Jani R, Gan O, Ali Y, Rodstrom R, Hancock S
Alcon Laboratories, Inc., Fort Worth, Texas.
J Ocul Pharmacol. 1994 Spring;10(1):57-67. doi: 10.1089/jop.1994.10.57.
A new novel delivery system for ophthalmic drugs was developed using an antiglaucoma agent Betaxolol Hydrochloride as a model. The new delivery system involved both the binding and release of drug from ion exchange resin particles. Betaxolol was studied in-vitro via a release model analysis. The ocular comfort of Betaxolol was greatly enhanced by reducing the availability of free drug molecules in the precorneal tear film. The amount of resin concentration was selected to obtain optimum binding of the drug. The zeta potential of suspended particles was adjusted to produce flocculated suspension. Drug resin particles were then incorporated into the structured vehicle, containing Carbomer 934P as a polymer, to enhance the physical stability and ease of resuspendability of the product. This delivery system also optimized the bioavailability of Betaxolol, reducing the total drug concentration in half to 0.25% Betaxolol in 0.25% BETOPTIC S Ophthalmic Suspension as compared with 0.5% Betaxolol in BETOPTIC 0.5% Sterile Ophthalmic Solution dosage form. Increased comfort of 0.25% BETOPTIC S Ophthalmic Suspension, as well as its bioequivalency data in animal models (rabbits), was confirmed in actual clinical trials of the product 0.25% BETOPTIC S Ophthalmic Suspension. The 0.25% BETOPTIC S Ophthalmic Suspension product has been approved gamma FDA and is marketed in U. S. since February 1990. The 0.25% BETOPTIC S Ophthalmic Suspension formulation has an increased bioavailability (equivalent to BETOPTIC 0.5% Sterile Ophthalmic Solution at half the concentration of drug); and pharmaceutically, is an elegant suspension product which settles slowly providing uniform dosage and increased ocular comfort.
以抗青光眼药物盐酸倍他洛尔为模型，开发了一种新型眼科药物递送系统。这种新型递送系统涉及药物与离子交换树脂颗粒的结合和释放。通过释放模型分析对倍他洛尔进行了体外研究。通过减少角膜前泪膜中游离药物分子的可用性，倍他洛尔的眼部舒适度得到了极大提高。选择树脂浓度以获得药物的最佳结合。调节悬浮颗粒的ζ电位以产生絮凝悬浮液。然后将药物树脂颗粒掺入含有卡波姆934P作为聚合物的结构化载体中，以提高产品的物理稳定性和再悬浮的便利性。该递送系统还优化了倍他洛尔的生物利用度，与倍他洛尔0.5%无菌眼用溶液剂型中0.5%的倍他洛尔相比，将0.25%倍他洛尔在0.25%BETOPTIC S眼用混悬液中的总药物浓度降低了一半。在0.25%BETOPTIC S眼用混悬液产品的实际临床试验中，证实了0.25%BETOPTIC S眼用混悬液的舒适度提高以及其在动物模型（兔子）中的生物等效性数据。0.25%BETOPTIC S眼用混悬液产品已获得美国食品药品监督管理局（FDA）的批准，并自1990年2月起在美国上市。0.25%BETOPTIC S眼用混悬液制剂具有更高的生物利用度（相当于药物浓度减半的倍他洛尔0.5%无菌眼用溶液）；并且在药学上，是一种优良的混悬液产品，沉降缓慢，提供均匀剂量并提高眼部舒适度。
