Improvement of the Pulmonary Absorption of (Asu1,7)-Eel Calcitonin by Various Protease Inhibitors in Rats

Pharmaceutical Research - Tập 11 Số 6 - Trang 909-913 - 1994
Morita, Takahiro1, Yamamoto, Akira2, Takakura, Yoshinobu1, Hashida, Mitsuru1, Sezaki, Hitoshi3
1Department of Basic Pharmaceutics, Faculty of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan
2Department of Biopharmaceutics, Kyoto Pharmaceutical University, Kyoto Japan
3Faculty of Pharmaceutical Sciences, Setsunan University, Hirakata, Osaka, Japan

Tóm tắt

The effects of protease inhibitors, Na-glycocholate, bacitracin, bestatin, nafamostat mesilate and soybean trypsin inhibitor (STI) on the pulmonary absorption of (Asu1,7)-eel calcitonin (ECT, molecular weight 3363) were investigated in rats. The pulmonary absorption of ECT was estimated by measuring its hypocalcemic effect. When ECT alone was administered into the lung, the pharmacological availability of ECT was 2.7%. Co-administration with STI or bestatin did not change the pharmacological effect of ECT. However, Na-glycocholate, bacitracin and nafamostat mesilate caused a significant hypocalcemic effect following the pulmonary absorption of ECT and a maximal effect was noted in the presence of 20 mM bacitracin, approaching the effect after intravenous administration of ECT. Bacitracin and Na-glycocholate reduced the degradation of 111In-ECT in rat lung homogenate. Therefore, protease inhibitors effectively improved the pulmonary absorption of ECT.

Từ khóa


Tài liệu tham khảo

citation_journal_title=Adv. Drug Delivery Rev.; citation_title=Penetration and enzymatic barriers to peptide and protein absorption; citation_author=V. H. L. Lee, A. Yamamoto; citation_volume=4; citation_publication_date=1990; citation_pages=171-207; citation_id=CR1

citation_journal_title=Int. J. Pharm.; citation_title=Effect of surfactants on the nasal absorption of insulin in rats; citation_author=S. Hirai, T. Yashiki, H. Mima; citation_volume=9; citation_publication_date=1981; citation_pages=165-172; citation_id=CR2

citation_journal_title=Res. Commun. Chem. Pathol. Pharmacol.; citation_title=Buccal absorption of insulin in the dog; citation_author=W. A. Ritschel, G. B. Ritschel, H. Forusz, M. Kraeling; citation_volume=63; citation_publication_date=1989; citation_pages=53-67; citation_id=CR3

citation_journal_title=J. Pharm. Pharmacol.; citation_title=Enhancement of rectal absorption of insulin using salicylates in dogs; citation_author=T. Nishihata, J. H. Rytting, A. Kamada, T. Higuchi, M. Routh, L. Caldwell; citation_volume=35; citation_publication_date=1983; citation_pages=148-151; citation_id=CR4

citation_journal_title=J. Pharmacol. Exp. Ther.; citation_title=The ocular route for systemic insulin delivery in the albino rabbit; citation_author=A. Yamamoto, A. M. Luo, S. Dodda-Kashi, V. H. L. Lee; citation_volume=249; citation_publication_date=1989; citation_pages=249-255; citation_id=CR5

citation_journal_title=J. Pharm. Sci.; citation_title=Vaginal absorption of a potent luteinizing hormone-releasing hormone analog (leuprolide) in rats I: Absorption by various routes and absorption enhancement; citation_author=H. Okada, I. Yamazaki, Y. Ogawa, S. Hirai, T. Yashiki, H. Mima; citation_volume=71; citation_publication_date=1982; citation_pages=1367-1371; citation_id=CR6

citation_journal_title=Int. J. Pharm.; citation_title=Bioavailability of leuprolide following intratracheal administration to beagle dogs; citation_author=A. Adjei, R. Doyle, M. Pratt, R. Finley, E. Johnson; citation_volume=61; citation_publication_date=1990; citation_pages=135-144; citation_id=CR7

citation_journal_title=J. Pharm. Pharmacol.; citation_title=Pulmonary absorption of aerosolised insulin in the rabbit; citation_author=A. L. Jones, I. W. Kellaway, G. Taylor; citation_volume=40S; citation_publication_date=1990; citation_pages=92P; citation_id=CR8

citation_journal_title=Pharm. Res.; citation_title=Pulmonary delivery of peptide drugs: Effect of particle size on bioavailability of leuprolide acetate in healthy male volunteers; citation_author=A. Adjei, J. Garren; citation_volume=7; citation_publication_date=1990; citation_pages=565-569; citation_id=CR9

citation_journal_title=Acta. Physiol. Scand.; citation_title=Permeability of the respiratory tract to different-sized macromolecules after intratracheal instillation in young and adult rats; citation_author=H. G. Folkesson, B. R. Westrom, B. W. Karlsson; citation_volume=139; citation_publication_date=1990; citation_pages=347-354; citation_id=CR10

