SUPERDISINTEGRANTS - A REVIEW

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SUPERDISINTEGRANTS

Sodium Starch Glycolate

(Primojel, Explotab)

Sodium starch glycolate is a super disintegrantmade from cross-linking sodium carboxymethylstarch. Sodium starch glycolates are generally spherical, a characteristic that accounts for their good flowability. The mechanism involves rapid absorption of water leading to an enormous increase in volume of granules result fast and uniform disintegration. The disintegrant efficiency of sodium starch glycolate is unimpaired in the presence of hydrophobic excipients, such as lubricants unlike many other disintegrants. Increasing the tablet compression pressure also appears to have no effect on disintegration time. It is used in tablets prepared by direct-compression as wel as wet-granulation processes. The usual concentration employed in a formulation is between 2% and 8%, with the optimum concentration about 4%, although in many cases 2% is sufficient.3-17


Croscarmellose Sodium

(Ac-Di-Sol, Primellose)

Croscarmellose sodium is derived from internally crosslinking a cellulose ether, sodium carboxymethylcellulose, which is a water soluble polymer. Cross linking makes it insoluble, hydrophilic, highly absorbent material, resulting in excellent swelling properties and its unique fibrous nature gives it excellent water wicking capabilities.  Croscarmellose sodium at concentrations up to 5% w/w may be used as a tablet disintegrant, although normally 2% w/w is used in tablets prepared by direct compression and 3% w/w in tablets prepared by a wet-granulation process.4-15


Crospovidone

(Polyplasdone XL, Kollidon CL)

Crospovidones are synthetic, cross linked homopolymers of N-vinyl-2-pyrrolidone. It is a water-insoluble tablet disintegrant and dissolution agent used at 2–5% concentration in tablets prepared by direct compression or wet- and dry-granulation methods. It rapidly exhibits high capillary activity and pronounced hydration capacity, with little tendency to form gels. In case of mouth-dissolving formulations, Crospovidone quickly wicks saliva into them to generate the volume expansion and hydrostatic pressures necessary to provide rapid disintegration in the mouth. When examined under a scanning electron  microscope, crospovidone particles appear granular and highly porous. This unique, porous particle morphology facilitates wicking of liquid into the tablet and particles to generate rapid disintegration. During tablet compression the crospovidone particles become highly deformed. As the deformed particles come in direct contact with water, the particles recover their normal structure and swell resulting in rapid volume expansion and high hydrostatic pressure that cause tablet disintegration. Due to its high crosslink density, crospovidone swells rapidly in water without gelling. Studies suggest that the particle size of crospovidone strongly influences disintegration of tablets. Larger particles provide a faster disintegration than smaller particles.2-15


Polacrilin Potassium

(Amberlite IRP88, Doshion P 544DS)

Polacrilin potassium is a mono functional minimally cross-linked carboxylic acid-exchange resin used in oral pharmaceutical formulations as a tablet disintegrant. Chemically, it is a partial potassium salt of a copolymer of methacrylic acid with divinyl benzene. It ionizes to an anionic polymer chain and potassium cations.  Concentrations of 2–10% w/w have been used as disintegrant, although 2% w/w of polacrilin potassium is usually sufficient. Polacrilin swells on hydration and disintegrates evenly, but does not dissolve or become cohesive, a feature commonly encountered with gums. It facilitates tablet compression for greater hardness and works equally well with hydrophilic as well as hydrophobic formulations. 8-14


Properties

Sodium Starch Glycolate

Croscarmellose Sodium

Crospovidone

Polacrilin Potassium

Mechanism

Swelling and wicking bothSwells 6-10 folds in <30  seconds

Swelling and wicking both. Swells 4-8 folds in <10 seconds.


Swelling and wicking both. Swells 7-12 folds in <30  seconds

Swelling and wicking both.

