Initial Development And In Vitro Transdermal Research Of Lappaconitine Cataplasm

This project preliminary developed Lappaconitine cataplasm, and conducted in vitro transdermal inspection of the own products. Specific research contents include:1. Lappaconitine HPLC method was established.The experimental results showed that the concentration had good linear relationship with peak area of Lappaconitine in the corresponding concentration range and the correlation coefficient was 0.9999; The recovery rate RSD of low, medium and high concentration were less than 3.0%, the detection method was accurate, reliable and convenient.2. The solubility of Lappaconitine in different media was measured, and also the solubility of Lappaconitine in cataplasm matrix system was inspected, the effect on the solubility of Lappaconitine of proportional relationship of water system, solubilizing agent, Transcutol P and ethyl alcohol was investigated. The experimental results showed that the solubility of Lappaconitine was largest in Tanscutol P with 1.438g·100g-1, ethanol was second with 1.017g·100g-1. The proportional relationship of water system and solubilizing agent had the most significant impact on the solubility, in the second place was the proportional change of water and glycerol, the proportional relationship of Transcutol P and ethanol had little effect on its solubility.3. The Prescription was researched of Lappaconitine cataplasm.Firstly the basic formula of matrix was determined referring to the literature and the preliminary experiments; then the maximum addition amount of drugs solvents was inspected on the basis of guaranteeing the molding of cataplasm combined with the actual, the largest amount can be added of Transcutol P or ethanol was 30% of the overall substrate; In the end, the filling agent and adhesion agent were screened by property tester and rotational rheometer for the solvent seepage problem if the cataplasm was placed for a long time, the results showed both comprehensive sensory and rheological characteristics were fairly ideal of cataplasm with 2.5% of aerosil and 2% of PVA.4. The transdermal characteristic of Lappaconitine cataplasm was researched.Firstly 50% of ethanol was screened as transdermal accept liquid according to the preliminary experiments, then a reliable method for the measurement of transdermal accept liquid was establish, lastly the in vitro transdermal absorption trait of Lappaconitine cataplasm was researched and transdermal promoters were screened by the modified Franz diffusion pool, the results showed that the in vitro transdermal effect was best when 2% of azone and 0.8% of tween-80 were as penetration enhancers in Lappaconitine cataplasm.