Bilayered Ppt

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BI-LAYER TABLET

GUIDED BY PRESENTED BYMr. VIKRAM M. PANDYA Mr. MAHMADASIF M. SHEIKH

M. PHARM Student of M. PHARM SEM- 2Lecturer Roll No. : 15

ToDepartment of pharmaceutics B. S. Patel pharmacy college

Saffrony institute of technology Linch, mehsana.

2011-2011 1



INTRODUCTION

Bilayer tableting

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+

Bilayer tablets can be a primaryoption to avoid chemicalincompatibilities between API byphysical separation, and toenable the development ofdifferent drug release profiles(immediate release withextended release)1.



ADVANTAGES

Release of both drugs starts immediately

Combination of incompatible drugs2

Physical/chemical incompatibility can be prevented by physical

separation of two drugs.

Combination of different release profiles

Immediate release and sustained release profile can be achieved in

single tablet by forming IR layer and SR layer.

Reduced Pill Burden

By reducing individual dose of two drug due to their additive effect.

Example: Salbutamol + Theophylline

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ADVANTAGES

4

Reduce the side effects Reduced by using one drug of thecombination for this purpose2.

Amiloride may prevent hypokalemia caused by

hydrochlorthiazide19, 20

Elegance to the product



ADVANTAGES

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Hypertension

Heart Disease

Diabetes

Hyperlipidemia

Obesity

Co-morbid Conditions2

Co-morbid Conditions means pertainingto a disease or other pathological processthat occurs simultaneously with another18.

Treat different ailments in the same

patient (co-morbidity), at the same time andwith one pill

Example: Combination of β- blocker and ACE

inhibitor or Diuretics is beneficial to treat

Hypertention and Heart failure.

Only Allows for synergistic combination



IDEAL CANDIDATE OF BILAYER TABLETS

Drug produces additive/synergistic effect

Anti- asthmatic: Salbutamol + Theophylline

Drugs having opposite side effects, may reduce the side effect

Omeprazole + NSAIDS

Hydroclorothiazide + Amiloride

Incompatible drugs

Low biological half life (ideal for modified release bilayer)

Unstable at intenstinal pH ( ideal for bilayer floating)

High first pass metabolism with low biological half life (ideal forbuccoadhesive bilayer)

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DIFFERENT TYPES

Bilayer modified release tabletExample:

Aceclofenac9 : NSAIDS, COX-2 inhibitor; t/2 = 3-4 hrs

Metoclopramide HCL + Ibuprofen13, 14:

Metoclopramide HCL is anti emetic; Given as immediate release

dose and Ibuprofen is NSAID; given as SR dose, due to its low t/2

(2 hrs).

This is widely used combination in treatment of migraine. It improve

the absorbance of Ibuprofen, whose absorption is less due to

gastric stasis10 especially in migraine.

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DIFFERENT TYPES Bilayer floating tablet

Example:

Rosiglitazone maleate6,7,8

Oral anti-diabetic; t/2 = 3-4 hrs; its solubility is decreased by

increasing pH.

Metoprolol Tartrate3,4,5

Β1-selective adrenergic blocker; t/2 = 3-4 hrs; it degraded in colon

Captopril11,12

ACE inhibitor; 37.5 – 75 mg dose is required in three times; most

stable at 1.2 pH.

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DIFFERENT TYPES Bilayer bucoadhesive tabletExample:

Propranolol HCL

Non-selective β-adrenergic blocker; t/2 = 3-5 hrs; high first passmetabolism.

Drug in buccoadhesive layer, Backing layer is consist of Ethyl

Cellulose.

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PRACTICAL PROBLEMS IN DEVELOPINGBILAYER TABLETS

What are Fixed Dose Combinations???15, 16, 17

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Maintenance Dose (A) =(KE × Minimum Effective

Concentration ×Vd)/1000(mg/hr)

Where, KE = elimination rate constant

Vd = volume of distribution

A = 0.693 × b ×h / t½ Where, b = Immediate release dose

h = time for releaset½ = biological half life



PRACTICAL PROBLEMS IN DEVELOPINGBILAYER TABLETS

Layer-separation

Order of layer sequence

Layer weight ratio

Elastic mismatch of the adjacent Layers

Cross contamination between layers.

