Date of Award

2002

Degree Type

Thesis

Degree Name

Master of Science in Pharmaceutical Sciences

Specialization

Pharmaceutics

Department

Biomedical Sciences

First Advisor

Hossein Zia

Abstract

This study investigates a new method of converting a crystalline drug to its amorphous form and studying the effect this conversion has on the solubility of the drug. The physical form of the drug is of great importance in the process of taking a drug molecule from its discovery to its formulation into an acceptable dosage form. For oral solid dosage forms, the physical state of the drug molecule influences various important parameters including bioavailability and stability. Bioavailability in tum is governed by factors like dissolution and solubility, which can be altered to give desired results. A review of the various methods involved in solid state modifications is provided to enable the reader to comprehend the importance and extensive applications of these techniques in the field of preformulation and pharmaceutical dosage form development. This study uses a poorly water-soluble drug, cefuroxime axetil, and determines the effects the treatment processes have on its solubility. The processes differ in that one renders the drug totally amorphous while the other disrupts the crystalline structure to an extent where it is in a partially crystalline state. The varied purposes of polymers used in this study have also been investigated. Polymers have been used to enhance solubility, act as impurities in the crystal structure, and in solution as crystallization inhibitors. The results of this study show that appropriate processpolymer combinations can yield significant results for solubility enhancements.

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