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用于青光眼治疗的马来酸噻吗洛尔眼用原位凝胶形成溶液的制剂与表征

Formulation and Characterization of Ophthalmic in Situ Gel Forming Solution of Timolol Maleate for Glaucoma.

作者信息

Rajagopal Kumaravelrajan, Kanmani Gokul, Venkatesan Suba, Palanivelu Amudha

机构信息

Department of Pharmaceutics, C.L. Baid Metha College of Pharmacy, The TN DR M.G.R. Medical University, Jothi Nagar, Thoraipakkam, Chennai, Tamil Nadu, India.

Department of Pharmacology, National Institute of Siddha, The TN DR.M.G.R.Medical University, Chennai, Tamil Nadu, India.

出版信息

Int J Pharm Compd. 2025 Mar-Apr;29(2):132-140.

Abstract

This study comprehensively investigates the physicochemical properties and performance of ophthalmic formulations containing timolol maleate with different polymers. Fourier-transform infrared (FTIR) spectroscopy revealed distinct spectral changes, indicating interactions between timolol maleate and Hydroxyethyl Cellulose (HEC), Xanthan gum, and Gellan gum. Clarity assessments confirmed transparency against white and black backgrounds. pH measurements ensured physiological compatibility (HEC: pH 6.90, Xanthan gum: pH 6.97, Gellan gum: pH 6.98). Evaluation of gelling capacity and strength highlighted Xanthan gum's superiority (Xanthan gum: 180 Pa, Gellan gum: 153 Pa). Viscosity studies demonstrated suitability for ocular use, with pre-gelling values of HEC: 100.11 cps, Xanthan gum: 112.55 cps, Gellan gum: 110.42 cps, and post-gelling values of HEC: 100.01 cps, Xanthan gum: 256.22 cps, Gellan gum: 206.21 cps. Osmolality aligned with ophthalmic norms (HEC: 272 mOsm/kg, Xanthan gum: 290 mOsm/kg, Gellan gum: 285 mOsm/kg). In vitro drug release profiles varied, with Xanthan gum showing sustained release (95.01% over 8 hours). Rabbit eye irritation studies confirmed safety. Stability assessments over three months validated consistent attributes, supporting their potential as effective ophthalmic formulations.

摘要

本研究全面调查了含有不同聚合物的马来酸噻吗洛尔眼科制剂的物理化学性质和性能。傅里叶变换红外(FTIR)光谱显示出明显的光谱变化,表明马来酸噻吗洛尔与羟乙基纤维素(HEC)、黄原胶和结冷胶之间存在相互作用。澄清度评估证实了在白色和黑色背景下的透明度。pH测量确保了生理相容性(HEC:pH 6.90,黄原胶:pH 6.97,结冷胶:pH 6.98)。胶凝能力和强度评估突出了黄原胶的优越性(黄原胶:180 Pa,结冷胶:153 Pa)。粘度研究表明其适合眼部使用,预胶凝值为HEC:100.11 cps,黄原胶:112.55 cps,结冷胶:110.42 cps,后胶凝值为HEC:100.01 cps,黄原胶:256.22 cps,结冷胶:206.21 cps。渗透压符合眼科标准(HEC:272 mOsm/kg,黄原胶:290 mOsm/kg,结冷胶:285 mOsm/kg)。体外药物释放曲线各不相同,黄原胶显示出缓释效果(8小时内释放95.01%)。兔眼刺激性研究证实了安全性。三个月的稳定性评估验证了其属性的一致性,支持它们作为有效眼科制剂的潜力。

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