Enhancement of intestinal absorption of poorly absorbed hydrophilic compounds by simultaneous use of mucolytic agent and non-ionic surfactant

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 62, Issue 1, 2006, Pages 52-58

  Takatsuka, Shinya ^a   Kitazawa, Takeo ^a   Morita, Takahiro ^a   Horikiri, Yuji ^a   Yoshino, Hiroyuki ^a  

^a MITSUBISHI TANABE PHARMA CORPORATION   (Japan)

Author keywords

Intestinal absorption; Mucolytic agent; Non ionic surfactant; Penetration enhancer; Poorly absorbed hydrophilic compounds

Indexed keywords

ACETYLCYSTEINE; DECANOATE SODIUM; DODECYL SULFATE SODIUM; FLUORESCEIN ISOTHIOCYANATE DEXTRAN; MUCOLYTIC AGENT; NONIONIC SURFACTANT; TARTARIC ACID; TAURODEOXYCHOLIC ACID; TRITON X 100; TYLOXAPOL; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG ACTIVITY; DRUG BIOAVAILABILITY; HYDROPHILICITY; INTESTINE ABSORPTION; JEJUNUM; MALE; MOLECULAR WEIGHT; MUCOLYSIS; MUCOSA; NONHUMAN; RAT;

ACETYLCYSTEINE; ANIMALS; BIOLOGICAL AVAILABILITY; DECANOIC ACIDS; DEXTRANS; DRUG COMBINATIONS; DRUG SYNERGISM; EXPECTORANTS; FLUORESCEIN-5-ISOTHIOCYANATE; FLUORESCENT DYES; INTESTINAL ABSORPTION; INTESTINAL MUCOSA; JEJUNUM; MALE; OCTOXYNOL; RATS; RATS, WISTAR; SURFACE-ACTIVE AGENTS; TARTRATES;

EID: 28444456377     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejpb.2005.07.008     Document Type: Article

References (26)

