Novel peroral dosage forms with protease inhibitol-γ activities. II. Design of fast dissolving poly(acrylate) and controlled drug-releasing capsule formulations with trypsin inhibiting properties

International Journal of Pharmaceutics

Volumn 138, Issue 1, 1996, Pages 13-23

  Akiyama, Yohko ^a   Lueßen, Henrik L ^b   De Boer, A G ^b   Verhoef, J Coos ^b   Junginger, Hans E ^b  

^a TAKEDA PHARMACEUTICAL COMPANY LIMITED   (Japan)

^b LEIDEN UNIVERSITY   (Netherlands)

Author keywords

Carbopol 934P; Freeze dreid sodium Carbopol 934P; Peptide drug delivery; Peroral solid dosage form; Poly(acrylic acid) derivatives; Polyglycerol ester of fatty acid (PGEF); Trypsin inhibition

Indexed keywords

BENZOYLARGININE ETHYL ESTER; CARBOMER; POLYACRYLIC ACID; TRYPSIN;

ARTICLE; DISPERSION; DISSOLUTION; DRUG CAPSULE; DRUG DEGRADATION; DRUG DELIVERY SYSTEM; DRUG DOSAGE FORM; DRUG FORMULATION; DRUG RELEASE; DRUG STABILITY; ENZYME INHIBITION; PRIORITY JOURNAL;

EID: 0030581138     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/0378-5173(96)04504-8     Document Type: Article

References (27)

