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 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 Formulation design, optimization & in vitro evaluation of novel orodissolving tablets of efavirenz for hiv infections

2015 ◽  
Vol 49 (3) ◽  
pp. 173-180
Author(s):  
T Ayyappan ◽  
C Poojitha ◽  
T Vetrichelvan
Keyword(s):  
Drug Release ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Sodium Starch Glycolate ◽  
Weight Variation ◽  
Wetting Time

In the present work, orodissolving tablets of Efavirenz were prepared by direct compression method with a view to enhance patient compliance. A 23 full factorial design was applied to investigate the combined effect of three formulation variables. Amount of crospovidone, croscarmellose sodium and sodium starch glycolate were used as superdisintegrant material along with direct compressible mannitol to enhance mouth feel. The prepared batches of tablets were evaluated for hardness, friability, weight variation, disintegration time, wetting time, drug content and in-vitro dissolution studies. Based on wetting time, disintegration time, the formulation containing crospovidone (5% w/v), carscarmellose sodium (5% w/v) and sodium starch glycolate (8% w/v) was found to be promising and tested for in-vitro drug release pattern (in 0.1 N HCl), short term stability and drug- superdisintegrants interaction. Surface response plots are presented to graphically represent the effect of independent variables (conc. of superdisintegrants) on the in-vitro dissolution time. The validity of the generated mathematical model was tested by preparing extra-design check point formulation. The formulation showed nearly faster drug release compared to the conventional commercial tablet formulation. Stability studies on the optimized formulation indicated that there was no significant change found in physical appearance, hardness, disintegration time, drug content and in-vitro drug release. DOI: http://dx.doi.org/10.3329/bjsir.v49i3.22131 Bangladesh J. Sci. Ind. Res. 49(3), 173-180, 2014

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.

Development and Evaluation of Guaifenesin Bilayer Tablet

2010 ◽  
Vol 3 (3) ◽  
pp. 1122-1128 ◽  
Author(s):  
Vijaya Kumar B ◽  
Prasad G ◽  
Ganesh B ◽  
Swathi C ◽  
Rashmi A ◽  
...  
Keyword(s):  
Drug Release ◽  
Angle Of Repose ◽  
Fickian Diffusion ◽  
In Vitro Dissolution ◽  
Burst Release ◽  
In Vitro Drug Release ◽  
Initial Burst ◽  
Drug Content ◽  
Bilayer Tablet

The objective of the present research was to develop a Bilayer tablet of guaifenesin (GBT) using superdisintegrant MCC and sodium starch glycolate for the fast release layer and metalose 90 SH and carbopol 934 for the sustaining layer. The guaifenesin SR granules of different formulation were evaluated for bulk density, tapped density, angle of repose, Carr’s index and Hausners ratio and results were found to be 0.460 ± 0.12 to 0.515 ± 0.03 gm/cm3 , 0.550 ±0.03 to 0.590 ±0.04 gm/cm3 , 19 ±0.01 to 26 ± 0.23, 13.72 ± 0.03 to 19.56 ± 0.04 & 1.137 to 1.196, respectively. The prepared bilayer tablets were evaluated for weight variation, hardness, friability, drug content and in vitro drug release. In vitro dissolution studies were carried out in a USP 24 apparatus I. The formulations gave an initial burst effect to provide the loading dose of the drug followed by sustained release for 12 h from the sustaining layer of matrix embedded tablets. In vitro dissolution kinetics followed the Higuchi model via a non-Fickian diffusion controlled release mechanism after the initial burst release. Stability studies conducted for optimized formulation did not show any change in physical appearance, drug content, matrix integrity and in vitro drug release. The results of the present study clearly indicated that GBT was a stable dosage form and a promising potential of the guaifenesin bilayer system as an alternative to the conventional dosage forms

scholarly journals Formulation and evaluation of Olmesartan Medoxomil solid dispersions to enhance its solubility and dissolution characteristics

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 1515-1525
Author(s):  
Christopher Vimalson D ◽  
Parimalakrishnan S ◽  
Jeganathan N S ◽  
Anbazhagan S
Keyword(s):  
Drug Release ◽  
Olmesartan Medoxomil ◽  
Angle Of Repose ◽  
Physical Parameters ◽  
In Vitro Drug Release ◽  
Peg 6000 ◽  
Drug Content ◽  
Pure Drug ◽  
Pvp K30

