Design and optimization of self-microemulsifying drug delivery system (SMEDDS) of felodipine for chronotherapeutic application

The objective of this research work was to design, develop and optimize the self micro-emulsifying drug delivery system (SMEDDS) of Felodipine (FL) filled in hard gelatine capsule coated with polymer in order to achieve rapid drug release after a desired time lag in the management of hypertension. Microemulsion is composed of a FL, Lauroglycol FCC, Transcutol P and Cremophor EL. The optimum surfactant to co-surfactant ratio was found to be 2:1. The resultant microemulsions have a particle size in the range of 65-85 nm and zeta potential value of -13.71 mV. FL release was adequately adjusted by using pH independent polymer i.e. ethyl cellulose along with dibutyl phthalate as plasticizer. Influence of formulation variables like viscosity of polymer, type of plasticizer and percent coating weight gain was investigated to characterize the time lag. The developed formulation of FL SMEDDS capsules coated with ethyl cellulose showed time lag of 5-7 h which is desirable for chronotherapeutic application.

O objetivo desse trabalho de pesquisa foi planejar, desenvolver e otimizar sistema de liberação de fármaco auto-microemulsificante(SMEDDS) de felodipino (FL) em cápsulas de gelatina dura revestidas com polímero, a fim de obter liberação rápida após tempo desejado no manejo da hipertensão. A microemulsão é composta de FL, lauroglilcol FCC, Transcutol P e Cremophor EL. A proporção ótima de tensoativo e de co-tensoativo foi de 2:1. As microemulsões resultantes têm tamanho de partícula na faixa de 65-85 nm com potencial zeta de -13,71 mV. A liberação de FL foi ajustada adequadamente, utilizando-se polímero independente de pH, como etilcelulose com ftalato de dibutila como plastificante. A influência das variáveis da formulação, como viscosidade do polímero, tipo de plastificante e ganho percentual de peso do revestimento foi investigada para caracterizar o intervalo de tempo de liberação. A formulação de cápsulas de FL SMEDDS revestidas com etilcelulose mostrou intervalo de tempo de liberação de 5 a 7 horas, o que é desejável para uma aplicação cronoterapêutica.

Clinical efficacy of the various drugs used in the treatment of gonorrhoea

Gonorrhoea is a purulent inflammation of mucus membrane of the genital tract and is a highly contagious sexually transmitted disease [STD] caused by the bacterium Neisseria gonorrhoae. Both men and women can be infected through a variety of sexual contact behaviours including vaginal, anal or oral intercourses. This comparative study was carried out in New Gulail Polyclinic Jeddah, KSA from Jan 2003 to March 2004 to find the clinical efficacy of ciprofloxacin, ceftriaxone and spectinomycin, the three commonly used drugs, in the treatment of gonorrhoea. A total number of 300 patients suffering from gonorrhoea were included in this study. They were randomly divided into 3 groups of 100 patients each. Group-A patients were given Tablet Ciprofloxacin 500 mg, Group-B patients Injection Ceftriaxone 500 mg, and Group-C patients were put on Injection Spectinomycin 2 gm, all in stat dosage. On the 5th day following the treatment, all patients were re-examined and their clinical and laboratory findings were recorded and analysed. On the 5th day following treatment the Group-A [n=100] showed 9 [9%] partial response and 11 [11%] cases showed no response to Ciprofloxacin. In the Group-B [n=100], 4 [4%] patients showed partial response and 6 [6%] patients showed no response to Ceftriaxone. In Group-C, out of 100 patients, 4 [4%] cases reported with partial response and 2 [2%] patients showed no response to Spectinomycin. The efficacy of these anti-microbial agents was the same in both the genders. Anti-microbial susceptibility of N. gonorrhoeae to various antibiotics is gradually decreasing. In order to ensure full cure, all gonorrhoea patients should be followed-up after a single dosage of any antibiotic. Further research should continue for newer, effective, and preferably oral medication for the treatment of gonorrhoea