Particle Size Distribution

30-100µm

43-74µm

30-115µm

75-150µm

Gel Forming Tendency

Yes

Yes

No

Yes

Incompatibilities

Incompatible with ascorbic acid

Incompatible with strong acids or with soluble salts of iron and some other metals such as aluminum,

mercury, and zinc.

Forms molecular adducts in solution with sulfathiazole, sodium salicylate,

salicylic acid, phenobarbital, tannin, and other compounds

Incompatible with strong oxidizing agents, amines, particularly

tertiary amines

REFERENCES
1. Lachman L, Liberman HA, Schwartz jb, “Theory and Practice of Industrial Pharmacy”, Second Edition, Volume I, 1989, 173-177.
2. Chandrashekhara S., Deshmkh H, Nagesh C., Murade A, Usgaunkar S, “Superdisintegrants: A Recent Investigation and Current Approach”, Asian J. Pharm. Tech. 2012; Vol. 2: Issue 1, Pg 19-25
3. Mangal M, Thakral S, Goswami M, Ghai P, “Superdisintegrants: An Updated Review”, International Journal of Pharmacy and Pharmaceutical Science Research, 2012; 2(2) 26-35
4. Swarbrick J, “Encyclopedia of Pharmaceutical Technology” Third Edition, VOLUME 1, pg 3553
5. Shihora H, Panda S, “ Superdisintegrants, Utility in Dosage Forms: A Quick Review”, JPSBR: Volume 1, Issue 3: Nov Dec 2011, 148-153
6. Bhise S, Chaulang G, Patel P, Patel B, Bhosale A and Hardikar S, “Superdisintegrants as Solubilizing Agent”, Research J. Pharm. and Tech.2 (2): April.-June. 2009,
7. Rowe RC, Sheskey PJ, Quinn ME, “Handbook of Pharmaceutical Excipients” Sixth Edition, 2009, 206-506
8. Shakar AAM, Razzak SMI, Hossain M, Arif H and Reza1 S, “Effect of Superdisintegrants on Some Physical Attributes and Release Profile of Paracetamol Immediate Release Tablets”, Bangladesh Pharmaceutical Journal ,2012, 15(1): 89-94
9. Leskinen E, “Tablet disintegration: Effects of temperature and pH of aqueous disintegrating fluid and influence of solubility of diluent on the behaviour of superdisintegrants”, Department of pharmacy, University of Helsinki, 2003
10. Zimmer L, Belniak P, Szopa A, Poleszak E, “Superdisintegrants in New Solid Dosage Forms- A Review”, Sectio Ddd, 2011, Vol XXIV, N2, 10
11. Mrudula HB, Derle DV, “Mechanism of disintegrant action of polacrilin potassium: Swelling or wicking”, Acta Pharmaceutica Sinica B 2012;2(1):70–76
12. Mrudula HB, Derle DV, “Effect of Polacrilin Potassium as Disintegrant on Bioavailability of Diclofenac Potassium in Tablets : a Technical Note, AAPS PharmSciTech, Vol. 13, No. 3, September 2012
13. Chaudhary SA, Chaudhary AB, Mehta TA, “ Excipients Updates for Orally Disintegrating Dosage Forms”, Int. J. Res. Pharm. Sci. Vol-1,2010, Issue-2, 103-107
14. Srikanth MV, Sunil SA, Rao NS, Uhumwangho MU, and Murthy KVR, “ Ion-Exchange Resins as Controlled Drug Delivery Carriers”, Journal of Scientific Research, 2010, 2(3), 597-611
15. Camarco W, Ray D, Druffner A, “Selecting Superdisintegrants for Orally Disintegrating Tablet Formulations”, Pharmaceutical Technology, 2006
16. Sethi V, Shrivastava P, “ A Review Article On: Superdisintegrants”, Journal of Global Pharma Technology, 2012; 10(4):15-20
17. Kumar GP, Nirmala R, “Fundamental Aspects Of Superdisintegrants: A Concise Review”, Journal of Global Pharma Technology. 2012; 4(02): 1-12

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