Study on the effect of different polymers on in-vitro dissolution profile of Fenofibrate by solid dispersion technique

2014 ◽  
Keyword(s):  
Solid Dispersion ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Dispersion Technique

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 OF ATOVAQUONE TABLET USING BIOSURFACTANT IN A TERNARY SOLID DISPERSION SYSTEM: IN VITRO AND IN VIVO EVALUATION

2019 ◽  
pp. 44-49
Author(s):  
UDAYKUMAR B. BOLMAL ◽  
PRAMOD H. J.
Keyword(s):  
Ternary System ◽  
Solid Dispersion ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
In Vivo Evaluation ◽  
Enhanced Dissolution ◽  
Bioavailability Study

Objective: The goal of the present investigation was to improve the solubility and bioavailability of atovaquone tablet, using in-house biosynthesized biosurfactant in the ternary system of solid dispersion containing hydrophilic polymers with varying concentrations of biosurfactant. Atovaquone is an anti-malarial agent and belongs to biopharmaceutical classification system class IV. Methods: The solid dispersion of binary and ternary mixture was prepared using hydroxyl propyl methyl cellulose (HPMC) and biosurfactant respectively by a solvent evaporation method. All the atovaquone tablet formulations were prepared by incorporation of physical mixture, binary and ternary solid dispersed products with excipients by direct compression method. Pre-compression and post-compression parameters of atovaquone tablets were evaluated. In vivo bioavailability study was performed using female albino rabbits. Results: In vitro dissolution profile of binary and ternary system of solid dispersion products showed 8.65% and 34.64% respectively. Precompression and post-compression values of all atovaquone tablets formulations were within the specified limits. In vitro dissolution efficiency of F2 and F5 were 1.44 fold and 6.62 fold respectively, in accordance to the F1. In vivo study revealed that bioavailability of optimized formulation F5 was increased by 2.5 times and time to reach peak concentration was reduced to 1.4 h, in accordance to pure atovaquone suspension. Conclusion: Potential application of biosurfactant in the solid dosage form of atovaquone tablet was proved for enhanced dissolution rate and bioavailability of atovaquone for malaria treatment.

scholarly journals Development and Biopharmaceutical Evaluation of Tablets Based on the Poorly Water-soluble Substance 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil

2020 ◽  
Vol 9 (4) ◽  
pp. 79-87
Author(s):  
D. V. Demchenko ◽  
E. A. Jain (Korsakova) ◽  
V. Yu. Balabanyan ◽  
M. N. Makarova ◽  
V. G. Makarov
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Active Pharmaceutical Ingredient ◽  
Oral Route ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Technological Properties ◽  
Enhanced Dissolution ◽  
Dispersion Technique

Introduction. 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil is a substance of scientific interest intended for the treatment of HIV-infection. However, its low bioavailability is a major limitation in successful drug delivery by oral route. Therefore, the objective of the present work was to enhance itssolubility by using solid dispersion technique followed by the development of a solid dosage form.Aim. Development of the composition and technology of tablets based on 1- [2-(2-benzoylphenoxy)ethyl]-6-methyluracil with the appropriate technological properties providing the most complete release of the active pharmaceutical ingredient (API) in vitro.Materials and methods. The pharmaceutical substance 1-[2-(2-benzoylphenoxy) ethyl]-6-methyluracil is a crystalline powder with poor solubility. Solid dispersions were prepared using Lactose, Kollidon® 17PF, Kollidon® 30, Kollidon® VA64, Kollidon 90F, and PEG-6000 as a carrier mostly in 1:4 ratio by two methods – co-melting and solvent evaporation. The technological properties of substance, tablet masses and tablet quality were determined according to the methods described in the State Pharmacopoeia of the Russian Federation (14th edition).Results and discussion. Article shows the results of development of the composition and technology of a medicine in the form of tablets based on the substance 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil. Solid dispersion technique was used to improve the biopharmaceutical properties of 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil.Conclusion. In vitro dissolution studies showed enhanced dissolution rate of the drug-loaded solid dispersion with Kollidon 17PF as a carrier as compared to pure drug.

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 Enhancement of Solubility and Dissolution Rate of Curcumin Using Porous Starch by Solid Dispersion Technique

2021 ◽  
Vol 23 (2) ◽  
Author(s):  
Indrayani D.Raut ◽  
◽  
Nikita D. Gidde D. Gidde ◽  
Priyanka V. Desai ◽  
Priyanka V. Bagade V. Bagade ◽  
...  
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
In Vitro Dissolution ◽  
Hydrophilic Matrix ◽  
Novel Method ◽  
Improved Performance ◽  
Dispersion Technique ◽  
Low Solubility ◽  
Biopharmaceutical Classification System

The poor dissolution characteristics of biopharmaceutical class II drugs are a major concern for scientists in thepharmaceutical industry. Solid dispersion is introduced as a novel method for enhancement of solubility. Class IIdrugs are low solubility and high permeability according to the biopharmaceutical classification system and arepromising candidates for improving solubility and bioavailability through solid dispersion. The purpose of the present attempt is to prepare a solid dispersion of curcumin and porous starch in order to increase the solubility and dissolution of drugs that are poorlysoluble. Solid dispersions (SDs) of BCS-II drugs were prepared by ball milling in ratio of drug: polymer i.e. curcumin: porous starch (1:0.5, 1:1, 1:2 and 1:3). Further, SDs were investigated by solubility, FTIR, XRD, DSC, micromeritics, and in-vitro dissolution. . Conclusively, porous starch offers a hydrophilic matrix to deliver poorwater soluble drugs and Solid dispersion system have demonstrated an improved performance. Solid dispersionsystem have demonstrated an improved performance

scholarly journals STUDIES ON REFINED LIQUISOLID SYSTEM FOR SIMULTANEOUS IMPROVEMENT OF CONTENT UNIFORMITY AND DISSOLUTION PROFILE OF GLIMEPIRIDE

