The in vitro release of some antimuscarinic drugs from monoolein/water lyotropic liquid crystalline gels

被引:75
作者
Geraghty, PB
Attwood, D
Collett, JH
Dandiker, Y
机构
[1] UNIV MANCHESTER, DEPT PHARM, MANCHESTER M13 9PL, LANCS, ENGLAND
[2] GLAXO WELLCOME RES & DEV LTD, INT INHALAT PROD DEV, WARE SG12 0DP, HERTS, ENGLAND
关键词
monoolein; lyotropic liquid crystals; propantheline bromide; oxybutynin hydrochloride; drug release;
D O I
10.1023/A:1016036908947
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Purpose, To investigate the potential use of a monoolein/water lyotropic liquid crystalline gel for the vaginal delivery of the antimuscarinic drags, propantheline bromide and oxybutynin hydrochloride to treat urinary incontinence, using Myverol 18-99 as a commercially available grade of monoolein. Methods, The influence of propantheline bromide and oxybutynin hydrochloride on the phase structure of Myverol 18-99/water gels was investigated using polarising microscopy. The in-vitro release of the antimuscarinic drugs from Myverol 18-99/water gels was determined and the release pattern interpreted with the aid of results from swelling studies and partition coefficient determinations. Results, Myverol 18-99 forms gels with lyotropic liquid crystalline structures in the presence of water. The addition of propantheline bromide and oxybutynin hydrochloride promoted the formation of gels with a lamellar phase structure. The gels absorbed water at a rate inversely proportional to their initial water content until they reached an equilibrium water content of similar to 40% w/w whilst maintaining their physical integrity. The release of the antimuscarinic drugs was sustained over a period of similar to 18 hours and followed square root of time kinetics indicating that the rate of release was diffusion controlled. Conclusions. The in-vitro release behaviour of Myverol 18-99/water gels suggested that they are suitable carriers to deliver propantheline bromide or oxybutynin hydrochloride. The results of swelling studies indicated that a confined area, such as the vaginal cavity, would be a suitable site of administration.
引用
收藏
页码:1265 / 1271
页数:7
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