scholarly journals Comparison of Different Solubility Enhancement Techniques for Clopidogrel

2021 ◽  
Vol 69 (1) ◽  
Author(s):  
Degala. Vishwanayani ◽  
Dr. P.Tripura Sundari
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Solubility Enhancement ◽  
Solvent Evaporation ◽  
Cyclodextrin Complexes ◽  
Drug Content ◽  
Beta Cyclodextrin ◽  
Peg 4000 ◽  
Release Studies

The present study is aimed to formulate and evaluate various formulations to enhance the solubility of poorly aqueous soluble drug Clopidogrel. For this we have selected different techniques like solid dispersion, Nanosuspension and cyclodextrin complexes. As a part of it we prepared solid dispersions of drug employing PVPk30 and PEG 4000. Beta cyclodextrin complexes are prepared by kneading and solvent evaporation methods. Whereas nanosuspension are prepared by employing polaxomer as polymer. The prepared formulations were evaluated for drug Content and drug release studies.

scholarly journals Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

2021 ◽  
Vol 9 (2) ◽  
pp. 127-135
Author(s):  
Anil Raosaheb Pawar ◽  
Pralhad Vitthalrao Mundhe ◽  
Vinayak Kashinath Deshmukh ◽  
Ramdas Bhanudas Pandhare ◽  
Tanaji Dilip Nandgude
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Peg 4000

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

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 Solid dispersion of meloxicam: Factorially designed dosage form for geriatric population

2008 ◽  
Vol 58 (1) ◽  
pp. 99-110 ◽  
Author(s):  
Deepa Pathak ◽  
Sunita Dahiya ◽  
Kamla Pathak
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Dosage Form ◽  
Solid Dispersions ◽  
Methyl Cellulose ◽  
Water Soluble ◽  
Hydroxyethyl Cellulose ◽  
Scanning Calorimetry ◽  
Geriatric Population ◽  
Peg 4000

Solid dispersion of meloxicam: Factorially designed dosage form for geriatric populationThe objective of the present work was to improve the dissolution properties of the poorly water-soluble drug meloxicam by preparing solid dispersions with hydroxyethyl cellulose (HEC), mannitol and polyethylene glycol (PEG) 4000 and to develop a dosage form for geriatric population. Differential scanning calorimetry, X-ray diffractometry, Fourier transform infrared spectroscopy and scanning electron microscopy were used to investigate the solid-state physical structure of the prepared solid dispersions. Higher invitrodissolution of solid dispersions was recorded compared to their corresponding physical mixtures and the pure drug. PEG 4000 in 1: 9 drug to carrier ratio exhibited the highest drug release (100.2%), followed by mannitol (98.2%) and HEC (89.5%) in the same ratio. Meloxicam-PEG 4000 solid dispersion was formulated into suspension and optimization was carried out by 23factorial design. Formulations containing higher levels of methyl cellulose and higher levels of either sodium citrate or Tween 80 exhibited the highest drug release.

scholarly journals Solubility Enhancement of Diclofenac Using Solid Dispersions

2021 ◽  
Vol 5 (1) ◽  
pp. 1-6
Author(s):  
Mohd. Aamir Mirza ◽  
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Diclofenac Sodium ◽  
Active Pharmaceutical Ingredient ◽  
Solubility Enhancement ◽  
Solvent Evaporation ◽  
Limiting Factor ◽  
Formulation Development ◽  
Enhanced Solubility ◽  
Evaporation Technique

Background: The phenomenon which gives rise to a homogenous system, formed by the dissolution of solute in a solvent is known as solubility. Low solubility is the limiting factor in formulation development. Diclofenac being BCS class II drug have low aqueous solubility of 0.00401mg/ml. Amongst various solubility enhancement techniques, solid dispersion is the easiest one. Objective: Present work is primarily focused on the development of solid dispersions of diclofenac through solvent evaporation technique utilizing Eudragit E100 as a carrier. Methods: Solid dispersion consists of at least one active pharmaceutical ingredient as a carrier in solid state. Various methods for preparing solid dispersions includes melt extrusion, fusion lyophilization, spray drying, solvent evaporation, and super critical fluid (SCF) technology. Solvent evaporation technique is used among various solid dispersion methods. Conclusion: The enhanced solubility found to be 0.485mg/ml. The dissolution was performed using USP Type II apparatus was %CDR of pure drug and its solid dispersion in 8 hr were found out to be 45.14926% and 98.04758% respectively. Henceforth, solid dispersion technique results marked solubility enhancement of diclofenac sodium.

