Optimized release of dexamethasone and gentamicin from a soluble ocular insert for the treatment of external ophthalmic infections

Optimized release of dexamethasone and gentamicin from a soluble ocular insert for the treatment of external ophthalmic infections
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DOI:
10.1016/s0168-3659(97)00212-5
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发表时间:
1998-03-02
影响因子:
10.8
通讯作者:
Gurny, R
Gurny, R
中科院分区:
医学1区
文献类型:
--
作者:
Baeyens, V;Kaltsatos, V;Gurny, R

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在眼外感染的情况下,需要反复滴注抗生素以达到治疗水平,高于最小抑菌浓度(MIC)。通常需要额外给予皮质类固醇,以限制由感染引起的角膜前损害。然而,反复使用皮质类固醇可增加眼内压,从而导致青光眼。为了克服两种产品分开重复滴注的缺点和避免地塞米松的副作用,开发了含有硫酸庆大霉素和磷酸地塞米松的可溶性插入物。新系统确保在治疗的前10小时内两种药物同时释放,随后在50小时内硫酸庆大霉素的浓度足够高,高于4.0 μ g ml(-1)的MIC,这是由于硫酸庆大霉素与邻苯二甲酸醋酸纤维素的组合降低了庆大霉素的溶解度。(C)1998年Elsevier Science B.V.
In the case of external ophthalmic infections, repeated instillations of antibiotics are required to reach therapeutic level, above the minimal inhibitory concentration (MIG). An additional administration of a corticosteroid is often needed, in order to limit the precorneal damages caused by the infection. However, repeated administration of a corticosteroid can increase intraocular pressure and thus lead to glaucoma. To overcome the disadvantages of separated and repeated instillations of two products and to avoid the side effects of dexamethasone, a soluble insert containing gentamicin sulfate and dexamethasone phosphate was developed. The new system ensures the concomitant release of the two drugs during the first 10 h of treatment, followed by an adequate concentration of gentamicin sulfate, above the MIC of 4.0 mu g ml(-1), during 50 h, due to a combination of gentamicin sulfate with cellulose acetate phthalate, which reduces the solubility of gentamicin. (C) 1998 Elsevier Science B.V.