Department of Ophthalmology, Ruijin Hospital Affiliated Medical School, Shanghai Jiaotong University, Shanghai, People's Republic of China.
Drug Des Devel Ther. 2021 May 18;15:2099-2107. doi: 10.2147/DDDT.S308448. eCollection 2021.
To establish a novel delivery system of pemirolast potassium-loaded gellan gum in situ gel in allergic conjunctivitis therapy.
The prepared in situ gels were studied in the following aspects: in vitro gelation, in vitro release, stability, viscosity measurement, in vivo tear kinetics and pharmacodynamics.
In this study, the results showed that the viscosity of the in situ gels significantly increased when the preparation was in contact with simulated tear fluid and it also exhibited good stability in a period of three months. In vitro release showed that the release of pemirolast potassium from in situ gels had a good sustained release ability. No ocular damage or abnormal clinical signs to the cornea, iris, or conjunctivae were visible. Consistent with the in vitro studies, pemirolast potassium in situ gels were highly efficient in suppressing the inflammatory symptoms and improving the ocular bioavailability.
Pemirolast potassium ocular in situ gels are safe and promising therapeutic alternatives to the existing medications for allergic conjunctivitis therapy.
为治疗过敏性结膜炎，建立一种载培美洛司他钾的新型卡拉胶原位凝胶给药系统。
对制备的原位凝胶进行了以下方面的研究：体外胶凝、体外释放、稳定性、黏度测定、体内泪液动力学和药效学。
研究结果表明，制剂与模拟泪液接触时，原位凝胶的黏度显著增加，且在三个月的时间内表现出良好的稳定性。体外释放结果表明，培美洛司他钾从原位凝胶中的释放具有良好的持续释放能力。角膜、虹膜或结膜无眼部损伤或异常临床迹象。与体外研究一致，培美洛司他钾原位凝胶能高效抑制炎症症状，提高眼部生物利用度。
培美洛司他钾眼用原位凝胶是治疗过敏性结膜炎现有药物的安全、有前途的治疗替代药物。
