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

Interdependence Of Physiological Surfactant And Drug Particle Size On The Dissolution Behavior Of Water Insoluble Drugs.

S. Lin, J. Menig, L. Lachman
Published 1968 · Chemistry, Medicine

Save to my Library
Download PDF
Analyze on Scholarcy
Share
A series of in vitro experiments was performed to demonstrate the interdependence of physiologic surfactant and drug particle size on the dissolution rate of glutethimide, griseofulvin, and a new diuretic Compound A. The presence of physiological concentrations of lysolecithin (a naturally occurring biosurfactant) is shown to exhibit micellar solubilizing properties on the drugs investigated. The data obtained from the dissolution rate studies showed that aqueous lysolecithin solution caused significant enhancement of the extent of solution of the drugs investigated. However, the reduction of particle size through micronization may not necessarily increase the in vitro dissolution rate. Data to support this statement are presented, and a plausible explanation for its occurrence is the electrostatic charge that develops on the solids after milling. This results in aggregates which can be larger in particle size than the unmilled drug.
This paper references
10.1002/JPS.2600540503
Dissolution kinetics of certain crystalline forms of prednisolone.
D. Wurster (1965)
10.1016/0926-6542(63)90043-X
The behavior and solubility of monoglycerides in dilute, micellar bile-salt solution
A. Hofmann (1963)
10.1002/JPS.2600561123
Solubilization and rate of dissolution of drugs in the presence of physiologic concentrations of lysolecithin.
T. R. Bates (1967)
10.1021/JA01664A001
THE SOLUBILITY AND SURFACE ENERGY OF CALCIUM SULFATE
M. L. Dundon (1923)
10.1002/JPS.3030341239
The National Formulary
J. L. Powers (1945)
10.3891/ACTA.CHEM.SCAND.11-0749
Studies of the Phospholipids of Human Bile and Small Intestinal Contents.
B. Borgström (1957)
10.1038/193588A0
Effect of Particle Size on Blood Griseofulvin-Levels in Man
R. Atkinson (1962)
10.1042/BJ0770526
The estimation of phospholipase A activity in aqueous systems.
W. L. Magee (1960)
10.1021/JA01848A011
The Solubilization of Water-insoluble Dye in Dilute Solutions of Aqueous Detergents*
J. Mcbain (1941)
10.3891/ACTA.CHEM.SCAND.03-1179
On the Solubilization of Steroid Hormones by Association Colloids.
P. Ekwall (1949)
10.1002/JPS.2600500503
Comparison of dissolution and absorption rates of different commercial aspirin tablets.
G. Levy (1961)
10.1172/JCI104146
A LECITHINASE A IN DUODENAL CONTENTS OF MAN.
W. Vogel (1960)
10.3891/ACTA.CHEM.SCAND.14-1295
The Beginning Solubilization of 20-Methylcholanthrene in Aqueous Solutions of Conjugated and Unconjugated Bile Acid Salts. Bile Acids and Steroids. 79.
A. Norman (1960)
10.1038/169029A0
Enzymatic Formation of Glycerophosphorylcholine
B. Shapiro (1952)
10.1051/JCP/1904020245
Recherches sur la vitesse de dissolution des sels dans leurs solutions aqueuses
J. Schürr (1904)
10.1021/J150461A009
Studies on the aging of precipitates and coprecipitation; the solubility of lead chromate as a function of the particle size.
May Dr (1948)
10.3891/ACTA.CHEM.SCAND.02-0733
On the Solubilization of Carcinogenic Hydrocarbons by Association Colloids.
P. Ekwall (1948)
10.1530/ACTA.0.0040179
Aqueous solutions of steroid hormones.
P. Ekwall (1950)
10.3891/ACTA.CHEM.SCAND.05-1383
The Polarographic Determination of Ketosteroids Solubilized in Aqueous Solutions of Association Colloids.
P. Ekwall (1951)
10.1021/IE50392A004
Solubilization of Water-Insoluble Dye in Aqueous Solutions of Commercial Detergents
J. Mcbain (1942)
10.1016/s0015-6264(64)80465-x
Biochemical problems of lipids
C. E. Clark (1963)
10.1002/JPS.2600520815
DISSOLUTION BEHAVIOR OF CRYSTALLINE SOLVATED AND NONSOLVATED FORMS OF SOME PHARMACEUTICALS.
É. Shefter (1963)
10.1002/JPS.2600570331
Electrostatic characteristics of pharmaceutical solids and packaging materials I. Design of testing equipment and preliminary findings.
L. Lachman (1968)
Physicochemical properties of drugs that control absorption rate after subcutaneous implantation.
B. E. Ballard (1962)
10.1042/BJ0890057
THE FUNCTION OF BILE SALTS IN FAT ABSORPTION. THE SOLVENT PROPERTIES OF DILUTE MICELLAR SOLUTIONS OF CONJUGATED BILE SALTS
Hofmann Af (1963)
10.3891/ACTA.CHEM.SCAND.05-0175
Further Investigations on the Solubilization of Carcinogenic Hydrocarbons by Association Colloids.
P. Ekwall (1951)
10.1002/JPS.2600500502
Biopharmaceutics: absorption aspects.
J. Wagner (1961)
10.1111/j.2042-7158.1959.tb12562.x
The Physical Properties of Lysolecithin and Its Sols
N. Robinson (1959)
10.1002/JPS.2600550213
Solubilizing properties of bile salt solutions. I. Effect of temperature and bile salt concentration on solubilization of glutethimide, griseofulvin, and hexestrol.
T. R. Bates (1966)
10.5555/URI:PII:002221436190052X
Measurement of lecithinase A in serum and other body fluids.
L. Zieve (1961)
10.1038/1901106A0
Micellar Solubilization of Fatty Acids and Monoglycerides by Bile Salt Solutions
A. Hofmann (1961)



