| 引用本文: | 费伟东,吴超,邱阳,郭威,张思敏.介孔二氧化硅纳米粒增溶型非诺贝特片剂的制备及体内外研究[J].中国现代应用药学,2015,32(9):1097-1102. |
| FEI Weidong,WU Chao,QIU Yang,GUO Wei,ZHANG Simin.Preparation and in Vitro and in Vivo Experiments of Mesoporous Silica Nanoparticles Solubilizing Fenofibrate Tablets[J].Chin J Mod Appl Pharm(中国现代应用药学),2015,32(9):1097-1102. |
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| 摘要: |
| 目的 制备介孔二氧化硅纳米粒(mesoporous silica nanoparticles，HK)增溶型非诺贝特(fenofibrate，FNB)片剂并进行体内外研究。方法 用吸附法以HK为FNB的载体制成固体分散体(FNB-HK)。采用差示扫描量热法、X射线衍射法和傅里叶红外光谱法分析非诺贝特在FNB-HK中的存在状态。通过考察体外溶出度，优化处方并制片。将自制片和市售片分别对家兔单剂量口服给药，采用高效液相色谱法测定家兔血浆药物浓度。结果 FNB-HK表征表明HK能够抑制非诺贝特的结晶。经过处方优化，乳糖做填充剂，8%羧甲基淀粉钠为崩解剂时，片剂能够达到最理想的溶出速率。自制片与市售片相比，体内达峰时间提前，达峰浓度增大，相对生物利用度为149.95%。结论 本研究研制的片剂能显著改善FNB的溶出速率，提高其口服生物利用度。 |
| 关键词: 非诺贝特 介孔二氧化硅纳米粒 吸附法 难溶性药物 生物利用度 |
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| 基金项目:辽宁省大学生创新创业训练计划项目(201310160027)；校长基金-奥鸿博泽基金-医药创新专项(XZJJ20130104-07) |
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| Preparation and in Vitro and in Vivo Experiments of Mesoporous Silica Nanoparticles Solubilizing Fenofibrate Tablets |
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FEI Weidong, WU Chao, QIU Yang, GUO Wei, ZHANG Simin
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Liaoning Medical University, Jinzhou 121001, China
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| Abstract: |
| OBJECTIVE To explore the preparation and in vitro and in vivo experiments of mesoporous silica nanoparticles(HK) solubilizing fenofibrate(FNB) tablets. METHODS HK was used as a carrier for FNB to make the solid dispersion(FNB-HK) with the method of adsorption. The existing state of fenofibrate in FNB-HK was analyzed by differential scanning calorimetry, X-ray diffraction and Fourier transform infrared spectroscopy. The dissolution experiment in vitro was conducted to optimize the formulation. Rabbits were administrated with the self-made tablets made according to the optimized formulation and commercial tablets in a single oral dose. The concentration of the rabbits’ plasma were determined by HPLC. RESULTS The characterization of FNB-HK showed that HK inhibited the crystallization of fenofibrate. Through optimizing formulation, the dissolution rate of tablets achieved an ideal state by using lactose as filler and 8% sodium carboxymethyl starch as a disintegrating agent. Compared with commercial tablets, the peak time of the self-made tablets advanced, and the peak concentration increased. The relative bioavailability was 149.95%. CONCLUSION This preparation of tablets can significantly improve the dissolution rate of FNB and improve the oral bioavailability. |
| Key words: fenofibrate mesoporous silica nanoparticles adsorption method insoluble drug bioavailbility |
