Design And Evaluation Of Osthol Patches For Antipsorisis

Psoriasis is a common skin disease characterized by over hyperplasia of epidermis and chronic inflammatory reaction of corium. The etiological factors of psoriasis have not yet been entirely clear, but it is assumed to be relate with heredity, immune defect and infection. Traditional Chinese medicines were developed rapidly in the field of treating psoriasis in recent years. Osthol has the functions of developing non-idiosyncratic immunity, antibacterial, anti-inflammatory action, anti-virus, local anesthesia, anti-allergic action and enlarging blood vessel, which are closely related to the recovery mechanism of psoriasis. The development and usage of osthol were restricted by the traditional dosage forms and extraction technology of Chinese medicines. We studied the project titled The Design and Evaluation of the Osthol Patches for antipsoriasis, in order to find an ideal osthol patch for treating psoriasis and make the further study on the therapy mechanism of psoriasis with osthol.The extracting technology of the main effective principle-osthol from cnidium monnieri (L.) cuss by supercritical carbon dioxide extraction was optimized with orthogonal experiment. The effects of extraction pressure, temperature, separating pressure, particle size and static time on the content of Osthol in extraction were studied. The optimum extraction conditions were: extraction pressure 25-30MP, temperature 50-55 ℃, separating pressure 5-7MP, particle size 40 mesh, static time 10min. The content of Osthol in extraction was increased under these conditions.In the paper, the assay methods were established and several important physical-chemical parameters of osthol were determined. The permeation of osthol via skin was studied and the resukts indicated that the diffusion behaviors of osthol through the rat skin in vitro conformed to the characteristics of zero-order kinetics. The apparent permeation coefficient (Pm) was 1.10×10-4 cm. h-1. The permeation enhancers such as chenopodium oil, menthol and Azone increased the percutaneous penetration of osthol in different degrees, and the enhancement factors were 3.09, 3.41and 4.38 respectively.The effects of triethyl citrate ,succinic acid and resin on the properties of pressure sensitive adhesive (PSA) were investigated in the study of the PSA matrix of the osthol patches. And the safe and effective formulations of the osthol patches were screened out.The ear vein perfused models were established in pig and rabbit. The activity of lactate dehydrogenase and the consumption of glucose in perfused solution were adopted as the indicators and used to evaluate the bioactivity of the tissue in the perfused site.The results showed that the models maintained a good bioactivity within 8 hours. The Evan' blue added in the perfused solution for monitoring the volume change of the solution was of great importance for accurately determining the total permeation amount of osthol.The permeability of osthol patches was studied with the model .The results indicated that the state flux of osthol in pig and rabbit were 1 .39 and 3. 17 ug.cm-2.h-1 respectively.The human being's skin in vitro being used as a model , the permeability of osthol patches was studied with the diffusion cells in this paper. The traditional tape-stripping technology was also used to quantify osthol in different skin layers. The innovative 3-D fluorescence spectra technology was applied to study the distribution of osthol in different skin layers after the isolated skin being treated with the osthol patches. When the 3-D fluorescence spectra technology was used, it was not necessary to extract the drug from the different skin layers. The section slices of skin can be scanned directly, which improves remarkably the selectivity and sensitivity in determining the test compound. The fingerprint of fluorescence spectra was reflected by the contour spectra drawing, which performed high specificity in identifying drugs in skin. The results indicated that the osthol concentrations in the stratum corneum were higher than th...