Development of novel sibutramine base-loaded solid dispersion with gelatin and HPMC: physicochemical characterization and pharmacokinetics in beagle dogs

International Journal of Pharmaceutics
Hyun-Tae LimHan-Gon Choi

Abstract

To develop a novel sibutramine base-loaded solid dispersion with enhanced solubility and bioavailability, various solid dispersions were prepared using a spray drying technique with hydrophilic polymers such as gelatin, HPMC and citric acid. Their solubility, thermal characteristics and crystallinity were investigated. The dissolution and pharmacokinetics of the sibutramine base-loaded solid dispersion were then compared with a sibutramine hydrochloride monohydrate-loaded commercial product (Reductil). The solid dispersions prepared with gelatin gave higher drug solubility than those prepared without gelatin, irrespective of the amount of polymer. The sibutramine base-loaded solid dispersions containing hydrophilic polymer and citric acid showed higher drug solubility compared to sibutramine base and sibutramine hydrochloride monohydrate. Among the formulations tested, the solid dispersion composed of sibutramine base/gelatin/HPMC/citric acid at the weight ratio of 1/0.8/0.2/0.5 gave the highest solubility of 5.03+/-0.24 mg/ml. Our DSC and powder X-ray diffraction results showed that the drug was present in an altered amorphous form in this solid dispersion. The difference factor (f(1)) values between solid dispersion and comme...Continue Reading

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Citations

Jan 7, 2014·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Jung Hyun ChoHan-Gon Choi
Apr 23, 2013·Drug Development and Industrial Pharmacy·Dong Hoon OhHan-Gon Choi
Sep 12, 2012·Drug Development and Industrial Pharmacy·Kwan Hyung Cho, Han-Gon Choi
Jul 24, 2012·International Journal of Pharmaceutics·Amrit PaudelGuy Van den Mooter
Aug 27, 2015·Drug Delivery and Translational Research·Dinesh Kumar MishraPradyumna Kumar Mishra
Sep 24, 2013·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Chau Le-Ngoc VoBeom-Jin Lee
Oct 27, 2017·Pharmaceutical Development and Technology·Ahmed H IbrahimAhmed M Samy
Mar 18, 2016·Archives of Pharmacal Research·Dong Wuk KimHan-Gon Choi

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