Online citations, reference lists, and bibliographies.
← Back to Search

Enhancement Of Dissolution Of Glyburide By Solid Dispersion And Lyophilization Techniques

G. Betageri, K. R. Makarla
Published 1995 · Chemistry

Cite This
Download PDF
Analyze on Scholarcy
Share
Abstract Glyburide (GLY) is an oral hypoglycemic agent that is poorly soluble in water. The present study describes the preparation of solid dispersions and lyophilization of the dispersions designed to increase the solubility. Solid dispersions of GLY were prepared using polyethylene glycol 4000 (PEG 4000), PEG 6000 and a mixture of PEG 4000 and PEG 6000 (h1 mixture). The effect of melt and solvent methods of preparation of solid dispersion on dissolution behavior was also investigated. Dissolution studies indicated a significant increase in dissolution of GLY when dispersed in PEGs. Physical mixtures containing PEGs also showed improved dissolution of GLY as compared with that of pure drug, indicating the solubilizing effect of PEGs. Solid dispersions containing GLY/PEG 6000, 1:8, showed a 14-fold increase in dissolution after 60 min (D60) and another dispersion containing GLY/PEG 4000, 1:10, showed an 8-fold increase in the phosphate buffer system. The dispersion containing six parts of the PEG mixture (PEG 4000/PEG 6000, 1:1 mixture) showed a 12-fold increase in D60 as compared with pure drug. When multi-carrier solid dispersion containing six parts of mixture was prepared by the solvent method, the D60 value was about 2-fold that of the same dispersion prepared by the melt method. The dissolution of lyophilized solid dispersions further increased the dissolution of GLY significantly.
This paper references
10.1111/j.1749-6632.1960.tb49987.x
PRINCIPLES OF FREEZE‐DRYING
H. Meryman (1960)
10.1016/0378-5173(94)90094-9
Characterization and dissolution of fenofibrate solid dispersion systems
Sheu Ming-Thau (1994)
10.3109/03639049009115990
Improving Dissolution Rates of Griseofulivin by Deposition on Disintegrants
Stephen L. Law (1990)
10.1002/JPS.2600650929
Physical characterization and activity in vivo of polymorphic forms of 7-chloro-5, 11-dihydrodibenz[b, e][1, 4]oxazepine-5-carboxamide, a potential tricyclic antidepressant.
I. Gibbs (1976)
10.1016/0378-5173(92)90060-F
Characterization of solid dispersions of piroxicam/polyethylene glycol 4000
M. Fernandez (1992)
10.1248/CPB.26.3033
Dissolution behaviors and gastrointestinal absorption of phenytoin in phenytoin-polyvinylpyrrolidone coprecipitate.
H. Sekikawa (1978)
10.3109/03639048509056896
Mechanisms of Dissolution of Fast Release Solid Dispersions
O. Corrigan (1985)
10.1002/JPS.2600580503
Dissolution rates of high energy polyvinylpyrrolidone (PVP)-sulfathiazole coprecipitates.
A. Simonelli (1969)
10.1002/JPS.2600720614
Physical chemistry of freeze-drying: measurement of sublimation rates for frozen aqueous solutions by a microbalance technique.
M. J. Pikal (1983)
10.1248/CPB.27.1223
Dissolution mechanisms of drug-polyvinylpyrrolidone coprecipitates in aqueous solution.
H. Sekikawa (1979)
10.1016/0378-5173(93)90375-P
Solid dispersions of oxazepam
R. Jachowicz (1993)
10.3109/03639048609043486
Biopharmaceutical Study of Glybornuride-Polyethylene Glycol Systems
J. L. Vila-jato (1986)



