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Preparation, Characterization and in vitro release of Ciprofloxacin Polylactic Acid Microspheres

Journal of Chinese Pharmaceutical Sciences 2005年第2期14卷 95-99页

作者：杨帆梁仁潘育方赵耀明旺朝阳徐安龙广东药学院药科学院广东广州510224 华南理工大学材料学院广东广州510640 中山大学生命科学学院广东广州510275

Aim Ciprofloxacin polylactic acid microspheres (CFX-PLA-MS) were preparedusing solvent evaporation method from a solid-in-oil-in-water emulsion system. Methods Orthogonalexperiment was used to optimize the method of CFX-PLA-MS preparation. Microspheres werecharacterized in terms of morphology, size, encapsulation efficiency, drug loading and in vitro drugrelease. Results The physical state of CFX-PLA-MS was determined by scanning electron microscopy(SEM) and differential scanning calorimetry (DSC) . Microspheres formed were spherical with smoothsurfaces. Drug was enveloped in microspheres without mixing physically with PLA. The averageparticle size was 280.80 ± 0.15 μm, with over 90% of microspheres falling in the range of 250 -390 μm. The encapsulation efficiency was 65.8% ± 0.58% and the drug loading was 34.1% ± 0.51% .In vitro release study revealed a profile of sustained release of Ciprofloxacin from CFX-PLA-MS. Theaccumulated release percentage and half-life (T_(1/2) of Ciprofloxacin microspheres were 84.0% in53.2 h, and 31.9 h, respectively. Higuchi equation was Q= -0.0043 + 0.003 9 t^(1/2), r = *** Ciprofloxacin microspheres have been successfully prepared and sustained release of CFXfrom microspheres is achieved.

关键词： ciprofloxacin polylactic acid microspheres preparation release in vitro

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release behavior and kinetic evaluation of berberine hydrochloride from ethyl cellulose/chitosan microspheres

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Frontiers of Materials Science 2014年第4期8卷 373-382页

作者： Hui-Yun ZHOU Pei-Pei CAO Jie ZHAO Zhi-Ying WANG Jun-Bo LI Fa-Liang ZHANG Chemical Engineering & Pharmaceutics College Henan University of Science and Technology Luoyang 471023 China

Novel ethyl cellulose/chitosan microspheres （ECCMs） were prepared by the method of w/o/w emulsion and solvent evaporation. The microspheres were spherical, adhesive, and aggregated loosely with a size not bigger than 5 pm. The drug loading efficiency of berberine hydrochloride （BH） loaded in microspheres were affected by chitosan （CS） concentration, EC concentration and the volume ratio of V（CS）/V（EC）. ECCMs prepared had sustained release efficiency on BH which was changed with different preparation parameters. In addition, the pH value of release media had obvious effect on the release character of ECCMs. The release rate of BH from sample B was only a little more than 30% in diluted hydrochloric acid （dHCl） and that was almost 90% in PBS during 24 h. Furthermore, the drug release data were fitted to different kinetic models to analyze the release kinetics and the mechanism from the microspheres. The released results of BH indicated that ECCMs exhibited non-Fickian diffusion mechanism in dHCI and diffusion-controlled drug release based on Fickian diffusion in PBS. So the ECCMs might be an ideal sustained release system especially in dHCl and the drug release was governed by both diffusion of the drug and dissolution of the polymeric network.

关键词： ethyl cellulose (EC) chitosan (CS) microsphere release in vitro releasekinetics

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Preparation and evaluation of nattokinaseloaded self-double-emulsifying drug delivery system

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Asian Journal of Pharmaceutical Sciences 2015年第5期10卷 386-395页

作者： Xiaona Wang Sifan Jiang Xinyue Wang Jie Liao Zongning Yin Key Laboratory of Drug Targeting and Drug Delivery Systems West China School of PharmacySichuan UniversityNo.17Block 3Southern Renmin RoadChengdu 610041China

In the present study,we prepared nattokinase-loaded self-double-emulsifying drug delivery system(SDEDDS)and investigated its preliminary *** type and concentration of oil phase,inner aqueous phase and emulsifier were screened to prepare optimum nattokinase-loaded ***,the optimum formulations were characterized based on microstructure,volume-weighted mean droplet size,self-emulsifying rate,yield,storage stability,in vitro release and in vivo pharmacodynamics *** water/oil/watermultiple emulsions exhibited typicalmultiple structure,with relatively small volumeweighted mean droplet size 6.0±0.7μm and high self-emulsifying ability(self-emulsifying timerelease of nattokinase within 8 h was about 30%,exhibiting a sustained release *** pharmacodynamics study indicated that nattokinase-loaded SDEDDS could significantly prolong the whole blood clotting time in mouse and effectively improve the carrageenan-induced tail thrombosis compared with nattokinase ***,we showed that SDEDDS could successfully self-emulsify into water/oil/water multiple emulsions upon dilution in dispersion medium with gentle stirring and effectively protect nattokinase activity in gastric *** findings suggested that SDEDDS could be a promising strategy for peptide and protein drugs by oral administration.

关键词： Self-double-emulsifying drug delivery system Nattokinase Yield release in vitro Pharmacodynamics study

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The Study of Dipivefrin Hydrochloride Ophthalmic Gel

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Journal of Chinese Pharmaceutical Sciences 2001年第3期10卷 128-132页

作者：王丽茹张强浙江医药股份有限公司新昌制药厂绍兴312500 北京大学药学院药剂研究室北京100083

Dipivefrin hydrochloride ophthalmic gel was prepared and the release test and the isolated cornea permeation test of the formulation in vitro were investigated. The release test of the formulation was studied by using permeable membrane. The content and the release amount of Dipivefrin hydrochloride from the gel base were measured by high performance liquid chromatography. The cornea permeation test of the formulation was studied by using isolated rabbit corneas. The formulation release behavior in vitro followed the first-order kinetic equation. The release amount of Dipivefrin hydrochloride raised significantly with less polymer in the formulation. The cornea permeation behavior of the drug in vitro followed the first-order kinetic equation. The eye irritancy of Dipivefrin hydrochloride gel is lower than that of eyedrops.

关键词： Dipivefrin hydrochloride Gel HPMC release in vitro HPLC Isolated cornea per-meation.

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