scholarly journals Enhancement of the dissolution rates of poorly water-soluble drugs by water-soluble gelatin.

1989 ◽  
Vol 37 (8) ◽  
pp. 2251-2252 ◽  
Author(s):  
Teruko IMAI ◽  
Tetsuyuki NISHIYAMA ◽  
Masao UENO ◽  
Masaki OTAGIRI
Keyword(s):  
Water Soluble ◽  
Dissolution Rates ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

scholarly journals Liquisolid technique as a tool for enhancement of poorly water-soluble drugs and evaluation of their physicochemical properties

2007 ◽  
Vol 57 (1) ◽  
pp. 99-109 ◽  
Author(s):  
Yousef Javadzadeh ◽  
Mohammad Siahi ◽  
Solmaz Asnaashari ◽  
Ali Nokhodchi
Keyword(s):  
Physicochemical Properties ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Scanning Calorimetry ◽  
Dissolution Rates ◽  
Compression Technique ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Liquisolid Compacts

Liquisolid technique as a tool for enhancement of poorly water-soluble drugs and evaluation of their physicochemical properties The potential of liquisolid systems to improve the dissolution properties of a water-insoluble agent (indomethacin) was investigated. In this study, different formulations of liquisolid tablets using different co-solvents (non-volatile solvents) were prepared and the effect of aging on the dissolution behaviour of indomethacin liquisolid compacts was investigated. To evaluate any interaction between indomethacin and the other components in liquisolid formulations, X-ray powder diffraction (XPD) and differential scanning calorimetry (DSC) were used. Dissolution test was carried out at two different pH, 1.2 and 7.2, to simulate the stomach or intestine fluid, respectively. The results showed that liquisolid formulations exhibited significantly higher drug dissolution rates at pH 1.2 and 7.2 compared to compacts prepared by the direct compression technique. The enhanced rate of indomethacin dissolution from liquisolid tablets was probably due to an increase in wetting properties and surface area of drug particles available for dissolution. In order to investigate the effect of aging on the hardness and dissolution rate of liquisolid compacts, the formulations were stored at 25 °C/75% relative humidity for a period of 12 months. The results showed that aging had no significant effect on dissolution profiles of liquisolid tablets. Liquisolid compacts containing propylene glycol as vehicle produced higher dissolution rates in comparison with liquisolid compacts containing PEG 400 or Tween 80 of the same concentration. The DSC and XPD results showed no changes in crystallinity of the drug and interaction between indomethacin and excipients (Avicel and silica) during the process.

scholarly journals Solubility enhancement of carvedilol using drug–drug cocrystallization with hydrochlorothiazide

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Shivarani Eesam ◽  
Jaswanth S. Bhandaru ◽  
Chandana Naliganti ◽  
Ravi Kumar Bobbala ◽  
Raghuram Rao Akkinepally
Keyword(s):  
Aqueous Solubility ◽  
Sem Analysis ◽  
Water Soluble ◽  
High Permeability ◽  
Poorly Water Soluble Drugs ◽  
Drug Discovery And Development ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Dissolution In Vitro

Abstract Background Increasing hydrophilicity of poorly water-soluble drugs is a major challenge in drug discovery and development. Cocrystallization is one of the techniques to enhance the hydrophilicity of such drugs. Carvedilol (CAR), a nonselective beta/alpha1 blocker, used in the treatment of mild to moderate congestive heart failure and hypertension, is classified under BCS class II with poor aqueous solubility and high permeability. Present work is an attempt to improve the solubility of CAR by preparing cocrystals using hydrochlorothiazide (HCT), a diuretic drug, as coformer. CAR-HCT (2:0.5) cocrystals were prepared by slurry conversion method and were characterized by DSC, PXRD, FTIR, Raman, and SEM analysis. The solubility, stability, and dissolution (in vitro) studies were conducted for the cocrystals. Results The formation of CAR-HCT cocrystals was confirmed based on melting point, DSC thermograms, PXRD data, FTIR and Raman spectra, and finally by SEM micrographs. The solubility of the prepared cocrystals was significantly enhanced (7.3 times), and the dissolution (in vitro) was improved by 2.7 times as compared to pure drug CAR. Further, these cocrystals were also found to be stable for 3 months (90 days). Conclusion It may be inferred that the drug–drug (CAR-HCT) cocrystallization enhances the solubility and dissolution rate of carvedilol significantly. Further, by combining HCT as coformer could well be beneficial pharmacologically too.

Interlaboratory Validation of Small-Scale Solubility and Dissolution Measurements of Poorly Water-Soluble Drugs

2016 ◽  
Vol 105 (9) ◽  
pp. 2864-2872 ◽  
Author(s):  
Sara B.E. Andersson ◽  
Caroline Alvebratt ◽  
Jan Bevernage ◽  
Damien Bonneau ◽  
Claudia da Costa Mathews ◽  
...  
Keyword(s):  
Water Soluble ◽  
Small Scale ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Interlaboratory Validation ◽  
Poorly Water Soluble
Sign in / Sign up

Export Citation Format

Share Document