Solid dispersion of dutasteride using the solvent evaporation method: Approaches to improve dissolution rate and oral bioavailability in rats

2018 ◽  
Vol 90 ◽  
pp. 387-396 ◽  
Author(s):  
Jin-Seok Choi ◽  
Sang-Eun Lee ◽  
Woo Suk Jang ◽  
Jong Chan Byeon ◽  
Jeong-Sook Park
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Evaporation Method

Formulation Design and Optimization of Repaglinide Solid Dispersions by Central Composite Design

2018 ◽  
Vol 11 (6) ◽  
pp. 4337-4348
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Srinivas I
Keyword(s):  
Central Composite Design ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Release Mechanism ◽  
Solvent Evaporation Method ◽  
Onset Of Action ◽  
Evaporation Method ◽  
Central Composite

Repaglinide is a pharmaceutical drug used for the treatment of type II diabetes mellitus, it is characterized with poor solubility which limits its absorption and dissolution rate and delays onset of action. In the present study, immediate release solid dispersion of repaglinide was formulated by solvent evaporation technique. Repaglinide solid dispersions were prepared using PEG 8000, Pluronic F 127 and Gelucire 44/14 by solvent evaporation method. A 3-factor, 3-level central composite design employed to study the effect of each independent variable on dependent variables. FTIR studies revealed that no drug excipient interaction takes place. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of repaglinide has been converted into an amorphous form from crystalline within the solid dispersion formulation. The correlation coefficient showed that the release profile followed Higuchi model anomalous behavior and hence release mechanism was indicative of diffusion. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of repaglinide.

scholarly journals Dissolution enhancement of poorly soluble drug by solvent evaporation method using hydrophilic polymer: a solid dispersion technique

2012 ◽  
Vol 1 (2) ◽  
Author(s):  
Md Armin Minhaz ◽  
Md Mofizur Rahman ◽  
Md Qamnul Ahsan ◽  
Abul Bashar Ripon Khalipha ◽  
Mohammed Raihan Chowdhury
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Dissolution Enhancement ◽  
Solvent Evaporation Method ◽  
Peg 6000 ◽  
Evaporation Method ◽  
Poorly Soluble ◽  
Pure Drug

In order to investigate the effect of polymers on release mechanism of poorly soluble drugs from solid dispersions, Clonazepam was used as a model drug for these purposes. Five types of solid dispersions were prepared using polyethylene glycol 6000 (PEG- 6000), Kollicoat IR, Kollidon VA 64 and Poloxomer in different drug-tocarrier ratios (1:2, 1:4, 1:6, 1:8, 1:10). The solvent evaporation method was used for preparation of solid dispersions. The in-vitro dissolution study with temperature of 37° C and a paddle method, 100 rpm was used in 1000 ml of distilled water as dissolution medium in each dissolution basket for the pure drug and solid dispersions. For pure Clonazepam showed very slow dissolution rate and the solid dispersion considerably enhanced the dissolution rate. Decreased crystalline and increased amorphous fraction of the drug was probably done by wettability and dispersibility. The highest improvement in wettability and dissolution rate of Clonazepam was observed in PEG-6000, Poloxomer and Kollidon VA 64 (1:10 ratio). Solid dispersions containing polymer (1:10 ratio) prepared by solvent method showed significant improvement in the release profile as compared to pure drug, Clonazepam. DOI: http://dx.doi.org/10.3329/ijpls.v1i2.12952 International Journal of Pharmaceutical and Life Sciences Vol.1(2) 2012

Preparation, characterization and bioavailability of oral puerarin nanoparticles by emulsion solvent evaporation method

RSC Advances ◽  
2016 ◽  
Vol 6 (74) ◽  
pp. 69889-69901 ◽  
Author(s):  
Yin Zhang ◽  
Yong Li ◽  
Xiuhua Zhao ◽  
Yuangang Zu ◽  
Weiguo Wang ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Oral Bioavailability ◽  
Freeze Drying ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Evaporation Method

In this paper, puerarin (PUE) was nanocrystallized by emulsion solvent evaporation (ESE) method, followed by freeze-drying. The solubility, dissolution rate and oral bioavailability of PUENs were significantly improved compared with raw PUE.

