Pharmacokinetics of sinomenine hydrochloride cubic liquid crystal injection based on microdialysis technology

摘要

Objective: The purpose of this study was to develop an injectable in situ liquid crystal formulation for intra-articular administration and evaluate its pharmacokinetics characteristics on Microdialysis Technology. Method: The cubic liquid crystal precursor (CLCP) was prepared on GMO/water system containing sinomenine hydrochloride (SH). Using a self-made SH solution as a control group, the male SD rats were used as the model animals to establish a microdialysis technique to dynamically sample blood and joint cavity of rats and to detect the pharmacokinetic behavior of SH-loaded CLCP. Samples were collected and then analyzed off-line by an UPLC instrument equipped with a mass spectrometer (LC/MS). Results: The pharmacokinetic study showed that the CLCP group could effectively reduce drug leakage into the blood circulation, and its AUC and C_(max) were both lower than that of the control group. The results of local pharmacokinetic study in rat articular cavity showed the t_(1/2), t_(max), and MRT of the CLCP group were significantly longer, and AUC of the CLCP group was 1.9 times higher than that of solution group. Conclusion: The CLCP group has a certain sustained-release effect, and a long retention time in vivo and fewer drugs entering the whole body, which is more conducive to the local effect of the joint cavity.