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RISS 인기검색어
- 검색키워드
- 저자 : Md. Akhlaquer Rahman (검색결과 2 건)
- 무료
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Md. Akhlaquer Rahman,Zeenat Ara Lila,Arshad Hussain 한국약제학회 2012 Journal of Pharmaceutical Investigation Vol.42 No.4
Sertraline is a selective serotonin reuptake inhibitors used as major therapeutic advances in psychiatry and is drug of choice for treatment of major depressive disorders. The drug (free base) encounters problem of poor aqueous solubility and vulnerability to enzymatic degradation in liver. The hydrochloride salts of free base revert back to its original form in gastrointestinal tract leading to slow/poor absorption. In the current study, sertraline loaded self-nanoemulsifying drug delivery systems (SNEDDS)were prepared in an attempt to circumvent the problems associated with poor aqueous solubility, vulnerability to enzymatic degradation in liver and to sort out the problems associated with salt formation. Preliminary screening was carried out to select proper ingredient combinations. Ternary phase diagrams were then constructed and an optimum system was designated. Formulations selected were then compared for optimization. The systems were assessed for robustness, globule size, cloud point, percentage transmittance, surface morphology and drug release. An optimum system composed of oil (25.42 %), surfactant (49.72 %), and co-surfactant (24.86 %). It possessed a mean globule size, cloud point and percentage transmittance of 63.5 nm, 90 C and 82.43 %, respectively. Transmission electron microscopy demonstrated spherical particle morphology. The drug release from the selected formulation was significantly higher than other SNEDDS and drug suspension as well. Optimized formulation was subjected to stability studies at different temperature and relative humidity and was found to be stable. No significant variations were observed in the formulation over a period of 3 months at accelerated conditions.
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Md. Akhlaquer Rahman,Md. Mujahid,Arshad Hussain,Zeenat Iqbal 한국약제학회 2017 Journal of Pharmaceutical Investigation Vol.47 No.4
The objective of the present study was to develop solid self-nanoemulsifying drug delivery system (SNEDDS) of poorly absorbed drug sertraline (SRT) and evaluation of its pharmacokinetic parameters in rats. The composition of optimized liquid SNEDDS was (25.42 % v/v) Labrafil M 2125 CS and Maisine 35-1 (1:1), (49.72 % v/v) Tween 80 and (24.86 % v/v) Lauroglycol 90 containing 25 mg SRT. Solid SNEDDS was prepared by spray-drying the liquid SNEDDS using dextran 40 as solid carrier. There was no significant difference (p[0.05) in the droplet size of reconstituted nanoemulsion between both liquid and solid SNEDDS. The surface characterization of spray-dried powder showed a satisfactory regular spherical shape of particles. The internal physical state of SRT was verified by X-ray diffraction analysis indicated the transformation of crystalline structure of SRT to amorphous and molecularly dispersed state. In vitro release of SRT from solid SNEDDS was highly significant (p\0.01) as compared to unformulated SRT. After oral administration of solid SNEDDS to adult Sprague–Dawley (SD) rats, the area under the curve (AUC) were 2.8- and 6.8-folds and the maximum plasma concentration (Cmax) were 3.5 -and 13-folds higher, respectively compared to those of conventional capsule and unformulated drug suspension. These results reveal that solid SNEDDS results in a significantly increased absorption of SRT compared with that from the marketed conventional capsule and aqueous suspension of SRT. Thus, this solid SNEDDS may provide a useful solid dosage form for oral delivery of poorly-water soluble lipophilic compounds.
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