scholarly journals Formulation and In-vitro Evaluation of Itraconazole Floating Microparticles

2020 ◽  
Vol 29 (1) ◽  
pp. 236-246
Author(s):  
Taha A. Basher ◽  
Entidhar J. Muhammad
Keyword(s):  
Fourier Transforms ◽  
Fungal Infections ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
Safflower Oil ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Water Solvent ◽  
Ph Dependent

Itraconazole (ITZ) is an antifungal drug (BCSII) used for the treatment of local and systemic fungal infections. Furthermore, ITZ used as an antifungal prophylaxis for immunocompromised patients. The objective of the study is to overcome the two problems of low and pH dependent solubility of ITZ by its preparation as floating microparticles. Firstly, pH-dependent floating microparticles were prepared using oil in water solvent evaporation method, from which the best one (F7) selected as a best pH-dependent formula with composition of   ITZ (200mg),EC (800mg), HPMC 15cps (200mg) and safflower oil (2ml) .Then, F7 was compared with the selected Relatively pH-independent ITZ floating microparticles formula  with composition of  ITZ(200mg), a first coat of HPMC15cps (200mg), a second coat of EC (800mg), HPMC 15cps (200mg) and safflower oil (2ml) which prepared by a dual coating solvent evaporation method using a first coat which provides relatively pH-independent solubility, while the second coat applied as a bouncy producing agents. Polyvinyl alcohol (PVA) was used as a surfactant in both cases. The prepared floating microparticles were subjected to various evaluation parameters such as yield percent, drug loading and drug entrapment efficiency (EE), particle size analysis, in- vitro bouncy, drug release, Fourier Transforms Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC) and X-ray Diffractometry (XRD) studies.

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 Design and Development of Sustained Release Microspheres of Ibuprofen by Emulsification Solvent Evaporation Method Using Polymeric Blend

2013 ◽  
Vol 16 (1) ◽  
pp. 39-44 ◽  
Author(s):  
Nandini Saha ◽  
Ikramul Hasan ◽  
Mehrina Nazmi ◽  
Md Selim Reza
Keyword(s):  
Drug Release ◽  
Fourier Transforms ◽  
In Vitro Release ◽  
Pharmaceutical Journal ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Dissolution Apparatus ◽  
Emulsification Solvent Evaporation

Ibuprofen, a non-steroidal anti-inflammatory drug was formulated as microspheres by using Methocel K4M & Eudragit RSPO. These microspheres were prepared by emulsification solvent evaporation method to provide sustained action and to minimize local side effect of Ibuprofen by avoiding the drug release in the upper gastrointestinal tract. The prepared microspheres were subjected to various evaluation and in-vitro release studies. In-vitro drug release was studied in a paddle type dissolution apparatus (USP Type II Dissolution Apparatus) using Phosphate buffer (pH 7.4) as the dissolution medium at 37.5oC for 6 hours (paddle speed 50 RPM). The release mechanisms were explored and explained with Zero Order, First Order, Higuchi and Korsmeyer-Peppas equations. The correlation coefficients values of the trend lines of the graphs showed that the formulations best fit with Korsmeyer-Peppas release pattern. Microspheres’ morphology and chemical integrity were studied by a scanning electron microscope (SEM) and Fourier transforms infrared spectroscopy (FTIR) respectively. DOI: http://dx.doi.org/10.3329/bpj.v16i1.14489 Bangladesh Pharmaceutical Journal 16(1): 39-44, 2013

scholarly journals Development and In-Vitro Evaluation of Betahistine Hydrochloride microspheres by Emulsification Solvent Evaporation Method

1970 ◽  
Vol 7 (5) ◽  
pp. 30-36
Author(s):  
Sandeep A Wathore
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Tween 80 ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Ftir Studies ◽  
Emulsification Solvent Evaporation ◽  
Polymer Ratio

The formulation of floating microspheres of Betahistine hydrochloride by the o/w emulsification and solvent evaporation method in the presence of tween 80 as an emulsifying agent. The influence of formulation factor Drug: Polymer ratio on particle size, encapsulation efficiency and invitro release characteristics of the microspheres were investigated. The microspheres have been analyzed for their size, drug loading capacity and drug release study. Spherical and smooth surfaced microspheres with desired encapsulation efficiencies were obtained. Slow drug release from microspheres observed up to 12 h. for formulation F4, F5. Optimized formulation F4 was evaluated for FTIR, DSC, SEM. DSC and FTIR studies showed that the nature of pure drug Betahistine hydrochloride remains unaffected till the completion of process of microspheres formation. SEM photographs showed that the Floating microspheres were spherical in nature with smooth surface and uniform distribution of the drug within the microsphere. Keywords: 

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 FORMULATION AND EVALUATION OF FLOATING MICROSPHERES OF CIPROFLOXACIN BY SOLVENT EVAPORATION METHOD USING DIFFERENT POLYMERS

2021 ◽  
pp. 101-108
Author(s):  
KAUSLYA ARUMUGAM ◽  
PAYAL D. BORAWAKE ◽  
JITENDRA V. SHINDE
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Angle Of Repose ◽  
Solvent Evaporation Method ◽  
Evaporation Method

Objective: The main intention of this research was to formulate and evaluate floating microspheres of ciprofloxacin using different polymers to prolong gastric residence time. Methods: The microspheres were formulated by the solvent evaporation method using different ratios of polymers like carbopol 940, ethylcellulose, and Hydroxy Propyl Methyl Cellulose K4M. Further, the floating microspheres were evaluated for micromeritic properties like bulk density, tapped density, angle of repose, etc., percentage yield, particle size, entrapment efficiency, floating capacity, in vitro drug release study, release kinetics, drug content, swelling index, and Fourier Transform Infrared Spectroscopy (FTIR) (Compatibility studies). Results: The ciprofloxacin microspheres showed the good flowing property. The particle size ranged from 258.1±2.21 µm to 278±2.86 µm and entrapment efficiency ranged from 63.17±0.43% to 89.90±1.32%. The IR spectrum revealed that there was no interaction between the drug and polymer. F7 formulation was found to be the best formulation. Drug release was found to be 90.70±0.89% i.e. in a controlled manner at the end of 10 h. Conclusion: The floating microspheres were prepared successfully and the results clearly stated that prepared ciprofloxacin microspheres may be safe and effective controlled drug delivery over an extended period which can increase bioavailability, patient compliance, and decrease dosing frequency.

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 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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