PHARMACEUTICAL TABLETS.pptx

Unit II, Industrial Pharmacy
III Year , Semester - V

1. Pharmaceutical Tablets R.Vijayakumar Research Scholar Dept. of Pharmaceutical Technology Anna University, Tiruchirappalli.

2. Pharmaceutical Tablets Tablet is defined as a compressed unit solid dosage form containing medicaments with or without excipients. According to the IP , Pharmaceutical tablets are solid, flat / biconvex dishes, unit dosage form, prepared by compressing a drugs or a mixture of drugs, with or without diluents. They vary in shape, size and weight – Depends on dosage. Most popular dosage form and 70% of the total medicines are dispensed in the form of Tablet.

3. Advantages of the Tablet They are unit dosage form and offer the greatest capabilities Cost is lowest of all oral dosage form. Lighter and compact , Easiest and cheapest to package (Strip) Easy to swallowing with least tendency for hang‐up. Sustained release product is possible by enteric coating. Objectionable odour and bitter taste can be masked by coating technique. Suitable for large scale production. Greatest chemical and microbial stability over all oral dosage form. Product identification is easy.

4. Disadvantages of the Tablet Difficult to swallow in case of children and unconscious patients. Some drugs resist compression into dense compacts, owing to amorphous nature, low density character. Drugs with poor wetting, slow dissolution properties, optimum absorption high in GIT may be difficult to formulate. Bi tt er t e s t i ng drug s , drug s with an objectionable odo r. Drug s that a r e sensit i v e to oxygen may require encapsulation or coating. In such cases, capsule may offer the best and lowest cost.

5. Ideal p r opertie s of T abl e t A tablet shoul d h av e elegant p r oduct identity. Should h av e suf f icient st r e ngt h t o withstand mechanica l shoc k (In the process of production packaging, shipping and dispensing) Should have the chemical and physical stability to maintain its physical attributes over time. Able to release the medicinal agents in a predictable and reproducible manner. M u s t h av e a chemica l stabilit y o v er time - No al t e r atio n of the medicinal agents.

6. Types of Tablets Tablets ingested orally: Compressed tablet , - Paracetamol tablet M ultipl e c omp r e sse d tablet - Layered tablets R e p e a t actio n tablet Delayed release tablet, - Enteric coated Bisacodyl tablet Sugar coated tablet, - Multivitamin tablet Film coated tablet - Metronidazole tablet Chewable tablet, - Antacid tablet (B) Tablets used in oral cavity: Buccal tablet - Oral antimicrobial agents Sublingual tablet -Nitroglycerine T r oc hes o r l o z e n g es - cofsils Dental cone - Analgesics and antimicrobial drugs T abl ets adminis t e r ed b y other r o u t e: Implantation tablet Vaginal tablet, e.g. Clotrimazole tablet Tablets used to prepare solution: Effervescent tablet Dispensing tablet Hypodermic tablet Tablet triturates

7. Compressed tablet - Paracetamol tablet M ultipl e c omp r e sse d tablet - Layered tablets

8. Delayed release tablet, - Enteric coated Bisacodyl tablet Sugar coated tablet, - Multivitamin tablet

9. Chewable tablet, - Antacid tablet Sublingual tablet -Nitroglycerine

10. T abl e t Ing r edients In additio n t o act i v e ing r edient s , tablet c ontains a number of inert ma t e rial s kn o wn as addit i v es or e x cipient s .

11. Diluents Diluents are fillers used to make required bulk of the tablet when the drug dosage . To provide better tablet properties - improve cohesion, to permit use of direct compression manufacturing They must be commercially available in acceptable grade N on toxic l o w c os t P hysiologically inert P hysically & chemically stable by themselves & in combination with the drugs. F ree from all microbial contamination. Col or c ompatible They d o not al t er the bio a v ailability of dru g .

12. T ablet diluents - Example L a c t os e‐an h y d r ous and sp r a y drie d lac t ose Di r e ct l y c omp r essed sta r c h‐Sta R x 1 500 Hydrolyzed starch‐ Emdex and Celutab Mic r oc r y stalline c e llulos e‐ A vi c el ( P H 101and P H 1 2) Dibasi c calciu m phospha t e de h y d r a t e Calciu m sulpha t e di h y d r a t e Mannitol Sorbitol Sucrose‐ Sugartab , DiPac , Nutab Dextrose

13. Binder s & A dhes i v e s Thes e ma t e rials a r e added eithe r d r y or i n w e t‐ f o r m t o f o r m g r anules or t o f o r m c o he s i v e c om p a c ts f or di r ect l y c o mp r e ssed tablet. Example: Acacia, tragacanth‐ Solution for 10‐25% Conc. Cellulose derivatives‐ Methyl cellulose, Hydroxy propyl methyl cellulose, Hydroxy propyl cellulose Gelatin ‐ 10‐20% solution Glucose‐ 50% solution Polyvinylpyrrolidone (PVP)‐ 2% conc. Starch paste‐10‐20% solution Sodium algina t e Sorbitol