The objective of the present learns to improve solubility and dissolution of Olmesartan Medoxomil (OM) by improving water solubility by reliable dispersion methods using fusion method (FM) and solvent evaporation (SE) method via hydrophilic polymers PEG 6000 and PVP K30 in different ratios.  Preformulation studies of OM: polymers were carried using DSC and FTIR proves that it is stable without any extra peaks, which implies no interaction among the drug and carrier. For OM in FM drug: polymer ratio was maintained in a range 1:1, 1:3, 1:5 and 1:7 w/w ratio of OM to PEG 6000 and  coded as SDOM1, SDOM2, SDOM3 and SDOM4 whereas for SE method OM to PVP K30  ratio was maintained in a range of 1:1, 1:3, 1:5 and 1:7 w/w ratio  and coded as SDOM5, SDOM6, SDOM7 and SDOM8. SDOM3 by FM and SDOM7 by SE method resulted in the highest production yield. The solubility studies have shown improved drug solubility compared with a pure drug in all medium. Percentage of drug content, flowability characters like the angle of repose and carr's index, bulk density, Hausner's, tapped density were within acceptable limits. In vitro drug release in the intestinal gastric medium of pH 1.2 was improved significantly when compared with pure drug. SDOM3 and SDOM7, selected for accelerated stability studies, had no significant change in physical parameters, drug content, with little changes in the in vitro  drug release pattern. Hence solubility and dissolution rate of OM is increased by using the PEG 6000 and PVP K30 polymers. 

scholarly journals SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF EZETIMIBE BY SOLID DISPERSION AND PELLETIZATION TECHNIQUES USING SOLUPLUS AS CARRIER

2019 ◽  
pp. 57-64
Author(s):  
Viswanadh Kunam ◽  
Vidyadhara Suryadevara ◽  
Devala Rao Garikapati ◽  
Venkata Basaveswara Rao Mandava ◽  
RLC Sasidhar
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Physicochemical Parameters ◽  
Solid Dispersions ◽  
Surface Characteristics ◽  
Sem Analysis ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Pure Drug

Objective: In the present investigation, an attempt was made to improve the surface characters and solubility of the drug by solid dispersion and coating it on the nonpareil sugar beads as pellets. Methods: Ezetimibe solid dispersions were prepared by kneading method using soluplus. Crospovidone was added as a disintegrant in pellets. Ezetimibe pellets were prepared by dissolving soluplus and crospovidone in ethanol in different ratios and coated on nonpareil sugar beads as a drug layer by pan coating technique. Various physicochemical parameters like particle size, friability, angle of repose and drug content were evaluated for the prepared solid dispersions and pellet formulations. In vitro dissolution studies were carried out in 1% SLS using USP apparatus II. FTIR and SEM analysis were performed for solid dispersions, pellet formulations and its polymers to determine the interactions and surface characteristics. Results: The physicochemical parameters were within the specified I. P limits. It was observed that the solid dispersion formulation ED5 showed better dissolution rate to the extent of 1.07 folds and 1.95 folds when compared to a marketed formulation and the pure drug, respectively. Similarly, pellet formulation EP5 containing 1:5 ratio of ezetimibe to soluplus showed an improved dissolution rate to the extent of 1.173 folds and 2.136 folds when compared to the marketed formulation and the pure drug, respectively. FTIR analysis revealed that there was no major interaction between the drug and the excipients.  Conclusion: From the present study, it was observed that the solubility of ezetimibe was enhanced by soluplus in pellet formulations when compared to solid dispersions.

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 F FORMULATION DEVELOPMENT AND EVALUATION OF CARBOPOL-INCORPORATED THERMOREVERSIBLE GELS OF PSEUDOEPHEDRINE FOR RECTAL DRUG DELIVERY

2019 ◽  
pp. 231-235 ◽  
Author(s):  
FIROZ S ◽  
PADMINI K ◽  
PADMASREE K ◽  
SRAVANI N ◽  
HEMALATHA A ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
In Vitro Dissolution ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Drug Content ◽  
Ir Studies ◽  
Thermoreversible Gels ◽  
Rectal Drug Delivery

