Processes for the preparation of delayed action and programmed release pharmaceutical forms and medicaments obtained thereby
Patent 5051262 Issued on September 24, 1991. Estimated Expiration Date: September 24, 2008. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
424/468, Sustained or differential release type424/469, Discrete particles in supporting matrix424/489Particulate form (e.g., powders, granules, beads, microcapsules, and pellets)
Specifically, the present invention relates to processes for preparing delayed action galenic forms. The process is characterized in that the application solutions of excipients, coatings and active constituents are adjusted to a desired pH. The independence of the rate of dissolution of a controlled release or sustained action oral pharmaceutical form is increased by admixing a pH adjusting agent with every application solution of medicament, excipeint or coating, throughout the course of formulation of the pharmaceutical form.
Other References
Ramsch, K. D., "Zur Pharmakokinetik von Nifedipin", S.M. 4, Heft 4:55-61 (1981)
Urquhart, J., "Controlled-Release Pharmaceuticals", APS Section of Pharmacology and Toxicology at the 27th National Meeting of the Academy of Pharmaceutical Sciences, Kansas City, MO (11/79)
Cabana, B. 37 Regulatory Consideration in Transdermal Controlled Medication", Drug Development and Industrial Pharmacy, 9(4), 707-724 (1983)
Kala and Dittgen, "In vitro and in vivo Availability of the Active Principles from Acrylic Polymer-Based Capsules", pp. 7-17
Imhof, Chem. Abstr. 85 #130521m "Pharmaceutical Preparations for Prophylactic and Therapeutic Treatment of Coronory Heart Disease"
Dittgen, Chem. Abstr. 85 #198123p "Preparation and in vitro Testing of Polyacrylate-Based Bead-Polymerizates Containing Pharmaceutically Active Ingredients"
Dittgen, Chem. Abst. 87 #189376n "Preparation an in vitro Testing of Polyacrylate-Based Polymers Containing . . . "
Dittgen, "Poliakrilate alapu gyogyszerhatoanyag-tartalmu gyongypolimerizatumok eloallitasa es in vitro vizsgalata", 20. evfolyam 7 szam
Vignon, et al., Chem. Abstr. 92 #82302m "Bioavailability of Indomethacin, Study of a Delayed-Release Formula"
Panoz, et al. Chem. Abstr. 93 #225639k "Oral Formulations with Programmed Action."
Volpi, et al., Chem. Abstr. 94 #36188x "Therapeutic Doses and Physicochemical Constants of Bases and Acids.
Kawata, et al. Chem. Abstr. 94 #127383y "Continuously Releasing Pharmaceutical Preparation of a Solid Drug Material"
Astier, et al., Chem. Abstr. 95 #225564y "Relative Bioavailability of a Sustained Release Indomethacin, Compared to Conventional Immediate Action Preparation"
Elan Reviews "Evaluation of Antibiotic Therapy, A New Perspective"(c. 1980)
Panoz, "Innovation and Creativity in the Design of New Pharmaceutical Disage Forms", 1981 Symposium
Corrigan, et al., "Development of a Controlled Absorption Quinidine Drug Delivery System", publ. Controlled Release Delivery Systems, Roseman & Mansdorf, (Chap. 12), pp. 163-167 (1983)
Evers, "Getting Drugs into your Bloodstream", publ. Technology Ireland, (Apr. 1982)
Elan Brochure, 2d Ed
Perucca, et al., "Pharmacokinetic and Pharmacodynamic Studies with a New Controlled-Release Formulation of Propranolol in Normal Volunteers: A Comparison with Other Commercially Available Formulations", B.J. Clin. Pharmac. 18 at 37-43 (1984)
Bottini, et al., "Comparative Oral Bioavailability of Conventional Propranolol Tablets and a New Controlled Absorption Propranolol Capsule", Drug Dev. and Ind. Pharm. 9(8) at 1475-1493 (1983)
Gibaldi, M.: Biopharmaceutics and Clinical Pharmacokinetics, Lea and Febiger, Philadelphia, 1977 (2nd Ed.)
