Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1994-01-27
2000-08-15
Webman, Edward J.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424487, 424501, A61K 922, A61K 916, A61K 4732
Patent
active
06103262&
ABSTRACT:
Pharmaceutical compositions having a modified release profile for once daily dosing of metronidazole, methods for making the pharmaceutical compositions, and methods for treating a microbial infection with once daily dosing of the pharmaceutical compositions of the invention are provided. The compositions given once daily exhibit substantial bioequivalence to immediate release metronidazole given three times per day. The compositions of the invention comprise:
(a) a first portion of metronidazole which is about 59 wt % to about 79 wt % metronidazole;
(b) about 1.5 wt % to about 3.0 wt % of an aqueous insoluble poly(meth)acrylic acid ester copolymer which is aqueous permeable, aqueous expandable and pH-independent;
(c) about 0.1 wt % to about 2.0 wt % detackifier;
(d) 0 to about 23 wt % of a first aqueous soluble pharmaceutical diluent;
(e) 0 to about 23 wt % of a second aqueous soluble diluent which is suitable for forming a pharmaceutical tablet when compressed with the granules of (a), the second aqueous soluble diluent being the same as or different from the first aqueous soluble diluent;
(f) 0 to about 20 wt % of a second portion of metronidazole;
(g) 0 to about 0.2 wt % glidant; and
(h) 0 to about 2 wt % lubricant;
wherein the composition comprises metronidazole containing granules comprising (a), (b), (c) and (d), wherein the sum of the weight percentages of metronidazole provided by (a) and (f) is between about 72 wt % and about 79 wt %, and wherein the sum of the weight percentages of the aqueous soluble diluent provided by (d) and (e) is between about 16 wt % and about 23 wt %.
REFERENCES:
patent: 2944061 (1960-07-01), Jacob et al.
patent: 4351825 (1982-09-01), Sothmann et al.
patent: 4892738 (1990-01-01), Takagishi et al.
patent: 4927639 (1990-05-01), Ghebre-Sellassie et al.
patent: 4954350 (1990-09-01), Jones et al.
Baichwal, M.R. et al., Indian Journal of Pharmaceutical Sciences 2, 48-51 (1980).
Braybrook, J.H. et al., Drug Design and Delivery 6, 73-86 (1990).
Chemtob, C. et al., Int. J. Pharm. 29, 1-7 (1986).
Chemtob, C. et al., Int. J. Pharm. 29, 83-92 (1986).
Chiba, N. et al., Am. J. of Gastroenterol. 87, 1716-1727 (1992).
Eudragit NE30D, "Application in the Production of Pharmaceutical Preparations" Info ED-I/e, Rohm Pharma Product Literature.
Eudragit NE30D, "Data Sheet" Info ED-2/e, Rohm Pharma Product Literature.
Eudragit NE30D, "Standard Sheet" Info ED-7/e, Rohm Pharma Product Literature.
Eudragit NE30D, "Technical Application Pamphlet" Info ED-11/e, Rohm Pharma Product Literature.
Eudragit NE30D, "Technical Application Pamphlet" Info ED-12/e, Rohm Pharma Product Literature.
Fauvelle, F. et al., Fundam. Clin. Pharmacol. 34, (4), 181 (1989).
Hentschel, E. et al., New England J. of Medicine 328, (5) 308-312 (1993).
Lugo-Miro, V. et al., JAMA 268, (1) 92-95 (1992).
Mandal, T.K. et al., Indian Drugs 23, (7) 400-403 (1986).
Read, N.W. et al., CRC Critical Reviews in Therapeutic Drug Carrier Systems 4, (3) 222-263 (1987).
Desai Subhash
Mancini Alan Mark
Schumann Steven Charles
G. D. Searle & Company
Webman Edward J.
LandOfFree
Modified-release metronidazole compositions and methods for maki does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Modified-release metronidazole compositions and methods for maki, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Modified-release metronidazole compositions and methods for maki will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2003818