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Drug transdermal absorption of Pharmacy in recent years, rapid development, research active areas. Effective transdermal drugs, drug transdermal accelerant, drug carriers such aspects, combined pharmacological comprehensive development of. This thesis focuses on the the baicalin active ingredients of traditional Chinese medicine, research baicalin transdermal absorption performance of its topical formulations, laid a theoretical foundation for the the further development baicalin new long-acting the topical transdermal drug delivery system. Firstly reliable baicalin HPLC detection method, and research baicalin in oil / water partition coefficient, the pKa of different solvent solubility and stability, etc., results showed that baicalin for weak acid drugs, oil / water partition coefficient decreased with increasing pH value. Baicalin solution of low concentration is less stable in an alkaline environment, the high concentration of baicalin solution stability, do not change with the change of pH. Baicalin containing 40% polyethylene glycol 400 saline stability, as baicalin transdermal diffusion can be accepted solution. Second, the paper system, respectively, from the oil phase and water phase study of baicalin in vitro transdermal performance and different penetration accelerator baicalin transdermal performance. The results show that, in the oil-phase system, the azone and oleic acid having the function to improve the baicalin transdermal diffusion performance. Azone concentration of less than 10% penetration performance is enhanced with the increase of the concentration, but there is a lag time of about 2 hours; penetration performance of the oleic acid has been showing increasing trend with the increase of the concentration, no hysteresis. Use of uniform design software visits Azone and oleic acid complex pairing baicalin transdermal performance impact, the results show that when Azone and oleic acid can produce synergistic effects of mixed use volume ratio of 10%: 0.5%, and significantly improve the penetration performance, and no hysteresis. The results showed that baicalin under alkaline conditions the transdermal diffusion effect is better than under acidic conditions in aqueous systems, the effects of pH and chitosan penetration of baicalin. And in the case of changing the chitosan concentration and pH value of the solution, each, there exists a critical value makes best baicalin permeability. X-ray photoelectron spectroscopy (XPS) test results show that the the baicalin and chitosan occurs between a certain chemical action under alkaline conditions, which may be one of the reasons of Chitosan baicalin transdermal absorption. Third, developed three different baicalin transdermal administration of the dosage form, i.e., patches, gels and ointments, investigated the in vitro penetration of these three formulations. The results showed that the three formulations are better vitro transdermal performance, best patch. Chitosan gel relative molar mass and concentration change, the existence of a critical value makes the the baicalin gel in vitro permeability. The papers also by plasma concentration method of the baicalin patch, gel and oral Dripping Pill pharmacokinetic study. Baicalin dripping pills and the main component of the patch baicalin in line with the two-compartment model with first order absorption process in rabbit medicine, one-compartment open model gels baicalin process in rabbit medicine. Baicalin patch manner administered slow way of absorption and elimination than orally in rabbits, and in vivo has certain cumulative adapted disposable administered. These results baicalin formulation of clinical dosing regimen has certain reference value.
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