scholarly journals Design and Evaluation of Rapidly Disintegrating Tablets of Racecadotril with Enhanced in-vitro Dissolution Achieved by Solid Dispersion Technique

2013 ◽  
Vol 47 (3) ◽  
pp. 56-63 ◽  
Author(s):  
Gautam Singhvi ◽  
Gautham Gampa ◽  
Nilesh Yadav ◽  
Vipin Kumar ◽  
Ravi Ukawala
Keyword(s):  
Solid Dispersion ◽  
In Vitro Dissolution ◽  
Dispersion Technique

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 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

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.

Solubility enhancement of glipizide and development of its fast-dissolving oral film

2021 ◽  
Vol 16 ◽  
Author(s):  
Harshal Ashok Pawar ◽  
Mohd Saif Mohd Akram Momin
Keyword(s):  
Solid Dispersion ◽  
In Vitro Dissolution ◽  
Average Weight ◽  
Onset Of Action ◽  
Disintegration Time ◽  
Poorly Soluble ◽  
Dispersion Technique ◽  
Solvent Evaporation Process ◽  
Tablet Dosage

Background: Difficulty in swallowing tablet dosage form is common among all ages people, especially old and pediatrics. Fast dissolving oral films (FDOFs) may represent an innovative dosage type that settles the issue of gulping and supply fast onset of action. Objective: The objective of the present investigation was to increase the solubility of poorly soluble Glipizide (BCS Class II) by solid dispersion technique and develop its FDOFs. Methods: A solvent evaporation process was used to make a solid dispersion of the Glipizide. The saturation solubility of glipizide and its solid dispersion was determined in a different solvent. For the film preparation, solvent casting method was chosen. The excipients were selected based on pre-formulation data. The composition of the film was optimized based on a trial-and-error basis using different concentrations of plasticizer. The average weight, thickness, disintegration time, tensile strength, surface pH, folding endurance, drug content, and in-vitro dissolution analysis of the films were all taken into consideration. Results: There was no incompatibility between drug / solid dispersion and the excipients. The solid dispersion of the glipizide showed improved solubility by almost 10 folds. Many of the formulated films disintegrated in less than 30 seconds. At the end of 5 minutes, the optimized film had released more than 90% of the compound. The prepared films were found to be stable at room temperature. Conclusion: The solubility of Glipizide was improved successfully by solubilization technique using soluplus. The FDOFs of the glipizide were successfully formulated using pullulan as polymer.

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.

BEHAVIOURAL STUDY OF CYCLODEXTRIN INCLUSION COMPLEX ON ENHANCEMENT OF SOLUBILITY OF ACECLOFENAC

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (11) ◽  
pp. 19-23
Author(s):  
J Shaikh ◽  
◽  
S. V. Deshmane ◽  
R. N Purohit ◽  
K. R. Biyani
Keyword(s):  
Inclusion Complex ◽  
Solid Dispersion ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Phase Solubility ◽  
Solubility Study ◽  
Cyclodextrin Inclusion ◽  
Poorly Water Soluble ◽  
Cyclodextrin Inclusion Complex

The main objective of the present study was to enhance the solubility and dissolution rate of poorly water soluble aceclofenac using its solid dispersion with β-cyclodextrin. FTIR and DSC study was carried out to find out any incompatibility. The phase solubility of drug was carried out in 1, 2, 5, and 10% of β-cyclodextrin in distilled water. Kneading method and solvent evaporation method was use to prepared solid dispersion of aceclofenac and β-cyclodextrin. Different evaluation tests like solubility study in different solvents, PXRD and in vitro dissolution study of aceclofenac- β-cyclodextrin inclusion complex were carried out. The overall finding indicated that β-cyclodextrin is a desirable water soluble carrier, that helps in increasing solubility of drug. Due to its structural feature, β-cyclodextrin forms a good inclusion complex that decreases contact angle of drug with water molecules by increasing wetting properties. Hence, it can be concluded that, β-cyclodextrin is better water soluble carrier molecule in terms of its compatibility and increasing solubility behavior of poorly water soluble drug aceclofenac.

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.

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