| 引用本文: | 陈洁,罗丹冬,陈婷婷,潘怀耿,陈睿,丘振文.超临界反溶剂流化床制备西罗莫司微米颗粒[J].中国现代应用药学,2022,39(10):1330-1335. |
| CHEN Jie,LUO Dan-dong,CHEN Ting-ting,PAN Huai-geng,CHEN Rui,QIU Zhen-wen.Preparation of Sirolimus Micron Particles by Supercritical Antisolvent Fluidized Bed[J].Chin J Mod Appl Pharm(中国现代应用药学),2022,39(10):1330-1335. |
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| 超临界反溶剂流化床制备西罗莫司微米颗粒 |
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陈洁1, 罗丹冬1, 陈婷婷2, 潘怀耿3, 陈睿4, 丘振文1
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1.广州中医药大学第一附属医院, 广州 510405;2.广州中医药大学中药学院, 广州 510006;3.广州中医药大学资产与实验管理处, 广州 510006;4.南通市华安超临界萃取有限公司, 江苏 海安 226681
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| 摘要: |
| 目的 使用超临界反溶剂流化床(supercritical anti-solvent fluidized bed,SASFB)包覆技术制备西罗莫司微米颗粒,考察颗粒形貌和体外溶出度。方法 以乳糖为载体,选取温度、压力、药液浓度3个工艺参数,通过正交试验对西罗莫司微米颗粒工艺进行优化。结果 药液浓度对西罗莫司包覆率的影响最大,压力次之,温度最小,最佳的工艺条件为温度45℃,压力8 MPa,药液浓度1 mg·mL-1。SASFB制备的西罗莫司亚微米颗粒均匀分散在载体表面,溶出度在20 min时,分别是超临界反溶剂样品和原料药的2.29和5.04倍,包覆率可达74.1%。结论 SASFB是一种新型的一步制备西罗莫司微米颗粒的药物制剂技术。 |
| 关键词: 西罗莫司 超临界反溶剂 流化床 包覆率 |
| DOI：10.13748/j.cnki.issn1007-7693.2022.10.011 |
| 分类号:R943 |
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| Preparation of Sirolimus Micron Particles by Supercritical Antisolvent Fluidized Bed |
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CHEN Jie1, LUO Dan-dong1, CHEN Ting-ting2, PAN Huai-geng3, CHEN Rui4, QIU Zhen-wen1
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1.The First Affiliated Hospital of Guangzhou University of Chinese Medicine, Guangzhou 510405, China;2.Guangzhou University of Chinese Medicine, School of Pharmaceutical Sciences,, Guangzhou 510006, China;3.Guangzhou University of Asset Management Office, Guangzhou 510006, China;4.Nantong Hua'an Supercritical Extraction Co., Ltd., Hai'an 226681, China
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| Abstract: |
| OBJECTIVE To prepare sirolimus micro-particles by supercritical anti-solvent fluidized bed(SASFB) coating technology, and to investigate the particle morphology and dissolution in vitro.METHODS Lactose was selected as carrier, and three process parameters including temperature, pressure and drug concentration were optimized by orthogonal experimental design.RESULTS The process optimization experiment demonstrated that drug concentration had the greatest effect on the coating efficiency of sirolimus, followed by pressure and temperature. The optimal conditions were temperature 45℃, pressure 8 MPa, drug concentration 1 mg·mL-1. The sirolimus particles prepared by SASFB were evenly dispersed on the surface of the carrier, the dissolution rate were 2.29 and 5.04 times of the supercritical anti-solvent sample and sirolimus active pharmaceutical ingredient in 20 min, and the coating efficiency could reach 74.1%.CONCLUSION SASFB is a new type of pharmaceutical preparation technology for preparing micron particles of sirolimus in one step. |
| Key words: sirolimus supercritical antisolvent fluidized bed coating efficiency |
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