Immediate-release dosage form; focus on disintegrants use as a promising excipient

Disintegrants are materials or mixtures of substances added in the drug formulations, which make easier dispersion or breakup of tablets and ingredients of capsules in small-scale particles for fast dissolution then it comes in contact with water in the GI tract. Immediate drug release dosage forms disintegrate rapidly after administration with an enhanced rate of dissolution. The superdisintegrants provide instantaneous disintegration of tablets after administration in the stomach. In this field, immediate-release liquid dosage forms and parenteral dosage forms have also been introduced for treating patients. The oral route is the most convenient route for the administration of solid dosage form, about 85% of solid dosage is administered by the oral route because of its advantages over others. The therapeutic activity of these formulations is obtained through a typical manner like disintegration followed by dissolution. Hence disintegration has a major role in facilitating drug activity. Diverse categories of superdisintegrants such as synthetic, semi-synthetic, natural, coprocessed blends, multifunctional superdisintegrants, etc. have been employed to develop effectual orodispersible tablets and to overcome the limitations of conventional tablet dosage forms. The objective of the present review article is to highlight the various kinds of traditional, Natural crude drugs containing gum and mucilage, Co-processed, semisynthetic and synthetic disintegrants along with a concentration in tablet and capsule disintegration and effect on drug release, which are being used in the formulation to provide the safer, effective drug delivery with patient compliance. Also highlights the mechanism and use of disintegrants in the immediate release dosage form.

Table 1: Traditional disintegrants

Sr. No.	Name of traditional disintegrants	Derivatives of disintegrants	Concentration % W/W	Mechanism of action	Ref
1	Starch	Starch USP Pregelatenized starch (1500) Sodium starch glycolate (explotab and primogel)	5-20 5-15 2-8	Swelling when it absorbs water, leading to faster disintegration of the tablet	50
2	Cellulose	Purified cellulose, Methylcellulose Carboxy methylcellulose Microcrystalline cellulose	5-10 2-10 5-10 10-20	ability to swell on contact with water	51
3	Alginate	Alginic acid Sdium alginate	1-5 2.5-10	Acts by swelling Fast wicking rate for water	56
4	Soy polysaccharides	Soy polysaccharides Emcosoy®	5-10	Rapid Dissolving	54
5	Chitin	Chitin and its deacetylated derivative chitosan	2-20	Mechanism of disintegration while dissolution related to swelling capacity.	52

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Kute VG, Patil RS, Kute VG, Kaluse PD, Immediate-release dosage form; focus on disintegrants use as a promising excipient, Journal of Drug Delivery and Therapeutics. 2023; 13(9):170-180
DOI: http://dx.doi.org/10.22270/jddt.v13i9.6217