This paper is referenced by
Dropping method as a new possibility in preparation of solid dispersions
Amir Bashiri-Shahroodi (2008)
10.1016/J.JDDST.2016.11.001
Controlled-release oral dosage forms containing nimodipine solid dispersion and hydrophilic carriers
Hyo-Jung Lee (2017)
10.1002/JPS.10590
Incorporation of lipophilic drugs in sugar glasses by lyophilization using a mixture of water and tertiary butyl alcohol as solvent.
D. V. van Drooge (2004)
10.1081/DDC-43918
Enhancement of Dissolution Rate of Valdecoxib Using Solid Dispersions with Polyethylene Glycol 4000
Chengsheng Liu (2005)
10.13188/2327-204x.1000025
Development of Controlled-Release Solid Dispersion Granules Containing a Poorly Water-Soluble Drug , Porous Calcium Silicate , and the Water-Soluble Polymer Polyvinylpyrrolidone
Yuko Uegaki (2018)
Techniques to improve the solubility of poorly soluble drugs
J. Patel (2012)
LYOPHILIZED GLICLAZIDE­POLOXAMER SOLID DISPERSIONS FOR ENHANCEMENT OF IN­ VITRO DISSOLUTION AND IN­VIVO BIOAVAILABILITY
F. Bandarkar (2011)
10.1211/jpp.61.12.0001
Review: physical chemistry of solid dispersions
Sandrien Janssens (2009)
Solid Dispersion: Methods and Polymers to increase the solubility of poorly soluble drugs.
Ladan Akbarpour Nikghalb (2012)
Enhancement of wettability and in vitro dissolution properties of lercanidipine hydrochloride by solid dispersion technique
Suneel Pandey (2012)
Studies on formulation development of a poorly water-soluble drug through solid dispersion technique
S. Dahiya (2010)
10.1002/JPS.10020
Improvement of dissolution and oral absorption of ER-34122, a poorly water-soluble dual 5-lipoxygenase/cyclooxygenase inhibitor with anti-inflammatory activity by preparing solid dispersion.
Ikuo Kushida (2002)
10.7324/JAPS.2016.60408
Development, Characterization and In Vitro Evaluation of Flurbiprofen Solid Dispersions using Polyethylene Glycols as Carrier -
B. Yadav (2016)
10.1080/17425247.2016.1198768
The role of the carrier in the formulation of pharmaceutical solid dispersions. Part I: crystalline and semi-crystalline carriers
Tu Van Duong (2016)
10.2147/IJN.S19151
Particle size reduction to the nanometer range: a promising approach to improve buccal absorption of poorly water-soluble drugs
Shasha Rao (2011)
10.1016/j.ijpharm.2008.05.003
High bioavailability from nebulized itraconazole nanoparticle dispersions with biocompatible stabilizers.
W. Yang (2008)
Solid Dispersion - A Strategy for Improving the Solubility of Poorly Soluble Drugs
Dixit Ak (2012)
10.1016/S0378-5173(00)00505-6
Physicochemical studies of lidocaine-menthol binary systems for enhanced membrane transport.
L. Kang (2000)
ANALYZE THE EFFECT OF POLYETHYLENE GLYCOL-6000 AND AVICEL ON POORLY WATER SOLUBLE DRUG ALBENDAZOLE BY SOLID DISPERSION METHOD
Md. Habibur Rahman (2008)
An Investigation on the Solid Dispersions of Chlordiazepoxide
A. Nokhodchi (2007)
10.3109/03639049609063230
Characterization of Glyburide-Polyethylene Glycol Solid Dispersions
G. Betageri (1996)
Functionality advancement of poorly soluble biovariable anti hypertensive Drug by sophisticated SD-FBP technology as per enhanced QbD.
A. Mukharya (2012)
10.1007/S11434-012-5094-2
Effects of drug-polymer dispersions on solubility and in vitro diffusion of artemisinin across a polydimethylsiloxane membrane
Y. Shahzad (2012)
SOLUBILITY ENHANCEMENT OF POORLY WATER SOLUBLE DRUGS BY SOLID DISPERSION
A. K. Chaturvedi (2012)
10.1155/2014/463895
Solubility and Bioavailability Enhancement of Poorly Aqueous Soluble Atorvastatin: In Vitro, Ex Vivo, and In Vivo Studies
Madhuri S. Rodde (2014)
10.2147/IJN.S194734
Engineering of solidified glyburide nanocrystals for tablet formulation via loading of carriers: downstream processing, characterization, and bioavailability
Hany S M Ali (2019)
10.22037/IJPR.2015.1725
Solid Dispersion Approach Improving Dissolution Rate of Stiripentol: a Novel Antiepileptic Drug
S. Afifi (2015)
LIQUISOLID SYSTEMS: SOLUBILITY ENHANCEMENT OF POOR SOLUBLE DRUGS
Nikhil B. Sinkar (2015)
Aripiprazole-Cyclodextrin Binary Systems for Dissolution Enhancement: Effect of Preparation Technique, Cyclodextrin Type and Molar Ratio
Shaimaa M. Badr-Eldin (2013)
10.4172/PHARMACEUTICAL-SCIENCES.1000279
Enhancement of the Solubility of Poorly Water Soluble Drugs through Solid Dispersion: A Comprehensive Review
G. Singh (2017)
10.1208/s12249-010-9441-9
Gliclazide Microcrystals Prepared by Two Methods of In Situ Micronization: Pharmacokinetic Studies in Diabetic and Normal Rats
R. Talari (2010)
10.1081/DDC-100104316
Enhancement of Dissolution of Ethopropazine Using Solid Dispersions Prepared with Phospholipid and/or Polyethylene Glycol
S. Prabhu (2001)
See more
Semantic Scholar Logo Some data provided by SemanticScholar