Effect of Biopolymer on the Dissolution and Stability of Itraconazole

2013 ◽  
Vol 747 ◽  
pp. 115-118 ◽  
Author(s):  
Benchawan Chamsai ◽  
Pornsak Sriamornsak
Keyword(s):  
Polyethylene Glycol ◽  
Drug Release ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
Crystalline Form ◽  
Dissolution Time ◽  
Polyethylene Glycol 4000 ◽  
Melting Method ◽  
Amorphous Form ◽  
X Ray

traconazole (ITZ) polyethylene glycol 4000 (PEG) solid dispersions (SDs) containing hydroxypropyl methylcellulose (HPMC) and/or low methoxy pectin (LMP) were prepared by melting method at a ratio of drug to carrier of 1:9. ITZPEG formulations showed the highest drug release (83.51%) when compared to the formulations containing HPMC and/or pectin (i.e., 43.02%, 40.64% and 59.94% for those containing HPMC, LMP and HPMC+LMP, respectively). Powder X-ray diffractograms of all formulations revealed that the drug was present in an amorphous form while a crystalline form was observed only in ITZ or its physical mixture. After storage at accelerated condition (40°C, 75%RH) for 2 and 12 months, the crystalline of ITZ was clearly not observed in all SDs. All formulations showed an increase in mean dissolution time (MDT) but the formulations containing biopolymer showed the lower MDT than that containing no biopolymer. The results suggested that either HPMC or LMP in SDs can help to inhibit the recrystallization of amorphous ITZ in SD, probably by a polymer anti-plasticizing effect.

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.

Effect of Drug Loading and Process Temperature on Physicochemical Properties of Manidipine Hydrochloride Solid Dispersion

2014 ◽  
Vol 1060 ◽  
pp. 176-179 ◽  
Author(s):  
Benchawan Chamsai ◽  
Pornsak Sriamornsak
Keyword(s):  
Solid Dispersion ◽  
Drug Loading ◽  
Solid Dispersions ◽  
Crystalline Form ◽  
Process Temperature ◽  
Melting Method ◽  
X Ray ◽  
Peg 4000 ◽  
Melting Technique ◽  
Clear Solution

Binary solid dispersions of manidipine hydrochloride (MDP) and polyethylene glycol (PEG) 4000 are prepared by melting method. Drug loading and process temperature are varied in the range of 5-30% and 150-210°C, respectively. After melting, only the formulation using 5% MDP and process temperature of 210°C showed yellow clear solution and halo pattern of powder X-ray diffractograms with the absence of peaks. These results indicated that the higher process temperature (210°C) can melt all MDP powders and provide the amorphous product. Moreover, only the higher carrier content can change the crystalline form of MDP to the amorphous form. A clear, solid solution could not be prepared when the drug loading was higher than 5%. In this study, the melting technique avoiding the use of organic solvent was successfully applied to prepared binary solid dispersion.

scholarly journals Combinations of Freeze-Dried Amorphous Vardenafil Hydrochloride with Saccharides as A Way to Enhance Dissolution Rate and Permeability

2021 ◽  
Vol 14 (5) ◽  
pp. 453
Author(s):  
Gabriela Wiergowska ◽  
Dominika Ludowicz ◽  
Kamil Wdowiak ◽  
Andrzej Miklaszewski ◽  
Kornelia Lewandowska ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Density Functional ◽  
Hydroxypropyl Methylcellulose ◽  
Fold Increase ◽  
Crystalline Form ◽  
Amorphous Form ◽  
Freeze Dried ◽  
Apparent Solubility ◽  
Gastrointestinal Epithelium ◽  
The Impact

To improve physicochemical properties of vardenafil hydrochloride (VAR), its amorphous form and combinations with excipients—hydroxypropyl methylcellulose (HPMC) and β-cyclodextrin (β-CD)—were prepared. The impact of the modification on physicochemical properties was estimated by comparing amorphous mixtures of VAR to their crystalline form. The amorphous form of VAR was obtained as a result of the freeze-drying process. Confirmation of the identity of the amorphous dispersion of VAR was obtained through the use of comprehensive analysis techniques—X-ray powder diffraction (PXRD) and differential scanning calorimetry (DSC), supported by FT-IR (Fourier-transform infrared spectroscopy) coupled with density functional theory (DFT) calculations. The amorphous mixtures of VAR increased its apparent solubility compared to the crystalline form. Moreover, a nearly 1.3-fold increase of amorphous VAR permeability through membranes simulating gastrointestinal epithelium as a consequence of the changes of apparent solubility (Papp crystalline VAR = 6.83 × 10−6 cm/s vs. Papp amorphous VAR = 8.75 × 10−6 cm/s) was observed, especially for its combinations with β-CD in the ratio of 1:5—more than 1.5-fold increase (Papp amorphous VAR = 8.75 × 10−6 cm/s vs. Papp amorphous VAR:β-CD 1:5 = 13.43 × 10−6 cm/s). The stability of the amorphous VAR was confirmed for 7 months. The HPMC and β-CD are effective modifiers of its apparent solubility and permeation through membranes simulating gastrointestinal epithelium, suggesting a possibility of a stronger pharmacological effect.

