Dissolution enhancement of an insoluble drug by physical mixture with a superdisintegrant: optimization with a simplex lattice design

Pharm Dev Technol. 1996 Jul;1(2):159-64. doi: 10.3109/10837459609029890.

Abstract

The aim of the present work was to optimize a tablet formulation containing a physical mixture of a practically insoluble drug (prednisone) with a superdisintegrant (croscarmellose sodium) and two filler-binders characterized by differing water solubility (dicalcium phosphate dihydrate and anhydrous beta-lactose). Crushing strength, disintegration, and dissolution were measured for 10 formulations distributed over a factor space according to a simplex lattice design for a special cubic model. Multiple linear regression analysis was used to assess the best fit for each variable. The model predicted that increasing the amount of disintegrant to a critical amount (50%) would result in reduced disintegration time for dicalcium phosphate/beta-lactose ratios > 0.3, no changes in disintegration time for ratios < 0.3, and for all ratios an improvement in dissolution at 10 min. Crushing strength values of dicalcium phosphate increased with increasing disintegration concentration but not for beta-lactose tablets. The physical mixture of a practically insoluble drug with a superdisintegrant was confirmed as a valid approach to the improvement of dissolution, even in presence of other components. The solubility of the filler-binders influenced the minimum amount of disintegrant needed; when a soluble diluent was used, the amount of disintegrant required was reduced.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents / administration & dosage
  • Anti-Inflammatory Agents / chemistry*
  • Calcium Phosphates / chemistry*
  • Carboxymethylcellulose Sodium / chemistry*
  • Excipients / chemistry*
  • Hardness Tests
  • Kinetics
  • Lactose / chemistry*
  • Prednisone / administration & dosage
  • Prednisone / chemistry*
  • Regression Analysis
  • Solubility
  • Stearic Acids / chemistry
  • Tablets

Substances

  • Anti-Inflammatory Agents
  • Calcium Phosphates
  • Excipients
  • Stearic Acids
  • Tablets
  • alpha-tricalcium phosphate
  • tetracalcium phosphate
  • stearic acid
  • calcium phosphate, monobasic, anhydrous
  • calcium phosphate
  • Lactose
  • Carboxymethylcellulose Sodium
  • calcium phosphate, dibasic, anhydrous
  • Prednisone