吡罗昔康PEG固体分散体中载体组成与制剂的体内外特性

本文报道以成分不同的PEG为载体制成吡罗昔康(PIR)固体分散体(Sd)制剂,与片剂相比,体内外特性存在着显著性差异。Sd用红外光谱、X射线衍射光谱加以证明,由Sd制成两种滴丸DⅠ、DⅡ,用转篮法测定了体外释药速度。用HPLC法测定了家兔的吸收速度。以PEG 4000与1000为混合载体制备的滴丸DⅠ,其体外释药速度远较单纯PEG 4000为载体的滴丸DⅡ为快,两者的T_(50)相差6.4倍。家兔吸收试验中,两种滴丸的T_m相差为6.5倍,与体外释药速度倍数十分吻合。进一步测定了滴丸DⅠ在8名志愿者的体内血药浓度,结果表明,DⅠ的T_m及K_α远较片剂快,而C_m AUC和片剂相近。

IN VITRO AND IN VIVO CHARACTERISTICS OF TWO DOSAGE FORMS OF PIROXICAM SOLID DISPERSION SYSTEM WITH DIFFERENT PEG BASES

Piroxicam (PIE) is a new non-steroidal anti-inflammatory drug of high potency, used in the treatment of arthritis.Two dropping pills dosage forms of PIE were prepared by the solid dispersion technique. One of them (DI) was prepared by using a mixture of PEG 4 000 and PEG 1 000 as base. Another (DII) was prepared by using PEG 4000 as carrier. It was confirmed by IK absorption spectra and X-ray diffraction pattens that two dosage froms were in a state of solid dispersion system.The serum levels of PIE after oral administration were determined by HPLC. The Tm of PIE after administrtaion as DI was 6.6 times faster than that as DII in rabbits. In human volunteers, the Cm and AUC of PIE after administration of DI were found close to that of sablets. However, the I'm and Ka appeared much shorter and smaller because of rapid absorption of PIE in DI.