Physicochemical characterization and in vivo properties of Zolpidem in solid dispersions with polyethylene glycol 4000 and 6000

1999 ◽  
Vol 184 (1) ◽  
pp. 121-130 ◽  
Author(s):  
Giuseppe Trapani ◽  
Massimo Franco ◽  
Andrea Latrofa ◽  
Maria Rosaria Pantaleo ◽  
Maria Rosaria Provenzano ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Polyethylene Glycol 4000

scholarly journals EFFECT OF SELECTED POLYMERS ON DISSOLUTION AND STABILIZATION OF AMORPHOUS FORM OF MELOXICAM

2017 ◽  
Vol 9 (9) ◽  
pp. 33
Author(s):  
Rana Obaidat ◽  
Bashar Al-taani ◽  
Hanan Al-quraan
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersions ◽  
Dissolution Profile ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Polyethylene Glycol 4000 ◽  
Amorphous Form ◽  
Molecular Weights ◽  
Low Solubility ◽  
Reproducible Manner

Objective: Meloxicam is classified as class II corresponding to its high permeability and low solubility (12μg/ml). This study aims to compare the effect of selected polymers on stabilization of amorphous form, and dissolution of meloxicam by preparation of different solid dispersions using selected polymers (chitosan oligomers, polyvinylpyrrolidone K30, and polyethylene glycols).Methods: These solid dispersions were prepared using two different methods; solvent evaporation method for the two molecular weights chitosan carriers (16 and 11KDa) and polyvinylpyrrolidone-K30 and melting method for the two different molecular weights polyethylene glycol (4000 and 6000). The physicochemical properties of solid dispersions were analyzed using differential scanning calorimetry, Fourier transform infra-red analysis, Powder X-ray diffraction, and scanning electron microscopy. Selected dispersions were then compared to two selected marketed drugs (Mobic® and Moven®).Results: Best dissolution rates were obtained for both polyvinylpyrrolidone-K30 and polyethylene glycol 6000, followed by chitosan 16 kDa, chitosan 11 kDa, and polyethylene glycol 4000. Increasing polymeric ratio increased dissolution rate except for chitosan. Precipitation of the drug as amorphous form occurred in chitosan and polyvinylpyrrolidone-K30 dispersions, while no change in crystallinity obtained for polyethylene glycol dispersions. Failure of polyvinylpyrrolidone-K30 in the maintenance of stability during storage time was observed while re-crystallization occurred in chitosan-based dispersions, which ends with preferences to polyethylene glycol dispersions. After comparing the release of selected dispersions with the two selected polymers; all dispersions got a higher release than that of the two marketed drugs release.Conclusion: The dissolution profile of meloxicam has been increased successfully in a reproducible manner.

scholarly journals Preparation and Evaluation of Immediate Release Ibuprofen Solid Dispersions Using Polyethylene Glycol 4000

2008 ◽  
Vol 31 (5) ◽  
pp. 939-945 ◽  
Author(s):  
Madhuri Newa ◽  
Krishna Hari Bhandari ◽  
Dong Xun Li ◽  
Jong Oh Kim ◽  
Dong Sung Yoo ◽  
...  
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersions ◽  
Immediate Release ◽  
Polyethylene Glycol 4000 ◽  
Preparation And Evaluation

scholarly journals Physicochemical characterization and solubility enhancement studies of allopurinol solid dispersions

2011 ◽  
Vol 47 (3) ◽  
pp. 513-523 ◽  
Author(s):  
Jagdale Swati Changdeo ◽  
Musale Vinod ◽  
Kuchekar Bhanudas Shankar ◽  
Chabukswar Anuruddha Rajaram
Keyword(s):  
Polyethylene Glycol ◽  
Solid State ◽  
Dissolution Rate ◽  
Solid Dispersions ◽  
Amorphous Material ◽  
Physicochemical Characterization ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Phase Solubility ◽  
Polyethylene Glycol 6000

Allopurinol is a commonly used drug in the treatment of chronic gout or hyperuricaemia associated with treatment of diuretic conditions. One of the major problems with the drug is that it is practically insoluble in water, which results in poor bioavailability after oral administration. In the present study, solid dispersions of allopurinol were prepared by solvent evaporation, kneading method, co-precipitation method, co-grinding method and closed melting methods to increase its water solubility. Hydrophilic carriers such as polyvinylpyrrolidone, polyethylene glycol 6000 were used in the ratio of 1:1, 1:2 and 1:4 (drug to carrier ratio). The aqueous solubility of allopurinol was favored by the presence of both polymers. These new formulations were characterized in the liquid state by phase solubility studies and in the solid state by differential scanning calorimetry, powder X-ray diffraction, UV and Fourier Transform Infrared spectroscopy. Solid state characterizations indicated that allopurinol was present as an amorphous material and entrapped in polymer matrix. In contrast to the very slow dissolution rate of pure allopurinol, the dispersion of the drug in the polymers considerably enhanced the dissolution rate. Solid dispersion prepared with polyvinylpyrrolidone showed highest improvement in wettability and dissolution rate of allopurinol. Mathematical modeling of in vitro dissolution data indicated the best fitting with Korsemeyer-Peppas model and the drug release kinetics primarily as Non-Fickian diffusion. Therefore, the present study showed that polyvinylpyrrolidone and polyethylene glycol 6000 have a significant solubilizing effect on allopurinol.

Exposure of rat colonic mucosa to human semen in vivo induces mucosal cytolysis, abolishes fluid absorption and raises paracellular permeability

1992 ◽  
Vol 82 (3) ◽  
pp. 277-282 ◽  
Author(s):  
M. V. Mendizabal ◽  
R. J. Naftalin
Keyword(s):  
Polyethylene Glycol ◽  
Seminal Plasma ◽  
Colonic Mucosa ◽  
Human Semen ◽  
Fluid Absorption ◽  
Colonic Wall ◽  
Polyethylene Glycol 4000 ◽  
Bacterial Collagenase ◽  
Colonic Lumen

1. The effects of human semen on rat descending colon fluid absorption, permeability to 3H-labelled polyethylene glycol 4000 and the histological appearance of the mucosa were examined. Also, the semen was fractioned by centrifugation into plasma and sperm fractions and the effects of these fractions on rat colonic function were examined. The effects of trypsin and bacterial collagenase, mimetics of acrosin and seminal collagenase activity, were examined in order to investigate which component of human semen alters colonic permeability. 2. Contact between human semen and rat descending colonic mucosa for 3 h decreased fluid absorption from 52.0 ± 2.9 μl h−1 cm−2 (control) to 10.7 ± 3.4 μl h−1 cm−2 (P >0.001), increased the permeability to polyethylene glycol 4000 from 0.099 ± 0.006 cm/h (control) to 0.31 ± 0.04 cm/h (P>0.001) and caused cytolysis of the surface mucosa. 3. Spermatazoa inside the colonic lumen were destroyed within 1 h with release of acrosomal contents; this raised the activity of the acrosomal proteolytic enzyme acrosin by 40-fold (P >0.005) and of seminal plasma metalloproteinase (collagenase) by about twofold (mean activity 1623 ± 240 units/ml of luminal fluid). 4. The changes in colonic permeability induced by seminal plasma were similar to those induced by similar activities of clostridial collagenase. 5. We conclude that seminal collagenase is present in sufficient amounts to cause acute damage to the colonic mucosa, and that this could be a factor in facilitating viral transmission across the colonic wall.

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