Preparation And Quality Evaluation Of Osthole Liposome Gel

Fructus Cnidii and its compound preparation used to cure skin itch,vulva eczema, woman pruritus vulvae, trichomonad sex vaginitis disease [1], due to the traditional formulation and preparation process of the inherent limitations, which restricts the development and utilization of the resources of Fructus Cnidii, is now listed as traditional compound preparation [2] and formulations exist Fructus Cnidii in high dosage, low content of effective component [3]. Liposomes with similar biological membrane structure can increase the difficult soluble drugs retention in the skin.It intends to develop new dosage forms,common cnidium fruit element liposome gel through optimizing prescription component and preparation technology and drug’s transdermal absorption and in vitro drug release test to evaluate cnidium monnieri element performance of liposome gel for relieving itching anti-inflammatory drugs cnidium monnieri follow-up development lay the foundation of the liposome gel, in order to further explore the therapeutic effect of fructus cnidii element for relieving itching anti-inflammatory mechanism provides material basis.1. To establish minicolumn centrifugation method for the determination of osthole liposome encapsulation rate. Methods: the establishment of osthole liposome method for the analysis of liposomes, homemade cnidiadin liposome, and using Sephadex G-25 micro gel column separation of the liposomes and free drug, Preferred fruits of osthole liposome encapsulation rate determination method. The results show that the established experimental method was stable and feasible, at 1500 r/min centrifugal 3min condition, micro column can basically meet the separation of osthole liposomes and free drug. Conclusion: the established method is stable and feasible, Sephadex G-25 micro column gel method is convenient and fast determination of osthole liposome encapsulation efficiency.2. To optimize osthole liposome prescription, and to evaluate its quality. Methods: Osthole liposomes were prepared by thin-film evaporation method. Based on the single factor test,we using central composite design-response surface methodology, and establish a multiple quadratic regression model equation with the entrapment rate as the dependent variable, and soy lecithin concentration,ratio of lipid to drug and surfactant content as the independent variables. Response surface method was used to predict and valiadate the optimal prescription. Results: The optimal preparation condition was as follows :soy lecithin concentration was 24.93mg?mL-1, ratio of lipid to drug was 22.66:1(mg?mg-1),and surfactant content was 1.67%.Under the conditions, the average entrapment rate of the three products was 94.7%. Conclusion: It is high predictive to optimize the preparing technology of osthole liposome by using single factor experiments combined with central composite design and response surface method, and the prepared osthole liposome is of high encapsulation efficiency.3. To prepare osthole liposome gel, and in vitro transdermal experiment. Methods: osthole liposome dispersed in the gel matrix of preparation of osthole liposomal gel agent, using Franz diffusion cell method respectively of osthole liposome suspension, cnidiadin liposome gel, Fructus Cnidii plain gel in vitro transdermal experiment, using high performance liquid chromatography determination to mensurate the cumulative release amount and skin storage allowance of osthole. Results: cnidiadin liposome gel and conventional gel through skin rate was higher than that of liposome, and Osthol liposomal gel 24 h after cutaneous drug storage higher than conventional gel and liposome suspension. Conclusion: osthol dispersed in the matrix of drug release have auxo-action and medicine is prepared by liposome and then dispersed in the gel matrix, will likely play a long-acting slow-release effect, also can increase the residence time of drug in the skin.4. To investigate the osthole liposome gel in vitro release experiments, and to evaluate its quality and stability. Methods: on the traits of osthole, content, centrifugal state, PH value were investigated. Optimize the in vitro release experiment conditions, in vitro release test was used to evaluate the osthole liposomal gel stability in 5, 15 and 30 days. Results: cnidiadin liposome gel drug release process with the Higuchi equation, and in 30 days is basically stable. Conclusion: osthole liposome gel is stable, and is worthy of further development.