Solid Dispersions Prepared by Continuous Cogrinding in an Air Jet Mill

Muehlenfeld, Christian; Kann, Birthe; Windbergs, Maike; Thommes, Markus

doi:10.1002/jps.23731

Cited by 15 publications

(18 citation statements)

References 47 publications

(49 reference statements)

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“…In addition, the mechanism of HPMC E5 LV on increasing solubility was also due to the intrinsic characteristic of HPMC as the hydrophilic polymer which soluble in the water 10,11,12 . Mechanical energy supplied during co-grinding process TMS -HPMC E5 LV in a planetary ball mill apparatus may cause crystalline phase of TMS underwent partial amorphization and TMS dispersed in a hydrophilic polymer network in the form of fine particles 14 . Thus, the dominant factors affecting drug dissolution from the co-grinding particles were the reduction of drug crystallinity, a probable decrease in drug particle size, an increase in the de-aggregation and wettability of hydrophobic drug particles.…”

Section: Solubility Testmentioning

confidence: 99%

Preparation and Characterization of Solid Dispersion Telmisartan – Hydroxypropyl Methyl Cellulose(HPMC) E5 LV by Co-Grinding Method

Zaini¹,

Fitriani²,

Effendy³

et al. 2017

Orient. J. Chem

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Telmisartan (TMS), an antihypertensive drug, is classified as class II according to Biopharmaceutical Classification System (BCS) with low solubility and high permeability. The purpose of this study was to prepare and characterize solid dispersion of TMS with hidroxypropyl methyl cellulose (HPMC) E5 LV to increase the solubility. Solid dispersion was prepared in three different ratio TMS:HPMC 2:1, 1:1, and 1:2 (w/w) by co-grinding method for 60 minutes. Solubility test was conducted in distilled water for 72 hours and the amount of TMS was determined by spectrophotometry UV. Result of Powder X-Ray Diffraction (PXRD) showed a decrease in intensity of TMS in accordance with the amount of HPMC E5 LV in solid dispersion. Fourier Transform Infra-Red(FT-IR)Spectra showed no significant shift of wavelength. Scanning Electron Microscopy (SEM) result presented the crystalline form of TMS, while both physical mixture and solid dispersion at different ratio showed TMS stick on the surface of HPMC E5 LV. Thermogram of Differential Scanning Calorimetry (DSC) showed an incline of endotherm peak as the ratio HPMC E5 LV increased. The solubility result of intact TMS was 0.49±0.03µg/mL, while the physical mixture and solid dispersion 2:1, 1;1 and 1:2 were 1.87±0.18 µg/mL, 5.36±0.48 µg/mL, 7.24±1.73µg/mL, and 14.89±1.49 µg/mL, respectively. In conclusion, solid dispersion of telmisartan-HPMC E5 LV enhanced the solubility of TMS.

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Section: Solubility Testmentioning

confidence: 99%

Preparation and Characterization of Solid Dispersion Telmisartan – Hydroxypropyl Methyl Cellulose(HPMC) E5 LV by Co-Grinding Method

Zaini¹,

Fitriani²,

Effendy³

et al. 2017

Orient. J. Chem

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show abstract

“…There are diverse methods to prepare drug‐loaded solid dispersions using polymers and other excipients meeting the requirements of the pharmaceutical industry . One of these methods is the melt extrusion, a solvent‐free continuous tool for dispersing API in a polymeric matrix, thereby improving its dissolution .…”

Section: Introductionmentioning

confidence: 99%

Plasticized Drug‐Loaded Melt Electrospun Polymer Mats: Characterization, Thermal Degradation, and Release Kinetics

Balogh

Drávavölgyi

Faragó

et al. 2014

Journal of Pharmaceutical Sciences

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“…2c-e). Thus, the semicrystalline drug was embedded in the hydrophilic carrier and its solid state properties changed to amorphous one [10]. Previous studies have reported that disappearance of the characteristic endothermic peaks of the valsartan dispersed in Gelucire 50/13 is due to melting of the drug in the matrix [13].…”

Section: Resultsmentioning

confidence: 99%

“…Solid dispersion can be defined as dispersion of active pharmaceutical ingredients in inert carriers or matrix in solid state. It can be prepared by solvent, melting and co-grinding method [10][11][12].…”

Section: Introductionmentioning

confidence: 99%

Improvement of Dissolution Rate of Valsartan by Solid Dispersion System Using D(−) Mannitol

Zaini

Umar

Nurhidayah

2017

Asian J Pharm Clin Res

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Objective: To improve dissolution rate of valsartan from solid dispersion system of valsartan and D(−) mannitol using co-grinding approach. Methods:Valsartan solid dispersion with different ratio of D(−) mannitol (1:1; 1:3 and 1: 5) were prepared by co-grinding method. Solid state characterization of the solid dispersion system was evaluated in term of crystallographic properties (powder X-ray diffraction), thermal behavior (differential scanning calorimetry [DSC]) and morphology (scanning electron microscope). The profile of dissolution rate was examined using USP dissolution apparatus type I at a temperature of 37±0.5°C. Results:Based on thermal analysis DSC and powder X-ray diffraction analysis, valsartan was transformed from semicrystalline phase to amorphous state as indicated by the disappearance of its melting endothermic peaks and the characteristic diffraction peaks. The in vitro dissolution rate study revealed that all solid dispersion system showed significant increase in dissolution rate compared with the intact valsartan. Conclusion:Solid dispersion of valsartan with D(−) mannitol prepared by co-grinding technique has successfully improved the dissolution rate compared with intact valsartan.

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Solid Dispersions Prepared by Continuous Cogrinding in an Air Jet Mill

Cited by 15 publications

References 47 publications

Preparation and Characterization of Solid Dispersion Telmisartan – Hydroxypropyl Methyl Cellulose(HPMC) E5 LV by Co-Grinding Method

Preparation and Characterization of Solid Dispersion Telmisartan – Hydroxypropyl Methyl Cellulose(HPMC) E5 LV by Co-Grinding Method

Plasticized Drug‐Loaded Melt Electrospun Polymer Mats: Characterization, Thermal Degradation, and Release Kinetics

Improvement of Dissolution Rate of Valsartan by Solid Dispersion System Using D(−) Mannitol

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