Excipients used in tablet

Part 2

Hydroxyl propyl methyl cellulose

• Hypermellose • As a food additive E464 • It is a semi synthetic inert polymer has many

uses

Uses in pharmaceutical industry• Used in oral tablet and capsule formulations– Depending on the grade as controlled release agent to

delay the release of a medicinal compound into the digestive tract

– Binder – Tablet coatings

• Used in ophthalmic solution– Substitute for tear-film– Lubricant – Hypromellose 2% solution has been documented to be

used during surgery to aid in corneal protection and during orbital surgery

Other uses

• Use in whole grain breads– Substitute for gluten in making all-oat and all-

barley breads– It is predicted that whole grain breads made with

HPMC will have cholesterol-lowering effects

Colloidal silicone dioxide

• Also called anhydrous silica

Uses

• Adsorbent • Anticaking agent• Emulsion stabilizer • Glidant• Suspending agent• Disintegrate • Thermal stabilizer• Viscosity increasing agent

Safety

• FDA approved for tablets, capsules,suspensions,transdermal preperation and vaginal ovules

• Preperations cotain it shouldn’t be used parentrally– It causes granulomas

Titanium dioxide

• E171• It is used as White pigment in film coating

tablet

Titanium dioxide and UV light

• It is a photocatalyst under ultraviolet (UV) light– Photocatalysis is the acceleration of a

photoreaction in the presence of a catalyst– The photocatalytic activity (PCA) depends on the

ability of the catalyst to create electron–hole pairs, which generate free radicals (hydroxyl radicals: ·OH) able to undergo secondary reactions

Uses • White pigment because of its brightness and very high

refractive index• Sunscreen and UV Absorber

– As pigment – A tattoo– Styptic pencils – Sunscreens designed for infants or people with sensitive skin

• based on titanium dioxide and/or zinc oxide, as these mineral UV blockers are believed to cause less skin irritation than chemical UV absorber ingredients

– The titanium dioxide particles used in sunscreens have to be coated with silica or alumina, because titanium dioxide creates radicals in the photocatalytic reaction• These radicals are carcinogenic and could damage the skin

Styptic pencil

• Hemostatic pencil• contains :– Anhydrous aluminum

sulfate– potassium alum – Titanium dioxide

• Works by causing blood vessels to contract at the site of the wound.

Safety

• FDA approved • Titanium dioxide dust, when inhaled, has recently

been classified by the International Agency for Research on Cancer (IARC) as an IARC Group 2B carcinogen possibly carcinogenic to humans

• Used in skin products has unknown health effects and has a carcinogenic effect on mice

• Incompatible with strong oxidizers and strong acids

Talc

• Mineral composed of hydrated magnesium silicate with

• Uses :– Talc is used in baby powder, an astringent powder

used for preventing rashes on the area covered by a diaper

– Glidant in food and pharmaceutical industry– Used as an additive for heroin, to expand volume and

weight• With intravenous use, it may lead to talcosis, a

granulomatous inflammation in the lungs

Safety

• FDA considers talc to be generally recognized as safe for use as an anti-caking agent in table salt in concentrations smaller than 2%

• inhalation of talc may causes ovarian and lung cancer

Polysorbate 80

• Nonionic surfactant and emulsifier derived from polyethoxylated sorbitan and oleic acid

• Other names:– Tween 80 – POE (80) sorbitan monooleate – E433

Pharmaceutical uses

• Used as an emulsifier in the manufacture of the popular anti-arrhythmic amiodarone

• Used to stabilize aqueous formulations of medications for parenteral administration

• It is also used as an excipient in some European and Canadian influenza vaccines

Other uses

• Emulsifier in foods, particularly in ice cream– Polysorbate is added to up to 0.5% (v/v)

concentration and makes the ice cream smoother and easier to handle, as well as increasing its resistance to melting

Safety • In Europe and America people eat about 0.1 g of polysorbate 80 in

foods per day• Influenza vaccines contain 0.000025 g of polysorbate 80 per dose• In general, polysorbate 80 is safe and well-tolerated, although a

small number of people are allergic to this substance • May be harmful to people with Crohn's disease• A 1993 study raised concerns that polysorbate 80 might decrease

fertility in rats• A 2008 study concluded that there was no observable adverse

effects at doses per body weight of up to 1.85 ml/kg·day, which is equivalent to a 70 kg person consuming about 140 g of this substance per day for 21 days

Starch pregelatinized

• Starch derivative • Prepared by physically, and chemically

treating native starch, thereby changing the properties of the starch and make it flowable and highly compressible

• Hygroscopic material

Uses

• Diluent • Disintegrant • Binder

Safety

• Non toxic non irritant matertial• Approved by FDA

Hydroxy propyl cellulose

• Derivative of cellulose with both water solubility and organic solubility

•

Uses

• As a food additive, HPC is used as a thickener, a low level binder and as an emulsion stabiliser

• It is used as a topical ophthalmic protectant and lubricant.

• In pharmaceuticals it is used as a – Disintegrant – Binder – Lubricant

Safety

• Non toxic non irritant matertial• Approved by FDA