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 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 PREPARATION AND EVALUATION OF METOLAZONE SOLID DISPERSIONS AND FAST DISSOLVING TABLETS USING STERCULIA FOETIDA SEED STARCH AND PLASDONE K-29/32 AS SUPERDISINTEGRANTS

2020 ◽  
pp. 144-151
Author(s):  
SANDEEP DOPPALAPUDI ◽  
VIDYADHARA SURYADEVARA
Keyword(s):  
Drug Release ◽  
Sodium Hydroxide ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
In Vitro Dissolution ◽  
Physical Parameters ◽  
Stability Studies ◽  
Compression Technique ◽  
Release Formulation

Objective: The objective of the current study is to improve the solubility of the Biopharmaceutical Classification System (BCS) Class-II drug, Metolazone, using various superdisintegrants. Methods: Starches were extracted from Sterculia foetida seed powder by water and alkali techniques i.e., sodium hydroxide at 0.1%, 0.25% and 0.5% concentrations. Several phytochemical and physicochemical parameters were evaluated on the extracted starches. Solid dispersions of Metolazone were prepared by the solvent evaporation technique using plasdone K-29/32 alone and by mixing plasdone K-29/32 with Sterculia foetida seed starch. Various physical parameters were evaluated for the prepared solid dispersions. Tablets were prepared using Metolazone solid dispersions and varying concentrations of Sterculia foetida seed starch by direct compression technique. Pre and post-compression parameters were evaluated along with in vitro drug release studies, characterization using Scanning Electron Microscopy (SEM) and stability studies. Results: Phytochemical tests showed the presence of starch in all extracts. Starch prepared from 0.1% sodium hydroxide (SFS2) showed best physicochemical properties. In vitro dissolution studies revealed that solid dispersion MS4 containing Metolazone and plasdone K-29/32 in 1:3 ratios showed better drug release. Formulation MPT6 containing MS5 solid dispersion with 15% w/w of SFS2 showed enhanced drug release. SEM studies revealed no major interactions between drugs and excipients. Accelerated stability studies showed that all tablets were stable. Conclusion: Sterculia foetida seed starch and plasdone K-29/32 have enhanced the solubility of Metolazone.

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.

Preparation, Characterization and In Vitro Evaluation of IVM Loaded Poly(lactic-Co-Glycolic Acid) (PLGA) Microspheres

2011 ◽  
Vol 311-313 ◽  
pp. 1751-1754
Author(s):  
Gui Yu Li ◽  
Xi Hong Lu ◽  
Xue Hu Li ◽  
Lei Tao ◽  
Jian Ping Liang
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
High Performance ◽  
Glycolic Acid ◽  
Drug Release Profile ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Drug Delivery Carrier ◽  
Drug Sustained Release

Drug was encapsulated in a novel copolymers of poly(lactic-co-glycolic acid) (PLGA) to investigate the sustained-release formulation of drug loaded polymer microspheres delivery system. Used a modified solid-in-oil-in-water (S/O/W) emulsion solvent evaporation method to prepare microspheres, its morphology and particle size distribution were estimated by scanning electron microscopy (SEM), the profile of in vitro drug release were assessed by High performance liquid chromatography (HPLC). Finally, an stable release buffer was utilized to obtain a detailed drug release profile, which was analyzed by HPLC also. Results showed that the microspheres morphology, encapsulation efficiency and the cumulative drug release efficiency were appropriate for veterinary medicine using. The modified preparation method was simple and optimized, PLGA microspheres with excellent controlled-release characteristics may serve as drug delivery carrier and may prolong the drug sustained-release effect.

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.

Development and Characterization of Glipizide Loaded Sustained Release Nanoparticles

2019 ◽  
Vol 9 (3) ◽  
pp. 232-242 ◽  
Author(s):  
Rutuja Deshmukh ◽  
Mrunal Waghulde ◽  
Satyendra Mishra ◽  
Jitendra Naik
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Drug Uptake ◽  
Sustained Drug Release ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Fourier Transformed Infrared Spectroscopy ◽  
Wide Range ◽  
Repeated Dosing