Harris, P. A. and Riegelman, S.: J. Pharm. Sci., 58(1):71, 1969
Gibaldi, M., Boyes, R. N. and Feldman, S.: J. Pharm. Sci., 60(9): 1338, 1971
Scheline, R. R.: Pharmacol. Rev., 25(4):451, 1973
Conolly, M. E., Davies, D. S., Dollery, C. T., et al.: Br. J. Pharmac., 46:458, 1972
Brunk, S. F., and Delle, M.: Clin. Pharmacol. Ther., 16(1):51, 1974
Gibaldi, M. and Perrier, D.: Drug Metab. Rev., 3(2):185, 1974
Goldman, P.: N. Engl. J. Med., 289(12):623, 1973
Shand, D. G. and Rangno, R. E.: Pharmacol., 7:159, 1972
Paterson, J. W., Conolly, M. E., Dollery, C. T., Hayes, A. and Cooper, R. G.: Pharmacol. Clin., 2:127, 1970
Evans, G. H. and Shand, D. G.: Clin. Pharmacol. Ther., 14(4): 494, 1973
Nies, A. S. and Shand, D. G.: Circulation, 52:6, 1975
Regårdh, C. G., Borg, K. O., Johansson, R., Johansson, G., and Palmer, L.: J. Pharmacokin. Biopharm., 2(4):347, 1974
Gibaldi, M.: J. Pharm. Sci., 64(6):1036, 1975
Wilkinson, G. R. and Shand, D. G.: Clin. Pharmacol. Ther., 18(4):377, 1975
Woodcock, B. G., Loh, W., Habedank, W. and Rietbrock, N.: Clin. Pharmacol. Ther., 32(5):622, 1982
Assinder, D. F., Chasseaud, L. F., Hunter, J. O., Jung, R. J., and Taylor, T.: Arzneim Forsch./Drug Res., 27:156, 1977
Assinder, D. F., Chasseaud, L. F. and Taylor, T.: J. Pharm. Sci., 66(6):775, 1977
Zylber-Katz, E., Koren, G., Granit, L. and Levy, M.: Biopharm. Drug Dis., 5:109, 1984
Woodcock, B. G., Schulz, W., Kober, G. and Rietbrock, N.: Clin. Pharmacol. Ther., 30(1):52, 1981
Gilmore, I. T. and Hoffman, A. F.: Gastroenterology, 78(1):177, 1980
Ueda, C. T., Williamson, B. J. and Dzindzio, B. S.: Clin. Pharmacol. Ther., 20(3):260, 1978
Levy, G., Leonards, J. R., and Procknal, J. A.: J. Pharm. Sci., 54(12):1719, 1965
Nelson, E.: J. Am. Pharm. Assoc. (Sci. Ed.), XLVII(4):297, 1958
Juncher, H. and Raaschou, F.: AM&CT, IV(9):497, 1957
Anderson, K. W.: Arch. Int. Pharmacodyn., 147(1-2):171, 1964
Epstein, L. C. and Lasagna, L.: J. Pharmacol. Exp. Ther., 164(2):433, 1968
Hogben, C. A. M., Schanker, L. S., Tocco, D. J. et al.: J. Pharmacol. Exp. Ther., 120:540, 1957
Schanker, L. S.: J. Med. Pharm. Chem., 2(4):343, 1960
Hogben, C. A. M., Tocco, D. J., Brodie, B. B., et al.: J. Pharmacol. Exp. Ther., 125:275, 1959
Shore, P. A., Brodie, B. B., Hogben, C. A. M.: J. Pharmacol. Exp. Ther., 119:361, 1957
Travell, J.: J. Pharmacol. Exp. Ther., 69:21, 1940
Bradley, W. B., Schnedorf, J. G. and Ivey, A. C.: Am. J. Digest. Dis. & Nut., 3:415, 1936
Schanker, L. S., Tocco, D. J. Brodie, B. B., et al.: J. Pharmacol. Exp. Ther., 123:81, 1958
Levine, R. R.: Digest. Dis., 15(2):171, 1970
Truitt, E. B., Jr. and Morgan, A. M.: J. Pharm. Sci., 53(2):129, 1964
Barr, W. H., Adir. J. and Garrettson, L.: Clin. Pharmacol. Ther., 12(5): 779, 1971
Lim, C. C., Presbury, D. G. C. and Adamson, J.: Practitioner, 212:728, 1974
Manners, B. T. B., Grob, P. R. and Gibbs, J.: Brit. J. Clin. Practice, 26(3):129, 1972
Pines, A., Greenfield, J. S. B., Raafat, H., Sreedharan, K. S., Khaja, G. and Linsell, W. D.: Brit. J. Clin. Practice, 26(10):475, 1972
Perera, P. M.: Brit. J. Vener, Dis., 51:333, 1975
Lucas, C. R., Mugglestone, C. J. and Thomas D. R.: J. Int. Med. Res., 5:124, 1977
Corrigan, O. I., Dunne, A., McLaughlin, J. Geoghegan, E. J., Killian, C. A. and Panoz, D. E.: p. 163, Marcel Dekkler, Inc., New York and Basel, 1983
Siurala, M., et al.: Scand. J. Gastroent., 4:269, 1969
George, C. F.: Clin. Pharmacokin., 4:433, 1979
Chasseaud, L. F., Down, W. H. and Grundy R. K.: Europ. J. Clin. Pharmacol., 8:157, 1975
Smith, S. S. and Rawlins, M. D.: Variability in Human Drug Response, Butterworths and Co., London, 1975 (2nd Ed.)
George, C. F., Orme, M. L., Buranapong, P., Macerlean, D., Breckenridge, A. M. and Dollery, C. T.: J. Pharmacokin. Biopharm., 4(1):17, 1976
Davies, D. S., George, C. F., Blackwell, E., et al.: Br. J. Clin. Pharmac., 1:129, 1974
Gibaldi, M.: Biopharmaceutics and Clinical Pharmacokinetics.Lea and Febiger, Philadelphia, 1979 (1st Ed.)
September 24, 2008. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
