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ABSTRACT:
The Poor Solubility of Drugs is a major problem which limits the development of highly potent pharmaceutics. Solubility Enhancement is one of the important parameters which should be considered for those drugs having poor aqueous solubility. Drugs belonging to Biopharmaceutical Classification System (BCS) class II are characterized by low aqueous solubility and high physiological permeability. Solid Dispersion Method Technique and Effervescence Assisted Solid Dispersion Techniques using Modified Fusion Method are the process to enhance the solubility of poorly water soluble drugs. In this work, BCS class-II drugs Clarithromycin was used as a model drugs, having poor solubility but high permeability is individually incorporated with Mannitol, Citric acid, and Sodium bicarbonate (Hydrophilic Carriers used as Excipients) in different ratio respectively. SDMs of Clarithromycin were prepared melting (Fusion) method using Mannitol. EASDs of Clarithromycin were prepared using Modified Fusion Method. Mannitol was melted and in this molten mannitol Citric acid (organic acid) was added and uniformly mixed by continuous stirring. Solubility of Drug Powders, Solid Dispersion, and EASDs was determined at 25 °C using shake flask method. The aqueous solubility of Clarithromycin were estimated using a U.V. spectrophotometer at 241nm (λmax). Scanning electron Micrographs, FTIR, DSC and PXRD CLN of drug powders, solid dispersion, and EASDs were compared. Scanning electron micrographs of EASDs showed better uniform distribution of drug particles in the carrier matrix. The present technique is better suitable for drugs having a low melting point or melt without charring. Effervescence assisted fusion technique of preparing solid dispersions can be employed for enhancing solubility of poorly soluble drugs.
KEYWORDS: EASDs, Solid dispersion, Clarithromycin, Solubility studies etc.
INTRODUCTION:
The enhancement of oral bioavailability of poorly water-soluble drugs remains one of the most challenging aspects of drug development.The major goals for enhancing solubility in order to achieve the site-specific action of the drug at the therapeutically optimal rate and dose regimen as well as to increase the aqueous solubility of poorly water soluble drugs1-5.
The present works deals with the preparation and characterization of Clarithromycin complex using solid dispersion technique and effervescence assisted solid dispersion technique by using modified fusion method for solubility enhancement. This technique is useful for those drugs which are poorly soluble in water. Clarithromycin, Fig. 1, is a semi-synthetic macrolide antibiotic...