scholarly journals Solid Dispersion Preparation by Different Methods to Improve Solubility & Dissolution Simvastatin

2021 ◽  
pp. 241-253
Author(s):  
Kamalpreet Kaur ◽  
Taranjit Kaur ◽  
Ajeet Pal Singh ◽  
Amar Pal Singh
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Methyl Cellulose ◽  
Competitive Inhibitor ◽  
In Vitro Dissolution ◽  
Absolute Bioavailability ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Gum Acacia

The improvement of a pure drug's solubility and dissolution rate in the treatment of hyperlipidemia. Simvastatin is a 5-percent absolute bioavailability selective competitive inhibitor of HMG Co-A reductase. For the selection of the carrier, a preliminary solubility investigation of solid dispersion was performed, and solid dispersion was made using Hydroxy Propyl Methyl Cellulose (HPMC) and gum acacia. Solid dispersion of medication with polymer was created and studied for solubility and in-vitro dissolution profile. Solid dispersion of drug with polymer has shown an increase in solubility and improved dissolution rate. On the obtained formulations, further FTIR, X-Ray, Scanning electron microscopy, and Differential scanning calorimetry experiments were conducted. The existence of amorphous form in a solid dispersion made with polymer in a 1:5 ratio is verified by characterization research. The research also showed that using a solid dispersion approach with Polymer, the dissolving rate of a pure medication may be significantly increased.

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.

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 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 IMPROVEMENT OF DISSOLUTION RATE OF VALSARTAN BY SOLID DISPERSION SYSTEM USING D(−) MANNITOL

2017 ◽  
Vol 10 (3) ◽  
pp. 288 ◽  
Author(s):  
Erizal Zaini ◽  
Salman Umar ◽  
Nurhidayah Nurhidayah
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
In Vitro Dissolution ◽  
Type I ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Dispersion System ◽  
Grinding Technique

ABSTRACTObjective: To improve dissolution rate of valsartan from solid dispersion system of valsartan and D(−) mannitol using co-grinding approach.Methods: Valsartan solid dispersion with different ratio of D(−) mannitol (1:1; 1:3 and 1: 5) were prepared by co-grinding method. Solid statecharacterization of the solid dispersion system was evaluated in term of crystallographic properties (powder X-ray diffraction), thermal behavior(differential scanning calorimetry [DSC]) and morphology (scanning electron microscope). The profile of dissolution rate was examined using USPdissolution apparatus type I at a temperature of 37±0.5°C.Results: Based on thermal analysis DSC and powder X-ray diffraction analysis, valsartan was transformed from semicrystalline phase to amorphousstate as indicated by the disappearance of its melting endothermic peaks and the characteristic diffraction peaks. The in vitro dissolution rate studyrevealed that all solid dispersion system showed significant increase in dissolution rate compared with the intact valsartan.Conclusion: Solid dispersion of valsartan with D(−) mannitol prepared by co-grinding technique has successfully improved the dissolution ratecompared with intact valsartan.Keywords: Valsartan, D(−) mannitol, Solid dispersion, Co-grinding, Dissolution rate.

DEVELOPMENT OF SOLID DISPERSION TABLET OF CARVEDILOL TO IMPROVE SOLUBILITY

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 54-59
Author(s):  
S. S Shelake ◽  
◽  
R. G Gaikwad ◽  
S Patil ◽  
F. I. Mevekari ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Media ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Water Soluble Drugs ◽  
Ft Ir

Crystalline state compounds are typically dissolution rate limited and dissolution rate is directly proportional to the solubility for BCS class II or class IV compounds. Solid dispersions are one of the most promising strategies to improve the oral bioavailability poorly water soluble drugs. The purpose of this study was to increase solubility of carvedilol by solid dispersion (SDs) technique with Poloxamer (PXM) 407 in aqueous media. The carvedilol- PXM 407 solid dispersion was prepared by solvent evaporation, kneading and melting method. It was characterized by differential scanning calorimetry (DSC), X-ray powder diffraction (XRD), Fourier transformation infra-red spectroscopy (FT-IR), scanning electron microscopy (SEM) and in vitro dissolution studies. The prepared solid dispersion were found to have higher dissolution rates as compared to intact carvedilol. During formulation of solid dispersion crystalline to amorphous transition has been observed.

