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 Enhancement of dissolution rate of Olmesartan medoxomil using urea as carrier by different solid dispersion techniques

2018 ◽  
Vol 1 (1) ◽  
pp. 36-42
Author(s):  
B Sangameswaran ◽  
M Gomathi
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Olmesartan Medoxomil ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Poor Solubility ◽  
Co Precipitation

The poor solubility of drug substances in water and their low dissolution rate in aqueous G.I.T fluid often leads to insufficient bioavailability. As per Biopharmaceutical Classification System (BCS), Olmesartan belongs to the class-II category having poor solubility and high permeability. Since only dissolved drug can pass the gastrointestinal membrane, the proper solubility of the drug is ultimately desired. Its oral bioavailability is 26%. Hence, an attempt was made to enhance its solubility by formulating solid dispersions using different techniques viz., Melting, Kneading, Co-precipitation, Solvent evaporation and Physical mixing etc., Drug and carrier (Urea) in different ratios like 1: 1, 1: 2, 1: 3 and 1:4 were used for formulating solid dispersions. The compatibility of the drug with the carrier was checked by FTIR studies, these results revealed that there was no interaction between them. The angle of repose, bulk density, tapped density; Carr’s index and Hausner ratio were calculated for the micrometric characterization of all the solid dispersions. The drug content was found to be high and uniform in all formulations. The prepared Solid dispersion SEM4 (1:4) showed minimal wetting time of 13 seconds compared with the other formulations. In vitro dissolution, release studies in Phosphate buffer pH of 6.8 revealed that the prepared solid dispersions showed faster drug release compared with the pure drug.  The in vitro dissolution profile showed ascendency on increasing the carrier concentration

scholarly journals Solubility enhancement of glimperide: Development of solid dispersion by solvent melt method, characterization and dosage form development

2018 ◽  
Author(s):  
Suchitra Kaushik ◽  
Kamla Pathak
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Dosage Form ◽  
Solid Dispersions ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Accelerated Stability ◽  
Form Development

The aim of the present work was to develop immediate release dosage form of the solid dispersion of glimperide (GLIM) for potential enhancement in the bioavailability. The solid dispersions of GLIM were prepared with PEG6000, PVP K30 and Poloxamer 188, in 1:1, 1:3 and 1:5 %w/w ratio by using solvent wetting and solvent melt method. The in vitro dissolution parameters (%DE10min, %DE30min, %DE60min, T50% and DP30) were used to select the optimized solid dispersion that was characterized by IR, PXRD, DSC and SEM. The optimized solid dispersion of GLIM (GSDSM3) was used as drug component for immediate release (IR) tablets that were evaluated for physical and pharmacopoeial parameters. The in vitro drug release studies identified G4 as the optimized tablet with a cumulative drug release (CDR) of 99.34% in 30 min in phosphate buffer, pH 7.4. The CDR was higher than the marketed tablet (91.15%, Amaryl®, Sanofiaventis), However, the f1 and f2 were 10.6 and 52 respectively, which confirmed similarity of the dissolution profile(s). Accelerated stability studies confirmed stability up to 6 months at 40°C/75% condition in the HDPE bottle pack.

scholarly journals FABRICATION AND EVALUATION OF SOLID DISPERSION CONTAINING GLIBENCLAMIDE

2018 ◽  
Vol 11 (8) ◽  
pp. 158
Author(s):  
Nikita Sehgal ◽  
Vishal Gupta N ◽  
Gowda Dv ◽  
Sivadasu P
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Amorphous State ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Stability Studies ◽  
Scanning Calorimetry ◽  
Dsc Studies

 Objective: The aim of the present study was to increase the dissolution rate of glibenclamide (GLIB) by molecular dispersion of drug in the polymeric matrix of Pluronic F-127.Methods: GLIB-loaded solid dispersions were formulated by fusion method. The formulated solid dispersions were characterized for scanning electron microscopy (SEM), X-ray diffractometry (XRD), differential scanning calorimetry (DSC), and evaluated for percentage yield, drug content, solubility, and in vitro dissolution profile, and stability studies were conducted as per International Conference on Harmonisation guidelines Q1A in stability chamber, both at intermediate and accelerated conditions.Results: Both XRD and DSC studies suggested that crystalline GLIB was converted to amorphous form after loading into carrier. SEM studies revealed that the prepared solid dispersions were in the form of irregular particles with the absence of crystalline material. Due to this conversion of crystalline to amorphous state, formulated solid dispersions had shown improved dissolution rate profile of GLIB and stability studies suggested that formulated solid dispersions showed no significant changes in appearance and also in drug content.Conclusion: Thus, from the obtained results, it can be concluded that dissolution profile of GLIB can be improved by formulating as solid dispersion.

