20mg/mL更昔洛韦人工泪液与眼科用注射用水的临时配制:制剂与稳定性研究

Extemporaneous Preparation of 20 mg/mL Ganciclovir in Artificial Tears in Comparison with Sterile Water for Ophthalmic Administration: Formulation and Stability Study.

作者信息

Leanpolchareanchai Jiraporn, Tangteerakoon Patamaporn, Supapsophon Patcharin, Sukavatcharin Somsiri, Simaroj Pornchai, Suksiriworapong Jiraphong

机构信息

Department of Pharmacy, Faculty of Pharmacy, Mahidol University, Bangkok 10400, Thailand.

Chemotherapy Pharmacy Unit, Drug Compounding Section, Pharmacy Department, Faculty of Medicine, Ramathibodi Hospital, Bangkok 10400, Thailand.

出版信息

Pharmaceutics. 2023 Jan 6;15(1):208. doi: 10.3390/pharmaceutics15010208.

Abstract

Ganciclovir is available as a lyophilized powder for reconstitution and is normally used to treat ophthalmic viral infections. The use of ganciclovir in artificial tears containing hydrocolloid polymers may prove beneficial to patients during drug application, by prolonging contact time and providing a moistening effect. Therefore, this study aimed to extemporaneously prepare 20 mg/mL ganciclovir in artificial tears and compare its stability with that of a similar concentration of ganciclovir in sterile water (SWI) for ophthalmic administration. First, a compatibility study of the drug with commercial artificial tears found that it was compatible with artificial tears containing sodium hyaluronate (HYA). Subsequently, ganciclovir/0.1% HYA (HYA0.1) and ganciclovir/SWI eyedrops (EDs) in low-density polyethylene (LDPE) eyedrop bottles packed in light-shielded zipper bags were evaluated for their stability at 5 ± 3 °C and 30 ± 2 °C. The results revealed that ganciclovir/SWI ED had good physicochemical and microbiological stability when stored at 5 ± 3 °C for 12 weeks and at 30 ± 2 °C for 8 weeks. Meanwhile, ganciclovir/HYA0.1 ED was stable for 8 weeks when kept at 5 ± 3 °C and at 30 ± 2 °C, but ganciclovir in 0.3% HYA ED could be stored at 5 ± 3 °C for 8 weeks. Nevertheless, particulate matter may need to be investigated using a suitable method to ensure the absence of invisible particles in these preparations. Of these results, ganciclovir/HYA artificial tears and SWI EDs show potential for use as home medications for the treatment of ophthalmic viral infections.

摘要

更昔洛韦有冻干粉末剂型,需重新配制,通常用于治疗眼部病毒感染。在含亲水胶体聚合物的人工泪液中使用更昔洛韦,可能通过延长接触时间并提供湿润效果,在给药过程中对患者有益。因此,本研究旨在临时配制20mg/mL的更昔洛韦人工泪液,并将其稳定性与类似浓度的用于眼部给药的无菌水(SWI)中的更昔洛韦进行比较。首先,对该药物与市售人工泪液的相容性研究发现,它与含透明质酸钠(HYA)的人工泪液相容。随后,对装在遮光拉链袋中的低密度聚乙烯(LDPE)滴眼瓶中的更昔洛韦/0.1%HYA(HYA0.1)和更昔洛韦/SWI滴眼液(EDs)在5±3°C和30±2°C下的稳定性进行了评估。结果显示,更昔洛韦/SWI滴眼液在5±3°C下储存12周、在30±2°C下储存8周时具有良好的物理化学和微生物稳定性。同时,更昔洛韦/HYA0.1滴眼液在5±3°C和30±2°C下保持稳定8周,但0.3%HYA滴眼液中的更昔洛韦可在5±3°C下储存8周。然而,可能需要使用合适的方法研究颗粒物,以确保这些制剂中不存在不可见颗粒。基于这些结果,更昔洛韦/HYA人工泪液和SWI滴眼液显示出作为治疗眼部病毒感染的家庭用药的潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0a5f/9866864/0126bb5d38fa/pharmaceutics-15-00208-g001.jpg

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