ABSTRACT
This study aims to establish a method for determination of paeonol(Pae), eugenol(Eug), and piperine(Pip) content in receptor liquid and research on the permeability and pharmacokinetics of Huoxue Zhitong gel patch and microemulsion gel. The Franz diffusion experiment was conducted to assess the percutaneous permeability, and the microdialysis method was employed to assess pharmacokinetics of Huoxue Zhitong gel patch and microemulsion gel. The content of Pae, Eug, and Pip in receptor liquid in vitro and in vivo was determined by HPLC and UPLC-MS. The Q_n and J_(ss) of Pae, Eug, and Pip in the gel patch were significantly higher than those in the microemulsion gel, indicating that the drug release was faster in the gel patch. The C_(max), AUC_(0-760), and MRT of Pae, Eug, and Pip in the gel patch were higher than those in the microemulsion gel, indicating that the gel patch can promote the penetration and prolong the skin residence of the drug. The results of this study provide reference for improving the dosage form of Huoxue Zhitong patch.
Subject(s)
Administration, Cutaneous , Chromatography, Liquid , Emulsions , Permeability , Skin/metabolism , Skin Absorption , Tandem Mass SpectrometryABSTRACT
Objective: To optimize the forming process of gel patch and explore the compatibility-synergistic mechanism of Aconiti Radix-Zanthoxyli Pericarpium volatile oil gel patch. Methods: According to the indexes of skin followability, disclosing ability, initial adhesion and peeling degree, the substrate-property of eight commercially gel patches was evaluated. Then, with the comprehensive sensory evaluation, initial adhesion, stickiness and peeling degree as the index, single factor experiment and mixture design experiment were used to screen the proportion of matrix excipients of gel patch. Taking the number of acetic acid-induced writhing in mice as the index, the drug loading of gel paste was screened by in vivo animal evaluation. In addition, the compatibility effect of Aconiti Radix-Zanthoxyli Pericarpium volatile oil gel patch was studied by using formaldehyde-induced pain model and metabolomics. Results: Different brands of gel plaster had great difference in their skin followability, disclosing ability, initial adhesion and peeling degree. The initial adhesion and peel degree of gel patch had great influence on its disclosing ability and the greater the initial adhesion and peel degree were, the worse disclosing ability was. The matrix of the Aconiti Radix gel patch was 3% polyacrylic acid sodium NP700, 1.5% carboxymethyl cellulose sodium, 0.25% Carbomer, 0.06% crystalline aluminum chloride, 0.1% ethylenediamine tetra acetic acid two sodium, 26% glycerol, 61.5% water, 4% diatomaceous earth, 0.15% tartaric acid; Drug dosage of each gel patch was 560 mg extracts of Aconiti Radix. Zanthoxyli Pericarpium olatile oil could enhance the analgesic effect of Aconiti Radix gel patch, which might be mainly through glycerol phospholipid metabolism and linoleic acid metabolism. Conclusion: To ensure better adherence and disclosure of gel patch, the initial adhesive force of gel patch should be controlled between 7-18 balls and the peel degree should be controlled between 0.03-0.97 kN/m. The Prepared Aconiti Radix gel patch has a good appearance, adhesion and shape with a clear analgesic effect, and Zanthoxyli Pericarpium olatile oil can enhance analgesic effect of Aconiti Radix gel patch. This study provides a basis for the development and application of new preparations for the external use in Aconiti Radix.
ABSTRACT
Objective To study and optimize the preparation process and abserve the related properties of electret flu-orouracil gel patch .Methods the adhesives and moistening agents were screened by preliminary experiment .The optimal matrix proportion in the blank gel patch was obtained with orthogonal design .The charge storage stability of the patch was studied by compensation method .The transdermal behaviors of the patch were evaluated by modified diffusion cell method and HPLC .Results The optimal matrix proportions of PAAS ∶ gelatin ∶ PVA ∶ Kaolin ∶ CMC-Na ∶ moistening agents were 0 .2∶0 .7∶0 .5∶0 .7∶0 .2∶12 .The patch had a good charge storage stability .All the electrets and 3% azone could enhance the cumulative penetration amount of drug and they had synergistic enhancing effect .Conclusion The qualified electret fluorouracil gel patch was prepared under the optimal process ,which had no skin irritation and the behavior of transdermal de-livery was better than that of the traditional gel patch .