Enhancement of Dissolution Rate of Quercetin Using Solid Dispersion Approach: In Vitro and In Vivo Evaluation

2020 ◽  
Vol 10 (3) ◽  
pp. 330-349
Author(s):  
Raghvendra Chaubey ◽  
Nimisha Srivastava ◽  
Apoorva Singh
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
Dissolution Profile ◽  
In Vivo Evaluation ◽  
Rat Paw Edema ◽  
Anti Inflammatory

Objective: The objective of present study was to enhance the potential activities of Quercetin by improving its solubility and dissolution profiles through solid dispersion approach. Method: A three level full factorial design (32) was adopted to study the possible combinations of polyethylene glycol (PEG) 6000 & pluronic F 127 (PF 127). The solid dispersions were prepared by solvent evaporation method and evaluated for percentage yield, drug content, aqueous solubility and drug release. For in vivo evaluations SD4 was incorporated into Carbopol base gel and subjected to anti-inflammatory activity using carrageenan-induced rat paw edema method. Results: SD4 batch with drug to carrier ratio 1:1 showed release of 82.96 ± 1.76 % in 240 min following Higuchi’s model. It was 5.54 fold increment in solubility as compared to quercetin. SD4 batch was further evaluated by FTIR, DSC, PXRD and SEM. The crystallinity was significantly reduced and drug was homogeneously dispersed in the carrier as shown by the results of DSC, PXRD and SEM. The DPPH scavenging assay showed significance in the IC50 value of SD4 as compared to pure quercetin and ascorbic acid when subjected to one way ANOVA at 0.05 level of significance (P<0.0001). In vivo anti-inflammatory study showed 78.17 ± 0.156 % inhibition of edema by SD4 and 58.64 ± 0.640 % by pure quercetin which is significantly lower (P<0.05). Conclusion: These findings demonstrate that the solid dispersion of quercetin shows increased solubility, dissolution profile, drug release and significant potential in enhancing the antiinflammatory activity of drug.

scholarly journals DEVELOPMENT AND IN VITRO DISSOLUTION STUDY OF BINARY AND TERNARY SOLID DISPERSIONS OF ACECLOFENAC

2019 ◽  
Author(s):  
Md. Shahidul Islam ◽  
Rasheda Akter Lucky
Keyword(s):  
Polyethylene Glycol ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Weight Ratio ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Peg 6000

The poor aqueous solubility of the drug exhibits in variable dissolution rate and hence poor bioavailability. Aceclofenac is poorly water soluble drug. The aim of the present study was to improve the water solubility and the dissolution rate of Aceclofenac by solid dispersion technique using different water soluble polymers. The term solid dispersions refer to the dispersions of one or more active ingredients in an inert carrier or matrix at solid state. In this study, binary solid dispersion of Aceclofenac were prepared by fusion method using Polyethylene glycol 6000 (PEG 6000), Polyethylene glycol 4000 (PEG 4000), Poloxamer as carrier. Different drug-carrier weight ratio was used for this study. The effect of the carrier on the solubility and in-vitro dissolution were studied. It was found the drug was released 26.86% after 5 minutes and only 40.19% within 60 mins from active Aceclofenac on the other hand the release pattern of Aceclofenac from the binary SD formulation containing PEG 6000 in 1:5 ratio (Formulation coding: A5) showed the best result in comparison of other binary and ternary SD formulations which was 62.29% after 5 min and 83.03% within 60 mins. The hydrophilic polymers used for the preparation of solid dispersion are showed significant increase in the solubility of Aceclofenac.

scholarly journals Formulation of Ramipril Tablets Containing Solid Dispersion Employing Selective Polymers to Enhance Dissolution Rate

2020 ◽  
Vol 10 (3-s) ◽  
pp. 142-149
Author(s):  
Inder Kumar ◽  
Sandeep Verma ◽  
Amit Chaudhary
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Phosphate Buffer ◽  
Flow Property ◽  
In Vitro Dissolution ◽  
Standard Data ◽  
Evaporation Technique ◽  
Good Flow

Objective: The present work based on formulation of Ramipril tablets containing solid dispersion employing selective polymers. The objective of the preparation is to prepare the solid dispersion of the Ramipril, which has more responsive value in terms of the dissolution rate. Method: Solid dispersion complex was prepared with two different carriers PEG 6000 and PVP K30. Nine formulations were developed and each formulation were subjected to pre compression and post compression parameters. Result and Discussion:  Pre-compression and post compression parameters were studied which had shown good flow property and compiled the standard data. In-vitro dissolution studies shows more than 90 % drug release in phosphate buffer pH 6.8 in 30 min. Out of all formulation F4 showed 92.55±0.67 % drug release with in 30min which was the best result rest of the formulation. Conclusion: Ramipril tablets were successfully prepared and evaluated. F4 formulation shows the greater dissolution rate in phosphate buffer pH 6.8 as compared to other formulations. When compared with marketed formulation it also shows better results. Therefore, Ramipril solid dispersion tablets enhanced the dissolution rate and can be more efficacious for improving oral bioavailability of Ramipril. Keywords: Solid dispersion, Ramipril, Solvent Evaporation Technique.

