kelly 2 qt. twin-shell V-blender

Flowability Apparatus: Hanson Research Flodex

Tablet Press: Korsch PH-106 rotary tablet press

Hardness Tester: Erweka TBH-30

Disintegration Tester: Erweka ZT-62Friability Tester: Erweka TA-3

Equipment:

tion as well as reducing lipid levels. It can be directly com-pressed using a combination of PROSOLV SMCC 50 and

PROSOLV SMCC 90.

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Tablet Mass: 150.7 mg

Hardness: 20 kp

Compaction Force: 23 kN

Tablet Disintegration Time: 158 sec

Page 1/1

# 4282-005

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414



30/76

Cimetidin 400 mgDirect Compression


JRS Products:VIVAPUR 12, VIVASTAR P, PRUV

FORMULATIONHANDBOOK

4282_

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Page 1/2

# 4282-025

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

Cimetidin is a histamine H2-receptor antagonist for treatment

of ulcus duodeni and ulcus ventriculi. Normally, this active is

wet granulated to achieve a better water solubility, because the


Formulation

Procedure



Compression Force: 14 - 15 kN

Hardness: 9.8 kp

Friability: 0.79 %Disintegration Time (in 200 ml Water): 47 sec

Mixing of all ingredients (10 min), compressing at a compaction force of approx. 14 - 15 kN

Blending:

Equipment:

cimetidin is only slightly water soluble. But it is not a problemto make tablets by direct compression usingVIVAPUR 12 as

a binder, getting good dissolution profiles as well.


PRUV (Sodium Stearyl Fumarate)

Cimetidin 400.0 57.1VIVAPUR 12 (Microcrystalline Cellulose) 265.0 37.9

VIVASTAR P (Sodium Starch Glycolate) 28.0 4.0

3.5 0.5


Tablet Press: Korsch EKO, Nr. 6087/64 , 13 mm punch

Hardness Tester: Schleuniger, Type 2 E

Dissolution Tester: Pharmatest, Type PTW 2 , Nr. 6276

Disintegration Tester: Pharmatest Standard, Type PTZ , Nr. 6454

Friability Tester: Pharmatest, Typ PTF 1, Nr. 6453

Spectrophotometer: Cecil Spektralphotometer, Series 1000 (CE 1021)

Comments:



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FORMULATIONHANDBOOK

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Cimetidin 400 mgDirect Compression


JRS Products:VIVAPUR 12, VIVASTAR P, PRUV

Page 2/2

# 4282-025

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

Dissolution Medium: 900 ml 0,1 N HCl, 37C, n=3.

Samples were taken after 1, 5, 10, 20, 30, 60 and 120 minutes.

The determination of the active ingredient was done by an U.V. spektrophotometer at Lambda = 220 nm.

Dissolution Test:

120

110

100

90

80

70

60

50

40

30

20

10

0

0 20 40 60 80 100 120 140

Time (min)

Disso




32/76

Ciprofloxacin HClDry Compaction

Key Words: VeryLowBulkDensity,

DryCompaction

JRS Products:VIVAPUR 12

FORMULATIONHANDBOOK

Ciprofloxacin HCl is a material of very low bulk density and has

to be precompacted. This can be done with a dry compactor or

by re-processing.

Ciprofloxacin is an antimicrobial agent that stops multiplication

of bacteria by inhibiting the reproduction and repair of their

genetic material (DNA).

Comments:


FormulationStep 1 (Granules)

Procedure



Compaction Force: 8.5 kN

Hardness: 109.7 N

DisintegrationTime: 540 sec

Friability: 0.36 %

In the first steptablets were made of 20 mm insize and in the second step the tablets have been crushed by passing

them through a dry granulator with a screen size of 19 mesh (800 m). The resulting granules have been compressed to

the final tablet by m andixing of all ingredients for 4 minutes compressing at a compaction force of approx. 8.5 kN.


CiprofloxacinHCl 500.0 500.0 85.1VIVAPUR 12 (Microcrystalline Cellulose) 75.0 12.8

MagnesiumStearate 7.5 1.3Fumed Silica (Aerosil 200) 5.0 0.8

Blending:

Ciprofloxacin is used to treat infections of the skin, lungs,

airways, bones, and joints caused by susceptible bacteria.

