Literature DB >> 8592652

Lipid microemulsions for improving drug dissolution and oral absorption: physical and biopharmaceutical aspects.

P P Constantinides1.   

Abstract

PURPOSE: This review highlights the state-of-the-art in pharmaceutical microemulsions with emphasis on self-emulsifying systems, from both a physical and biopharmaceutical perspective. Although these systems have several pharmaceutical applications, this review is primarily focused on their potential for oral drug delivery and intestinal absorption improvement.
METHODS: Physicochemical characteristics and formulation design based on drug solubility and membrane permeability are discussed.
RESULTS: Case studies in which lipid microemulsions have successfully been used to improve drug solubilization/dissolution and/or intestinal absorption of poorly absorbed drugs/peptides are presented.
CONCLUSIONS: Drug development issues such as commercial viability, mechanisms involved, range of applicability, safety, scale-up and manufacture are outlined, and future research and development efforts to address these issues are discussed.

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Year:  1995        PMID: 8592652     DOI: 10.1023/a:1016268311867

Source DB:  PubMed          Journal:  Pharm Res        ISSN: 0724-8741            Impact factor:   4.200


  21 in total

1.  Improvement of peroral absorption of cyclosporine A by microemulsions.

Authors:  W A Ritschel; S Adolph; G B Ritschel; T Schroeder
Journal:  Methods Find Exp Clin Pharmacol       Date:  1990-03

2.  Insulin drug delivery systems: rectal gels.

Authors:  W A Ritschel; G B Ritschel; G Sathyan
Journal:  Res Commun Chem Pathol Pharmacol       Date:  1988-10

3.  Reduced inter- and intraindividual variability in cyclosporine pharmacokinetics from a microemulsion formulation.

Authors:  J M Kovarik; E A Mueller; J B van Bree; W Tetzloff; K Kutz
Journal:  J Pharm Sci       Date:  1994-03       Impact factor: 3.534

4.  Improved dose linearity of cyclosporine pharmacokinetics from a microemulsion formulation.

Authors:  E A Mueller; J M Kovarik; J B van Bree; W Tetzloff; J Grevel; K Kutz
Journal:  Pharm Res       Date:  1994-02       Impact factor: 4.200

Review 5.  The pharmacokinetics of Sandimmun Neoral: a new oral formulation of cyclosporine.

Authors:  D W Holt; E A Mueller; J M Kovarik; J B van Bree; K Kutz
Journal:  Transplant Proc       Date:  1994-10       Impact factor: 1.066

6.  Effect of medium-chain glycerides on physiological properties of rabbit intestinal epithelium in vitro.

Authors:  P Y Yeh; P L Smith; H Ellens
Journal:  Pharm Res       Date:  1994-08       Impact factor: 4.200

7.  A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability.

Authors:  G L Amidon; H Lennernäs; V P Shah; J R Crison
Journal:  Pharm Res       Date:  1995-03       Impact factor: 4.200

8.  Intestinal permeability enhancement: efficacy, acute local toxicity, and reversibility.

Authors:  E S Swenson; W B Milisen; W Curatolo
Journal:  Pharm Res       Date:  1994-08       Impact factor: 4.200

9.  Improvement of bioavailability of poorly absorbed drugs. II. Effect of medium chain glyceride base on the intestinal absorption of cefmetazole sodium in rats and dogs.

Authors:  M Sekine; H Terashima; K Sasahara; K Nishimura; R Okada; S Awazu
Journal:  J Pharmacobiodyn       Date:  1985-04

10.  Enteral, oral, and rectal absorption of ceftriaxone using glyceride enhancers.

Authors:  G Beskid; J Unowsky; C R Behl; J Siebelist; J L Tossounian; C M McGarry; N H Shah; R Cleeland
Journal:  Chemotherapy       Date:  1988       Impact factor: 2.544

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  100 in total

1.  Once-a-day oral dosing regimen of cyclosporin A: combined therapy of cyclosporin A premicroemulsion concentrates and enteric coated solid-state premicroemulsion concentrates.

Authors:  C K Kim; H J Shin; S G Yang; J H Kim; Y K Oh
Journal:  Pharm Res       Date:  2001-04       Impact factor: 4.200

2.  Controlled release of oral tetrahydrocurcumin from a novel self-emulsifying floating drug delivery system (SEFDDS).

Authors:  Saipin Setthacheewakul; Wichan Kedjinda; Duangkhae Maneenuan; Ruedeekorn Wiwattanapatapee
Journal:  AAPS PharmSciTech       Date:  2010-12-23       Impact factor: 3.246

3.  Water-in-oil microemulsions containing medium-chain fatty acids/salts: formulation and intestinal absorption enhancement evaluation.

Authors:  P P Constantinides; G Welzel; H Ellens; P L Smith; S Sturgis; S H Yiv; A B Owen
Journal:  Pharm Res       Date:  1996-02       Impact factor: 4.200

4.  Monitoring of in vitro fat digestion by electron paramagnetic resonance spectroscopy.

Authors:  Andrea Rübe; Sandra Klein; Karsten Mäder
Journal:  Pharm Res       Date:  2006-08-10       Impact factor: 4.200

5.  Mass transport properties of progesterone and estradiol in model microemulsion formulations.

Authors:  Laura M Land; Ping Li; Paul M Bummer
Journal:  Pharm Res       Date:  2006-08-23       Impact factor: 4.200

6.  Increasing the proportional content of surfactant (Cremophor EL) relative to lipid in self-emulsifying lipid-based formulations of danazol reduces oral bioavailability in beagle dogs.

Authors:  Jean F Cuiné; William N Charman; Colin W Pouton; Glenn A Edwards; Christopher J H Porter
Journal:  Pharm Res       Date:  2007-02-15       Impact factor: 4.200

7.  Preparation and in vivo evaluation of SMEDDS (self-microemulsifying drug delivery system) containing fenofibrate.

Authors:  Ashok R Patel; Pradeep R Vavia
Journal:  AAPS J       Date:  2007-10-26       Impact factor: 4.009

8.  Incorporation of antitubercular drug isoniazid in pharmaceutically accepted microemulsion: effect on microstructure and physical parameters.

Authors:  S K Mehta; Gurpreet Kaur; K K Bhasin
Journal:  Pharm Res       Date:  2007-06-19       Impact factor: 4.200

9.  Tween-embedded microemulsions--physicochemical and spectroscopic analysis for antitubercular drugs.

Authors:  S K Mehta; Gurpreet Kaur; K K Bhasin
Journal:  AAPS PharmSciTech       Date:  2010-01-20       Impact factor: 3.246

10.  Enhanced solubility and oral bioavailability of γ-tocotrienol using a self-emulsifying drug delivery system (SEDDS).

Authors:  Saeed Alqahtani; Alaadin Alayoubi; Sami Nazzal; Paul W Sylvester; Amal Kaddoumi
Journal:  Lipids       Date:  2014-06-17       Impact factor: 1.880

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