scholarly journals ENHANCEMENT OF GLIBENCLAMIDE DISSOLUTION RATE BY SOLID DISPERSION METHOD USING HPMC AND PVP

2019 ◽  
pp. 19-24 ◽  
Author(s):  
ARIF BUDIMAN ◽  
IYAN SOPYAN ◽  
DENIA SEPTY RIYANDI
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Hydroxypropyl Methylcellulose ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Rate Test ◽  
Ft Ir

Objective: The aim of this study was to investigate the effects of changing in the proportions of the solid dispersion formula on the dissolution rate of glibenclamide. Methods: Solid dispersions were prepared by solvent evaporation method by using methanol as solvent, hydroxypropyl methylcellulose (HPMC) and polyvinyl pyrrolidone (PVP) as polymers. The prepared product was evaluated by the saturated solubility test and the dissolution rate test. The prepared product was characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) and Scanning Electron Microscopy (SEM). Results: The result showed solid dispersion with a ratio of glibenclamide: PVP: HPMC (1: 3: 6) has the highest increase in solubility (20 fold) compared to pure glibenclamide. This formula also showed an improvement in dissolution rate from 19.9±1.19% (pure glibenclamide) to 99±1.60% in 60 min. Characterization of FT-IR showed that no chemical reaction occurred in solid dispersion of glibenclamide. The results of X-ray diffraction analysis showed an amorphous form in all solid dispersion formulas. The results of DSC analysis showed that endothermic peak melting point of solid dispersion occurred, and the morphology of solid dispersion was more irregular than pure glibenclamide based on SEM characterization Conclusion: The solid dispersion of glibenclamide using PVP: HPMC as carriers can increase the solubility and dissolution rate compared to pure glibenclamide.

Studies on the Preparation, Characterization and Solubility of -Cyclodextrin-Roxythromycin Inclusion Complexes

2009 ◽  
Vol 2 (2) ◽  
pp. 523-530
Author(s):  
D. Nagasamy Venkatesh ◽  
S. Karthick ◽  
M. Umesh ◽  
G. Vivek ◽  
R.M. Valliappan ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Inclusion Complexes ◽  
Phase Solubility ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Ir Studies ◽  
Poorly Soluble ◽  
Poorly Soluble Drug

Roxythromycin/ β-cyclodextrin (Roxy/ β-CD) dispersions were prepared with a view to study the influence of β-CD on the solubility and dissolution rate of this poorly soluble drug. Phase-solubility profile indicated that the solubility of roxythromycin was significantly increased in the presence of β-cyclodextrin and was classified as AL-type, indicating the 1:1 stoichiometric inclusion complexes. Physical characterization of the prepared systems was carried out by differential scanning calorimetry (DSC), X-ray diffraction studies (XRD) and IR studies. Solid state characterization of the drug β-CD binary system using XRD, FTIR and DSC revealed distinct loss of drug crystallinity in the formulation, ostensibly accounting for enhancement of dissolution rate.

scholarly journals Preparation and evaluation of azithromycin binary solid dispersions using various polyethylene glycols for the improvement of the drug solubility and dissolution rate

2016 ◽  
Vol 52 (1) ◽  
pp. 1-13 ◽  
Author(s):  
Ehsan Adeli
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Polyethylene Glycols ◽  
X Ray Diffraction ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Peg 4000 ◽  
Poorly Soluble

ABSTRACT Azithromycin is a water-insoluble drug, with a very low bioavailability. In order to increase the solubility and dissolution rate, and consequently increase the bioavailability of poorly-soluble drugs (such as azithromycin), various techniques can be applied. One of such techniques is "solid dispersion". This technique is frequently used to improve the dissolution rate of poorly water-soluble compounds. Owing to its low solubility and dissolution rate, azithromycin does not have a suitable bioavailability. Therefore, the main purpose of this investigation was to increase the solubility and dissolution rate of azithromycin by preparing its solid dispersion, using different Polyethylene glycols (PEG). Preparations of solid dispersions and physical mixtures of azithromycin were made using PEG 4000, 6000, 8000, 12000 and 20000 in various ratios, based on the solvent evaporation method. From the studied drug release profile, it was discovered that the dissolution rate of the physical mixture, as the well as the solid dispersions, were higher than those of the drug alone. There was no chemical incompatibility between the drug and polymer from the observed Infrared (IR) spectra. Drug-polymer interactions were also investigated using Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD) and Scanning Election Microscopy (SEM). In conclusion, the dissolution rate and solubility of azithromycin were found to improve significantly, using hydrophilic carriers, especially PEG 6000.