2019 ◽  
pp. 396-405
Author(s):  
Manish Dhall ◽  
Parmita Phaugat ◽  
Suchitra Nishal
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Xrd Analysis ◽  
Solvent System ◽  
In Vitro Dissolution ◽  
Time Interval ◽  
Content Uniformity ◽  
Dissolution Profile ◽  
Characteristic Analysis

Objective: To improve and compare dissolution contour of poorly soluble BCS Class II drug Glimepiride (GLD) by altering it to conventional solid dispersion (CSD), surface solid dispersion (SSD) and refined liquisolid system (RLS). Methods: The three formulations of GLD namely CSD, SSD and RLS were fabricated using the conventional methods by employing the suitable polymer and solvent system. These formulations were optimized on the basis of powder flow properties, FTIR, DSC and XRD analysis. All the optimized formulations were compared to the marketed formulation for content uniformity and dissolution rate. Results: The characteristic analysis of all the optimized formulations was obtained in the standard range. The average content uniformity (% age) of Marketed formulation, CSD, SSD and RLS found to be 88.28±0.721, 92.91±0.789, 95.98±0.478, 99.32±0.744 respectively. The in vitro dissolution rate  (%age at 30 min time interval) fall in the range 59.78±0.036, 75.78±0.013, 93.11±0.019, 93.99±0.062 and 98.55±0.043 for pure drug, Marketed formulation, CSD, SSD and RLS respectively. All the analytical studies exhibited improved homogeneity/distribution of the drug in RLS. Conclusion: The RLS formulation presented sheer expansion in the content uniformity and dissolution contour of GLD at a minimal cost.

scholarly journals Evaluation of in vitro Dissolution Profile and Physicochemical Characterization of Polymer Based Formulations of Sparingly Soluble Rosuvastatin

2021 ◽  
Vol 20 (2) ◽  
pp. 199-211
Author(s):  
KM Yasif Kayes Sikdar ◽  
Md Shahoriar Nazir ◽  
Md Mahbubul Alam ◽  
Md Raihan Sarkar ◽  
Sad Al Rezwan Rahman
Keyword(s):  
Solid Dispersion ◽  
Fourier Transforms ◽  
Promising Result ◽  
Physicochemical Characterization ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Physical Mixing

Rosuvastatin (RVT) is a BCS class II antilipidemic crystalline drug, which exhibits low bioavailability due to its very poor aqueous solubility; therefore, it is challenging to develop a proper formulation of RVT. To enhance solubility and bioavailability of this API, an attempt has been made by implementing solid dispersion technique. Solid dispersion (SD) technique is a solubility enhancing technique where one or more active entities are dispersed in an inert medium (matrix or carrier) at solid state. In this study, different ratios of Kollicoat® IR (KIR) and Kollidon® 90F (KF90) polymers were used with API to prepare various formulations by physical mixing (PM) and SD approaches; here solvent evaporation technique was used whereas methanol was used as solvent which was completely evaporated from the homogenously dispersed system by placing in a water-bath at 60-65°C and then in oven for 30 minutes at 50 °C. Among the formulations, RVT-KF90 SD formulations showed the most promising result in in-vitro study in terms of drug release profile (78.04 – 99.21%) in comparison to pure RVT (63.1%) and physical mixing of RVT with those polymers. USP dissolution apparatus type II was used at 37°C ± 0.5°C with 50 rpm to conduct the in-vitro experiment. The experiment also unraveled that the dissolution of RVT improved with increasing the amounts of polymers. Subsequently, stability of the developed formulations was conducted by Fourier transforms infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) as well as scanning electron microscopy (SEM). The results obtained from FTIR ensured no involvement of any significant drug-excipient interaction. Moreover, the DSC study signified thermal stability at high temperature. Besides, the SEM micrograph illustrated homogenous distribution of RVT in the polymer and transformation of crystal-like RVT into amorphous formulations. Dhaka Univ. J. Pharm. Sci. 20(2): 199-211, 2021 (December)

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.

FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF LORATADINE SOLID DISPERSION USING SUPER DISINTEGRANTS

INDIAN DRUGS ◽  
2019 ◽  
Vol 56 (08) ◽  
pp. 84-87
Author(s):  
S Kumar ◽  
J. V. Kumar ◽  
P Singhal ◽  
Keyword(s):  
Solid Dispersion ◽  
In Vitro Dissolution ◽  
Dissolution Behavior ◽  
Direct Compression ◽  
Compression Method ◽  
Equilibrium Solubility ◽  
Sodium Starch Glycolate ◽  
Croscarmellose Sodium ◽  
Dispersion Technique

The aim of the present investigation was to prepare solid dispersion (SD) of the water insoluble drug. Loratadine using super disintegrants as carrier and formulate it as fast dissolving tablets (FDTs) with an objective to improve solubility and enhance dissolution of drug. The SD’s of the drug were prepared by melt dispersion technique using polyethylene glycol (PEG) 6000 in diferent ratios 1 : 2.5, 1 : 5 and 1 : 7.5. The prepared SD formulations were characterized for equilibrium solubility, Fourier Transform Infrared spectroscopy (FTIR) and in vitro dissolution study. The batch containing SD formulation of loratadine showed fastest dissolution (99.87% drug release in 60 min). In this study, fast dissolving tablets were prepared by direct compression method using Croscarmellose sodium, sodium starch glycolate and polyplasdone XL as the super disintegrants. Effect of various super disintegrants on dissolution behavior of tablets was evaluated in phosphate buffer pH 6.8.

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