注射用盐酸米诺环素微球贮库的制备及其性能研究

张婷; 廖航; 程玉婷; 吴小红

doi:10.11665/j.issn.1000-5048.20210107

注射用盐酸米诺环素微球贮库的制备及其性能研究

张婷^1,2,3,
廖航^1,2,3,
程玉婷^1,2,3,
吴小红^1,2,3

1.
重庆医科大学附属口腔医院，重庆 401147
2.
口腔疾病与生物医学重庆市重点实验室，重庆 401147
3.
重庆市高校市级口腔生物医学工程重点实验室，重庆 401147

基金项目: 国家自然科学基金资助项目（No.81970914）

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出版历程
- 收稿日期: 2020-08-31
- 修回日期: 2020-12-06
- 刊出日期: 2021-02-24

Preparation and properties of injectable minocycline hydrochloride microsphere depot

ZHANG Ting^1,2,3,
LIAO Hang^1,2,3,
CHENG Yuting^1,2,3,
WU Xiaohong^1,2,3

1.
Department of Prosthodontics, Affiliated Hospital of Stomatology, Chongqing Medical University, Chongqing 401147
2.
Chongqing Key Laboratory of Oral Diseases and Biomedical Sciences, Chongqing 401147
3.
Chongqing Municipal Key Laboratory of Oral Biomedical Engineering of Higher Education, Chongqing 401147, China

Funds: This study was supposed by the National Natural Science Foundation of China(No.81970914)

摘要

摘要: 制备盐酸米诺环素微球贮库，并评价其体外缓释效果及理化性质。以聚乳酸-羟基乙酸共聚物［poly （lactic-co-glycolic acid），PLGA］为原材料，采用静电喷雾的方法制备得到盐酸米诺环素微球，并通过偏振光显微镜以及扫描电镜对微球形态大小进行表征，将其与蔗糖乙酸酯异丁酸酯（sucrose acetate isobutyrate，SAIB）原位贮库以1∶10的比例混合形成盐酸米诺环素微球贮库，并考察其体外释放性能及孔隙率变化。结果表明，盐酸米诺环素微球表面光滑，直径（5.294±1.222）μm。盐酸米诺环素微球与SAIB混合形成盐酸米诺环素微球贮库后，盐酸米诺环素的突释大幅度降低，在第1天从60%降至3.27%并持续释放至第42天。同时结果表明该贮库在0～15 d孔隙率由（12.53±0.43）%迅速增加到（32.53±0.43）%，15～45 d孔隙率由（32.53±0.43）%缓慢增加到（33.81±0.54）%。本研究制备的盐酸米诺环素微球贮库制备工艺简单、释药性能良好，有望成为盐酸米诺环素给药的一种有效途径。
- 盐酸米诺环素 /
- 聚乳酸-羟基乙酸共聚物 /
- 蔗糖乙酸酯异丁酸酯 /
- 静电喷雾
Abstract: To prepare a minocycline hydrochloride microsphere depot and evaluate its release performance and physicochemical properties, poly (lactic-co-glycolic acid) (PLGA) was used as raw material, the minocycline hydrochloride microspheres were prepared by electrospray, and the morphology and size distribution of the microspheres were characterized by polarizing microscopy and scanning electron microscopy (SEM). The microspheres were then mixed with sucrose acetate isobutyrate (SAIB) depot at a ratio of 1:10 to form a minocycline hydrochloride microsphere depot, and its release performance and porosity changes were evaluated. The results showed that the microspheres had smooth surface and the diameter was (5.294 ± 1.222) μm. After the microspheres were added into SAIB depot, the burst release of minocycline hydrochloride significantly decreased from 60% to 3.27% at the first day, and then the release lasted for 42 days . Additionally, the porosity of the depot increased rapidly from (12.53 ± 0.43)% to (32.53 ± 0.43)% during days 0-15, and increased slowly from (32.53 ± 0.43)% to (33.81 ± 0.54)% during days 15-45. The minocycline hydrochloride microsphere depot prepared in this study is expected to be an effective way for the application of minocycline hydrochloride for its good release performance and simple preparation process.
- minocycline hydrochloride /
- poly(lactic-co-glycolic acid) /
- sucrose acetate isobutyrate /
- electrospray

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参考文献(31)

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注射用盐酸米诺环素微球贮库的制备及其性能研究

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Preparation and properties of injectable minocycline hydrochloride microsphere depot

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