Abstract

SOLUBILITY ENHANCEMENT OF POORLY WATER-SOLUBLE DRUG NIFEDIPINE FOR PARENTERAL ROUTE OF ADMINISTRATION

Riha Patel*, B. K. Dubey, Mansi Gupta and Deepak Basedia

.

Abstract

The aim of the present research study was to explore the possibility of employing mixed hydrotropic solubilization technique in the formulation and evaluation of aqueous parenteral of a poorly watersoluble drug. In the present study, slightly water-soluble drug, nifedipine was tried to solubilize by employing the combination of physiologically compatible hydrotropic agents to attempt its parenteral and oral liquid formulations. The aqueous solubility of a nonelectrolyte can be increased by a variety of techniques. The first step in selecting a method of solubilization is to determine why the drug is insoluble. The easiest way to determine whether DD is a determinant of the drug’s insolubility is to look at its melting point. If MP > 200°C, DD is probably a factor significant in reducing the solubility whereas if MP > 300°C, DD is a major factor. As stated above, each 100°C increase in melting point above 25°C corresponds to at least a 10-fold decrease in solubility. If the drug is a liquid or if it melts below 100°C, it is not likely that crystal interactions have any significant effect on solubility. Nifedipine, the prototype of the dihydropyridine class of calcium channel blockers (CCBs), is similar to other dihydropyridines including amlodipine, felodipine, isradipine, and nicardipine. There are at least five different types of calcium channels in Homo sapiens: L-, N-, P/Q-, R- and T-type. CCBs target L-type calcium channels, the major channel in muscle cells that mediates contraction. Similar to other DHP CCBs, nifedipine binds directly to inactive calcium channels stabilizing their inactive conformation. Since arterial smooth muscle depolarizations are longer in duration than cardiac muscle depolarizations, inactive channels are more prevalent in smooth muscle cells.

Keywords: Solubilization, Nifedipine, Calcium Channel Blockers, Solubility enhancers, Phase solubility analysis, Excess solute method.