Home About us Contact
|
Home About us Contact | ||
|
|
||
Dissolution Method (dissolution + method)
Selected AbstractsEvaluation of drug precipitation of solubility-enhancing liquid formulations using milligram quantities of a new molecular entity (NME)JOURNAL OF PHARMACEUTICAL SCIENCES, Issue 11 2007Wei-Guo Dai Abstract A precipitation screening method using a 96-well microtiter plate was developed to evaluate in vitro drug precipitation kinetics of liquid formulations for poorly water-soluble compounds, using milligram quantities of compounds and milliliter volumes of biorelevant media. By using this method we identified three formulations showing distinct in vitro precipitation kinetics (fast, slow, and no precipitation) for a model new molecular entity (JNJ-25894934). The in vitro precipitation profiles in simulated intestinal fluid (SIF), fasted state simulated intestinal fluid (FaSSIF), and fed state simulated intestinal fluid (FeSSIF) were compared with those measured by a USP dissolution method, and with in vivo absorption at the fasted and fed states in canine pharmacokinetic (PK) studies. The precipitation kinetics of all three formulations in the initial hours measured by the screening method correlated to those determined by the USP method (R2,=,0.96). The PK results showed that the fast-precipitation formulation had the lowest bioavailability. However, a similar bioavailability was observed for the slow- and no-precipitation formulations. The oral bioavailability of JNJ-25894934 at the fed state was also significantly higher than that at the fasted state for all three formulations (p,<,0.05). In addition, the in vitro precipitation profiles in FeSSIF correlated better with in vivo absorption than those in SIF and FaSSIF. © 2007 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 96: 2957,2969, 2007 [source] Functionalization of LDPE by Melt Grafting with Glycidyl Methacrylate and Reactive Blending with Polyamide-6MACROMOLECULAR CHEMISTRY AND PHYSICS, Issue 8 2003Qian Wei Abstract Low-density polyethylene (LDPE) was functionalized by melt radical grafting with glycidyl methacrylate (GMA) and employed for reactive blending with polyamide-6 (PA6). The effect of the reaction procedure on the grafting degree of LDPE- g -GMA samples (0.5,12.5 wt.-% GMA) was analyzed as a function of the concentration of GMA monomer, radical initiator (BTP), and addition of styrene as co-monomer. Optimized grafting conditions were obtained when the amount of the monomer is below 10 wt.-% and that of peroxide in the range 0.2,0.4 wt.-%. Binary blends of PA6 with LDPE- g -GMA (3.5 wt.-% GMA) and with LDPE at various compositions (80/20, 67/33, 50/50 wt.-%) were prepared in an internal mixer and their properties were evaluated by torque, SEM and DSC analyses. Morphological examination by SEM showed a large improvement of phase dispersion and interfacial adhesion in PA6/LDPE- g -GMA blends as compared with PA6/LDPE blends. The average diameter of dispersed polyolefin particles was about 0.4 ,m for LDPE- g -GMA contents <,50 wt.-%. A marked increase of melt viscosity was observed for the compatibilized blends depending on the concentration of grafted polyolefin, and it was accounted for by the reaction between the epoxy groups of GMA and the carboxyl/amine end-groups of PA6. The variation of torque was thus related to the molar ratio of reactive group concentration. The analysis of crystallization and melting behavior pointed out marked differences in the phase structure of the blends due to the presence of the functionalized polyolefin. Finally, the in situ formation of a graft copolymer between LDPE- g -GMA and PA6 was investigated by means of a selective dissolution method (Molau test) and by FT-IR and DSC analyses. SEM micrograph of fracture surface of PA6/LDPE- g -GMA 50/50 blend. [source] Carrier effects on oxygen mass transfer behavior in a moving-bed biofilm reactorASIA-PACIFIC JOURNAL OF CHEMICAL ENGINEERING, Issue 5 2009Jie Ying Jing Abstract This study investigates the carrier effects on the oxygen mass transfer behavior of a gas,liquid biofilm surface, and aims to provide evidence for parameter optimization in the practical operation of a moving-bed biofilm reactor (MBBR) during the coking-plant wastewater process. By using the dynamic oxygen dissolution method, the volumetric oxygen mass transfer coefficient KLa was measured by varying the suspended carrier stuffing rate and the intensity of aeration. Within the range of fluidizable flow rate, the efficiency of oxygen mass transfer increased with suspended carrier stuffing rate, and KLa reached its peak value when the stuffing rate was 40%. KLa has an increasing trend with an increase of the aeration intensity, but high aeration intensity was not favorable for reactor operation. Better oxygen mass transfer effect and higher oxygen transfer efficiency could be achieved when the aeration intensity was 0.3 m3 h,1 and the suspended carrier stuffing rate was 30,50%. The possible mechanisms that can account for carrier effects on oxygen mass transfer are the changes in the gas,liquid interfacial area. The ammonia nitrogen removal performance of the coking-plant wastewater in MBBR was satisfied by using the above-suggested conditions. Copyright © 2009 Curtin University of Technology and John Wiley & Sons, Ltd. [source] Miniaturization of Powder Dissolution Measurement and Estimation of Particle SizeCHEMISTRY & BIODIVERSITY, Issue 11 2009Alex Avdeef Abstract The objective was to investigate the applicability and limitations of an approach for estimating particle size from powder dissolution measurement using as little as 50,,g of sample in 1,ml of buffer solutions. The powder dissolution profiles of five sparingly-soluble drugs (hydrochlorothiazide, phenazopyridine hydrochloride, 2-naphthoic acid, indomethacin, and dipyridamole) were evaluated with a novel biexponential spherical particle equation and also the Wang,Flanagan spherical particle non-sink equation. The results were compared to particle sizing based on measured specific surface area by the Brunauer,Emmett,Teller (BET) method, and also based on Coulter counting. With the exception of hydrochlorothiazide, the model compounds indicated some agglomeration in the dissolution media. The dry-state specific surface area was larger than expected from either the Coulter method or the powder-dissolution data, especially for phenazopyridine hydrochloride. The particle radii estimated by the powder dissolution method ranged from 10 to 68,,m, with equilibrium solubilities spanning from 5,,g/ml (dipyridamole) to 911,,g/ml (hydrochlorothiazide). Powder dissolution data collected with the miniaturized apparatus can be used to determine particle size, with estimated values agreeing reasonably with those measured by the Coulter counter method. [source] | ||||||||||