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Development of a Novel Oral Micellar Formulation of Propofol

机译:新型异丙酚口服胶束配方的开发

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Propofol is a poorly soluble liquid anaesthetic drug available commercially as an emulsion for iv administration (Diprivan® Baxter Inc). Propofol has also been shown to display efficacy in the amelioration of intractable migraine and as a potential treatment for nausea and vomiting, indications for which liquid emulsions are not well suited. Here we describe the development of a solid formulation of propofol for oral administration that uses novel micellar technology to improve oral bioavailability. We first describe the formulation of propofol within polymeric micelles (PM) comprising amphiphilic block copolymers and go on to describe the preparation of a solid spray dried preparation suitable for compression or capsule filling. We report the ability of the micellar formulation to enable translocation of propofol across Caco-2 monolayers in vitro and present in vivo data demonstrating the enhanced oral bioavailability of propofol achieved by the formulation.
机译:丙泊酚是难溶性液体麻醉药,可作为乳剂静脉输注市售(Diprivan®Baxter Inc)。还显示丙泊酚在改善顽固性偏头痛方面具有显示功效,并且可作为恶心和呕吐的潜在疗法,这表明液体乳状液不适合使用。在这里,我们描述了使用新型胶束技术改善口服生物利用度的口服异丙酚固体制剂的开发。我们首先描述包含两亲性嵌段共聚物的聚合物胶束(PM)中丙泊酚的制剂,然后继续描述适用于压缩或胶囊填充的固体喷雾干燥制剂的制备。我们报告了胶束制剂能够使丙泊酚在体外跨Caco-2单层转运的能力,并提供了体内数据,证明了通过制剂实现的丙泊酚口服生物利用度的提高。

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