Objectives: The present study describes the preparation and evaluation of a Poloxamer 188 (P188)-based thermoreversible gel using Carbopol 934P (C934P) as a mucoadhesive polymer of pseudoephedrine for enhancing the bioavailability and to avoid the first-pass metabolism. Materials and Methods: Five formulations (F1-F5) were prepared using cold method. The prepared gels were characterized by pH, drug content, spreadability, mucoadhesive force, gelation temperature, and drug release profile. Thermoreversibility of P188/C934P gel was demonstrated by rheological studies. The drug-polymer compatibility was studied using Fourier transform infrared (FTIR). Results: The incorporation of carbopol into P188 gel also reduced the amounts of drug released from the gel formulations. FT-IR studies revealed that there are no interactions between the drug and polymers. Drug content of gels was estimated and the results were found to be satisfactory. In vitro dissolution studies revealed a good drug release from the gels. The drug release was higher in formulations F4 and F5 and lower in F1, F2, and F3 formulations. The order of drug release was found to be F5>F4>F3>F2>F1. Conclusion: These findings suggested that developed thermoreversible gels could be used as promising dosage forms to rectal drug delivery for prolonged periods in the management of hemorrhoids.

scholarly journals Formulation Development and Evalua Tion of Fluoxetine Effervescent Floating Tablet

2019 ◽  
Vol 9 (4-A) ◽  
pp. 358-366
Author(s):  
Nilesh V. Pakhale ◽  
S.B. Gondkar ◽  
R.B. Saudagar
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Study Drug ◽  
In Vitro Dissolution ◽  
Formulation Development ◽  
Drug Content ◽  
Antidepressant Agent ◽  
Floating Tablet ◽  
Effervescent Tablet

The objective of the present study was to formulate and evaluate Effervescent Floating Tablet of Fluoxetine for the treatment of antidepressant agent. Tablets were prepared by direct compression using directly compressible polymers such as HPMC K4M, and Carbopol 934 were evaluated for drug-excipient compatibility, density, buoyancy test, swelling study, drug content and In-Vitro release profile. Sodium bicarbonate and citric acid were used producing effervescent base for buoyancy of tablets. Analysis of drug release from tablet indicates drug release by zero order, first order rate kinetics. No significant change was observed in physical appearance, drug content, floatability or in-vitro dissolution pattern after storage at 450C/750C RH for three months. Keywords: Floating effervescent tablet, GIT, Fluoxetine , HPMC K4M, Carbopol 934.                                                                                              

scholarly journals Bioavailability Enhancement of Ritonavir by Solid Dispersion Technique

2021 ◽  
Vol 11 (5) ◽  
pp. 52-56
Author(s):  
Teja Velupula ◽  
Gayathri Devi Amboru ◽  
Sneha Chowdary Gundapaneni ◽  
Bhavya Kadiyala ◽  
Phani Sreenidhi Kanakagiri ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Wave Number ◽  
In Vitro Dissolution ◽  
Phase Solubility ◽  
Dissolution Studies ◽  
Drug Content ◽  
Ft Ir ◽  
Dispersion Technique

Ritonavir is an antiretroviral agent used in the treatment of HIV-infection. It is a BCS class IV drug having poor aqueous solubility leading to poor bioavailability. Bioavailability is the amount of drug that enters the systemic circulation. The bioavailability is affected by various factors like solubility, dissolution and stability. In order to improve bioavailability, many techniques like solid dispersions, nanoparticles, liposomes, encapsulation methods were present. The main aim of this study is to improve the bioavailability of ritonavir with the help of Polyvinyl Pyrrolidone (PVP) K-30 by using solid dispersion technique. Different formulations were made with varied concentrations of polymer. Characterization of solid dispersion was done by phase solubility, drug content, Fourier transformed infrared spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC) and in-vitro dissolution studies.  From phase solubility studies that apparent solubility constant was found to be 42.227M-1. The drug content of the binary system of ritonavir and PVP was found to be ranging from 99.17% to 103.06%. %. FT-IR studies revealed that there was no drastic change in the wave number indicating polymer compatibility with drug. In-vitro dissolution studies proved that there was an increase in drug release of ritonavir with incremental ratios of polymer and F5 formulation has shown almost 95% of drug release. Keywords: Bioavailability, Solid dispersion, Polyvinyl pyrrolidine, Solvent evaporation, Dissolution.

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