Multicomponent Pharmaceutical Adducts of alpha-Eprosartan: Physicochemical Properties and Pharmacokinetic Study

Khare Sawani G.; Jena Sunil K.; Sangamwar Abhay T.Khullar SadhikaMandal Sanjay K.

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Multicomponent Pharmaceutical Adducts of alpha-Eprosartan: Physicochemical Properties and Pharmacokinetic Study

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Pharmaceutical adducts of alpha-eprosartan (EPR) with nicotinamide (NIC) and p-hydroxy benzoic acid (PHB) were prepared by a liquid assisted grinding technique. Prior to conducting this study, the single crystal structure of EPR was determined. This study was designed: to improve the pH dependent solubility and dissolution rate of EPR and hence its oral absorption across the gastrointestinal tract. Initially, differential scanning calorimetry and powder X-ray diffraCtometty were used as a screening tool for rapid cocrystal or eutectic Mixture screening. The eutectic mixture of EPR with PHB in a 1:3 stoidhiometry ratio shows a better solubility and dissolution rate in all aqueous buffers as compared to EPR/NIC coctystals and pure EPR. The EPR/NIC cocrystal in a 1:1 stoichiotnetry ratio shows a better dissolution rate initially as compared to pure EPR but does revert back to EPR within the first 30 min in pH 1.2 ancl 6.8. Absorption and desorption profile of EPR adducts are reversible, suggesting no solid state transformation under experimental conditions. A significant increase in oral bioavailability in overnight fasted Sprague Dawley rats is achieved with the EPR/NIC cocrystal (2,4 -fold) and EPR/PHB eutectics (6.1 -fold), even when the cocrystal transformation is suspected based on in vitro studies.

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《Crystal growth & design》 |2017年第4期|1589-1599|共11页
作者
Khare Sawani G.; Jena Sunil K.; Sangamwar Abhay T.Khullar SadhikaMandal Sanjay K.;
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Natl Inst Pharmaceut Educ & Res, Sect 67, Dept Pharmacoinformat, Sas Nagar 160062, Punjab, India;

Natl Inst Pharmaceut Educ & Res, Sect 67, Dept Pharmaceut Technol Formulat, Sas Nagar 160062, Punjab, India;

Natl Inst Pharmaceut Educ & Res, Sect 67, Dept Pharmaceut, Sas Nagar 160062, Punjab, IndiaIndian Inst Sci Educ & Res Mohali, Sect 81, Dept Chem Sci, Sas Nagar 140306, Punjab, India;

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中图分类晶体学;
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Multicomponent Pharmaceutical Adducts of alpha-Eprosartan: Physicochemical Properties and Pharmacokinetic Study

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