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

Pharmaceutical Research

Volumn 13, Issue 2, 1996, Pages 210-215

  Constantinides, Panayiotis P ^a,c   Welzel, Gus ^a   Ellens, Harma ^a   Smith, Philip L ^a   Sturgis, Sandra ^b   Yiv, Seang H ^b   Owen, Albert B ^b  

^a GLAXOSMITHKLINE   (United Kingdom)

^b Bio Pharm Drug Delivery Services   (United States)

^c ABBOTT LABORATORIES   (United States)

Author keywords

Calcein; Enhancer; Intestinal absorption; Medium chain fatty acids salts; Medium chain glycerides; w o microemulsions

Indexed keywords

CALCEIN; DECANOIC ACID; LAURIC ACID; MEDIUM CHAIN FATTY ACID; OCTANOIC ACID; PENETRATION ENHANCING AGENT; WATER OIL CREAM;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG FORMULATION; ENVIRONMENTAL TEMPERATURE; INTESTINE ABSORPTION; IONIC STRENGTH; NONHUMAN; ORAL DRUG ADMINISTRATION; PHASE TRANSITION; PRIORITY JOURNAL; RAT; TIME;

ANIMALS; CHEMISTRY, PHARMACEUTICAL; CHEMISTRY, PHYSICAL; DECANOIC ACIDS; EMULSIONS; FATTY ACIDS; FLUORESCEINS; INTESTINAL ABSORPTION; IONS; LAURIC ACIDS; MALE; OCTANOIC ACIDS; RATS; RATS, SPRAGUE-DAWLEY; SALTS; SOLUBILITY; WATER;

EID: 0030028851     PISSN: 07248741     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1016030812272     Document Type: Article

References (15)

1. P. P. Constantinides. Lipid microemulsions for improving drug dissolution and oral absorption: Physical and biopharmaceutical aspects. Pharm. Res. 12:1561-1572 (1995).
2. E. J. Van Hoogdalem, A. G. Boer and D. D. Breimer. Rectal absorption of rate-controlled delivered amphicillin sodium by sodium decanoate in conscious rats. Pharm. Weekbl. Sci. 10:76-79 (1988).
3. E. J. van Hoogdalem, M. A. Hardens, A. G. de Boer and D. D. Breimer. Absorption enhancement of rectally infused cefoxitin sodium by medium-chain fatty acids in conscious rats: concentration-effect relationship. Pharm. Res. 5:453-456 (1988).
4. M. Tomita, M. Shiga, M. Hayashi and S. Awazu. Enhancement of colonic drug absorption by the paracellular permeation route. Pharm. Res. 5:341-346 (1988).
5. P. P. Constantinides, J. P. Scalart, C. Lancaster, J. Marcello, G. Marks, H. Ellens and P. L. Smith. Formulation and intestinal absorption enhancement evaluation of water-in-oil microemulsions incorporating medium-chain glycerides. Pharm. Res. 11:1385-1390 (1994).
6. P. P. Constantinides, C. M. Lancaster, J. Marcello, D. Chiossone, D. Orner, I. Hidalgo, P. L. Smith, A. B. Sarkahian, S. H. Yiv and A. J. Owen. Enhanced intestinal absorption of an RGD peptide from water-in-oil microemulsions of different composition and particle size. J. Control. Rel. 34:109-116 (1995).
7. 2 in rats, dogs and monkeys. Life Sci. 47:29-36 (1990).
8. P. P. Constantinides and S. H. Yiv. Pharmaceutical emulsion compositions. PCT Publication WO 94/08610, 28 April 1994.
9. H. T. Davis. Factors determining emulsion type: hydrophile-lipophile balance and beyond. Colloids Surfaces A: Physicochem. Eng. Aspects 91:9-24 (1994).
10. G. J. Marks, G. Welzel, P. L. Smith, P. P. Constantinides and H. Ellens. Bioavailability enhancement of hydrophilic molecules by medium-chain glycerides in the rat. Proceed. Intern. Symp. Control. Rel. Bioact. Mater. 22:260-261 (1995).
11. M. Sekine, K. Sasahara, R. Okada and S. Awazu. Improvement of bioavailability of poorly absorbed drugs. IV. Mechanism of the promoting effect of medium-chain glyceride on the rectal absorption of water soluble drugs. J. Pharmacobio-Dyn. 8:645-652 (1985).
12. M. Tomita, M. Hayashi, T. Horie, T. Ishizawa and S. Awazu. Enhancement of colonic drug absorption by the transcellular permeation route. Pharm. Res. 5:786-789 (1988).
13. M. Tomita, T. Sawada, T. Ogawa, H. Ouchi, M. Hayashi and S. Awazu. Differences in the enhancing effects of sodium caprate on colonic and jejunal drug absorption. Pharm. Res. 9:648-653 (1992).
14. T. Sawada, T. Ogawa, M. Tomita, M. Hayashi and S. Awazu. Role of paracellular pathway in nonelectrolyte permeation across rat colon epithelium enhanced by sodium caprate and sodium caprylate. Pharm. Res. 8:1365-1371 (1991).
15. K. Takahashi, T. Murakami, R. Yumoto, T. Hattori, Y. Higashi and N. Yata. Decanoic acid induced enhancement of rectal absorption of hydrophilic compounds in rats. Pharm. Res. 11:1401-1404 (1994).