马来酸替马洛尔眼用缓释体凝胶的研制与表征

Ankit Acharya, P. Goudanavar, V. Joshi
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引用次数: 3

摘要

眼部给药的主要目标是改进现有的常规剂型和开发新的给药系统,以提高其治疗效率。眼疾患者局部使用滴眼液的情况相当普遍。常用的常规滴眼液由于泪液持续分泌、泪液周转、眨眼、反射和鼻泪液快速引流,导致眼部生物利用度低。注入剂量后立即开始正常引流,基本在5分钟内完成(Achouri et al., 2013)。通常,由于角膜前停留时间短,滴眼液的眼生物利用度不到5%。因此,需要经常滴注浓溶液以达到所需的治疗效果。为了克服这些问题,人们研究了各种眼科配方,如粘性溶液、软膏、凝胶、纳米颗粒或聚合物插入物(Patel et al., 2013)。这些载体不同程度地增加了角膜接触时间。但是,由于视力模糊(如软膏)或缺乏患者依从性(如插入物),它们并未被一致接受。因此,局部给药后良好的眼部生物利用度仍然是一个有待解决的挑战(Li et al., 2010)。
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Development and characterization of prolonged release Timolol maleate cubosomal gel for ocular drug delivery
The main objective of ocular drug delivery is to improve the currently available conventional dosage form and exploit newer drug delivery system, with the view to improve their therapeutic efficiency. Topical application of eye drops is quite common among the patients suffered from the eye diseases. Commonly used conventional eye drops shows low ocular bioavailability due to constant lachrymal secretion, tear turnover, blinking, reflex and rapid nasolachrymal drainage. Normal drainage of an instilled dose commences immediately on instillation and is essentially completed within 5 min (Achouri et al., 2013). Typically less than 5% of ocular bioavailability is achieved for eye drops due to the short precorneal residence times. Consequently, there is a need for frequent instillation of concentrated solutions to achieve the desired therapeutic effect. To overcome these problems various ophthalmic formulations, such as viscous solutions, ointments, gels, nanoparticles or polymeric inserts have been investigated (Patel et al., 2013). The corneal contact time has been increased to varying degrees by these vehicles. But, they have not been unanimously accepted, because of blurred vision (e.g. ointments) or lack of patient compliance (e.g. inserts). As a result, good ocular bioavailability following topical delivery of a drug to the eye remains a challenge and yet to be resolved (Li et al., 2010).
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