scholarly journals FORMULATION OF SOLID DISPERSIONS FOR ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF SIMVASTATIN

2021 ◽  
pp. 94-100
Author(s):  
PAYAL D. BORAWAKE ◽  
KAUSLYA ARUMUGAM ◽  
JITENDRA V. SHINDE
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Fourier Transforms ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Drug Content ◽  
Pvp K30

Objective: The objective of the present work was to formulate the solid dispersions of simvastatin for enhancement of its aqueous solubility and dissolution rate. Methods: In the present study, solid dispersions of simvastatin were prepared by Kneading and Solvent evaporation methods. The polymeric carriers like Polyethylene glycol (PEG) 6000 and Polyvinyl Pyrrolidone (PVP) K30 were used in different ratios (ratio of drug: carrier was 1:1, 1:2) to formulate solid dispersions. The prepared solid dispersions were characterized by differential scanning calorimetry (DSC), Fourier transforms infrared spectroscopy (FTIR), and evaluated for drug content, percentage yield, saturation solubility, in vitro dissolution studies. The best formula of the solid dispersion was selected according to the solubility and dissolution data. Results: The F7 formulation was found to be an optimized formulation containing PVP K30 in the ratio 1:1 prepared by solvent evaporation technique. The Drug content was found to be higher i.e. 94.89 in the F7 batch. The FT-IR spectra revealed that there was no interaction between drugs and carriers. DSC thermogram indicated entrapment of simvastatin in PVP K30 and the conversion of crystalline simvastatin into an amorphous form. The F7 formulation showed maximum drug release i.e. 98.60% in 60 min which is 2 times greater than pure drug making it an optimized formulation. Conclusion: The solubility of simvastatin was successfully enhanced through the solid dispersion technique. Solid dispersions prepared with solvent evaporation method were more soluble than solid dispersions prepared with kneading method with carrier PVP K30.

scholarly journals FORMULATION AND INVITRO EVALUATION OF SOLID DISPERSION TABLETS OF SILYMARIN

2021 ◽  
Vol 9 (12) ◽  
pp. 363-369
Author(s):  
Ayesha Naz ◽  
◽  
Syeda Kulsum ◽  
Mehraj Begum ◽  
Mohammed Omer ◽  
...  
Keyword(s):  
Quality Control ◽  
Drug Release ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Angle Of Repose ◽  
Control Parameters ◽  
Solvent Evaporation Method ◽  
Peg 4000 ◽  
Quality Control Parameters ◽  
Tapped Density

Objective: The research aims to formulate and evaluate Solid Dispersion tablets of Silymarin. Methods: Solid dispersions of Silymarin were prepared with various concentrations of carriers by using solvent evaporation method. The prepared solid dispersions were compressed into tablets by using 8 mm punch rotary tablet punching machine, with the hardness of 3.5kg /cm2.The formulated tablets were evaluated for various quality control parameters. Results: Silymarin was mixed with various proportions of excipients which showed no drug-excipients interactions. The precompression blend of Silymarin solid dispersions were characterized with respect to angle of repose, bulk density, tapped density, Carrs index and Hausners ratio. The precompression blend of all the batches indicated good to fair flowability and compressibility. Conclusion: The tablet passed all the tests. Among all the formulations F4 formulation containing, Drug and PEG 4000 in the ratio of 1:4 showed good result that is 94.95 % in 60 minutes. As the concentration of polymer increased the drug release was increased. While the formulations containing PEG 6000 showed less release. Hence from the dissolution data it was evident that F4 formulation is the better formulation.

scholarly journals Sustained release formulation of metformin-solid dispersion based on gelucire 50/13- PEG4000: an in vitro study

2017 ◽  
Vol 9 (3) ◽  
pp. 52
Author(s):  
Mumini A Momoh ◽  
Calister E Ugwu ◽  
Tenderwealth Clement Jackson ◽  
Ngumezi C Udodiri
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Encapsulation Efficiency ◽  
Solid Dispersions ◽  
In Vitro Study ◽  
Release Rates ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Peg 4000

