Pharmacophore an International Research Journal
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Open Access | Published: 2020 - Issue 5

Enhancement of Solubility and Dissolution of Clopidogrel Bisulfate by Solid Dispersion in Combination with Surface Adsorbent‎ Download PDF

Priyal Patel, Ashok Mahajan, NileeThakor

The main objective of this work was to prepare solid dispersion adsorbate to improve solubility, dissolution of poorly water-soluble drug Clopidogrelbisulfate. The various carriers like PEG 4000, PEG 6000, Poloxomer 188, and Locust bean gum were used to prepare solid dispersion of Clopidogrelbisulfate, having different ratios using two methods solvent evaporation and hot melt method. Clopidogrelbisulfate containing surface solid dispersion was prepared using different carriers in different ratios and Neusilin as adsorbent by using two solvent evaporation and hot melt methods. To determine the effect of formulation variables, 32 Factorial design was applied. The angle of repose, % DE30 and Q30 were selected as dependent variables. Using Design Expert software (version 7.0.0) the optimized batch of Clopidogrelbisulfate was derived statistically. The animal study of the optimized batch was performed using the Albino rat where bleeding time and blood volume were checked. In solid dispersion, PEG 4000 gave the highest amount of drug release (1:2 ratio of drug:polymer) compared to other carriers when prepared by the solvent evaporation method. The tablets containing Clopidogrelbisulfate, PEG 4000, and Neusilin in a ratio of 1:2:1 were considered as optimized formulation. The Clopidogrelbisulfate containing an optimized formulation of surface solid dispersion showed 85.69% drug release in 30 min. The conversion from crystalline to the amorphous form of Clopidogrelbisulfate was confirmed by XRD studies. From the platelet aggregation inhibition study, it was concluded that when the rat was treated with surface solid dispersion, the bleeding time and the collected blood volume increased.

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ISSN: 2229-5402

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