Manufacture of Ternary Solid Dispersions Composed of Nifedipine, Eudragit® E and Adsorbent

2011 ◽  
Vol 317-319 ◽  
pp. 185-188 ◽  
Author(s):  
Pornsak Sriamornsak ◽  
Srisuda Kontong ◽  
Yotsanan Weerapol ◽  
Jurairat Nunthanid ◽  
Srisagul Sungthongjeen ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersions ◽  
Ternary Systems ◽  
Dissolution Enhancement ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Ternary Solid Dispersions ◽  
Diffraction Patterns ◽  
Physical Mixtures

The aim of this study was to manufacture the ternary solid dispersions composed of nifedipine, Eudragit® E and adsorbent. Dissolution enhancement of nifedipine was also investigated. The inert solid carriers were added in the mixtures of nifedipine and Eudragit® E at varying ratios. The physicochemical properties of ternary systems, compared to physical mixtures, were analyzed using powder x-ray diffraction (PXRD) and differential scanning calorimetry (DSC). The dissolution of nifedipine from ternary systems was compared to the drug alone. The influence of drug:polymer: adsorbent ratio and type of adsorbent on the dissolution rate of the drug was also evaluated. The PXRD and DSC results of the systems with high amount of polymer showed that the drug was present in an amorphous form. On the other hand, the diffraction patterns and DSC thermograms of the physical mixtures revealed that to some extent the drug was present in a crystalline form. The results from this study demonstrated that an improvement in dissolution rate of nifedipine with Eudragit® E and adsorbents was obtained.

scholarly journals IMPROVEMENT OF DISSOLUTION RATE OF VALSARTAN BY SOLID DISPERSION SYSTEM USING D(−) MANNITOL

2017 ◽  
Vol 10 (3) ◽  
pp. 288 ◽  
Author(s):  
Erizal Zaini ◽  
Salman Umar ◽  
Nurhidayah Nurhidayah
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
In Vitro Dissolution ◽  
Type I ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Dispersion System ◽  
Grinding Technique

ABSTRACTObjective: 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 statecharacterization 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 USPdissolution 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 amorphousstate as indicated by the disappearance of its melting endothermic peaks and the characteristic diffraction peaks. The in vitro dissolution rate studyrevealed 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 ratecompared with intact valsartan.Keywords: Valsartan, D(−) mannitol, Solid dispersion, Co-grinding, Dissolution rate.

Enhancement of Dissolution Rate of Daidzein in Ternary Solid Dispersions

2012 ◽  
Vol 550-553 ◽  
pp. 1000-1004 ◽  
Author(s):  
Hui Wang ◽  
Hong Xin Xu ◽  
Na Zhang ◽  
Lian Dong Hu
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
X Ray Diffraction ◽  
Positive Role ◽  
X Ray ◽  
Dissolution Tests ◽  
Ternary Solid Dispersions ◽  
Pvp K30

The purpose of this study was to enhance the dissolution rate of daidzein (DZ) by solid dispersions. DZ solid dispersion was prepared by solvent method, with PVP K30 and surfactant as carriers. The influences of drug-carrier proportion, the kind of surfactant and the amount of surfactant on the dissolution of DZ were examined. Solid dispersions were characterized by infrared spectroscopy (IR), X-ray diffraction spectroscopy, and dissolution tests. When appropriate amount of poloxamer was added into the solid dispersion, the dissolution of DZ could be improved obviously. The data of IR showed that the absence of well-defined drug-polymer interactions. The data of X-ray diffraction showed that the drug might exist in the form of amorphism or molecule in solid dispersions. Both the binary and ternary solid dispersions enhanced the dissolution of DZ. Moreover, poloxamer played an important positive role in improving the dissolution rate of DZ in the solid dispersion.