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 In Vitro Evaluation of Different Approaches and Dissolution Enhancement Technique of Poorly Water-Soluble Drug Ibuprofen

2016 ◽  
Vol 64 (2) ◽  
pp. 169-175
Author(s):  
ASM Monjur Al Hossain ◽  
Konika Rani Dutta ◽  
Md Lokman Hossain
Keyword(s):  
Dissolution Rate ◽  
Methyl Cellulose ◽  
Water Soluble ◽  
Poloxamer 407 ◽  
In Vitro Dissolution ◽  
Dissolution Enhancement ◽  
Dissolution Profile ◽  
Physical Mixing ◽  
Pregelatinized Starch

Ibuprofen Solid Dispersion (SD) was prepared by simple Physical Mixing (PM) and Kneading Method (KM). In these two cases, four polymers named poloxamer 407, sodium carboxy methyl cellulose, croscarmellose sodium and pregelatinized starch were used to enhance the dissolution profile of Ibuprofen. In both methods, the ratio of drug and carrier were 1:1, 1:2, 1:3 of which the ratio of 1:3 in KM gave comparatively better result than PM method. In vitro dissolution study was performed in distilled water in 50 rpm and at 37 ± 0.5°C. In case of pure Ibuprofen, dissolution rate was only 26% after 60 minutes (mins) of dissolution. While in KM, Ibuprofen pregelatinized starch formulation at 1:3 ratio showed better dissolution rate. After 60 mins, dissolution rate of Ibuprofen was 72%. The SD formulations of Ibuprofen-pregelatinized starch and Ibuprofen-Na-CMC of physical mixing and kneading techniques (1:3 ratio) were characterized by Fourier Transform Infrared Spectroscopy (FTIR). Dhaka Univ. J. Sci. 64(2): 169-175, 2016 (July)

scholarly journals Artemether-Soluplus Hot-Melt Extrudate Solid Dispersion Systems for Solubility and Dissolution Rate Enhancement with Amorphous State Characteristics

2013 ◽  
Vol 2013 ◽  
pp. 1-15 ◽  
Author(s):  
Ritesh A. Fule ◽  
Tarique S. Meer ◽  
Ajay R. Sav ◽  
Purnima D. Amin
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Amorphous State ◽  
Polymer Melt ◽  
Aqueous Solubility ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Peg 400 ◽  
Hot Melt

This work studied artemether (ARTM) solid dispersion (SD) formulation using mixture of polymer excipient Soluplus, PEG 400, Lutrol F127, and Lutrol F68 melts at temperatures lower than the melting point of ARTM using a laboratory-size, single-screw rotating batch extruder. The effects of three surfactants PEG 400, Lutrol F127, and Lutrol F68 and parameters like mixing temperature, screw rotating speed, and residence time were systematically studied. SEM, XRD, and FT-IR were employed to investigate the evolution of ARTM’s dissolution into the molten excipient. Differential scanning calorimetry (DSC) was used to quantitatively study the melting enthalpy evolution of the drug. The results showed that the dissolution rate increased with increasing the ratio of polymer and surfactant to that of drug. It was concluded that the dissolution of the drug in the polymer melt is a convective diffusion process and that laminar distributive mixing can significantly enhance the dissolution rate. The aqueous solubility and dissolution rate of prepared solid dispersion were significantly enhanced. In vitro antimalarial studies revealed marked improvement in IC50 values. Thus hot-melt extrusion (HME) is a promising technology for improving solubility and dissolution profile of ARTM.

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