citation_journal_title=Int. J. Pharm.; citation_title=Intratracheal delivery of insulin: Absorption from solution and aerosol by rat lung; citation_author=K. Okumura, S. Iwakawa, T. Yoshida, T. Seki, F. Komada; citation_volume=88; citation_publication_date=1992; citation_pages=63-73; citation_id=CR11

citation_journal_title=J. Pharm. Pharmacol.; citation_title=Absorption enhancement of intrapulmonary administered insulin by various absorption enhancers and protease inhibitors in rats; citation_author=A. Yamamoto, S. Umemori, S. Muranishi; citation_volume=46; citation_publication_date=1994; citation_pages=14-18; citation_id=CR12

citation_journal_title=Int. J. Appl. Isot.; citation_title=The preparation and labelling of DTPA-coupled albumin; citation_author=D. J. Hnatowich, W. W. Layne, R. L. Childs; citation_volume=33; citation_publication_date=1982; citation_pages=327-332; citation_id=CR13

citation_journal_title=Am. J. Physiol.; citation_title=Absorption of saccarides and urea from the rat lung; citation_author=S. J. Enna, L. S. Schanker; citation_volume=222; citation_publication_date=1972; citation_pages=409-414; citation_id=CR14

citation_journal_title=Biol. Pharm. Bull.; citation_title=Effects of various absorption promoters on pulmonary absorption of drugs with different molecular weight; citation_author=T. Morita, A. Yamamoto, M. Hashida, H. Sezaki; citation_volume=16; citation_publication_date=1993; citation_pages=259-262; citation_id=CR15

citation_journal_title=Int. J. Pharm.; citation_title=Effect of absorption enhancers for pulmonary absorption of fluorescein isothiocyanate dextrans with various molecular weights; citation_author=T. Ohtani, M. Murakami, A. Yamamoto, K. Takada, S. Muranishi; citation_volume=77; citation_publication_date=1991; citation_pages=141-150; citation_id=CR16

citation_journal_title=J. Pharm. Sci.; citation_title=Enhanced rectal absorption of (Asu1,7)-eel calcitonin in rats using polyacrylic acid aqueous gel base; citation_author=K. Morimoto, H. Akatsuchi, R. Aikawa, M. Morishita, K. Morisaka; citation_volume=73; citation_publication_date=1984; citation_pages=1366-1368; citation_id=CR17

citation_journal_title=Chem. Pharm. Bull.; citation_title=Percutaneous absorption of elcatonin and hypocalcemic effect in rat; citation_author=T. Ogiso, M. Iwaki, I. Yoneda, M. Horinouchi, K. Yamashita; citation_volume=39; citation_publication_date=1991; citation_pages=449-453; citation_id=CR18

citation_journal_title=Life Sci.; citation_title=Insulin and proinsulin proteolysis in mucosal homogenates of the albino rabbit: Implication in peptide delivery from nonoral routes; citation_author=A. Yamamoto, E. Hayakawa, V. H. L. Lee; citation_volume=47; citation_publication_date=1990; citation_pages=2465-2474; citation_id=CR19

citation_journal_title=Biochem. Biophys. Res. Commun.; citation_title=Bacitracin: an inhibitor of the insulin degrading activity of glutathione-insulin transhydrogenase; citation_author=R. A. Roth; citation_volume=98; citation_publication_date=1981; citation_pages=431-438; citation_id=CR20

citation_journal_title=Pharm. Res.; citation_title=The adjuvant effect of bacitracin on nasal absorption of gonadorelin and buserelin in rats; citation_author=S. C. Raehs, J. Sandow, K. Wirth, H. P. Merkle; citation_volume=5; citation_publication_date=1988; citation_pages=689-693; citation_id=CR21

citation_journal_title=Jap. J. Pharmacol.; citation_title=Pharmacological studies of FUT-175, nafamostat mesilate. 1. Inhibition of protease activity in in vitro and in vivo experiment; citation_author=T. Aoyama, Y. Ino, M. Ozeki, M. Oda, T. Sato, Y. Koshiyama, S. Suzuki, M. Fujita; citation_volume=35; citation_publication_date=1984; citation_pages=203-227; citation_id=CR22

citation_journal_title=Pharm. Res.; citation_title=Enhanced bioavailability of subcutaneously injected insulin by pretreatment with ointment containing protease inhibitors; citation_author=M. Takeyama, T. Ishida, N. Kokubu, F. Komada, S. Iwakawa, K. Okumura, R. Hori; citation_volume=8; citation_publication_date=1991; citation_pages=60-63; citation_id=CR23

Thông tin
Thông tin xuất bản

Pharmaceutical Research

Tập 11 Số 6

909-913

Thông tin tác giả