COMPLEX OF ELUXADOLINE WITH SODIUM CAPRYLATE FOR IMPROVED SOLUBILITY AND DISSOLUTION RATE

INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (11) ◽  
pp. 22-26
Author(s):  
Manisha Dhere ◽  
◽  
Arti Majumdar ◽  
Neelesh Malviya
Keyword(s):  
Dissolution Rate ◽  
Solvent Evaporation ◽  
Drug Dissolution ◽  
Dissolution Enhancement ◽  
Solvent Evaporation Method ◽  
Scanning Calorimetry ◽  
Evaporation Method ◽  
Solubility Study ◽  
Sodium Caprylate

In the present research, newly developed complex with sodium caprylate was investigated for solubility and dissolution enhancement of eluxadoline. Complexes were prepared in different ratios by solvent evaporation method and characterised solubility study, Infrared spectroscopy (IR), Diffrential scanning calorimetry (DSC), X-Ray Diffraction (XRD), drug content analysis and in vitro Drug release. The solubility and dissolution rate revealed most suitable ratio of eluxadoline and sodium caprylate (1:4). The IR, DSC and X-RD data also confirmed the results. It was concluded that complex prepared with (1:4 drug:sodium caprylate ratio) using solvent evaporation method showed significant improvement in solubility and drug dissolution.

scholarly journals Water Solubility Enhancement of Atorvastatin by Solid Dispersion Method

1970 ◽  
Vol 3 (2) ◽  
pp. 43-46
Author(s):  
Riaz Uddin ◽  
Farzana Ali ◽  
Subrata Kumar Biswas
Keyword(s):  
Key Words ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Solid Dispersions ◽  
Solubility Enhancement ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Dispersion Method ◽  
Evaporation Method

Key Words: Solid dispersions; solvent evaporation method; atorvastatin; HPMCDOI: http://dx.doi.org/10.3329/sjps.v3i2.8036 S.J. Pharm. Sci 3(2): 43-46

scholarly journals Improvement in vitro Dissolution Rate of Quercetin Using Cocrystallization of Quercetin-Malonic Acid

2018 ◽  
Vol 18 (3) ◽  
pp. 531 ◽  
Author(s):  
Dwi Setyawan ◽  
Sukma Adhi Permata ◽  
Ahmad Zainul ◽  
Maria Lucia Ardhani Dwi Lestari
Keyword(s):  
Dissolution Rate ◽  
Malonic Acid ◽  
Fourier Transforms ◽  
Solvent Evaporation ◽  
Physical Mixture ◽  
Original Position ◽  
In Vitro Dissolution ◽  
Solvent Evaporation Method ◽  
Evaporation Method

The aim of the study was to improve the in-vitro dissolution rate of quercetin (Qu) using cocrystallization of quercetin. Cocrystals of quercetin (Co Qu) were produced with malonic acid (Ma) as coformer at ratio 1:2 using solvent evaporation method. Cocrystals quercetin-malonic acid (Co Qu-Ma) was characterized using Differential Thermal Analysis (DTA), Powder X-Ray Diffraction (PXRD), Scanning Electron Microscope (SEM), and Fourier Transforms Infrared Spectrophotometer (FTIR) and in-vitro dissolution study. A new endothermic peak at 277.9 °C was shown from the thermogram. Diffractogram of Co Qu-Ma showed a new diffraction peak at 2θ 9.81, 12.99, and 19.80°. Microphotograph showed that Qu and Ma exhibited a columnar-shaped and a pebble-shaped crystal, respectively, and FTIR wavenumber of O-H functional group of quercetin was shifted from its original position at 3411 to 3428 cm-1 in the physical mixture (pm) of Qu-Ma and 3418 cm-1 in Co Qu-Ma, respectively. The physicochemical characterizations using DTA, PXRD, SEM and FTIR indicated that Co Qu-Ma were successfully obtained through solvent evaporation method. The in-vitro dissolution rate of Co Qu-Ma was 95.30% at 60 min. Cocrystals effectively increased dissolution rate and dissolution efficiency in comparison to the pure quercetin and physical mixture of quercetin-malonic acid.

scholarly journals Physicochemical Characterization and Dissolution Enhancement of Bilastine by Solid Dispersion

2021 ◽  
Vol 69 (1) ◽  
Author(s):  
Sanjesh G. Rathi ◽  
Dhruv B. Chaudhari
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Physicochemical Characterization ◽  
Solvent Evaporation ◽  
Dissolution Enhancement ◽  
Solvent Evaporation Method ◽  
In Vitro Drug Release ◽  
Evaporation Method ◽  
Pvp K30