scholarly journals ENHANCEMENT OF SOLUBILITY AND OPTIMIZATION OF ORALLY DISINTEGRATING FILMS OF ACYCLOVIR

2018 ◽  
Vol 11 (9) ◽  
pp. 280 ◽  
Author(s):  
Bikash Pandey ◽  
Arshad Bashir Khan
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Antiviral Agent ◽  
Disintegration Time ◽  
Casting Technique ◽  
Accelerated Stability ◽  
Full Factorial

Objective: The objective of this work was to prepare and optimize orally disintegrating films of acyclovir (ACV), which is a known antiviral agent. To enhance the solubility of ACV, solid dispersions of ACV were made.Methods: The films were prepared using a solvent casting technique. Full factorial design was utilized for the optimization of the effect of independent variables such as the amount of hydroxypropyl methylcellulose 5 cps, sodium starch glycolate, and propylene glycol on the disintegration time. Other evaluation tests such as drug release, drug content, thickness, and folding endurance of film were also conducted.Results: Compatibility studies by Fourier transform infrared showed that there was no significant interaction between the drug and excipients used. Disintegration time was found to be 43 s for the optimized batch. The in vitro release profile of formulation response disintegrating time in phosphate buffer pH 6.8 revealed that there was a significant increment in drug release of the optimized batch in comparison to the screening batches. Further, short-term accelerated stability studies carried out for 4 weeks for the optimized formulation which proved that the formulated films were stable at the accelerated conditions of temperature and humidity (40±2°C/75±5% RH).Conclusions: It was concluded that such ACV solid dispersion films could be beneficial in enhancement of dissolution and consequently the oral bioavailability of ACV.

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

Formulation, Characterization and Solubility Enhancement of Manidipine Solid Dispersions

2019 ◽  
Vol 12 (2) ◽  
pp. 4453-4460
Author(s):  
Laxmi Raj A ◽  
Y. Shravan Kumar
Keyword(s):  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
In Vitro Dissolution ◽  
X Ray Diffraction ◽  
Amorphous Form ◽  
X Ray ◽  
Solvent Evaporation Process

The study was aimed to formulate solid dispersions of Manidipine by using different novel carriers like Labrafac PG, Kolliwax RH 40, Soluplus, Kolliwax GMS II, Kolliphor EL and SLS in drug carrier ratio by using solvent evaporation method. The formulations were characterized for physical appearance, solubility and in vitro dissolution studies. The optimized formulation was characterized and Formulation SD13 was found to be optimized one based on the solubility, dissolution and other parameters using Kolliwax GMS II and SLS.  The drug release of the optimized formulation was found to be 99.41±5.38% within 90 min. Powder X-ray diffraction studies performed on solid dispersion showed that Manidipine existed in the amorphous form within the solid dispersion formulation fabricated using the solvent evaporation process. Additionally, scanning electron microscopy studies suggested the conversion of crystalline Manidipine to an amorphous form. Therefore, the solid dispersions using Kolliwax GMS II as hydrophilic carrier in the combination of SLS can be successfully used for improvement of solubility and dissolution of Manidipine.  

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 Fluoroquinolone Amorphous Polymeric Salts and Dispersions for Veterinary Uses

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 268 ◽  
Author(s):  
Hanah Mesallati ◽  
Anita Umerska ◽  
Lidia Tajber
Keyword(s):  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
Amorphous Solid ◽  
Ionic Bond ◽  
Amorphous Solid Dispersions ◽  
X Ray ◽  
Poorly Soluble ◽  
Pure Drug ◽  
Poorly Soluble Drug ◽  
Pharmaceutical Properties

Enrofloxacin (ENRO) is a poorly soluble drug used in veterinary medicine. It differs from the more widely used fluoroquinolone ciprofloxacin (CIP) by the presence of an ethyl substituent on its piperazine amino group. While a number of recent studies have examined amorphous composite formulations of CIP, little research has been conducted with ENRO in this area. Therefore, the main purpose of this work was to produce amorphous solid dispersions (ASDs) of ENRO. The solid-state properties of these samples were investigated and compared to those of the equivalent CIP ASDs, and their water uptake behavior, solubility, dissolution, and antibacterial activity were assessed. Like CIP, X-ray amorphous solid dispersions were obtained when ENRO was ball milled with acidic polymers, whereas the use of neutral polymers resulted in semi-crystalline products. Proton transfer from the carboxylic acids of the polymers to the tertiary amine of ENRO’s piperazine group appears to occur in the ASDs, resulting in an ionic bond between the two components. Therefore, these ASDs can be referred to as amorphous polymeric salts (APSs). The glass transition temperatures of the APSs were significantly higher than that of ENRO, and they were also resistant to crystallization when exposed to high humidity levels. Greater concentrations were achieved with the APSs than the pure drug during solubility and dissolution studies, and this enhancement was sustained for the duration of the experiments. In addition, the antimicrobial activity of ENRO was not affected by APS formation, while the minimum inhibitory concentrations and minimum bactericidal concentrations obtained with the APS containing hydroxypropyl methylcellulose acetate succinate grade MG (HPMCAS-MG) were significantly lower than those of the pure drug. Therefore, APS formation is one method of improving the pharmaceutical properties of this drug.

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