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Improvement of dissolution rate of tacrolimus by solid dispersion technique
Shital S. Panchal,Tejal A. Mehta,Pranav V. Patel 한국약제학회 2013 Journal of Pharmaceutical Investigation Vol.43 No.1
Tacrolimus has a poor solubility in water ranging from 4 to 12 lg mL-1. The mean bioavailability is *21 %.The present study was carried out with a view to enhance the dissolution rate of poorly water-soluble drug tacrolimus using Gelucire 44/14 and Gelucire 50/13 as carriers and lactose monohydrate as an adsorbent. A combination of melt and adsorption techniques was employed for the preparation of solid dispersions (SD) to make final product easy for handling. Phase solubility study was conducted to evaluate the effect of carriers on aqueous solubility of tacrolimus. In order to elucidate the mechanism of dissolution enhancement, solid state characteristics were investigated using Fourier transform infrared spectroscopy,differential scanning calorimetry and powder X-ray diffraction. Mathematical modeling of in vitro dissolution data indicated the best fitting with Korsemeyer–Peppas model and the drug release kinetics primarily as Fickian/anomalous diffusion. All prepared solid dispersions showed dissolution improvement compared to pure drug, with Gelucire 50/13 as the superior carrier over Gelucire 44/14. Almost similar dissolution profile was obtained as a function of storage time; this can be explained by no change in XRD and DSC pattern after 45 days storage period.
Jigar N. Shah,Kashyap N. Shah,Tejal A. Mehta 한국약제학회 2015 Journal of Pharmaceutical Investigation Vol.45 No.1
Promethazine hydrochloride (PMZ-HCl) is a classical anti-motion sickness drug which has oral bioavailability (25 %) due to extensive hepatic first pass metabolism. To overcome this drawback, novel, fast dissolving sublingual film (FDSF) of drug was developed. FDSF was formulated using pullulan and propylene glycol (PG) by solvent casting method. Complete taste masking was successfully obtained with HP β-CD, aspartame and grape fruit flavour. Complex of drug was proved using Fourier transfer infrared spectroscopy, differential scanning calorimetry and X-ray diffraction studies. Optimization of concentration of pullulan and PG was done using 32 full factorial design. Batches were evaluated for the parameters like elongation, tensile strength, folding endurance and in vitro disintegration studies. In vitro dissolution indicated 100 % drug release within 7.5 min. Environmental scanning electron microscopy studies also showed uniform drug distribution and integrity of film. In vivo sublingual absorption in human indicated that 70 % of drug absorbed in 10 min. The stability studies indicated that label should state ‘‘Store at cool, dry place’’ at temperature 25 ˚C. So by formulating the taste masked FDSF of PMZ-HCl will give faster onset of action and avoid unnecessary drug intake leading to traveller friendly formulation.