Ciprofloxacin is also frequently used to treat urinary infections

caused by bacteria such as E. Coli.

4282_

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mg/tablet Contribution (%)

Ciprofloxacin Granules 587.5 85.1VIVAPUR 12 (Microcrystalline Cellulose) 93.5 13.6

Magnesium Stearate 5.0 0.7Fumed Silica (Aerosil 200) 4.0 0.6

Step 2 (Tablets)

Page 1/2

# 4282-006

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414



33/76

FORMULATIONHANDBOOK

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120

110

100

90

80

70

60

50

40

30

20

10

0

0 50 100 150 200 250 300 350

Time (min)

DissolvedActiveIngre

dient(%)

Diagram 1:

Typical Dissolution Profile Diagram of a CiprofloxacinTablet, ProducedAccording to theAbove Given Formulation.

Granulator: Erweka 20240



Hardness Tester: Schleuniger Type 2 E

FriabilityTester: Pharmatest Type PTF 1, Nr. 6453

DisintegrationTester: Pharmatest Standard, Type PTZ, Nr. 6454

DissolutionTester: Pharmatest PTW II, with 6 vessels, flat blade paddle

Spectrophotometer: Cecil Spectrophotometer, Series 1000 (CE 1021)

Equipment:

Ciprofloxacin HClDry Compaction

Key Words: VeryLowBulkDensity,

DryCompaction

JRS Products:VIVAPUR 12

Page 2/2

# 4282-006

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414


Samples are taken after 1, 5, 10, 20, 30, 60, 90, 120, 180, 240 and 300 minutes. The determination of the active

ingredient is done by an UV-spectrophotometer atl= 278.7 nm.

Dissolution Test:



34/76

CitramonChewable Tablet

Key Words : Acetylsalicylic Acid, Paracetamol,

Caffein, Direct Compression

JRS Products: EMDEX , PRUV

FORMULATIONHANDBOOK

The acetylsalicylic acid and the paracetamol are two of the

widest used pain relief actives world-wide. The combination

with caffein is often found in many headache and cold

medicinal compositions. A common problem with this

Comments:


Formulation

Procedure

All substances were blended for 20 minutes. Ready for direct compression.


Acetylsalicylic Acid 240.0 240 12.06

Paracetamol 200.0 200 10.05

Caffein 30.0 30 1.51

Milk Powder 199 10.00

1150 57.79

Cacao Powder 129 6.48

Citric Acid 12 0.60

Aspartame 10 0.50PRUV (Sodium Stearyl Fumarate) 20 1.01

Total 1990.0 100.00

EMDEX (Dextrates)

Blending:




Equipment:

formulation is the unpleasant bitter taste of the paracetamol

and the caffein. We developed a direct compressionformulation with EMDEX as a binder and taste improver, and

PRUV as a lubricant.

4282_

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Compaction Force: 16-17 kN

Hardness: 8-9 kp

Page 1/1

# 4282-041

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414



35/76

CitramonDirect CompressionChewable Tablet

Key Words : Acetylsalicylic Acid, Paracetamol,

Caffein, Direct Compression

JRS Products: EMDEX , PRUV

FORMULATIONHANDBOOK

The acetylsalicylic acid and the paracetamol are two of the

widest used pain relief actives world-wide. The combination

with caffein is often found in many headache and cold

medicinal compositions. The most of the formulations on the

Comments:


Formulation

Procedure

All substances except were blended for 15 minutes. The was added and the powder was mixed for another

3 min. Ready for direct compression.

PRUV PRUV


Acetylsalicylic acid 240.0 240.0 30.19

Paracetamol 200.0 200.0 25.16

Caffein 30.0 30.0 3.77

292.0 36.73

Cacao Powder 20.0 2.52

Citric Acid 5.0 0.63PRUV (Sodium Stearyl Fumarate) 8.0 1.00

Total 795.0 100.00

EMDEX (Dextrates)

Blending:


Hardness Tester Scleuniger 6D


Friability Tester Pharmatest Standard PTF

Equipment:

market are made with microcrystalline cellulose. We

developed a direct compression formulation with water soluble matrix usingEMDEX as a binder and PRUV as a

lubricant.

