高效液相色谱法测定喷昔洛韦凝胶的含量

目的:建立HPLC法测定喷昔洛韦凝胶含量测定的方法。方法:采用HypersilODSC18色谱柱(250mm×4.6mm),以0.02mol·L-1磷酸二氢钾溶液(用磷酸调节pH至7.0)甲醇(90∶10)为流动相;检测波长为252nm。结果:喷昔洛韦在90～210mg·L-1范围内,浓度与峰面积呈良好线性关系。平均回收率为98.8%,RSD为1.1%。结论:HPLC法灵敏、准确,可用于喷昔洛韦凝胶的含量测定。

喷昔洛韦凝胶的制备与质量控制

目的研制喷昔洛韦凝胶，并建立其质量标准。方法以卡波姆为凝胶基质，制备喷昔洛韦凝胶剂。采用高效液相色谱法测定凝胶中喷昔洛韦的含量，固定相：Diamonsil C18色谱柱（4.6mm×250mm，5μm）；流动相：甲醇-0．01mol·L^-1磷酸二氢钾（KH2PO4）缓冲液（用三乙胺调pH值至7．0）（10：90）；检测波长：252nm；进样量：而止。结果喷昔洛韦在5．00～100．00p,g·mL^-1范围内线性关系良好，r=0．9997，平均回收率为99．80％，RSD为0．75％。结论该凝胶符合要求，质量控制方法可靠。

喷昔洛韦凝胶的稳定性研究

目的研究不同条件下喷昔洛韦凝胶的稳定性。方法建立喷昔洛韦凝胶质量标准,进行影响因素实验、加速实验、长期贮存稳定性实验,考察其性状、含量、有关物质变化。结果该品对光、热均不稳定。结论该品应置密闭、避光容器中,置阴凉处贮存,有效期暂定18个月。

喷昔洛韦凝胶中不同促渗剂对透皮作用的影响

目的:考察聚山梨酯80(Tw80)、丙二醇(PG)作为单一促渗剂和二元促渗剂对喷昔洛韦凝胶体外透皮作用的影响。方法:选用直立式Franz扩散池,以离体鼠皮为屏障,分别采用10％PG,10％PG+1％Tw80,20％PG+1％Tw80为促渗剂,HPLC测定接受液中喷昔洛韦的含量,计算药物累积渗透量。结果:Tw80可促进喷昔洛韦的透皮吸收,不同浓度PG对喷昔洛韦的透皮吸收影响较小。结论:促渗剂Tw80与PG联用效果更佳。

Preparation and evaluation of ophthalmic thermosensitive in situ gels of penciclovir

Aim To develop pluronic F127 （PF127） based formulations of penciclovir （PCV） aimed at enhancing its ocular bioavailability. Methods Thermosensitive in situ gels of penciclovir were prepared through combination of HPMC K4M or carbopol 934P and pluronic F127. Optimized formulations were examined through measuring gelation temperature, rheology speciality, drug release behavior, pharmacokinetics and ocular irritation. Results The gelation temperature was reduced by adding HPMC K4M or carbopol 934P, and the viscosity was enhanced slightly. Either HPMC K4M or carbopol 934P delayed the release of PCV from in situ gel. PCV was released by non-Fickian diffusion. The study of ocular irritation for different PCV formulations did not show any irritation or damage for the cornea. PCV bioavailability from combination of carbopol 934P and pluronic F127 gels was higher than that obtained from any other gels. Conclusion Pluronic F127 formulations of PCV can be used as liquid for administration by instilling into the eye. Facilitated by the appropriate eye temperature, the formulations were transformed to gel phase. On the basis of in vitro and in vivo results, PCV formulations containing HPMC K4M or carbopol 934P and low concentration of pluronic F127 （12%） showed potential for use as a drug delivery system with improved ocular bioavailability.