Background: Treating the disease like diabetes is essential due to its wide range of spreading and heredity issues. Glipizide is the commonly used drug for the treatment of diabetes. Glipizide loaded sustained release nanoparticles have been developed to avoid repeated dosing. Objective: The study aimed to develop glipizide-loaded sustained release nanoparticles and characterize them for different studies. Methods: The aim of the present study was to develop glipizide-loaded sustained release nanoparticles using different polymers by the solvent evaporation method. The polymers; Eudragit (RS 100) in combination with Polycaprolactone (PCL) were used to encapsulate glipizide. Optimization of all parameters was performed as per Design Expert software by utilizing a 32 full factorial design. The developed nanoparticles were characterized using Fourier transformed infrared spectroscopy, X-ray diffraction, scanning electron microscopy and in-vitro drug release study. Results: FE-SEM showed that the surface morphology of nanoparticles was smooth and spherical as well as in an oval shape. FTIR shows there is no interaction between polymers and drug. XRD results showed that the crystallinity of pure glipizide reduced from 89.5 to 56.7% when converted into sustained release nanoparticles formulation. Sustained drug release over the period of 12 h was observed due to well encapsulation of glipizide by the polymers. Conclusion: Glipizide loaded nanoparticles were developed with good encapsulation efficiency using a combination of two different biocompatible polymers. The drug release behavior showed that they can be used to develop the sustained release formulation to reduce the side effect caused by over drug uptake as compared to the conventional formulation.

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 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.

scholarly journals Formulation And In Vitro/In Vivo Evaluation Of Olmesartan Medoxomil Solid Dispersions Incorporated E/R Trilayer Matrix Tablets By Geomatrix

2017 ◽  
Vol 8 (4) ◽  
Author(s):  
M Balakrishnaiah ◽  
V. Rama Mohan Gupta
Keyword(s):  
Solid Dispersion ◽  
Guar Gum ◽  
Solid Dispersions ◽  
Olmesartan Medoxomil ◽  
Matrix Tablets ◽  
Dissolution Profile ◽  
In Vivo Evaluation ◽  
Release Formulation

<p>An attempt has been made to develop and optimize an novel anti hypertensive trilayered controlled release matrix tablets incorporated with Olmesartan medoxomil solid dispersion prepared by direct compression and consisted of middle active layer with different grades of hydroxypropylmethylcellulose (HPMC), guar gum, ethyl cellulose. Upper and lower layers are prepared with Carnauba wax, guar gum and sodium CMC. The developed drug delivery system provided prolonged drug release rates over a period of 24 h. The release profile of the optimized formulation (HF14) was described by the Zero-order and Higuchi model. In-vivo bioavailability studies were carried out with the optimized formulation (HF14) and reference standard A fair correlation between the dissolution profile and bioavailability for the optimized formulation was observed. The results indicate that the approach used could lead to a successful development of a trilayer extended release formulation up to 24h. These results also demonstrated that the Olmesartan solid dispersion incorporated trilayer tablets shown more bioavailability because of its conversion from crystalline to amorphous form.</p>

scholarly journals Implementation of time release technology in formulation development and evaluation of sustained release tablet of Lornoxicam

2014 ◽  
Vol 2 (01) ◽  
pp. 68-75 ◽  
Author(s):  
Swapnil J. Kodalkar ◽  
Rohan A. Khutale ◽  
Sachin S. Salunkhe ◽  
Sachin S. Mali ◽  
Sameer J. Nadaf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Kinetic Studies ◽  
Release Kinetic ◽  
Matrix Tablet ◽  
Formulation Development ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Sustained Drug Delivery

In present study, the attempts have been made to formulate sustained release tablets of lornoxicam by direct compression method. Based on viscosity grades different proportions of hydrophilic polymers (HPMC K4M, HPMC K15M, HPMC K100M) are used for preparation of lornoxicam sustained release matrix tablet. The drug excipient mixtures were subjected to preformulation studies comprising of micromeritic properties. The tablets were subjected to various studies like as physicochemical studies, in vitro drug release, kinetic studies, etc. FTIR studies shown there was no interaction between drug and polymers. The physicochemical properties of tablets were found within the limits. Lornoxicam is a first generation analgesic, inflammatory and antipyretic agent used in relieving symptoms of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute sciatica and low back pain. From developed formulations batch F1 have shown zero order drug release behavior and prolong drug release over a period of 12 h which was deemed as suitable and optimum formulation for sustained drug delivery. Results of the present study indicated the suitability of the low viscous polymer in the proportion of (drug:polymer) 1:1 in the preparation of sustained release formulation of lornoxicam.

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