Pharmaceutical Studies On ZSM Cataplasm

Zushima is the stem cortex and root bark of Daphne giraldii Nitsche, a folk herb used inwest of China.Determining on the Daphnetin content of Zushima through HPLC and the totalcoumarins content through ultraviolet spectrometry, the same time, carrying on methodsinvestigation to found the standard quality control of Zushima. The accuracy, stability,repeatability and recovery of determining method all accord with the relevant regulations.To gain the total coumarins of Zushima （TCZ）, we compared three means, such asmacoropore adsorbed resin, supercritical CO₂ extraction, organic solvent extraction etc. Asa result, EtoAC extraction was selected to prepare TCZ. Through optimum choice onEtoAC extraction by orthogonal experimental design, we got the optimum extractiontechnology and the total coumarins in Zushima extract could amount to more than 50percent. TCZ was determined as the active part of Zushima which treated rheumatoidarthritis by means of pharmacodynamic research, such as anti-inflammation, promoting theblood and easing pain. In order to increase the concentration of TCZ in inflammatory jointlocation and enhance its anti-inflammatory effect, meanwhile reduce its adverse reactionsby oral administration. We developed ZSM cataplasm and studied its release, penetration invitro etc.According to the result of the apparent partition coefficient between water and octanol,we get the result of the logPo/w of TCZ is about 1, which is very proper for transdermally.Normal saline containing 10% PEG400 and 30% alcohol （95%） was used as receptorsolution in in vitro percutaneous penetration experiments because the solubility andstability of TCZ in the solution are rate.TP-5 automatic diffusion cells were adopted as the apparatus for in vitro skinpermeation to study the effects of percutaneous absorption enhancer on the transdermalcharacters of Daphetin through rat excised skin in this paper, which shows that comparedwith blank skin, Azone/prolylene glycol, borneol/prolylene were found to be the properpenetration enhancers in the transdermal preparations of Daphne, and Azone/prolylene werethe best penetration enhancers to Daphne（P＜0.05）.The component of the cataplasm matrix was optimized by uniform design. While adhension strength, cohesive strength and sensory index general assign mark were used asindexes. The process conditions were optimized by orthogonal design, while sensory indexgeneral assign mark was used as index. The effect of drug loading on penetration rate wasinvestigated, which showed the best drug loading was 3.5%, and the best concentration ofAzone is 1% by comprehensive consideration of permeation and time-delay.The release pattern of TCZ and daphne into aqueous medium followed by Higuchiequation. The amour of TCZ and daphnetin release at 12h was 55% and 79% ofadministration dose and the release rate constant was 15.91079h^-1 and 22.943h^-1. TCZ anddaphnetin in cataplasm was both permeated at zero rate. The test of the Shape-keepingcharacteristic and adhesive ability of ZSM cataplsm showed that the ZSM cataplasm wasgood.The accelerated test of ZSM cataplasm showed that the stabilization of ZSMcataplasm was ideal. The result of skin irritation study showed that ZSM cataplasm had noskin irritation which was proved by the volunteers.