SOLUBILITY ENHANCEMENT OF ATORVASTATIN BY DIFFERENT SOLUBILITY ENHANCEMENT TECHNIQUES -A COMPARISION STUDY.

Autor: Saiyed, Namira, Nathani, Charmi, Patel, Smit, Saduwala, Zinatakhtar, Ugle, Vedanshu, Patel, Mansi, Shah, Chainesh, Upadhyay, Umesh
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Zdroj: Pharma Science Monitor; Apr-Jun2023, Vol. 14 Issue 2, p39-54, 16p
Abstrakt: Atorvastatin is anti lipedimic drug. It belongs to class II under BCS and possess low oral bioavailability (< 26%) due to its poor aqueous solubility. purpose of study was to enhance aqueous solubility of Atorvastatin by three different approaches; solid dispersion, complexation and selfemulsification. solid dispersion was prepared by solvent evaporation method using poloxamer 188 as carrier. In complexation technique, inclusion complex of drug and β- cyclodextrin was formulated following solvent evaporation technique. In selfemulsification method soya bean oil, tween 80 and PEG 400 were used as oil, surfactants and co-surfactant respectively. prepared formulations were characterized for compatibility, solubility phase. In comparison to pure drug and physical mixtures of different carriers used, both drug solubility and its dissolution rate were significantly increased from different preparations. Among all methods solid dispersion (SD_ATN_3) containing drug: poloxamer188 in ratio of 1:4 showed rapid and higher drug release (88.36% within 45 min). in-vitro drug release data was fitted to various kinetic models and all formulations showed first order kinetics following super case II mechanism. increase in dissolution rate of Atorvastatin from solid dispersion of poloxamer 188 might be due to reduction of crystal size of drug, conversion of drug to amorphous or microcrystalline state and hence decreasing hydrophobicity of drug. increase in solubility of Atorvastatin was found in order; solid dispersion> complexation> selfemulsification > pure drug. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index