PHYSICAL-PROPERTIES AND DISSOLUTION PROFILES OF TABLETS DIRECTLY COMPRESSED WITH BETA-CYCLODEXTRIN

In this study, β-CD was evaluated as a direct compression vehicle either singly or in blends with spray-dried lactose (sp.d.l.) for preparing tablets containing either phenobarbitone, diazepam, prednisolone or spironolactone. These drugs are examples of slightly soluble drugs forming inclusion complexes with β-CD in different molar ratios. Generally, it was found that β-CD and its combinations with sp.d.l. produced tablets having very good mechanical properties and higher dissolution rate. The uniformity of weight and thickness were good (coefficient of variation, c.v., less than 2%) for all formulations containing up to 60% β-CD, after which the c.v. exceeds 2%. In each drug formulation, the dissolution rate was progressively increased with the increase in β-CD concentration up to a certain limit after which the dissolution rate was not significantly changed or only slightly decreased. The dissolution rate of the selected drugs was improved by about 6-10-fold compared to that of tablets prepared by wet granulation or those containing 100% sp.d.l. The optimum formulation was found to vary from one drug to another depending upon its nature, dose and molar ratio of inclusion complex with β-CD. © 1990.