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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。
Objective To prepare mesoporous silica nanoparticles (HK) solubilized fenofibrate (FNB) tablets for in vitro and in vivo studies. Methods The solid dispersion (FNB-HK) was prepared by the adsorption method using HK as the carrier of FNB. The existence of fenofibrate in FNB-HK was analyzed by differential scanning calorimetry, X-ray diffraction and Fourier transform infrared spectroscopy. By examining in vitro dissolution, prescription optimization and preparation. The self-made tablets and the commercially available tablets were administered orally to a single dose of rabbit respectively, and the plasma drug concentrations of rabbits were determined by high performance liquid chromatography. Results FNB-HK characterization indicated that HK inhibited the crystallization of fenofibrate. After prescription optimization, lactose filler, 8% sodium carboxymethyl starch as disintegrating agent, the tablet can achieve the best dissolution rate. Self-made tablets compared with the commercial tablets, the peak time in advance in vivo, the peak concentration increases, the relative bioavailability of 149.95%. Conclusion The tablets developed in this study can significantly improve the dissolution rate of FNB and increase its oral bioavailability.