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含Δ9-四氢大麻酚的羟丙基纤维素聚合物基质系统的温度稳定性和生物粘附特性

Temperature stability and bioadhesive properties of delta9-tetrahydrocannabinol incorporated hydroxypropylcellulose polymer matrix systems.

作者信息

Repka Michael A, ElSohly Mahmoud A, Munjal Manish, Ross Samir A

机构信息

Department of Pharmaceutics, School of Pharmacy, The University of Mississippi, University, MS 38677-1848, USA.

出版信息

Drug Dev Ind Pharm. 2006 Jan;32(1):21-32. doi: 10.1080/03639040500387914.

Abstract

The purpose of this study was to determine and compare the bioadhesive profiles of hydroxypropylcellulose (HPC) polymer matrices as a function of delta9-tetrahydrocannabinol (THC) content. In addition, the effect of processing temperature on the stability of THC and its extent of degradation to cannabinol (CBN) was investigated. A hot-melt cast molding method was used to prepare HPC polymer matrix systems incorporated with THC at 0, 4, 8, and 16 percent. Bioadhesive measurements including peak adhesive force, area under the curve, and elongation at adhesive failure were recorded utilizing the TA.XT2i Texture Analyzer. Data obtained from these tests at various contact time intervals suggested that the incorporation of THC led to an increase in the bioadhesive strength of the HPC polymer matrices. To determine the stability of THC and the resulting CBN content in the matrices, three different processing temperatures were utilized (120, 160, and 200 degrees C). Post-production High Performance Liquid Chromotography (HPLC) analysis revealed that the processed systems contained at least 94% of THC and the relative percent formation of CBN was 0.5% at 120 degrees C and 0.4% at 160 degrees C compared to 1.6% at 200 degrees C. These findings indicate that the cannabinoid may be a plausible candidate for incorporation into systems utilizing hot-melt extrusion techniques for the development of an effective mucoadhesive transmucosal matrix system for delivery of THC.

摘要

本研究的目的是确定并比较羟丙基纤维素(HPC)聚合物基质的生物粘附特性与δ9-四氢大麻酚(THC)含量之间的关系。此外,还研究了加工温度对THC稳定性及其降解为大麻酚(CBN)程度的影响。采用热熔浇铸成型法制备了分别含有0%、4%、8%和16%THC的HPC聚合物基质系统。利用TA.XT2i质构分析仪记录生物粘附测量值,包括峰值粘附力、曲线下面积和粘附破坏时的伸长率。在不同接触时间间隔下从这些测试中获得的数据表明,加入THC会导致HPC聚合物基质的生物粘附强度增加。为了确定基质中THC的稳定性以及由此产生的CBN含量,采用了三种不同的加工温度(120℃、160℃和200℃)。生产后的高效液相色谱(HPLC)分析显示,加工后的系统中至少含有94%的THC,CBN的相对生成百分比在120℃时为0.5%,在160℃时为0.4%,而在200℃时为1.6%。这些发现表明,大麻素可能是利用热熔挤出技术开发用于递送THC的有效粘膜粘附性透粘膜基质系统的一个合理候选物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2e40/2921171/5b66c612f3b2/nihms224624f1.jpg

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