4282_

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Tablet Weight: 795.0 mgTablet Diameter: 13 mm

Compaction Force: 18-20 kN

Hardness: 8-9 kp

Friability 0.8 %

Page 1/1

# 4282-042

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414



36/76

Creatine MonohydrateDirect Compression

Key Words: Creatine Monohydrate, Direct

Compression, High Dosage

JRS Products: EMDEX PRUV

FORMULATIONHANDBOOK

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Page 1

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JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

Creatine is a nitrogenous organic acid that naturally occurs in

vertebrates and helps to supply energy to muscle cells. Its

functions as part of a system based on arginine/

phosphoarginine that operates in many invertebrates. The

presence of this energy shuttle keeps the ATP/ADP ratio high

which ensures that the free energy of ATP remains high and

minimizes the loss of adenosine nucleotides, which would

cause cellular dysfunction. Such high energy phosphate

buffers are known as phosphagens. Creatine supple-

mentation has been, and continues to be, investigated as a

possible therapeutic approach for the treatment of muscular,

neurological and neuromuscular diseases (arthritis,

congestive heart failure, disuse atrophy, gyrate atrophy,

McArdle's disease, Huntington's disease, miscellaneous

neuromuscular diseases, mitochondrial diseases, muscular

dystrophy, neuroprotection, etc.).

Formulation

active content/tablet (mg) Contribution (%)

(Dextrates)PRUV (Sodium Stearyl Fumarate)

Creatine Monohydrate 1000.0 83.33

EMDEX 190.0 15.83

10.0 0.84

Total 1200.0 100.00




Compression Force: 32 kN

Hardness: 6 kp

Procedure

The creatine mohohydrate and EMDEX were blended for 18minutes. The

PRUVwas added and the tabletting powder was

mixed for another 3 min. Ready for direct compression.

Comments:




37/76

DiazepamKey Words: Low Dosage, Direct Compression JRS Products:VIVAPUR 12,EMCOMPRESS ,

EXPLOTAB /VIVASTAR

FORMULATIONHANDBOOK

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Page 1/2

# 4282-022

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

Diazepam, better known under the original name Valium, is a

benzodiazepine derivative.

It is for short-term management of moderate degrees of

anxiety, tension, agitation, fear or aggressiveness. It is often

used in certain medical procedures (e.g. surgery ) to reduce


Formulation

Procedure

Tablet Weight: 140 mgTablet Diameter: 8 mm


Hardness: 7,3 kp

Disintegration Time: 20 sec

Friability: 0,1 %

Mix all ingredients except PRUV for 10 minutes. Add PRUV and mix another 3 minutes. The powder is for direct compression.

Blending:

Equipment:

tension and anxiety. Normally the dosage in tablets is

between 2 and 10 mg.

This formulation is an example for a low dosage active

ingredient, workable in direct compression.


Diazepam 10,0 7,1VIVAPUR 12(Microcrystalline Cellulose) 59,0 42,1

EMCOMPRESS (CalciumHydrogen Phosphate) 65,5 46,8VIVASTAR (Sodium Starch Glycolate) 4,0 2,9

PRUV (Sodium Stearyl Fumarate) 0,8 0,6

Fumed Silica (Aerosil 200) 0,7 0,5




Dissolution Tester: Pharmatest PTW 2

Spectrophotometer: Cecil Spektralphotometer, Series 1000

Comments:



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FORMULATIONHANDBOOK

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DiazepamKey Words: Low Dosage, Direct Compression JRS Products:VIVAPUR 12,EMCOMPRESS ,

EXPLOTAB /VIVASTAR

Page 2/2

# 4282-022

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414

Dissolution Medium: 900 ml 0,1 N HCl, 37C, n = 6

Samples were taken after 1, 5, 10, 20, 30, 60 and 120 minutes. The determination of the active ingredient was done by

an UV spectrometer at = 242 nm.

Dissolution Test:

120

110

100

90

80

70

60

50

40

30

20

10

0

0 5 10 15 20 25 30 35 40 45 50 55 60 65 70

Time (min)

Dissolve

dActiveIngredient(%)



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EnalaprilDirect Compression

Key Words: Poor Flowability, Low Dosage,

Direct Compression

JRS Products: PROSOLV SMCC 90, EMCOMPRESS , VIVASTAR P, PRUV

FORMULATIONHANDBOOK

Enalapril is an angiotensin converting enzyme (ACE) inhibitor

used in the treatment of hypertension and some types of

chronic heart failure.

