Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, P.O. Box 12065, Jerusalem 91120, Israel.
Institute for Drug Research, School of Pharmacy, Faculty of Medicine, The Hebrew University of Jerusalem, P.O. Box 12065, Jerusalem 91120, Israel.
Int J Pharm. 2020 May 15;581:119276. doi: 10.1016/j.ijpharm.2020.119276. Epub 2020 Mar 31.
Delivery of drugs through oral mucosa enables bypass of the gastrointestinal tract and "first pass" metabolism in the liver and the gut. Thus, a higher and less variable bioavailability can be obtained. Mechanisms of this administration route for cannabidiol were investigated in the current research in pigs. Results show that cannabidiol has substantially low permeability rate over 8 h through oral mucosa and accumulates significantly within it. Furthermore, following the removal of the delivery device, residual prolongation of release from the oral mucosa into systemic blood circulation continues for several hours. This method of delivery enabled acquisition of clinically relevant plasma levels of cannabidiol. The absorption profile indicates that cannabidiol, as well as other lipophilic molecules, should be delivered through oral mucosa for systemic absorption from a device that conceals the drug and prevents its washout by the saliva flow and subsequent ingestion into gastrointestinal tract.
药物经口腔黏膜给药可绕过胃肠道和肝脏及肠道的“首过”代谢。因此，可以获得更高且更稳定的生物利用度。本研究旨在探讨大麻二酚经口腔黏膜给药的机制。结果表明，8 小时内大麻二酚经口腔黏膜的渗透速率极低，且在口腔黏膜内大量蓄积。此外，给药装置去除后，药物仍会在数小时内从口腔黏膜持续缓慢释放至全身血液循环。该给药方式可使大麻二酚达到临床相关的血浆水平。吸收特征表明，对于亲脂性分子如大麻二酚，应该使用能够隐匿药物、防止唾液冲刷和随后吞入胃肠道的给药装置，通过口腔黏膜给药以实现全身吸收。
