阿昔洛韦眼用混悬液助悬剂筛选.docVIP

阿昔洛韦眼用混悬液助悬剂筛选摘要：目的筛选阿昔洛韦眼用混悬液的助悬剂。方法以羟丙纤维素（HPC）、卡波姆940、聚乙二醇(PEG)、羟丙甲纤维素（HPMC）、透明质酸钠（HA）以及HA/HPMC组合作为助悬剂制备阿昔洛韦眼用混悬液，以沉降体积比、粒度及再分散性作为考察指标筛选最佳助悬剂；同时考察温度和光照对阿昔洛韦眼用混悬液的影响。结果HA/HPMC组合助悬效果最好，二者单独使用次之，其余助悬剂效果不理想；以0.05 %HA和0.05 %HPMC为助悬剂制备的混悬液，沉降体积比为0.998，粒度均匀，再分散性好；60 ℃和4～8 ℃条件下，混悬液粒径增大，沉降体积比减小；强光照射不改变混悬液的沉降体积比、粒度及再分散性。结论0.05 %透明质酸钠和0.05 %羟丙基甲基纤维素为阿昔洛韦眼用混悬液的理想助悬剂，温度对此混悬液的稳定性有较大影响。 关键词：阿昔洛韦；眼用混悬液；助悬剂；稳定性 中图分类号：R988.1文献标识码：A文章编号：1672-979X(2008)11-0021-03 Screening of Suspending Agent for Acyclovir Ophthalmic Suspension LIU Jie, YANG Sheng-lin, CHEN Jian-ying* (Institute of Biopharmaceuticals of Shandong Province, Jinan 250101, China) Abstract：Objective To screen suspending agent for acyclovir ophthalmic suspension. Methods Acyclovir ophthalmic suspensions were prepared with HPC, Carbomer 940, PEG, HPMC, hyaluronic acid(HA) and the combination of HA and HPMC (HA/HPMC) as suspending agents, respectively. The sedimentation volume ratio, particle size and redispersibility were used as indexes for the screening of optimal suspending agent. The effects of temperature and light on the suspension were also investigated. Results The suspending effect of HA/HPMC was best and that of HA or HPMC alone was better than the others. The suspension with the combination of 0.05 % HA and 0.05 %HPMC as a suspending agent had uniform particle size and good dispersity with sedimentation volume ratio of 0.998. At 60 ℃ or 4～8 ℃, the particle size of the suspension increased, while the sedimentation volume ratio decreased. Under strong light exposure, the particle size, sedimentation volume ratio and redispersibility of the suspension were invariable. Conclusion The combination of 0.05 % HA and 0.05 % HPMC may be the optimal suspending agent for acyclovir ophthalmic suspension, and temperature has a significant effect on the stability of the suspension. Key words：acyclovir; ophthalmic suspension; suspending agent; stability 阿昔洛韦（acyclovir，ACV）是一种高效抗病毒药，眼科用于治疗单疱病毒性角膜炎（HSK），具有疗