Comments:


Formulation

Procedure




Hardness: 10.8 kp

Friability: 0.03 %Disintegration Time: 14 sec

Enalapril maleate, 90, EMCOMPRESS and P were blended to homogeneity for 10 minutes.

Then PRUV was added and mixed for another 3 minutes. The powder-mix was ready for direct compression.

PROSOLV SMCC VIVASTAR


Enalapril Maleate 10.0 10.0 5.1PROSOLV SMCC 90(Silicified Microcrystalline Cellulose) 93.7 47.8

EMCOMPRESS (Calcium Hydrogen Phosphate) 85.4 43.6VIVASTAR P (Sodium Starch Glycolate) 5.9 3.0

(Sodium Stearyl Fumarate) 1.0 0.5PRUV

Blending:



Friability Tester: Pharmatest PFT


Equipment:

Enalapril which is a poor flowing API can be directly compressed usingPROSOLV SMCC 90 and EMCOMPRESS as

binders.

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Page 1/1

# 4282-007

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414



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Enalapril HydrochlorothiazideDirect Compression

Key Words : Enalapril, Hydrochlorothiazide,

Direct Compression

JRS Products: PROSOLV SMCC 50, VIVASTAR P,PRUV

FORMULATIONHANDBOOK

Enalapril and Hyrochlorothiazide are two actives, used in

combination to treate high blood pressure. The syergistic effect

of an ACE-inhibitor (Enalapril) and a diuretic (Hydrochlor-

othiazide) for the treatment of the hypertension was observed

years ago and applied successful in many drug compositions.

Comments:


Formulation

Procedure

All substances except were blended for 15 minutes. The was added and the powder was mixed for another

3 min. Ready for direct compression.

PRUV PRUV


Enalapril 10.0 10.0 6.71

Hydrochlorothiazide 25.0 25.0 16.78PROSOLV SMCC 50(Silicified Microcrystalline Cellulose) 107.0 71.82

VIVASTAR P (Sodium Starch Glycolate) 2.0 1.34PRUV (Sodium Stearyl Fumarate) 2.0 1.34

Sodium Hydrogencarbonate 3.0 2.01

Total 149.0 100.00

Blending:




Friability Tester Pharmatest Standard PTF

Equipment:

JRS PHARMA developed a direct compression formulationusing silicified microcrystalline cellulose (PROSOLV SMCC 50)

as a filler and binder,VIVASTAR P as superdisintegrant andPRUV as a lubricant.

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Compaction Force: 6-6.5 kN

Hardness: 11-12 kp

Friability 0.2 %

Disintegration 12 sec

Page 1/1

# 4282-043

JRS PHARMA LP

Customer Service:






USA + CANADA

+1 (845) 878-3414



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Extract of CartilageDirect Compression

Key Words: Very Hygroscopic, Sticky,

Direct Compression

JRS Products: PROSOLV SMCC 90, EMCOMPRESS , ARBOCEL P 290, VIVASOL , PRUV

FORMULATIONHANDBOOK

The extract of Cartilage is a hygroscopic substance with a very

high water content. The substance is very sticky. The extract

is a product made from the cartilage of the common dogfish

shark.There are several diseases which can affect the

Comments:


Formulation

Procedure


Compaction Force: 9.1 kN / 18.4 KN / 22 KN

Hardness: 2.5 kp / 7.3 kp / 9.7 kp

Friability: 0.26 %

Disintegration Time: 15 min

Active content (mg) mg/tablet Contribution (%)Extract of Cartilage 186.9 186.9 35.6

Ascorbic Acid Crystalline 43.5 8.3PROSOLV SMCC 90(Silicified Microcrystalline Cellulose) 199.0 37.9

EMCOMPRESS (Calcium Hydrogen Phosphate) 70.3 13.4 ARBOCEL P290(Powdered Cellulose) 5.25 1.0

Talcum 9.45 1.8VIVASOL (Croscarmellose Sodium) 8.0 1.5

(Sodium Stearyl Fumarate) 2.6 0.5PRUV

Blending:




FriabilityTester: Pharmatest PTF

Equipment:

cartilage, for example arthr

FormualtionHandbook 12-2007

Documents

Transcript of FormualtionHandbook 12-2007