← Back to Search
Design And Characterization Of A Submicronized O/w Emulsion Of Diazepam For Parenteral Use
M. Y. Levy, S. Benita
Published 1989 · Chemistry
Download PDFAnalyze on Scholarcy
Abstract An innovative, injectable, submicronized emulsion delivery system into which diazepam was incorporated has been developed. This emulsion has been formulated to meet all the requirements for injection either i.v. or i.m. The technique utilized a high shear mixer followed by a two stage pressure homogenizer yielding a very fine monodispersed emulsion, the mean droplet size of which ranged from 100 to 150 nm. The combination of purified egg yolk phospholipid and non-ionic emulsifier, as a complex emulgator, together with a highly efficient emulsification technique yielded a fine diazepam emulsion with improved stability properties. An increase in the oil phase volume ratio caused a moderate but significant increase in the mean droplet size of the diazepam emulsion. A sharp and parallel elevation in mean droplet size and viscosity was observed in the emulsions containing 30% or more oily phase. The ζ-potential of the emulsified droplets was affected by the alteration of the pH, whereas no significant effect on mean droplet size was observed. The mean droplet size of diazepam emulsion decreased with increasing concentrations of the non-ionic emulsifier until reaching a minimum constant value. Mean droplet size of diazepam emulsion decreased, while ζ-potential increased with increasing phospholipid concentration. No changes in the various physicochemical properties were observed with increasing diazepam concentration.
This paper references
Thrombophlebitis with diazepam used intravenously.
D. Langdon (1973)
Local Discomfort and Thrombophlebitis Following Intravenous Injection of Diazepam
D. Selander (1981)
Precipitation of diazepam from intravenous preparations.
W. Jusko (1973)
Effect of Homogenization Conditions on the Physicochemical Properties of Emulsion Bases
A. Takamura (1983)
Fat emulsion as a vehicle for diazepam. A study of 9492 patients.
O. von Dardel (1983)
Stability of a fat emulsion based intravenous feeding mixture
W. R. Burnham (1982)
The stability of fat emulsions for intravenous administration
S. Davis (1983)
HYPERSENSITIVITY TO INTRAVENOUS ANAESTHETIC AGENTS
J. Dundee (1976)
Poloxamer 188 as vehicle for injectable diazepam.
A. Prancan (1980)
RESEARCH AND REPORTS:STUDIES ON FAT EMULSIONS IN COMBINED NUTRITION SOLUTIONS
S. Davis (1986)
Pluronic surfactants affecting diazepam solubility, compatibility, and adsorption from i.v. admixture solutions.
S. Lin (1987)
Diazepam in Emulsion Form for Intravenous Usage
Otto VonDardel (1976)
Physostigmine emulsion: a new injectable controlled release delivery system
S. Benita (1986)
The function of phospholipids of soybean lecithin in emulsions
L. Rydhag (1981)
The influence of the route of administration on the clinical action of diazepam
R. Assaf (1975)
Role of diazepam in the management of eclampsia.
A Study of Intravenous Emulsion Compatibility: Effects of Dextrose, Amino Acids, and Selected Electrolytes
Curtis D. Black (1981)
Venous complications after i.v. administration of Diazemuls (diazepam) and Dormicum (midazolam).
S. Jensen (1981)
Incompatibility of diazepam injection in plastic intravenous bags.
W. Parker (1979)
The ultrastrucutre of lipid particles in emulsions prepared with various emulsifiers.
R. Jeppsson (1974)
Parenteral Use of Diazepam in an Emulsion Formulation. A Clinical Study
A. Thorn-Alquist (1977)
The preparation and properties of sterile intravenous emulsions.
Hansrani Pk (1983)
Parenteral emulsions as drug carrier systems.
M. Singh (1986)
THE EFFECT OF ADDITIVES ON THE PHYSICAL PROPERTIES OF A PHOSPHOLIPID‐STABILIZED SOYBEAN OIL EMULSION
C. Kawilarang (1980)
Reduction of venous sequelae of i.v. diazepam with a fat emulsion as solvent.
M. Mattila (1981)
The benzodiazepines. A review of their actions and uses relative to anaesthetic practice.
J. Dundee (1970)
Membrane models with phospholipids.
A. Bangham (1968)
Use of diazepam in treatment of severe convulsive status epilepticus.
M. Parsonage (1967)
Availability of diazepam from plastic containers.
J. Cloyd (1980)
Diazepam Infusion in the Treatment of Tetanus
J. Tehrani (1977)
ADVERSE REACTIONS TO INTRAVENOUS ANAESTHETICS: A Survey of 100 Reports
R. S. Clarke (1975)
Polyethylene glycol as a solvent for diazepam: bioavailability and clinical effects after intramuscular administration, comparison of oral, intramuscular and rectal administration, and precipitation from intravenous solutions.
K. Korttila (1976)
Local reactions to i.v. diazepam in three different formulations.