This paper is referenced by
A CRITICAL REVIEW ON DIFFERENT PHARMACEUTICAL ASPECTS OF SOLID DISPERSION TECHNIQUE FOR SOLUBILITY ENHANCEMENT
R. Gupta (2015)
10.4172/2329-9053.1000108
Novel Drug Delivery System: Liquid Solid Compacts
Manasa Gangotri Peddi (2013)
10.1002/JPS.2600650126
Effect of dioctyl sodium sulfosuccinate and poloxamer 188 on dissolution and intestinal absorption of sulfadiazine and sulfisoxazole in rats.
R. K. Reddy (1976)
Research Article Enhancement of Solubility and Dissolution Rate of Escitalopram Oxalate by Liquisolid Compact Technology
M. S. Kumbhar (2013)
Non Micronized Piroxicam-Liquid-Filled Dispersion (SEDDS) into Hard Gelatine Capsules: An Approach to Improve Dissolution and Stability of Piroxicam Formulation
S. Singh (2015)
10.1177/106002807000400106
Biopharmaceutics: 16. Rate of Dissolution Part I. Chronological Bibliography
J. G. Wagner (1970)
10.1002/JPS.2600590713
Dissolution of slightly soluble powders under sink conditions. I. Development of an apparatus and dissolution studies of salicylic acid powders.
I. Ullah (1970)
10.1016/S0928-0987(96)00256-4
Improvement of dissolution of poorly soluble drugs by solid deposition on a super disintegrant. II. The choice of super disintegrants and effect of granulation
G. Bolhuis (1997)
Formulation and Evaluation of Carvedilol Liquisolid Tablets
Burra Shashidher (2012)
10.3109/03639045.2011.650645
Formulation of ternary complexes of glyburide with hydroxypropyl-β-cyclodextrin and other solubilizing agents and their effect on release behavior of glyburide in aqueous and buffered media at different agitation speeds
S. Singh (2012)
10.1002/JPS.2600580918
A critical analysis of a capsule dissolution test.
R. J. Withey (1969)
10.1016/S0928-0987(00)00138-X
Direct estimation of the in vivo dissolution of spironolactone, in two particle size ranges, using the single-pass perfusion technique (Loc-I-Gut) in humans.
L. Bønløkke (2001)
10.3109/02652048809036721
Effect of surface active agents on drug release from polylactic acid-hydrocortisone microcapsules.
N. Leelarasamee (1988)
A SELF-MICROEMULSIFYING DRUG DELIVERY SYSTEM (SMEDDS)
Maulik J. Patel (2010)
10.1016/J.IJPHARM.2007.03.034
Liquisolid technique for dissolution rate enhancement of a high dose water-insoluble drug (carbamazepine).
Y. Javadzadeh (2007)
10.1002/9780470921920.EDM066
The Impact of Solubility and Dissolution Assessment on Formulation Strategy and Implications for Oral Drug Disposition
J. Alsenz (2012)
10.1016/J.EJPB.2007.06.011
Cogrinding enhances the oral bioavailability of EMD 57033, a poorly water soluble drug, in dogs.
M. Vogt (2008)
10.1517/17425247.2011.548801
Drug release from liquisolid systems: speed it up, slow it down
A. Nokhodchi (2011)
10.1016/S0378-5173(00)00602-5
Wetting characteristics of media emulating gastric fluids.
P. Luner (2001)
Design and Development of Fast Dissolving Tablets of Felodipine Using Different Methods
Vinayak Bavikar Jagdishchandra (2012)
10.1007/BF00779223
Drugs in solid gelatin capsules (review)
L. N. Berezovskaya (2004)
10.1080/03639040701542291
Interactive Mixture as a Rapid Drug Delivery System
C. Lee (2008)
Solubility improvement by solid dispersion and their characterization : indomethacin and phenytoin
V. Sridhar (2013)
10.1002/9780470711415.CH4
Solubility Parameters for Prediction of Drug/Polymer Miscibility in Hot‐Melt Extruded Formulations
A. Gryczke (2012)
10.1080/03639040802277672
Effect of Some Commercial Grades of Microcrystalline Cellulose on Flowability, Compressibility, and Dissolution Profile of Piroxicam Liquisolid Compacts
Y. Javadzadeh (2009)
LIQUISOLID COMPACT: A NEW TECHNIQUE FOR ENHANCEMENT OF DRUG DISSOLUTION
Sahil M. Gavali (2011)
10.1111/j.2042-7158.1975.tb09419.x
The solubilization of some local anaesthetic esters of p‐aminobenzoic acid by lysophosphatidylcholine
M. J. Hunt (1975)
10.1002/JPS.2600610918
Use of adsorbents in enhancement of drug dissolution. II.
D. Monkhouse (1972)
10.3109/03639048409038307
Effect of Particle Size and Excipients on the Dissolution Rate of Metronidazole from Solid Dosage Forms: II
J. A. Lauwo (1984)
10.4333/KPS.2004.34.4.289
Effect of Types and Mixing Ratios of Water-Soluble Polymers on In Vitro Release Profile of Sold Dispersion for Acyclovir
Yong-San Ahn (2004)
10.1016/S0065-7743(08)60667-3
Chapter 27. Pharmaceutics, Pharmacokinetics and Biopharmaceutics
O. E. Araujo (1969)
10.1002/JPS.2600740309
Surfactant effect on the dissolution of sulfanilamide granules.
P. Heng (1985)
See more
Semantic Scholar Logo Some data provided by SemanticScholar