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Oral dosage form of tetrahydrocannabinol and a method of avoiding and/or suppressing hepatic first pass metabolism via targeted chylomicron/lipoprotein delivery

机译:四氢大麻酚的口服剂型和通过靶向乳糜微粒/脂蛋白递送避免和/或抑制肝首过代谢的方法

摘要

Self-emulsifying drug delivery systems are provided to improve dissolution, stability, and bioavailability of drug compounds of dronabinol or other cannabinoids. The drug compound(s) are dissolved in an oily medium (e.g. triglycerides and/or mixed glycerides and/or free fatty acids containing medium and/or long chain saturated, mono-unsaturated, and/or poly-unsaturated free fatty acids) together with at least one surfactant. The surfactant promotes self-emulsification, thereby promoting targeted chylomicron/lipoprotein delivery and optimal bioavailability through the mammalian intestinal tract. A dosage form can optionally include co-solvents, anti-oxidants, viscosity modifying agents, cytochrome P450 metabolic inhibitors, P-GP efflux inhibitors, and amphiphilic/non-amphiphilic solutes to induce semi-solid formation for targeted release rates.
机译:提供了自乳化的药物递送系统以改善屈大麻酚或其他大麻素的药物化合物的溶解,稳定性和生物利用度。药物化合物一起溶解在油性介质中(例如,甘油三酸酯和/或混合甘油酯和/或包含中链和/或长链饱和,单不饱和和/或多不饱和游离脂肪酸的游离脂肪酸)与至少一种表面活性剂。表面活性剂促进自我乳化,从而促进靶向乳糜微粒/脂蛋白的递送和通过哺乳动物肠道的最佳生物利用度。剂型可以任选地包括助溶剂,抗氧化剂,粘度调节剂,细胞色素P450代谢抑制剂,P-GP外排抑制剂和两亲/非两亲溶质,以针对目标释放速率诱导半固体形成。

著录项

  • 公开/公告号US9265724B2

    专利类型

  • 公开/公告日2016-02-23

    原文格式PDF

  • 申请/专利权人 RAM B. MURTY;SANTOS B. MURTY;

    申请/专利号US20100876292

  • 发明设计人 RAM B. MURTY;SANTOS B. MURTY;

    申请日2010-09-07

  • 分类号A61K31/352;A61P1/08;A61P25/06;A61P27/06;A61P25/22;A61P25/30;A61K9/107;A61K9/48;A61K31/353;A61K31/655;A61K47/10;A61K47/12;A61K47/14;A61K47/22;A61K47/44;

  • 国家 US

  • 入库时间 2022-08-21 14:30:21

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