de Vos F, de Muynck C, Geerts M, Remon J P
Laboratory of Pharmaceutical Technology, State University of Gent, Belgium.
J Pharm Pharmacol. 1991 Apr;43(4):237-41. doi: 10.1111/j.2042-7158.1991.tb06675.x.
The percutaneous absorption of indomethacin from transparent oil in water gels (TOW gels) has been studied in rabbits and compared with absorption from a hydrophilic gel and from a spray formulation. The area under the curve and the Cmax values in plasma were significantly higher for the TOW gels in comparison with the other formulations after single application. The pH of the aqueous phase of the TOW gels did not significantly influence the bioavailability. After multiple application the TOW gels induced a larger increase in AUC (vs first application) in comparison with the other formulations. None of the formulations without drug damaged the skin after multiple application. For indomethacin formulations skin damage was more pronounced with the hydrophilic gel than for the TOW gels and spray formulation.
已在兔子身上研究了吲哚美辛从水包油透明凝胶(TOW凝胶)中的经皮吸收情况,并与从亲水性凝胶和喷雾制剂中的吸收情况进行了比较。单次给药后,与其他制剂相比,TOW凝胶的血浆曲线下面积和Cmax值显著更高。TOW凝胶水相的pH值对生物利用度没有显著影响。多次给药后,与其他制剂相比,TOW凝胶的AUC(与首次给药相比)增加幅度更大。多次给药后,无药物的制剂均未损伤皮肤。对于吲哚美辛制剂,亲水性凝胶对皮肤的损伤比对TOW凝胶和喷雾制剂更明显。