The solid dispersions of Bilastine with HPMC, PVP K30 and HPC have been prepared in different weight ratios by using solvent evaporation method. DSC was used to characterize the samples of solid dispersions and pure drug. Drug found compatible with the excipients. The highest improvements in solubility and in-vitro drug release were observed in solid dispersion prepared with HPC (F14) by solvent evaporation method. The increased dissolution rate of drug from solid dispersion may be due to surface tension lowering effect of polymer to the medium and increased wettability and dispersibility of drug. Hence, F14 Solid dispersion with the HPC carrier considered as most satisfactory among all solid dispersions.

scholarly journals SOLID DISPERSION TECHNIQUE TO ENHANCE THE SOLUBILITY AND DISSOLUTION OF FEBUXOSTAT AN BCS CLASS II DRUG

2019 ◽  
Vol 11 (1) ◽  
pp. 241 ◽  
Author(s):  
D. Christopher Vimalson ◽  
S. Parimalakrishnan ◽  
N. S. Jeganathan ◽  
S. Anbazhagan
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Fusion Method ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Drug Content ◽  
Bcs Class Ii ◽  
Percentage Yield

Objective: The present study was aimed to enhance the solubility of poorly water-soluble drug (BCS Class II) Febuxostat using water-soluble polymers.Methods: Pre-formulation studies like drug excipient compatibility studies by Fourier-transform infrared spectroscopyDifferential scanning calorimetry and determination of saturation solubility of drug individually in various media like distilled water and pH 7.4 phosphate buffer. Solid dispersions of Febuxostat was prepared using Polyethylene glycol (PEG 6000) (fusion method) and Polyvinyl pyrrolidone (PVP K30) (solvent evaporation method) in various ratios like 1:1, 1:2, 1:3 and 1:4 separately. The formulated solid dispersions were evaluated for percentage yield, drug content and in vitro dissolution studies.Results: From the results of pre-formulation studies it was revealed that there was no interaction between drug and excipients and the pure drug was poorly soluble in water. The percentage yield of all formulations was in the range of 54-78 %, and drug content was in the range of 43-78 mg. The solid dispersion containing polyvinylpyrrolidone K 30 in 1:4 ratio showed the highest amount of drug release at the end of 30 min than other formulations.Conclusion: Finally it was concluded that solid dispersion prepared with PVP K-30 in 1:4 ratio by solvent evaporation method was more soluble than by fusion method.

scholarly journals ENHANCEMENT OF SOLUBILITY AND DISSOLUTION OF IBUPROFEN BY SOLID DISPERSION TECHNIQUE AND FORMULATION OF SUSTAINED RELEASE TABLETS CONTAINING THE OPTIMISED BATCH OF SOLID DISPERSION

2017 ◽  
pp. 37-44
Author(s):  
ABHIK KAR ◽  
ABDUL BAQUEE AHMED
Keyword(s):  
Sustained Release ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Poloxamer 407 ◽  
In Vitro Dissolution ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Sustained Release Tablets

Objective: The present study was aimed to enhance the solubility of poorly water soluble drug Ibuprofen using solid dispersion technique and to develop sustained release tablets containing solid dispersion granules of the optimized batch. Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic, and anti-inflammatory propertiesMethods: Solid dispersions of Ibuprofen were prepared by using PEG 20000 and Poloxamer 407 in different weight ratios by fusion and solvent evaporation method. Drug-carrier physical mixtures were also prepared. Solid dispersions were characterized by saturation solubility, drug content, in vitro dissolution, FTIR and DSC analysis. Solid dispersion formulation, SDF9 (PEG 20000 and Poloxamer 407, 1:3:3) prepared by solvent evaporation method was considered as the optimized batch. Sustained release tablets containing the solid dispersion granules of the optimized batch were prepared by direct compression method using HPMC K100M at three concentrations (10%, 14%, 18% w/w). The prepared formulations were evaluated for hardness, thickness, weight variation, friability, in vitro dissolution studies and release kinetics modelling.Results: Solid dispersion formulation, SDF9showed 95.09% drug release in 60 min and considered as the optimized batch. Tablet formulation, FT3 (HPMC K100M 18% w/w) showed 96% drug release for 12 h.Conclusion: Solid dispersions of ibuprofen using a combination of PEG 20000 and poloxamer 407 by solvent evaporation method may result in higher aqueous solubility of the drug. Also sustained release tablets containing solid dispersion granules of ibuprofen, using HPMC K100M may be a promising approach to extend the release rate of the drug from the solid dispersion for 12 h.

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