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Inclusion of Amiloride Hydrochloride in Microporous Accurel MP 1000: Effect of solvents, drug loading and in vitro release | Abstract
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Abstract

Inclusion of Amiloride Hydrochloride in Microporous Accurel MP 1000: Effect of solvents, drug loading and in vitro release

Author(s): Gaurav Ahuja and Kamla Pathak*

The project was aimed at development of amiloride hydrochloride adsorbates using microporous accurel MP1000 to achieve controlled release floating system of highly water soluble drug. Of the four different methods used for preparing drug loaded adsorbates the method, stirring followed by vacuum using dichloromethane as the drug loading solvent was optimized after pharmacotechnical evaluation of the adsorbates (A1-A16). The polarity of solvent used for drug loading, drug loading methodology and surface properties of the adsorbent demonstrated crucial effect on adsorption and therefore on the release of drug from the porous carrier. Adsorbate A15 demonstrated highest drug content, maximum drug release and highest zeta potential (ζ = 2.92). A15 was characterized for solid state analysis by DSC, FTIR, SEM and PXRD and the studies revealed physical deposition of drug crystals in the micropores of adsorbent without chemical interaction. The optimized adsorbate when developed into a directly compressible tablet resulted in a formulation that exhibited zero order release (r2= 0.9985) of highly water soluble drug and remain floated for 6 hr. Dissolution of drug was realised as the main mechanism of drug release.


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