Evaluations of the Mechanism of Disintegrant Action

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Abstract
The disintegrant properties of eight tablet disintegrants (a cation exchange resin, cross-linked carboxymethyl cellulose, sodium starch glycolate, U.S.P., Crospovidone, U.S.P., corn starch, an insoluble anionic cellulose polymer, a modified food starch, and a soybean cellulose derivative) have been evaluated. Three techniques were applied to some or all of the materials. Water uptake rates and capacities were determined for all disintegrants in bulk powders. Disintegration times of tablets formulated with varying concentrations of the different disintegrants in a matrix comprising 75% unmilled dibasic calcium phosphate dihydrate and 25% anhydrous lactose were measured. For four disintegrants, a novel computer assisted cinsphotomicrographic technique was applied to investigate the interaction of water with individual disintegrant particles, both in terms of swelling rate and maximum water capacity Comparative evaluation of tablet disintegrants and studies of the mechanism of disintegrant action have quite properly attracted the attention of a number of pharmaceutical scientists. (1–16) However, it is clear that at present there is no concensus concerning a general theory rationalizing disintegrant action and at least five separate mechanism have been proposed (1, 2, 4) In the present paper, the disintegrant action of eight disintegrants has been studied using three separate approaches. Firstly, the rate and capacity of the bulk powders to take up water and to swell as a result has been evaluated using an apparatus similar to that used by Nogami and coworkers (5). Secondly, the disintegration times of tablets containing varying concentrations of disintegrant and compressed using a matrix of 75% unmilled dibasic calcium phosphate dihydrate and 25% anhydrous lactose were determined in a manner similar to that described by Rudnic and his associates (6). Thirdly, the authors are able to report - apparently for the first time - the use of a new method for evaluating the rate and extent of swelling of individual units in an assembly of disintegrant particles. This method exploits a cinephotomicrographic technique in which groups of disintegrant particles are photographed under a microscope by a high speed movie camera with the resultant film being analyzed by a special computer technique which allows the size of both individual and all particles, in any given visual field, to be followed over the very short period of time which elapses during the interaction of the disintegrant particles with water. The results presented in this paper demonstrate that a combination of the three methods described above and, in particular, the computer assisted cinemicrophotographic technique allow considerable insight to be gained of the disintegration process

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