1. Akiyama, Y., Lueßen, H.L., De Boer, A.G., Verhoef, J.C. and Junginger, H.E., Novel peroral dosage forms with protease inhibitory activities. I. Design of capsules with fast drug-releasing properties. Int. J. Pharm., 136 (1996) 155-163.
2. Akiyama, Y., Nagahara, N., Hirai, S. and Toguchi, H., In vitro and in vivo evaluation of mucoadhesive microspheres prepared for the gastrointestinal tract using polyglycerol esters of fatty acids. Pharm. Res., 12 (1995) 397-405.
3. Bartunik, H.D., Summers, L.J. and Bartsch, H.H., Crystal structure of bovine ß-trypsin at 1.5 Å resolution in a crystal form with low molecular packing density: active site geometry, ion pairs and solvent structure. J. Mol. Biol.. 210 (1989) 813-828.
4. Constantinides, P.P., Scarlet, J.-P., Lancaster, C., Marcello, J., Marks, G., Ellens, H. and Smith, P.L., Formulation and intestinal absorption enhancement evaluation of water-in-oil microemulsions incorporating medium-chain glyceride. Pharm. Res., 11 (1994) 1385-1390.
5. Davis, S.S., Hardy, J.G. and Fara, J.W., The transit of pharmaceutical dosage forms through the small intestine. Gut, 27 (1986) 886-892.
6. 2+ to trypsinogen and its relation to the mechanism of activation. Biochem. Biophys. Res. Commun., 28 (1967) 390-394.
7. Drewe, J., Meier, R., Vonderscher, J., Kiss, D., Posanski, U., Kissel, T. and Gyr, K., Enhancement of the oral absorption of cyclosporin in man. Br. J. Clin. Pharmacol., 34 (1992) 60-64.
8. Fukunaga, M., Miller, M.M. and Deftos, L.J., Liposome entrapped calcitonin and parathyroid hormone are orally effective in rats. Horm. Metab. Res., 23 (1991) 166-167.
9. Foster, S.N.E., Pearson, J.P., Hutton. D.A., Allen, A. and Dettmar, W., Interaction of polyacrylate with porcine pepsin and the gastric mucous barrier: a mechanism for mucosal protection. Clin. Sci., 87 (1994) 719-726.
10. Gabel, D. and Kasche, V., Autolysis of ß-trypsin. Acta Chem. Scand., 27 (1973) 1971-1981.
11. Hashizume, M., Douen, T., Murakami, M., Yamamoto, A., Takada, K. and Muranishi, S., Improvement of large intestinal absorption of insulin by chemical modification with palmitic acid in rats. J. Pharm. Pharmacol., 44 (1992) 555-559.
12. Hutton, D.A., Pearson, J.P., Allen, A. and Foster, S.N.E., Mucolytic activity of the colonic mucus barrier by fecal proteinases: inhibition by interacting poly(acrylate). Clin. Sci., 78 (1990) 265-271.
13. Kompella, U.B. and Lee, V.H.L., Delivery systems for penetration enhancement of peptide and protein drugs: design considerations. Adv. Drug Deliv. Rev., 8 (1992) 115-162.
14. Lee, V.H.L., Dodda-Kashi, S. and Rubas, W., Oral route of peptide and protein drug delivery. In Lee, V.H.L. (Ed.), Peptide and Protein Drug Delivery, Marcel Dekker, New York, 1991, pp. 691-718.
15. Lehr, C.-M., Bouwstra, J.A., Kok, W., De Boer, A.G., Tukker, J.J. and Junginger, H.E., Intestinal transit of bioadhesive microspheres in an in situ loop in the rat. -A comparative study with copolymers and blends based on poly(acrylic acid). J. Control. Rel., 13 (1990) 51-62.
16. Lehr, C.-M., Bouwstra, J.A., Kok, W., De Boer, A.G., Tukker, J.J., Verhoef, J.C., Breimer, D.D. and Junginger, H.E., Effects of the mucoadhesive polymer polycarbophil on the intestinal absorption of a peptide drug in the rat. J. Pharm. Pharmacol., 44 (1992) 402-407.
17. Leung, S.S., Nagai, T. and Machida, Y., Mucoadhesive dosage forms for peptide and protein drug delivery. In Lee, V.H.L. (Ed.), Peptide and Protein Drug Delivery, Marcel Dekker, New York, 1991, pp. 741-767.
18. Longer, M.A., Ch'ng, H.S. and Robinson, J.R., Bioadhesive polymers as platforms for oral controlled drug delivery III: Oral delivery of chlorothiazide using a bioadhesive polymer. J. Pharm. Sci., 74 (1985) 406-411.
19. Lueßen, H.L., De Leeuw, B.J., Pérard, D., Lehr, C.-M, De Boer, A.G., Verhoef, J.C. and Junginger, H.E., Mucoadhesive polymers in peroral peptide drug delivery. I. Influence of mucoadhesive excipients on the proteolytic activity of intestinal enzymes. Eur. J. Pharm. Sci., 4 (1996) 117-128.
20. Lueßen, H.L., Lehr, C.-M., Rentel, C.-O., Noach, A.B.J., De Boer, A.G., Verhoef, J.C. and Junginger, H.E., Bioadhesive polymers for the peroral delivery of peptide drugs. J. Control. Rel., 29 (1994) 329-338.
21. Lueßen, H.L., Verhoef, J.C., Borchard, G., Lehr, C.-M., De Boer, A.G. and Junginger, H.E., Mucoadhesive polymers in peroral peptide drug delivery. II. Carbomer and polycarbophil are potent inhibitors of the intestinal proteolytic enzyme trypsin. Pharm. Res., 12 (1995) 1293-1298.
22. Lundin, S. and Vilhardt, H., Absorption of 1-deamino-8-D-arginine vasopressin from different regions of the gastrointestinal tract in rabbits. Acta Endocrinol., 112 (1986) 457-460.
23. Michel, C., Aprahamian, M., Defontaine, L., Couvreur, P. and Damgé, C., The effect of site of administration in the gastrointestinal tract on the absorption of insulin from nanocapsules in diabetic rats. J. Pharm. Pharmacol., 43 (1991) 1-5.
24. Rubinstein, A., Tirosh, B., Baluom, M., Nassar, T., David, A., Radai, R., Gliko-Kabir, I. and Friedman, M., The rationale for peptide drug delivery to the colon and the potential of polymeric carriers as effective tools. J. Control. Rel., in press.
25. Saffran, M., Kumar, G.S., Schavariar, C., Burnham, J.C., William, F. and Neckers, D.C., A new approach to the oral administration of insulin and other peptide drugs. Science, 233 (1986) 1081-1084.
26. Touitou, E., Enhancement of intestinal peptide absorption. J. Control. Rel., 21 (1992) 139-144.
27. Zhou, X.H., Overcoming enzymatic and absorption barriers to non-parenterally administered protein and peptide drugs. J. Control. Rel., 29 (1994) 239-252.