scholarly journals Preparation and Characterization of a Novel Cocrystal of Atorvastatin Calcium with Succinic Acid Coformer

2019 ◽  
Vol 19 (3) ◽  
pp. 660
Author(s):  
Yudi Wicaksono ◽  
Dwi Setyawan ◽  
Siswandono Siswandono ◽  
Tri Agus Siswoyo
Keyword(s):  
Succinic Acid ◽  
Dissolution Rate ◽  
Intermolecular Hydrogen Bond ◽  
Acid Amide ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Atorvastatin Calcium ◽  
Hydrogen Bond Interactions

Preparation and characterization of a novel cocrystal of atorvastatin calcium with succinic acid coformer were successfully performed. This research aims to modify the crystalline form of atorvastatin calcium through cocrystallization with succinic acid coformer. The cocrystal was prepared by a solvent evaporation method and characterized by Powder X-Ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR) and Scanning Electron Microscopy (SEM). The atorvastatin calcium-succinic acid cocrystal has new crystalline peaks at 2θ of 12.9, 18.2 and 26.7° indicating the formation of a new crystalline phase. The cocrystal showed the melting point at 205.7 °C with an enthalpy of fusion 30.2 J/g which is different from the initial components. The FTIR spectra of cocrystal showed the shifting of absorption peaks of groups of initial components indicating of formation of atorvastatin calcium-succinic acid cocrystal through acid–amide intermolecular hydrogen bond interactions. The solubility and dissolution test showed that the cocrystal has solubility and dissolution rate significantly higher than the solubility and dissolution rate of pure atorvastatin calcium.

scholarly journals Enhancement of solubility and dissolution rate of ebastine fast-disintegrating tablets by solid dispersion method

2020 ◽  
Vol 19 (9) ◽  
pp. 1797-1805
Author(s):  
Nayyer Islam ◽  
Muhammad Irfan ◽  
Nasir Abbas ◽  
Haroon Khalid Syed ◽  
Muhammad Shahid Iqbal ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Kneading Method ◽  
The Impact ◽  
Fast Disintegrating Tablets

Purpose: To investigate the efficiency of different solubilizing agents in improving solubility as well as dissolution rate of ebastine (a BCS class II drug) by incorporating prepared solid dispersion into fast disintegrating tablets.Method: The solubility of ebastine was determined in distilled water, lipids and solubilizing agents. Subsequently, the binary solid dispersions were prepared by kneading method using varying weight ratios of ebastine and solubilizing agents. The solid dispersions were then incorporated into fast disintegrating tablets (SD-FDT). Central composite rotatable design (CCD) was used to determine the impact of super disintegrating agents on disintegration time and friability of tablets. The solubility and dissolution rate of developed SD-FDT were compared with a marketed brand. The solid dispersion particles were characterized by Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), powder x-ray diffraction (P-XRD) and scanning electron microscopy (SEM).Results: The saturated solubility of pure ebastine in water was 0.002 ± 0.041 mg/ml while the aqueous solubility of EBT/poloxamer solid dispersion SET3 (P) was 0.018 ± 2.510 mg/ml; on the other hand, EBT/soluplus solid dispersion SET1(S) has an aqueous solubility of 0.242 ± 1.390 mg/ml. Within 30 min, drug release was 14.00 ± 1.77, 78.00 ± 2.31 and 98.70 ± 2.54 % from pure EBT, SET3 (P) and SET1(S), respectively.Conclusion: The solubility and dissolution rate of ebastine has been successfully enhanced by incorporating its solid dispersion in fast-disintegrating tablets (SD-FDT). Keywords: Ebastine, Solid dispersion, Poloxamer 188, Soluplus, Solubility, Dissolution

