de Leede L G, Govers C P, de Nijs H
Contraception. 1986 Dec;34(6):589-602. doi: 10.1016/s0010-7824(86)80015-4.
A multi-compartment contraceptive vaginal ring system has been designed for the simultaneous zero-order release of contraceptive steroids, the rates of which can be programmed independently. This vaginal ring system consists of two or more drug-containing Silastic tubes with an outer diameter of 5 mm. The tubes with different lengths, with a total length of 16.5 cm are connected with specially-shaped glass stoppers to obtain a ring with an outer diameter of 60 mm. The stopper prevents migration of the steroids from one compartment to the other and guarantees optimal release characteristics of both steroids even after long-term storage. An additional advantage of glass is the good adherence to Silastic, enabling construction of systems with sufficient tensile strength. The release characteristics have been followed in vitro and can be programmed independently by changing the wall thickness of the tube (membrane thickness) and/or the length of each individual steroid-containing compartment. Multicompartment vaginal rings were made and tested with 3-keto-desogestrel and ethinylestradiol. The rings had an outer diameter of 60 mm, and were fabricated with independent in vitro release rates ranging from 75 to 300 micrograms/day and 10 to 30 micrograms/day for, respectively, 3-keto-desogestrel and ethinylestradiol. Using the multi-compartment vaginal ring system, contraceptive devices can be fabricated relatively simply with pre-programmed release rates for a progestogen and an estrogen to investigate the optimal daily doses for vaginal hormonal contraception.
一种多隔室避孕阴道环系统已被设计用于同时实现避孕甾体激素的零级释放,其释放速率可独立编程。这种阴道环系统由两根或更多根外径为5毫米的含药硅橡胶管组成。这些长度不同、总长度为16.5厘米的管子通过特殊形状的玻璃塞连接,以获得外径为60毫米的环。该塞子可防止甾体激素从一个隔室迁移到另一个隔室,即使在长期储存后也能保证两种甾体激素的最佳释放特性。玻璃的另一个优点是与硅橡胶的良好粘附性,这使得能够构建具有足够拉伸强度的系统。已在体外跟踪释放特性,并且可以通过改变管的壁厚(膜厚度)和/或每个含甾体激素隔室的长度来独立编程。制作了多隔室阴道环并用3-酮去氧孕烯和炔雌醇进行了测试。这些环的外径为60毫米,制造出的环体外释放速率分别为3-酮去氧孕烯75至300微克/天和炔雌醇10至30微克/天,且释放速率相互独立。使用多隔室阴道环系统,可以相对简单地制造出具有预先设定的孕激素和雌激素释放速率的避孕装置,以研究阴道激素避孕的最佳日剂量。