Abstract
The aims of this study are (1) to compare the disintegration efficiency, and (2) to develop a discriminating test model for the 3 classes of superdisintegrants represented by Ac-Di-Sol, Primojel, and Polyplasdone XL10. Using a digital video camera to examine the disintegration process of tablets containing the same wt/wt percentage concentration of the disintegrants, Ac-Di-Sol was found to disintegrate tablets rapidly into apparently primary particles; Primojel also apparently disintegrated tablets into primary particles but more slowly; Polyplasdone XL10 disintegrated tablets rapidly but into larger masses of aggregated particles. The differences in the size distribution generated in the disintegrated tablets likely contribute to the drug dissolution rate differences found for aspirin tablets with similar disintegration rates. The aspirin tablet matrix is proposed as a model formulation for disintegrant efficiency comparison and performance consistency testing for quality control purposes.
Keywords: Superdisintegrants, aspirin tablet, disintegration, dissolution test
Full Text
The Full Text of this article is available as a PDF (192.0 KB).
References
- 1.Bi YX, Sunada H, Yonezawa Y, Danjo K. Evaluation of rapidly disintegrating tablets prepared by a direct compression method. Drug Dev Ind Pharm. 1999;25:571–581. doi: 10.1081/DDC-100102211. [DOI] [PubMed] [Google Scholar]
- 2.Sallam E, Ibrahim H, Abu Dahab R, Shubair M, Khalil E. Evaluation of fast disintegrants in terfenadine tablets containing a gas-evolving disintegrant. Drug Dev Ind Pharm. 1998;24:501–507. doi: 10.3109/03639049809085650. [DOI] [PubMed] [Google Scholar]
- 3.Bi Y, Sunada H, Yonezawa Y, et al. Preparation and evaluation of a compressed tablet rapidly disintegrating in the oral cavity. Chem Pharm Bull (Tokyo) 1996;44:2121–2127. doi: 10.1248/cpb.44.2121. [DOI] [PubMed] [Google Scholar]
- 4.Massimo G, Catellani PL, Santi P, et al. Disintegration propensity of tablets evaluated by means of disintegrating force kinetics. Pharm Dev Technol. 2000;5:163–169. doi: 10.1081/PDT-100100531. [DOI] [PubMed] [Google Scholar]
- 5.Caramella C, Colombo P, Conte U, et al. Water uptake and disintegrating force measurements: towards a general understanding of disintegration mechanisms. Drug Dev Ind Pharm. 1986;12:1749–1766. doi: 10.3109/03639048609042607. [DOI] [Google Scholar]
- 6.Johnson JR, Wang LH, Gordon MS, Chowhan ZT. Effect of formulation solubility and hygroscopicity on disintegrant efficiency in tablets prepared by wet granulation, in terms of dissolution. J Pharm. Sci. 1991;80:469–471. doi: 10.1002/jps.2600800514. [DOI] [PubMed] [Google Scholar]
- 7.Pandit JK, Tripathi MK, Babu RJ. Effect of tablet disintegrants on the dissolution stability of nalidixic acid tablets. Pharmazie. 1997;52:538–540. [Google Scholar]
- 8.Sakr A, Bose M, Menon A. Comparative effectiveness of superdisintegrants on the characteristics of directly compressed triamterene hydrochlorothiazide tablets. Pharm Ind. 1993;55:953–957. [Google Scholar]
- 9.Chen CR, Cho SL, Lin CK, Lin YH, Chiang ST, Wu HL. Dissolution difference between acidic and neutral media of acetaminophen tablets containing a super disintegrant and a soluble excipient. II. Chem Pharm Bull (Tokyo). 1998;46:478–481. doi: 10.1248/cpb.46.478. [DOI] [PubMed] [Google Scholar]
- 10.Zhao N, Augsburger LL. The influence of swelling capacity of superdisintegrants in different pH media on the dissolution of hydrochlorothiazide from directly compressed tablets. AAPS PharmSciTech. 2005;6:E120–E126. doi: 10.1208/pt060119. [DOI] [PMC free article] [PubMed] [Google Scholar]
- 11.Gordon MS, Rudraraju VS, Dani K, Chowhan ZT. Effect of the mode of super disintegrant incorporation on dissolution in wet granulated tablets. J Pharm Sci. 1993;82:220–226. doi: 10.1002/jps.2600820222. [DOI] [PubMed] [Google Scholar]
- 12.United States Pharmacopeia, 27th revision. Rockville, MD: USP Convention, Inc; 2004. pp. 2302–2302. [Google Scholar]
- 13.Rizk S, Barthelemy C, Duru C, Guyot-Herman AM. Investigation on a new modified USP xanthan with tablet-disintegrating properties. Drug Dev Ind Pharm. 1997;23:19–26. [Google Scholar]
- 14.Chang RK, Shinwari M, Leonzio M, Wu LS, Hussain MA. Evaluation of the disintegrant properties for an experimental, crosslinked polyalkylammonium polymer. Int J Pharm. 1998;173:87–92. doi: 10.1016/S0378-5173(98)00218-X. [DOI] [Google Scholar]
- 15.Colombo P, Conte U, Caramella C, Geddo M, Manna A. Disintegrating force as a new formulation parameter. J Pharm Sci. 1984;73:701–705. doi: 10.1002/jps.2600730531. [DOI] [PubMed] [Google Scholar]
- 16.Zhao N, Augsburger LL. On the development of a disintegrating functionality test for superdisintegrants. AAPS PharmSci. 2003;5:M1256–M1256. [Google Scholar]
- 17.Shah U, Augsburger LL. Evaluation of the functional equivalence of crospovidone NF from different sources. 2. Standard performance test. Pharm Dev Technol. 2001;6:419–430. doi: 10.1081/PDT-100002250. [DOI] [PubMed] [Google Scholar]
- 18.Zhao N. Investigation of Super Disintegrant Functionality and Development of Discriminating Test Methods [dissertation] Baltimore, MD: University of Maryland; 2005. [Google Scholar]