الفهرس | Only 14 pages are availabe for public view |
Abstract Therapeutic effectiveness of a drug depends upon the bioavailability and ultimately upon the solubility of drug molecules. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Currently only 8% of new drug candidates have both high solubility and permeability. The objective of work in this thesis is to compare three different techniques used to enhance solubility and bioavailability using glibenclamide as a model of poorly water soluble drug. Glibenclamide (GBM) is a second-generation sulfonylurea oral hypoglycemic agent used in the treatment of non insulin dependent diabetes mellitus. It causes hypoglycemia by stimulating release of insulin from pancreatic cells and by increasing the sensitivity of peripheral tissue to insulin. Thus the work in this thesis is divided into four chapters: Chapter I: Enhancement of the solubility of glibenclamide by lyophilized dry emulsion technique Chapter II: Enhancement of the solubility of glibenclamide by surface solid dispersion technique Chapter III: Enhancement of the solubility of glibenclamide by liquisolid technique Chapter IV: Bioequivalence study of the selected glibenclamide formulations CHAPTER I Enhancement of the solubility of glibenclamide by lyophilized dry emulsion technique The aim of work in this chapter to enhance the solubility of glibenclamide using lyophilized dry emulsion technique. Eight formulae, each containing glibenclamide (5 mg/tablet) were proposed adopting a factorial design (23), in which three factors were tested. They were namely, type of surfactant (x1), type of oil (x2), and type of carrier (x3). Two types of surfactants were chosen; Tween 80 (low level (-1)) and Cremophor EL (high level (+1)). The oils were sesame oil (low level (-1)) and miglyol 812 (high level (+1)). Finally, carriers were lactose monohydrate (low level (+1)) and maltodextrin (high level (+1)). The lyophilized dry emulsion (LDE) tablets were obtained by freeze-drying the emulsions (o/w) containing GBM. The prepared emulsions prior. |