A. Schou Olesen (1980)
The particle size distribution of emulsions containing diazepam for intravenous use
R. Jeppsson (1976)
Fat emulsions. Effect of polyoxyethylene and alkyl content of emulsifiers on stability to sterilization
W. Singleton (1958)
Surface properties of acidic phospholipids: interaction of monolayers and hydrated liquid crystals with uni- and bi-valent metal ions.
D. Papahadjopoulos (1968)
This paper is referenced by
Drug release from submicronized o/w emulsion: a new in vitro kinetic evaluation model
M. Y. Levy (1990)
UNIVERZA V LJUBLJANI FAKULTETA ZA FARMACIJO URŠKA TREIBER UPORABNOST DIFERENČNE DINAMIČNE KALORIMETRIJE ZA DOLOČANJE KONCENTRACIJE UČINKOVINE V LIPIDNIH NANODELCIH APPLICABILITY OF DIFFERENTIAL SCANNING CALORIMETRY FOR THE DETERMINATION OF DRUG CONCENTRATION IN LIPID NANOPARTICLES
UNIVERZA V LJUBLJANI (2014)
Lipid & surfactant based systems for improved delivery of poorly soluble APIs
Sri Satyasai Nagendra Babu Punyamurthula (2015)
Solid Lipid Nanoparticles: Concepts, Procedures, and Physicochemical Aspects
K. Mäder (2005)
Preformulation as an Aid to Product Design in Early Drug Development
G. Steele (2016)
A method for the preparation of submicron particles of sparingly water-soluble drugs by precipitation in oil-in-water emulsions. I: Influence of emulsification and surfactant concentration.
B. Sjoestroem (1993)
Oil-in-water lipid emulsions: implications for parenteral and ocular delivering systems.
S. Tamilvanan (2004)
Unexplored Areas and New Findings in Lipid Emulsion Serving as a Potential Drug Carrier for Lipophilic Drugs: A Review
Dixha Angare (2012)
Hydroxypropylmethylcellulose (HPMC) as emulsifier for submicron emulsions: influence of molecular weight and substitution type on the droplet size after high-pressure homogenization.
M. Schulz (2000)
Characterization of submicrometer emulsions using sedimentation field-flow fractionation with power field programming
Shulamit Levin (1994)
Efficacy Evaluation of a Novel Submicron Miconazole Emulsion in a Murine Cryptococcosis Model
M. Y. Levy (2004)
Naproxen incorporated lipid emulsions. I. Formulation and stability studies
S. Nasirideen (1998)
The influence of customized geometries and process parameters on nanoemulsion and solid lipid nanoparticle production in microsystems
J. H. Finke (2012)
Solid lipid nanoparticles: production, characterization and applications.
W. Mehnert (2001)
Sequential statistical optimization of a positively-charged submicron emulsion of miconazole.
P. Wehrlé (1996)
Evidence for Phospholipid Bilayer Formation in Solid Lipid Nanoparticles Formulated with Phospholipid and Triglyceride
H. Heiati (2004)
Colloidal carriers for benzathine penicillin G: nanoemulsions and nanocapsules.
N. Santos-Magalhães (2000)
Development of a Novel Parenteral Formulation for Tetrazepam Using a Lipid Emulsion
M. Jumaa (2001)
Development of positively charged colloidal drug carriers: Chitosan-coated polyester nanocapsules and submicron-emulsions
P. Calvo (1997)
A new in vitro technique for the evaluation of drug release profile from colloidal carriers - ultrafiltration technique at low pressure
B. Magenheim (1993)
Top ten considerations in the development of parenteral emulsions.
Injectable Lipid Emulsions—Advancements, Opportunities and Challenges
Ketan Hippalgaonkar (2010)
The influence of alkali fatty acids on the properties and the stability of parenteral O/W emulsions modified with solutol HS 15.
K. Buszello (2000)
Mixture experiments with the oil phase of parenteral emulsions.
M. Jumaa (1998)
Microsystems for Emulsification
H. Bunjes (2016)
Development of nanoemulsion for efficient brain parenteral delivery of cefuroxime: designs, characterizations, and pharmacokinetics
Siti Norhawani Harun (2018)
Microencapsulation of lipid nanoparticles containing lipophilic drug
K. E. Lee (2003)
Ocular Disposition of the Hemiglutarate Ester Prodrug of ∆9-Tetrahydrocannabinol from Various Ophthalmic Formulations
Tushar Hingorani (2013)
Cefpodoxime-proxetil protection from intestinal lumen hydrolysis by oil-in-water submicron emulsions
S. Crauste-Manciet (1998)
A submicron emulsion of HU-211, a synthetic cannabinoid, reduces intraocular pressure in rabbits
N. Naveh (2000)
Development of intravenous lipid emulsion of tanshinone IIA and evaluation of its anti-hepatoma activity in vitro.
T. Chu (2012)
Comparative effects of different cosurfactants on sterile prednisolone acetate ocular submicron emulsions stability and release.
Shaimaa S Ibrahim (2009)See more