title: Preparation, characterization and pharmacokinetics evaluation of clarithromycin-loaded Eudragit(®) L-100 microspheres.
abstract: The aim of this work was to prepare pH-dependent clarithromycin microsphere formulation by emulsion solvent evaporation method, employing Eudragit(®) L-100. Prepared microspheres were evaluated by carrying out in vitro release and in vivo pharmacokinetics studies. Drug-polymer interactions were studied by differential scanning calorimetry, X-ray diffractometry analyses and results showed that clarithromycin was molecularly dispersed in the polymer. The particle size distribution of microspheres was found over the range of 10~50 μm. The drug is hardly released in the HCl solution pH 1.2 in the first 2 h, but is rapidly released in phosphate buffer pH 7.2, and the cumulated release reached 98.1 % at 8 h. The pharmacokinetic profiles were conducted open, randomized, two-period crossover design with a 7-day interval between doses in healthy beagle dogs. The results indicated that the extent of absorption of the clarithromycin-load microspheres was the same as pure drug, but different in the rate of drug absorption in vivo.
authors: School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang, 110016, China.
authors: Jinghua
authors: J
authors: Xu
authors: School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
authors: Wei
authors: W
authors: Li
authors: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
authors: Zhuo
authors: Z
authors: Liu
authors: School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
authors: Jinghan
authors: J
authors: Li
authors: School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang, 110016, China.
authors: Xiaoyun
authors: X
authors: Zhao
authors: School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.
authors: DongYang
authors: D
authors: Li
authors: School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, Shenyang, 110016, China.
authors: Shuang
authors: S
authors: Guo
authors: School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China. zhangxr@vip.sina.com.|School of Pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China. zhangxr@vip.sina.com.
authors: Xiangrong
authors: X
authors: Zhang
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D017291:Clarithromycin / Q000737:chemistry* / Q000493:pharmacokinetics*; D004285:Dogs; D004337:Drug Carriers / Q000737:chemistry; D004655:Emulsions / Q000737:chemistry / Q000493:pharmacokinetics; D005260:Female; D006863:Hydrogen-Ion Concentration; D008297:Male; D008863:Microspheres; D010316:Particle Size; D011108:Polymers / Q000737:chemistry; D011109:Polymethacrylic Acids / Q000737:chemistry*; D012995:Solubility; D012997:Solvents / Q000737:chemistry
chemical_list: D004337:Drug Carriers; D004655:Emulsions; D011108:Polymers; D011109:Polymethacrylic Acids; D012997:Solvents; C038300:methylmethacrylate-methacrylic acid copolymer; D017291:Clarithromycin
keywords: Clarithromycin; Emulsion solvent evaporation; Eudragit L-100; Microsphere; Pharmacokinetics
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