中国畜牧兽医2024，Vol.51Issue(5)：2132-2142,11.DOI:10.16431/j.cnki.1671-7236.2024.05.034
替米考星肠道定位制剂的制备、体外释放度考察及表征鉴定
Preparation,in vitro Release,and Phase Identification of an Enteric-located Formulation of Tilmicosin
摘要
Abstract
[Objective]The experiment was aimed to prepare enteric formulations of temicoxacin using solid dispersion technology,improve its stability in acid,enable its targeted release in small intestine,improve its dissolution rate and bioavailability,and provide theoretical references for the development and clinical application of new dosage forms of the drug.[Method]Acrylic resin Eudragit L100 and polyvinylpyrrolidone(PVP)were used to form a binary carrier,and the intestinal pH-triggered localized release formulation was prepared by the co-precipitation method.With in vitro cumulative solubility as the evaluation index,the optimal preparation conditions were screened by orthogonal test,and X-ray diffraction,Fourier infrared spectroscopy and scanning electron microscopy were used for the identification of the physical phase.[Result]The optimal preparation process of tilmicosin solid dispersion enteric formulation was Eudragit L100∶PVP=10∶1,drug-carrying ratio of 1∶2,stirring time of 2 h,curing time of 12 h.The dissolution of this formulation was＜10％in an acidic environment for 2 h,and the degree of solubility reached 75.02％in buffer solution at pH 6.8 for 2 min,and it was completely dissolved in 10 min,which significantly improved the dissolution rate of tilmicosin.The dissolution rate of tilmicosin was significantly improved.X-ray diffraction result showed that the diffraction intensity of the solid dispersion at 17° and 23° was higher than that of tilmicosin API.Fourier infrared spectroscopy result showed that the sharp absorption peaks of solid dispersion of tilmicosin at 1 593 and 1 457 cm 1 were disappeared.Scanning electron microscopy diagrams showed that tilmicosin had been uniformly dispersed in the carrier,the solid dispersion of tilmicosin was formed.[Conclusion]Tilmicosin solid dispersion enteric formulation was prepared successfully by choosing the combined carrier,which was stable in acid and dissolved in pH 6.8 buffer with a good dissolution degree.关键词
替米考星/肠道定位制剂/固体分散体/溶出度/表征鉴定Key words
tilmicosin/enteric-coated formulation/solid dispersion/dissolution/phase identification分类
农业科技引用本文复制引用
刘栩沂,陈芷欣,王鸿鑫,叶钰莹,韩梓杰,张楠,张德显,邓桦,杨鸿..替米考星肠道定位制剂的制备、体外释放度考察及表征鉴定[J].中国畜牧兽医,2024,51(5):2132-2142,11.基金项目
广东省高校科技服务重点领域专项(2021ZDZX4015) （2021ZDZX4015）
