Pharmaceutical research of Ligusticum chuanxiong oil microcapsule analgesic gel patch by D-optimal mixture design / 中草药

ABSTRACT

Objective: The volatile oil of Ligusticum chuanxiong was made into microcapsule as intermediate and applied to gel paste to solve the instability characteristics of L. chuanxiong oil (LCO). The formulation and in vitro transdermal rate were optimized and the pharmacodynamics was preliminary studied. Methods: D-optimal mixture design was adopted, and initial adhesion, adhesion holding and peeling strength were used as evaluation indexes to optimize the preparation process. The in vitro transdermal behavior of ligustilide was studied by Franz in vitro transdermal test instrument. The efficacy was evaluated by acetic acid writhing experiment. Results: The optimal prescription of LCO microcapsule analgesic gel patch was as follow NP700, glycerin, hydroxyaluminum, kaolin, azone, tartaric acid, microcapsule PVPK30, 0.5% capom 940 was 1.250, 5.000, 0.025, 0.250, 0.600, 0.025, 1.000, and 2.700 g, respectively. Ligustilide transdermal rate in the gel patch was 5.129 7 μg/(cm2∙h). The retention rate of high temperature, high humidity and strong light irradiation on the 5th and 10th day was 93.17%, 91.21%, 98.94%, 92.36%, 68.03%, and 60.78%, respectively, and the analgesic rate was 63.14%. Conclusion: The optimal prescription of the gel patch had good viscosity, which solved the problem that ligustilide was difficult to be applied to the gel patches due to the instability of LCO and provided a reference for the application of volatile oil to new dosage forms such as gel patch.