DEVELOPMENT OF SOLID DISPERSION TABLET OF CARVEDILOL TO IMPROVE SOLUBILITY

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 54-59
Author(s):  
S. S Shelake ◽  
◽  
R. G Gaikwad ◽  
S Patil ◽  
F. I. Mevekari ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Media ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Water Soluble Drugs ◽  
Ft Ir

Crystalline state compounds are typically dissolution rate limited and dissolution rate is directly proportional to the solubility for BCS class II or class IV compounds. Solid dispersions are one of the most promising strategies to improve the oral bioavailability poorly water soluble drugs. The purpose of this study was to increase solubility of carvedilol by solid dispersion (SDs) technique with Poloxamer (PXM) 407 in aqueous media. The carvedilol- PXM 407 solid dispersion was prepared by solvent evaporation, kneading and melting method. It was characterized by differential scanning calorimetry (DSC), X-ray powder diffraction (XRD), Fourier transformation infra-red spectroscopy (FT-IR), scanning electron microscopy (SEM) and in vitro dissolution studies. The prepared solid dispersion were found to have higher dissolution rates as compared to intact carvedilol. During formulation of solid dispersion crystalline to amorphous transition has been observed.

scholarly journals Study on the Miscibility of Polypyrrole and Polyaniline Polymer Blends

2018 ◽  
Vol 2018 ◽  
pp. 1-5 ◽  
Author(s):  
Tekalign A. Tikish ◽  
Ashok Kumar ◽  
Jung Yong Kim
Keyword(s):  
Differential Scanning Calorimetry ◽  
Polymer Blends ◽  
Processing Method ◽  
Phase Behaviour ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Amorphous Nature ◽  
Ft Ir

We report on the miscibility and phase behaviour of polypyrrole-polyaniline (PPy/PANI) as a function of blend composition. The PPy/PANI blends were prepared by solution processing method, using dimethyl sulfoxide (DMSO) solvent. Characterization of the polymer blends was carried out based on the data analysis from Fourier transform infrared spectroscopy (FT-IR), X-ray diffraction (XRD), and differential scanning calorimetry (DSC). The PPy/PANI system was successfully formed blends in DMSO solvent. The polymer blends showed almost amorphous nature in XRD spectra because of intermolecular interaction between PPy and PANI macromolecules, which was confirmed by FT-IR data. Specifically, the DSC result for the PPY : PANI = 50 : 50 wt.% blend showed only one glass transition temperature (Tg), which indicates that the two polymers are well miscible without undergoing any phase separation.

scholarly journals Preparation and Characterization of Cetyl Trimethylammonium Intercalated Sericite

2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Hao Ding ◽  
Yuebo Wang ◽  
Yu Liang ◽  
Faxiang Qin
Keyword(s):  
Ion Exchange ◽  
Interlayer Space ◽  
Xrd Analysis ◽  
Acid Activation ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Ft Ir ◽  
Ft Ir Spectroscopy

Intercalated sericite was prepared by intercalation of cetyl trimethylammonium bromide (CTAB) into activated sericite through ion exchange with the following two steps: the activation of sericite by thermal modification, acid activation and sodium modification; the ion exchange intercalation of CTA+into activated sericite. Effects of reaction time, reaction temperature, CTAB quantity, kinds of medium, and aqueous pH on the intercalation of activated sericite were examined by X-ray diffraction (XRD) analysis, Fourier transform infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC), and thermogravimetric analysis (TGA). The results indicated that the CTA+entered sericite interlayers and anchored in the aluminosilicate interlayers through strong electrostatic attraction. The arrangement of CTA+in sericite interlayers was that alkyl chain of CTA+mainly tilted at an angle about 60° (paraffin-type bilayer) and 38° (paraffin-type monolayer) with aluminosilicate layers. The largest interlayer space was enlarged from 0.9 nm to 5.2 nm. The intercalated sericite could be used as an excellent layer silicate to prepare clay-polymer nanocomposites.

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