| Tulobuterol(TUL),also known as butochoter,is a third-generation β-adrenergic agonist.In 1981,it was developed by Japan’s Hondabe Pharmaceutical and approved for marketing as a drug for asthma treatment.Transdermal patches have great market prospects as a pharmaceutical dosage form that is continuously administered,convenient and can maintain a constant drug delivery rate.The research content of this article is as follows:1.Using o-chloroacetophenone as raw material,tuloterol was synthesized by Kornblum oxidation,condensation and reduction reaction with tertbutylamine.The reaction temperature,reaction time,molar ratio of raw materials,solvent,separation and purification processes were optimized,and tuloterol was synthesized with high yield.The method is simple in process,mild in condition,convenient in operation,and suitable for industrial production.2.Studies were conducted on the prescription of tuloterol patches.Taking the toloterol patch produced by Nitto Electric as the reference preparation,and taking the permeability and related substances as the evaluation index,the prescription screening and optimization were carried out,and the prescription composition of toloterol 5%,pressure-sensitive adhesive A 60%,pressuresensitive adhesive matrix material B 20%,osmoizant C 15% g,and osmotropic agent D 0.4% was determined3.The quality of tuloterol patch was studied and evaluated,and the HLPC method of toloterol content,related substances and release degree in tuloterol transdermal patch was determined,and systematic methodological verification was carried out.The results show that the specificity,system applicability,linearity,etc.of the analysis method meet the requirements.According to the quality evaluation standards of the 2020 edition of the Chinese Pharmacopoeia patch,the adhesion force,in vitro transdermal and release degree of three batches of homemade patches were investigated,and the data of each item met the quality requirements of the patch.The comparative experimental results show that the self-made transdermal tuloterol patch reaches the level of the toloterol patch produced by Nitto Denko in terms of main quality indicators. |