14. Disin t eg r ants A dde d t o a tablet f o r m u lat i on t o facilita t e it s b r eaking or disintegration when it contact with the GIT fluid . Example: Starch ‐ 5‐ 15 % of tablet weight. Starch derivative – Primogel and Explotab (1‐8%) Clays‐ Veegum HV, bentonite 10% level in colored tablet only Cellulose Cellulose derivatives‐ Ac‐ Di‐Sol (sodium carboxy methyl cellulose) Alginate PVP (Polyvinylpyrrolidone), cross‐linked

15. Superdisintegrants Swells up to ten fold within 30 seconds when contact water. Example: Crosscarmellose ‐ cross‐linked cellulose, Crosspovidone ‐ cross‐linked povidone (polymer) Sodium starch glycolate‐ cross‐linked starch. -These cross‐ linked products swell upto 10n fold with in 30 seconds when in contact with water. A portion of disintegrant is added before granulation and a portion.

16. Lubricant and Glidants Lubricants are intended to prevent adhesion of the tablet materials to the surface of dies and punches, reduce inter particle friction and m a y i mp r o v e the r a t e of f l o w of the tablet g r anulation. Lubricant s ‐ S t eari c a cid , S t eari c a ci d sal t ‐ S t eari c acid , M agnesium s t ea r a t e, T alc, PE G ( P o l y et hy lene gl y c ols), Surfactants Glidants are intended to promote flow of granules or powder material by reducing the friction between the particles. E x ample: Corn Starch – 5‐10% conc., Talc‐5% conc., Silica derivative ‐ Colloidal silicas such as Cab‐O‐Sil, Syloid , Aerosil in 0.25‐3% conc

17. Coloring agent The use of colors and dyes: Masking of off color drugs Product Identification Production of more elegant product All coloring agents must be approved and certified by FDA. Two forms of colors are used in tablet preparation – FD &C D & C dyes. These dyes are applied as solution in the granulating agent Example : FD & C yellow 6‐sunset yellow FD & C yellow 5‐ Tartrazine FD & C green 3‐ Fast Green FD & C blue 1‐ Brilliant Blue FD & C blue 2 ‐ Indigo carmine D&C red 3‐ Erythrosine. D&C red 22 – Eosin Y

18. Fl a v oring a g ents & Sw ee t enin g a g ents Fl a v oring a g ents: F or che w able table t ‐ F l a v or oil a r e used - Mint,Orange Sw ee t enin g a g ents: F or che w able tablets: Suga r , M anni t ol. Sa c c harine (arti f icial) : 500 tim e ’ s s w ee t er than suc r ose Disa dv anta g e: Bi tt er af t e rtas t e and ca r c ino g enic Aspartame (artificial) Disadvantage: Lack of stability in presence of moisture.

19. Granulation

20. T abl e t C omp r e ssion M a chi ne

21. T abl e t C omp r e ssion M a chi ne T abl ets a r e mad e b y c omp r essing a f ormulatio n c ontaining a dru g or drug s with e x cipients on stamping machine calle d p r esse s . B asic components of C omp r e ssion M a chi ne Hopper for holding and feeding granulation Dies that define the size and shape of the tablet. Punches for compressing the granulation within the dies. Ca m t r ack s f or guiding the m o v ement of the punche s . A feeding mechanism for moving granulation from hopper into the dies

22. E v al u at i on of T abl e t General Appearance Size & Shape Unique identification marking Organoleptic properties Hardness and Friability

23. Hardness Tester Friability: Friability of a tablet can determine in laboratory by Roche friabilator . This consist of a plastic chamber that revolves at 25 rpm, dropping the tablets through a Distance of six inches in the friabilator , which is then operate for 100 revolutions. The tablets are reweighed. Compress tablet that lose less than 0.5 to 1.0 % of the T abl et w ei g h a r e c o n s i d er a cc ept abl e.

24. Drug C on t e nt and R e l e as e : Weight Variation test Content Uniformity Test Disintegration Test (U.S.P.) Disintagration Testing apparatus ---

25. Dissolution T e st ( U .S. P .): Apparatus‐1: A single tablet is placed in a small wire mesh basket attached to the bottom of the shaft. The basket is immersed in a dissolution medium contained in a 900 ml flask. The flask is cylindrical with a hemispherical bottom. The flask is maintained at 37±0.5 C by a constant temperature bath. The motor is adjusted to turn at the specified speed and sample of the fluid are withdrawn at intervals to determine the amount of drug in solutions. Apparatus‐2: except the basket is replaced by a paddle.

26. Dissolution T e sting Apparatus

27. Problems in tableting Capping Lamination / Laminating Chipping Cracking Sticking / Filming Picking Binding Mottling Double impression