RESUMO
OBJECTIVE: To explore the effect of phase transition process of compound L-carnitine plastics on the characters of transdermal absorption, provide a theoretical evidence for the penetration enhancing effect produced from phase transition process. METHODS: The accumulated transdermal percentage of capsaicin and L-carnitine were used as measurement indicators, the experiment was finished by improved Franz diffuser and disembodied rabbit skin, the content of different components in transdermal receiving solution and in skin that received in different time was determined by HPLC, the curve of transdermal was drawn been drawn, the rule and the characters of transdermal were analyzed. RESULTS: The transdermal dynamics curve before and after the phase transition of compound L-carnitine plastics is a kind of continuous function, while it become a kind of non-continuous function during the process of the phase transition. The 95% confidence interval of the parameters of transdermal velocity and amount between sample A with transdermal enhancer and sample B without transdermal enhancer shows overlap, the difference shows no statistical significance between sample A and B. It was showed that the sample A have the same transdermal rate and amount as B. While 95% confidence interval of the parameters of transdermal velocity and amount among sample A,B and C (without film-former materials) shows no overlap, the difference shows statistical significance among sample A,B and C. When the capsaicin was used as indicators, the transdermal rate of sample A and B respectively are 1.459 times and 1.450 times of C, the transdermal amount of sample A and B respectively are 2.53 times and 1.907 times of C. When the capsaicin was used as indicators, the transdermal rate of sample A and B respectively are 1.153 times and 1.169 times of C, the transdermal amount of sample A and B respectively are 1.722 times and 1.692 times of C. CONCLUSION: Phase transition process can significantly increase both transdermal rate and transdermal amount of compound L-carnitine plastics, the time increased by phase transition process correspond to film-former time of plastics, the penetration enhancing effect produced from phase transition process is far greater than the penetration enhancing effect produced from transdermal absorption penetration enhancers(P0.05).
RESUMO
Objective To prepare a new kind of preparation formulation of the total alkaloids from seed of Strychni Semen (TASS), by which could improve their drug loading content and the transdermal function. Methods TASS-LLCN were prepared by hot solvent and high pressure homogeneous method. Using encapsulation efficiency (EE) measured by ultrafiltration as index, the prescription of TASS-LLCN was optimized by response surface methodology with central composite design, and the basic properties of the optimized TASS-LLCN was evaluated. The Franz diffuser method was used to compare the transdermal capacity of both LLCN gel and ordinary gel of TASS. Results The best prescription of TASS-LLCN was as follow: the content of glycerin monooleate (GMO) was 1 403.19 mg/mL, the ratio between GMO and F127 was 7.25:1, the drug loading content was 9.48% and the predicted encapsulation efficiency was 64.01%. The evaluation of basic properties of the optimized TASS-LLCN showed that the average grain diameter was about 186 nm, zeta potential was -33.1 mV, pH was 6.83, the stability was good. The transdermal experiment in vitro showed that the cumulate osmotic quantities in 24 h and the permeation rate of TASS-LLCN gel were both better than ordinary gel of TASS, which had obvious discrepancy (P < 0.05) and showed that LLCN could promote the absorption of active components; the skin retention volume of LLCN gel was still bigger than ordinary gel, which showed that LLCN gel of TASS could store in the skin and release the drug sustainedly. Conclusion TASS-LLCN could obviously enhance the drug loading content and the transdermal function. It is a potential new kind of preparation formulation which have the sustainable effect.