{"title":"乙酰氯芬酸透皮贴剂的研制与评价","authors":"Rakesh Patel, G. Patel, A. Baria","doi":"10.5138/IJDD.2009.0975.0215.01005","DOIUrl":null,"url":null,"abstract":"The purpose of this research was to develop a matrix-type transdermal therapeutic system containing drug Aceclofenac with different ratios of hydrophilic (hydroxyl propyl cellulose) and hydrophobic (ethyl cellulose) polymeric systems by the solvent evaporation technique by using 15 % w/w of dibutyl phthalate to the polymer weight, incorporated as plasticizer. Different concentrations of oleic acid and isopropyl myristate were used to enhance the transdermal permeation of Aceclofenac. The physicochemical compatibility of the drug and the polymers studied by differential scanning calorimetry and infrared spectroscopy suggested absence of any incompatibility. Formulated transdermal films were physically evaluated with regard to thickness, weight variation, drug content, flatness, tensile strength, folding endurance, percentage of moisture content and water vapour transmission rate. All prepared formulations indicated good physical stability. In-vitro permeation studies of formulations were performed by using Franz diffusion cells. Formulation prepared with hydrophilic polymer containing permeation enhancer showed best in-vitro skin permeation through rat skin (Wistar albino rat) as compared to all other formulations. The results followed the release profile of Aceclofenac followed mixed zero-order and first-order kinetics in different formulation. However, the release profile of the optimized formulation F9 (r2 = 0.9935 for Higuchi) indicated that the permeation of the drug from the patches was governed by a diffusion mechanism. Formulation F9 showed highest flux among all the formulations and 1.369 fold enhancements in drug permeation. These results indicate that the formulation containing 15 % of oleic acid with 10 % Isopropyl myristate give better penetration of Aceclofenac through rat skin. Keywords: Aceclofenac, Transdermal Film, Permeation enhancer, In-vitro permeation study.","PeriodicalId":13912,"journal":{"name":"International Journal of Drug Delivery","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"2009-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"125","resultStr":"{\"title\":\"Formulation and evaluation of transdermal patch of Aceclofenac\",\"authors\":\"Rakesh Patel, G. Patel, A. Baria\",\"doi\":\"10.5138/IJDD.2009.0975.0215.01005\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"The purpose of this research was to develop a matrix-type transdermal therapeutic system containing drug Aceclofenac with different ratios of hydrophilic (hydroxyl propyl cellulose) and hydrophobic (ethyl cellulose) polymeric systems by the solvent evaporation technique by using 15 % w/w of dibutyl phthalate to the polymer weight, incorporated as plasticizer. Different concentrations of oleic acid and isopropyl myristate were used to enhance the transdermal permeation of Aceclofenac. The physicochemical compatibility of the drug and the polymers studied by differential scanning calorimetry and infrared spectroscopy suggested absence of any incompatibility. Formulated transdermal films were physically evaluated with regard to thickness, weight variation, drug content, flatness, tensile strength, folding endurance, percentage of moisture content and water vapour transmission rate. All prepared formulations indicated good physical stability. In-vitro permeation studies of formulations were performed by using Franz diffusion cells. Formulation prepared with hydrophilic polymer containing permeation enhancer showed best in-vitro skin permeation through rat skin (Wistar albino rat) as compared to all other formulations. The results followed the release profile of Aceclofenac followed mixed zero-order and first-order kinetics in different formulation. However, the release profile of the optimized formulation F9 (r2 = 0.9935 for Higuchi) indicated that the permeation of the drug from the patches was governed by a diffusion mechanism. Formulation F9 showed highest flux among all the formulations and 1.369 fold enhancements in drug permeation. These results indicate that the formulation containing 15 % of oleic acid with 10 % Isopropyl myristate give better penetration of Aceclofenac through rat skin. Keywords: Aceclofenac, Transdermal Film, Permeation enhancer, In-vitro permeation study.\",\"PeriodicalId\":13912,\"journal\":{\"name\":\"International Journal of Drug Delivery\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2009-07-05\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"125\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"International Journal of Drug Delivery\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.5138/IJDD.2009.0975.0215.01005\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Drug Delivery","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.5138/IJDD.2009.0975.0215.01005","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Formulation and evaluation of transdermal patch of Aceclofenac
The purpose of this research was to develop a matrix-type transdermal therapeutic system containing drug Aceclofenac with different ratios of hydrophilic (hydroxyl propyl cellulose) and hydrophobic (ethyl cellulose) polymeric systems by the solvent evaporation technique by using 15 % w/w of dibutyl phthalate to the polymer weight, incorporated as plasticizer. Different concentrations of oleic acid and isopropyl myristate were used to enhance the transdermal permeation of Aceclofenac. The physicochemical compatibility of the drug and the polymers studied by differential scanning calorimetry and infrared spectroscopy suggested absence of any incompatibility. Formulated transdermal films were physically evaluated with regard to thickness, weight variation, drug content, flatness, tensile strength, folding endurance, percentage of moisture content and water vapour transmission rate. All prepared formulations indicated good physical stability. In-vitro permeation studies of formulations were performed by using Franz diffusion cells. Formulation prepared with hydrophilic polymer containing permeation enhancer showed best in-vitro skin permeation through rat skin (Wistar albino rat) as compared to all other formulations. The results followed the release profile of Aceclofenac followed mixed zero-order and first-order kinetics in different formulation. However, the release profile of the optimized formulation F9 (r2 = 0.9935 for Higuchi) indicated that the permeation of the drug from the patches was governed by a diffusion mechanism. Formulation F9 showed highest flux among all the formulations and 1.369 fold enhancements in drug permeation. These results indicate that the formulation containing 15 % of oleic acid with 10 % Isopropyl myristate give better penetration of Aceclofenac through rat skin. Keywords: Aceclofenac, Transdermal Film, Permeation enhancer, In-vitro permeation study.