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REFERENCE

1. Patel Mehul, et al; Challenges in the formulation of bilayered tablets: a

review. IJPRD; Vol. 2; 2010, 30-42.2. Pharmaceutical Development with Focus

on Paediatric formulations. WHO/FIP TRAINING WORKSHOP;28 April2008 – 2 May 2008.

3. Hoffman BB. Catecholamines, sympathomimetics drugs, and

adrenergic receptor antagonists. In: Hardman JG, Limbird LE, eds.Goodman and Gilman’s The Pharmacological Basis of Therapeutics.

10th ed. New York, NY: McGraw-Hill; 2001:255Y256.

4. Kendall MJ, Maxwell SR, Sandberg A, Westergren G. Controlledrelease metoprolol. Clinical pharmacokinetic and therapeutic

implications. Clin Pharmacokinet. 1991;21:319Y330.

5. Hwang SJ, Park H, Park K. Gastric retentive drug-delivery systems.Crit Rev Ther Drug Carrier Syst. 1998;15:243Y284.

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REFERENCE 6. J. E. F. Reynolds. Martindale-the extra Pharmacopoeia. Director of the

Council of Royal Pharmaceutical Society of Great Britain, 2005, 34:345.

7. G. K. McEvoy. AHFS Drug Information. Authority of the board of theAmerican Society of the Health-System Pharmacists, 2004, 3055-3058.

8. M. C. Chapel Sky, K. Thompson-culkin, A. K. Miller, et al.Pharmacokinetics of rosiglitazone in patients with varying degrees ofrenal insuffi ciency. J. Clin. Pharmacol., 2003, 43: 252-259.

9. British Pharmacopoeia 2005 v1983ol-1. P.No:40 & http/www .medindia.net/doctors/drug-information/aceclofenac htm.

10. http://en.wikipedia.org/wiki/Gastric_stasis

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REFERENCE 11. C. Dollery, Therapeutics Drugs, Churchill Livingstone, New York 1999,

pp. c38 –c43.12. N. H. Anaizi and C. Swenson, Instability of captopril solution, Am. J.

Hosp. Pharm. 50 (1993) 486 –488.

13. B. G. Wells, J. T. DiPiro, T. L. Schwinghammer, and C. W. Hamilton.Pharmacotherapy Handbook, McGraw-Hill, New York, 2006, pp. 535 –547.

14. Bhavesh Shiyani, Surendra Gattani and Sanjay Surana. Formulationand Evaluation of Bi-layer Tablet of Metoclopramide Hydrochloride andIbuprofen, AAPS PharmSciTech, Vol. 9, No. 3, September 2008, 818-827.

15. Deelip Derle, Omkar Joshi, Ashish Pawar, Jatin Patel, Amol Jagadale;

formulation and evaluation of buccoadhesive bi-layer tablet ofpropranolol hydrochloride. International Journal of Pharmacy and Pharmaceutical Sciences, Vol. 1, Issue 1, July-Sep. 2009; 206-212.

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REFERENCE 16. Gosh R., Modern concept in pharmacology and therapeutics, 24th

edition, Hilton and Co., p 761.

17. Chong H. Choe, Selim S. Bouhaouala, Itzhak Brook, Thomas B. Elliott,Gregory B. Knudson. In Vitro development of resistance to Ofloxacinand doxycycline in Bacillus anthracis sterne, Antimicrobial agents andchemotherapy. June 2000; 44(6): 1766.

18. Cedillo-Ramírez E, Villafuerte-Robles L, Hernandez-leon A Effect ofadded Pharmatose DCL11 on the sustained-release of metronidazolefrom Methocel K4M and Carbopol 971P NF floating matrices, Dev IndPharm 2001; 31(4): 200-208.

19. http://medical-dictionary.thefreedictionary.com/comorbid

20. http://congestive-heart-failure.emedtv.com/amiloride/side-effects-of-amiloride.html

21. http://blood-pressure.emedtv.com/hydrochlorothiazide/side-effects-of-hydrochlorothiazide.html

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THANK

YOU16

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