Preparation and evaluation of oral solid heparin using emulsifier and adsorbent for in vitro and in vivo studies

International Journal of Pharmaceutics

Volumn 317, Issue 2, 2006, Pages 114-119

  Ito, Yukako ^a   Kusawake, Tomohiro ^a   Prasad, Y V Rama ^a   Sugioka, Nobuyuki ^a   Shibata, Nobuhito ^a   Takada, Kanji ^a  

^a KYOTO PHARMACEUTICAL UNIVERSITY   (Japan)

Author keywords

Absorption enhancement; Adsorbent; Labrasol; Low molecular weight heparin; Magnesium alminometa silicate; Microporous calcium silicate; Silicon dioxide

Indexed keywords

ADSORBENT; BLOOD CLOTTING FACTOR 10A; CALCIUM SILICATE; EMULSIFYING AGENT; EUDRAGIT; FLORITE; LABRASOL; LOW MOLECULAR WEIGHT HEPARIN; MAGNESIUM ALMINOMETA SILICATE; MAGNESIUM DERIVATIVE; NEUSILIN; PARNAPARIN; SILICON DIOXIDE; SURFACTANT; SYLYSIA; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; COMPARATIVE STUDY; CONTROLLED STUDY; DISPERSION; DOG; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CAPSULE; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG RELEASE; DRUG SCREENING; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME BLOOD LEVEL; IN VITRO STUDY; IN VIVO STUDY; MALE; NONHUMAN; POROSITY; PRIORITY JOURNAL; RAT; SOLID STATE;

ADMINISTRATION, ORAL; ADSORPTION; ANIMALS; ANTICOAGULANTS; CALCIUM COMPOUNDS; CAPSULES; CHEMISTRY, PHARMACEUTICAL; DOGS; EMULSIFYING AGENTS; HEPARIN, LOW-MOLECULAR-WEIGHT; INJECTIONS, INTRAVENOUS; JEJUNUM; MALE; ORGANIC CHEMICALS; PARTICLE SIZE; RATS; RATS, WISTAR; SILICATES; SOLUBILITY;

EID: 33745200966     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2006.02.056     Document Type: Article

References (22)

1. Ageno W. Treatment of venous thromboembolism. Thromb. Res. 97 (2000) V63-V72
2. Agnelli G., and Sonaglia F. Prevention of venous thromboembolism. Thromb. Res. 97 (2000) V49-V62
3. Amidon G.L., Lennernas H., Shah V.P., and Crison J.R. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res. 12 (1995) 413-420
4. Aungst B.J., and Saitoh H. Intestinal absorption barriers and transport mechanisms, including secretary transport, for a cyclic peptide, fibrinogen antagonist. Pharm. Res. 13 (1996) 114-119
5. Bianchini P., Bergonzini G.L., Parma B., and Osima B. Relationship between plasma antifactor Xa activity and the antithromtic activity of heparins of different molecular mass. Haemostasis 25 (1995) 288-298
6. Boneu B. Low molecular weight heparins: are they superior to unfractionated heparins to prevent and to treat deep vein thrombosis?. Thromb. Res. 100 (2000) V113-V120
7. Hashimoto K., Takada K., Nakayama T., and Shimizu M. Stabilization of the tight junction of the intestinal Caco-2-cell monolayer by milk whey proteins. Biosci. Biotech. Biochem. 59 (1995) 1951-1952
8. Hashimoto K., Nakayama T., and Shimizu M. Effect of β-lactoglobulin on the tight-junctional stability of Caco-2-SF monolayer. Biosci. Biotechnol. Biochem. 62 (1998) 1819-1821
9. Hirsh J., Dalen J.E., and Poller L. Heparin: mechanism of action, pharmacokinetics, dosing considerations, monitoring, efficacy and safety. Chest 4 (1992) 337s-351s
10. Hu Z., Tawa R., Konishi T., Shibata N., and Takada K. A novel emulsifier, Labrasol, enhances gastrointestinal absorption of gentamicin by inhibiting transporter. Life Sci. 69 (2001) 2899-2910
11. Ito Y., Arai H., Uchino K., Iwasaki K., Shibata N., and Takada K. Effect of adsorbents on the absorption of lansoprazole with surfactant. Int. J. Pharm. 289 (2005) 69-77
12. Ito Y., Kusawake T., Ishida M., Tawa R., Shibata N., and Takada K. Oral solid gentamicin preparation using emulsifier and adsorbent. J. Control. Rel. 105 (2005) 23-31
13. Kinoshita M., Baba K., Nagayasu A., Yamabe K., Shimooka T., Takeichi T., Azuma M., Houchi H., and Minakuchi K. Improvement of solubility and oral bioavailability of a poorly water-soluble drug, TAS-301, by its melt-adsorption on a porous calcium silicate. J. Pharm. Sci. 91 (2002) 362-370
14. Leone-Bay A., Paton D.R., Freeman J., Lercara C., O'Toole, Doris, Gschneidner D., Wang E., Harris E., Rosado C., Rivera T., and Baughman R.A. Synthesis and evaluation of compounds that facilitate the gastrointestinal absorption of heparin. J. Med. Chem. 41 (1998) 1163-1171
15. Nissan E.Z., Kidron M., Bar-On H., Friedman G., Hyam G., and Eldor A. Intestinal absorption of low molecular weight heparin in animals and human subjects. Haemostasis 30 (2000) 225-232
16. Prasad Y.V.R., Eaimtrakarn S., Ishida M., Kusawake Y., Tawa R., Yoshikawa Y., Shibata N., and Takada K. Evaluation of oral formulations of gentamicin containing Labrasol in beagle dogs. Int. J. Pharm. 268 (2003) 13-21
17. Prasad Y.V.R., Minamimoto T., Yoshikawa Y., Shibata N., Mori S., Matsumura A., and Takada A. In situ intestinal absorption studies on low molecular weight heparin in rats using Labrasol as absorption enhancer. Int. J. Pharm. 271 (2004) 225-232
18. Sha X., Yan G., Wu Y., Li J., and Fang X. Effect of self-microemulsifying drug delivery systems containing Labrasol on tight junctions in Caco-2 cells. Eur. J. Pharm. Sci. 24 (2005) 477-486
19. Shimizu M., Tsunogai M., and Arai S. Transepithelial transport of oligopeptides in the human intestinal cell, Caco-2. Peptides 18 (1997) 681-687
20. Swenson E.S., and Curatolo W.J. Means to enhance penetration (2) intestinal permeability enhancement for proteins, peptides and other drugs: mechanisms and potential toxicity. Adv. Drug Del. Rev. 8 (1992) 39-92
21. Takashima Y., Yuasa H., Kanaya Y., and Okada H. Application of a pharmaceutical excipient, porous calcium silicate, for preparing higher functional solid dosage forms. Pharm. Technol. Jpn. 19 (2003) 135-146
22. ® 934P. Pharm. Res. 18 (2001) 1638-1641