scholarly journals Effect of Amphiphilic Graft Co-Polymer Carrier on Solubility and Dissolution Enhancement of Ambrisentan

2021 ◽  
pp. 329-338
Author(s):  
Rahul Radke ◽  
Neetesh K. Jain
Keyword(s):  
Ftir Spectroscopy ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Dissolution Enhancement ◽  
Polymer Carrier ◽  
Dissolution Study

Aim: Ambrisentan is a endothelin type A selective receptor antagonist used in the management of pulmonary arterial hypertension. Ambrisentan is BCS Class II drug haves very poor solubility in water and shows incomplete absorption after oral administration. The present work was aimed to study the effect of amphiphilic graft co-polymer carrier on enhancement of solubility and dissolution rate of poorly water soluble drug ambrisentan. To improve the aqueous solubility of ambrisentan solid dispersion was formulated by using novel carrier amphiphilic graft co-polymer (Soluplus® ). Materials and Methods: Solid dispersion was prepared by kneading technique by utilizing various ratios of carrier. Obtained solid dispersions ware evaluated for solubility, percentage yield, drug content and in vitro dissolution study. Powder characterization was performed by infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and X-ray diffraction (XRD). Results: FTIR spectroscopy shows no interaction between drug and polymer. DSC study showed that endothermic peak of drug was completely disappeared in Solid dispersion suggesting complete miscibility of drug in Soluplus®. XRD study suggest the conversion of crystalline ambrisentan in to amorphous form. All solid dispersions prepared with Soluplus® as a carrier showed increase in solubility. Solubility of ambrisentan was found to be increased 7.17 fold in optimized SD formulation ASD5. In vitro dissolution study showed the faster drug release from SD formulation compare to its pure form. All solid dispersion formulation’s release more than 50% of drug in first 10 min. Conclusion: This study conclude that the preparation of amphiphilic graft co-polymer based solid dispersion prepared by kneading technique is found to be useful in enhancement the solubility and dissolution rate of ambrisentan.

scholarly journals Financial Soundness and Shareholder Value of Private Banks in India

2018 ◽  
Vol 5 (01) ◽  
Author(s):  
K. Abirami
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
X Ray Diffraction ◽  
Ftir Studies ◽  
Private Banks ◽  
Financial Soundness ◽  
Physical Mixtures

The objective of this study was to develop solid dispersions of Nifedipine which has low aqueous solubility and bioavailability. Preliminary solubility studies were carried out using various hydrophilic polymers. The formulations were then optimized and evaluated by in-vitro dissolution studies, X-ray diffraction, FTIR and SEM. Formulation with 1:4:2 ratios of Nifedipine, Labrosol and SLS was found to be the best as it possessed better drug release properties compared to pure drug and other physical mixtures. The optimized formulation SD12 was found to have better drug release of 98.74±5.19% in 90 minutes. From FTIR studies no interaction was takes place between drug and polymers. XRD peaks indicate the successful transformation of drug from crystalline to amorphous form. The final results indicate that the solid dispersion of Nifedipine remained stable over 90 days.

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>

Development, Optimization, Characterization and Impact of In vitro Lipolysis on Drug Release of Telmisartan Loaded SMEDDS

2019 ◽  
Vol 9 (4) ◽  
pp. 330-340 ◽  
Author(s):  
Ravinder Verma ◽  
Deepak Kaushik
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Oral Bioavailability ◽  
Research Work ◽  
Mixture Design ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
In Vitro Lipolysis ◽  
Globule Size

Objective: The objective of the current research is systematic optimization and development of microemulsion preconcentrates to get better solubility that results in improvement of oral bioavailability profile of Telmisartan utilizing D-optimal mixture design. Methods: Solubility studies in a variety of lipidic ingredients and optimization of formulations were carried out for the development of liquid SMEDDS. D-optimal mixture design was utilized for assessing the interaction performance of desired responses (such as % cumulative drug release and globule size) and optimized using desirability approach. The optimized batch was evaluated for its % cumulative drug release and globule size performance for determining the dissolution rate and oral bioavailability of drug. Results: The optimized batch (F-8), which contained 10% oil (Capmul MCM EP), 45% surfactant (Labrasol) and 45% co-surfactant (Transcutol HP) resulted in desired qualities of measured responses with 84.6nm globule size and 98.5% drug release within 15 minutes. Optimized SMEDDS showed brilliant goodness of fit between drug release. Stability studies indicated stability of the optimized SMEDDS batch over 3-month storage at 40°C/75% RH and improved dissolution rate in contrast to pure API. The optimized SMEDDS showed no impact of in vitro lipolysis on drug release. Conclusion: Developed and optimized SMEDDS showed improved in vitro dissolution rate and dissolution profile in contrast to pure drug. These investigations further confirm dose reduction in SMEDDS by gaining an equivalent therapeutic profile with non-SMEDDS formulation. This research work successfully shows the potential usage of SMEDDS for delivery of BCS-II class drugs.

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