Formulation development studies on cyclodextrin complexation of BCS-Class II anti-diabetic drugs for controlled release

Abstract

ABSTRACT OF THE Ph. D THESIS ENTITILED newlineFORMULATION DEVELOPMENT STUDIES ON CYCLODEXTRIN COMPLEXATION OF BCS -CLASS II ANTI-DIABETIC DRUGS FOR newlineCONTROLLED RELEASE newlineThe overall objective of the present investigation is to design controlled release formulations in the form of microcapsules and matrix tablets of (i) glipizide and (ii) pioglitazone, two anti diabetic BCS Class II drugs. These two anti diabetic drugs required controlled release formulation owing to their short biological half lives and for better control of blood glucose levels to prevent hypoglycemia, to enhance clinical efficacy, to reduce gastrointestinal disturbances and to enhance patient compliance. Because low aqueous solubility and dissolution rate, these BCS Class II drugs (glipizide and pioglitazone) pose problems in the design of controlled release products. When these drugs are coated with or embeded in water imperivious polymers and materials in the design of controlled release products, the drug release rates are much reduced leading to inadequate blood levels and reduced bioavailability and therapeutic efficacy. In such cases enhancement in the solubility and dissolution rate of drugs before formulating them into controlled release products avoid the problem low release rates and inadequate blood levels. In the present study complexation of glipizide and pioglitazone with and#946;CD was tried to enhance the solubility and dissolution rate of these two poorly solubule drugs. The major objective of the investigation is to evaluate the feasibility of employing and#946;CD complexes in the design of controlled release microcapsules and matrix tablets of the selected BCS class II drugs for obtaining slow, controlled and complete drug release in 24 h. newlineThe complexation of glipizide and pioglitazone with and#946;CD was evaluated by phase solubility, DSC, XRD and FTIR studies.