Enhanced Solubility and Bioavailability of Sibutramine Base by Solid Dispersion System with Aqueous Medium

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概要

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• To develop a novel sibutramine base-loaded solid dispersion with improved solubility bioavailability, various solid dispersions were prepared with water, hydroxypropylmethyl cellulose (HPMC), poloxamer and citric acid using spray-drying technique. The effect of HPMC, poloxamer and citric acid on the aqueous solubility of sibutramine was investigated. The physicochemical properties of solid dispersion were investigated using scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and X-ray powder diffraction. The dissolution and pharmacokinetics in rats of solid dispersion were evaluated compared to the sibutramine hydrochloride monohydrate-loaded commercial product (Reductil®). The sibutramine base-loaded solid dispersion gave two type forms. Like conventional solid dispersion system, one type appeared as a spherical shape with smooth surface, as the carriers and drug with relatively low melting point were soluble in water and formed it. The other appeared as an irregular form with relatively rough surface. Unlike conventional solid dispersion system, this type changed no crystalline form of drug. Our results suggested that this type was formed by attaching hydrophilic carriers to the surface of drug without crystal change, resulting from changing the hydrophobic drug to hydrophilic form. The sibutramine-loaded solid dispersion at the weight ratio of sibutramine base/HPMC/poloxamer/citric acid of 5/3/3/0.2 gave the maximum drug solubility of about 3 mg/ml. Furthermore, it showed the similar plasma concentration, area under the curve (AUC) and Cmax of parent drug, metabolite I and II to the commercial product, indicating that it might give the similar drug efficacy compared to the sibutramine hydrochloride monohydrate-loaded commercial product in rats. Thus, this solid dispersion system would be useful to deliver poorly water-soluble sibutramine base with enhanced bioavailability.

著者

• Kim Young

  College of Pharmacy, Chungnam National University

• Li Dong

  College of Pharmacy, Yeungnam University

• Jang Ki-Young

  College of Pharmacy, Yeungnam University

• Kang Wonku

  College of Pharmacy, Catholic University of Daegu

• Bae Kyoungjin

  College of Pharmacy, Catholic University of Daegu

• Lee Mann

  College of Pharmacy, Catholic University of Daegu

• Oh Yu-Kyoung

  College of Pharmacy, Seoul National University

• Jee Jun-Pil

  College of Pharmacy, Seoul National University

• Park Young-Joon

  Research Center, Samil Pharmaceutical Co., Ltd.

• Oh Dong

  College of Pharmacy, Yeungnam University

• Seo Youn

  College of Pharmacy, Yeungnam University

• Kim Jong

  College of Pharmacy, Yeungnam University

• Woo Jong

  College of Pharmacy, Yeungnam University

• Yong Chul

  College of Pharmacy, Yeungnam University

• Choi Han-Gon

  College of Pharmacy, Yeungnam University

• Yong Chul

  College Of Pharmacy Yeungnam University

• Choi Han-gon

  College Of Pharmacy Yeungnam University

• Kang Wonku

  College Of Pharmacy Catholic University Of Daegu

• Kim Young

  College Of Pharmacy And Research Institute Of Pharmaceutical Science Seoul National University

• Kim Jong

  College Of Oriental Medicine Daegu Haany University

• Li Dong

  College Of Pharmacy Yeungnam University

• Kim Jong

  College Of Medicine Yeungnam University

• Kim Young

  Colledge of Pharmacy, Wonkwang University

• Li Dong

  College of Life Sciences, Hebei University

• Kim Young

  College of Pharmacy, Yeungnam University

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