1. M.M. Struck Biopharmaceutical R&D success rates and development times: a new analysis provides benchmarks for the future Bio/Technology 12 1994 674 677
2. G. Walsh Biopharmaceutical benchmarks - 2003 Nat. Biotechnol. 21 2003 865 870
3. P.A. Sayani, and Y.W. Chien Systemic delivery of peptides and proteins across absorptive mucosae Crit. Rev. Ther. Drug Carrier Syst. 13 1996 85 184
4. A. MacAdam The effect of gastro-intestinal mucus on drug absorption Adv. Drug Deliv. Rev. 11 1993 201 220
5. A. Wikman Larhed, P. Artursson, J. Gråsjö, and E. Björk Diffusion of drugs in native and purified gastrointestinal mucus J. Pharm. Sci. 86 1997 660 665
6. V.H.L. Lee, and A. Yamamoto Penetration and enzymatic barriers to peptide and protein absorption Adv. Drug Deliv. Rev. 4 1990 171 207
7. B.J. Aungst Intestinal permeation enhancers J. Pharm. Sci. 89 2000 429 442
8. A. Leone-Bay, D.R. Paton, B. Variano, H. Leipold, T. Rivera, J. Miura-Fraboni, R.A. Baughman, and N. Santiago Acylated non-α-amino acids as novel agents for the oral delivery of heparin sodium, USP J. Control. Release 50 1998 41 49
9. A. Bernkop-Schnürch The use of inhibitory agents to overcome the enzymatic barrier to perorally administered therapeutic peptides and proteins J. Control. Release 52 1998 1 16
10. Y. Iiboshi, R. Nezu, J. Khan, K. Chen, L. Cui, H. Yoshida, M. Wasa, M. Fukuzawa, S. Kamata, Y. Takagi, and A. Okada Developmental changes in distribution of the mucous gel layer and intestinal permeability in rat small intestine J. Parenter. Enteral. Nutr. 20 1996 406 411
11. A. Bernkop-Schnürch, and R. Fragner Investigations into the diffusion behaviour of polypeptides in native intestinal mucus with regard to their peroral administration Pharm. Sci. 2 1996 361 363
12. S. Michael, M. Thöle, R. Dillmann, A. Fahr, J. Drewe, and G. Fricker Improvement of intestinal peptide absorption by a synthetic bile acid derivative, cholylsarcosine Eur. J. Pharm. Sci. 10 2000 133 140
13. M. Miyamoto, H. Natsume, S. Iwata, K. Ohtake, M. Yamaguchi, D. Kobayashi, K. Sugibayashi, M. Yamashina, and Y. Morimoto Improved nasal absorption of drugs using poly-l-arginine: effects of concentration and molecular weight of poly-l-arginine on the nasal absorption of fluorescein isothiocyanate-dextran in rats Eur. J. Pharm. Biopharm. 52 2001 21 30
14. M. Tomita, M. Hayashi, and S. Awazu Absorption-enhancing mechanism of sodium caprate and decanoylcarnitine in Caco-2 cells J. Pharmacol. Exp. Ther. 272 1995 739 743
15. T. Lindmark, Y. Kimura, and P. Artursson Absorption enhancement through intracellular regulation of tight junction permeability by medium chain fatty acids in Caco-2 cells J. Pharmacol. Exp. Ther. 284 1998 362 369
16. A.C. Chao, J.V. Nguyen, M. Broughall, A. Griffin, J.A. Fix, and P.E. Daddona In vitro and in vivo evaluation of effects of sodium caprate on enteral peptide absorption and on mucosal morphology Int. J. Pharm. 191 1999 15 24
17. M. Hayashi, T. Sakai, Y. Hasegawa, T. Nishikawahara, H. Tomioka, A. Iida, N. Shimizu, M. Tomita, and S. Awazu Physiological mechanism for enhancement of paracellular drug transport J. Control. Release 62 1999 141 148
18. E.S. Swenson, and W. Curatolo Intestinal permeability enhancement for proteins, peptides, and other polar drugs: mechanisms and potential toxicity Adv. Drug Deliv. Rev. 8 1992 39 92
19. E.S. Swenson, W.B. Milisen, and W. Curatolo Intestinal permeability enhancement: efficacy, acute local toxicity, and reversibility Pharm. Res. 11 1994 1132 1142
20. E.K. Anderberg, C. Nyström, and P. Artursson Epithelial transport of drugs in cell culture. VII. Effects of pharmaceutical surfactant excipients and bile acids on transepithelial permeability in monolayers of human intestinal epithelial (Caco-2) cells J. Pharm. Sci. 81 1992 879 887
21. E.K. Anderberg, and P. Artursson Epithelial transport of drugs in cell culture. VIII. Effects of sodium dodecyl sulfate on cell membrane and tight junction permeability in human intestinal epithelial (Caco-2) cells J. Pharm. Sci. 82 1993 392 398
22. K.A. Walters, P.H. Dugard, and A.T. Florence Non-ionic surfactants and gastric mucosal transport of paraquat J. Pharm. Pharmacol. 33 1981 207 213
23. G.P. Martin, C. Marriott, and I.W. Kellaway Direct effect of bile salts and phospholipids on the physical properties of mucus Gut 19 1978 103 107
24. K. Ichikawa, I. Ohata, M. Mitomi, S. Kawamura, H. Maeno, and H. Kawata Rectal absorption of insulin suppositories in rabbits J. Pharm. Pharmacol. 32 1980 314 318
25. E.S. Swenson, W.B. Milisen, and W. Curatolo Intestinal permeability enhancement: structure-activity and structure-toxicity relationships for nonylphenoxypolyoxyethylene surfactant permeability enhancers Pharm. Res. 11 1994 1501 1504
26. W.J. Xia, and H. Onyuksel Mechanistic studies on surfactant-induced membrane permeability enhancement Pharm. Res. 17 2000 612 618