<p>Metformin is a hydrophilic hypoglycemic agent with permeability and short half-life problems which leads to its low bioavailability. Solid dispersion is one of the unique approaches, to improve bioavailability profiles of drugs. The aim of this study was to prepare and evaluate solid dispersions (SDs) of metformin with polyethylene glycol 4000 (PEG 4000) and Gelucire®50/13 in order to increase its permeability and bioavailability. Solid dispersions of Metformin containing various ratios of PEG 4000: Gelucire®50/13 (1:1, 1:2, 2:1, 1:4, 4:1 as Batch A, Batch B, Batch C, Batch D and Batch E) were prepared using solvent evaporation and fusion techniques. The physical mixtures which served as controls were also prepared. The SDs were evaluated using encapsulation efficiency, percentage yield. The formulations were also characterized with FTIR and DSC. The in vitro drug release studies were also evaluated. The results obtained showed that solid dispersion formulations at pH, 1.2 and 7.4 demonstrated higher release rates than the pure drug. The SDs showed high drug release rates and encapsulation efficiency (% EE) although Batch C containing PEG 4000 and Gelucire 50/13 in the ratio of 2:1 appeared as the batch with most % EE, drug release with broad melting peak. The release rate of metformin increased with increasing amount of PEG 4000. Batch C, SDs containing PEG 4000 and Gelucire 50/13 in the ratio of 2:1 were found to be the most optimized batch with enhanced encapsulation efficiency, most drug release and therefore, improved permeability and bioavailability of metformin.</p>

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 STUDIES ON SOLID DISPERSIONS OF LEFLUNOMIDE

2020 ◽  
pp. 187-190
Author(s):  
MAHAPARALE PR ◽  
THORAT VP
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
Poloxamer 188 ◽  
Evaporation Method ◽  
Enhanced Solubility

Objective: Leflunomide is Non steroidal Anti-Inflammatory drug, which is poorly water soluble. In present study attempt has been made to prepare and characterize solid dispersions of leflunomide to increase solubility of drug.Method:  In Preparation of solid dispersion of leflunomide different polymer like PEG 4000, PEG 6000, Poloxamer 188 and Poloxamer 407 were used.  Effects of several variables such as type of carrier used, drug: carrier ratios, method of preparation were studied. The evaluation of solid dispersions was done by solubility study, dissolution study and X-ray diffractometry. Result: Improvement in dissolution of drug was observed in all solid dispersions as compared to pure drug alone. Solid dispersions prepared using Poloxamer 188 showed fastest in vitro drug release. Solid dispersions prepared using solvent evaporation method showed relatively faster drug release than melt evaporation method. XRD patterns indicated reduced crystallinity of drug particles, which suggests mechanism of enhanced solubility and dissolution of drug in solid dispersion systems.Conclusion:  A significant result obtained with the study indicated that solid dispersion by solvent evaporation can successfully be further explored and employed to improve solubility and dissolution characteristics of poorly soluble drugs.Keywords: Leflunomide, Solid dispersion, Carrier

scholarly journals FORMULATION DEVELOPMENT AND CHARACTERISATION OF MECLIZINE HYDROCHLORIDE FAST DISSOLVING TABLETS USING SOLID DISPERSION TECHNIQUE

2018 ◽  
Vol 10 (4) ◽  
pp. 141 ◽  
Author(s):  
Prashant Bhide ◽  
Reeshwa Nachinolkar
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Phosphate Buffer ◽  
Solid Dispersions ◽  
In Vitro Dissolution ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Pure Drug

Objective: The aim of the present investigation was to design and evaluate fast dissolving tablet (FDT) for the oral delivery containing solid dispersion of meclizine (MCZ) hydrochloride, an antiemetic drug.Methods: The solubility of meclizine was increased by preparing solid dispersions using mannitol as a carrier by fusion method. The prepared solid dispersion, was subjected for in vitro drug release, percent practical yield, drug content, infrared spectroscopy (IR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM). Optimized solid dispersion was incorporated to prepare fast dissolving tablets. Preformulation studies were carried out on tablet blends. The prepared solid dispersion, as well as pure drug fast dissolving tablets, was evaluated for drug content, weight variation, hardness, friability, in vitro drug release, wetting time, disintegration time, water absorption ratio, in vitro dispersion time.Results: Meclizine pure drug, solid dispersions formulations SD1, SD3 and SD5 showed 12.8, 31.68, 38.92 and 53.28% cumulative drug release in phosphate buffer pH 6.8 after 60 min, respectively. Thus faster dissolution rate was exhibited by the solid dispersion containing 1:5 (w/w) ratio of meclizine: mannitol. Percent cumulative drug release for control and solid dispersion tablets after 60 min in phosphate buffer pH 6.8 was 92.04 and 98.2% respectively. The release of drug meclizine from best formulation SD5 FDT was found to be faster than pure drug FDT.Conclusion: Fast dissolving tablet of optimized solid dispersion showed better in vitro dissolution result then FDT of pure drug at the end of one hour.

Sign in / Sign up

Export Citation Format

Share Document