Prodrug compositions

Details Prodrug compositions Prodrug compositions

1993-02-22

1996-03-12

Springer, David B.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546272, 546281, 546341, 548536, 560143, 562887, C07D20926

Patent

active

054987296

ABSTRACT:
Compositions degrading by hydrolysis to release a bioactive compound having carboxylic acid moieties, which are organic acid anhydrides having the following formula: ##STR1## wherein R' is a residue of a therapeutic bioactive compound, for example, a non-steroidal anti-inflammatory agent; a penicillin or cephalosporin antibiotic; or bioactive compounds for non-therapeutic use, for example, herbicides, insecticides, fungicides, antimicrobials, pesticides, pheromones, and fertilizers; m is an integer of between 1 and 3; and R is a carrier. The resulting mixed anhydrides are characterized by having between one and three drug molecules attached to a single carrier molecule. The prodrugs are highly susceptibility to hydrolytic degradation in a predictable and controlled fashion, have variable solubilities in water and lipids, with increased biomembrane transport, elicit a bio-affecting/pharmacological response, and are less irritating to topical and gastric or intestinal mucosal membranes.

REFERENCES:
patent: 2236125 (1941-03-01), Wiezevich
patent: 2423569 (1947-07-01), Sokol
patent: 2577699 (1949-09-01), Cooper
patent: 3763152 (1973-10-01), Wolf et al.
patent: 3875224 (1975-04-01), Finkbeiner et al.
patent: 4757128 (1988-07-01), Domb et al.
patent: 4789724 (1988-12-01), Domb et al.
patent: 4851426 (1989-07-01), Ladkani et al.
patent: 4857311 (1989-08-01), Domb et al.
patent: 4863965 (1989-09-01), Jansen et al.
patent: 4868201 (1989-09-01), Fukaya et al.
patent: 4888176 (1989-12-01), Langer et al.
Leong, K. W., "Bioerodible Polyanhydrides as Drug-Carrier Matrices, I: Characterization, Degradation and Release Characteristics," J. Biomed. Mat. Res., vol. 19, 941-955 (1985).
Leong, K. W., et al., "Bioerodible Polyanhydrides as Drug-Carrier Matrices, II: Biocompatibility and Chemical Reactivity," J. Biomed. Mat. Res., vol. 20, 51-64 (1986).
Kydonieus, A. F., Controlled Release Technologies, CRC Press, Inc., Boca Raton, Florida (1977).
Harrison, I. T., et al., Nonsteroidal Antiinflammatory Agents, (1970).
Child, R. G., et al., Journal of Pharmaceutical Sciences, 66(4) (1977).
Tocoo, D. J., et al., Drug Metabolism and Disposition, 10(1) (1982).
Tipnis, V., et al., Journal of Chromatography, 345, 396-401 (1985).
I. T. Harrison, et al., "Nonsteroidal Antiinflammatory Agents 6-Substituted 2-Naphthylacetic Acids", J. Med. Chem. 13, 203-205 (1970).
R. G. Child, et al., "Fenbufen, a New Anti-Inflammatory Analgesic: Synthesis and Structure-Activity Relationships of Analogs", J. Pharm. Sci. 66(4), 466-476 (1977).
D. J. Tocco, et al., "The Physiological Disposition and Metabolism of Enalapril Maleate in Laboratory Animals", Drug Metab. Disp. 10(1), 15-19 (1982).
V. Tipnis, et al., "Determination of pentopril, an angiotensin converting enzyme inhibitor, and its active metabolite in urine", J. Chromatog. 345, 396-401 (1985).

Affiliated with

Also associated with

Rating

Prodrug compositions does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Prodrug compositions, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Prodrug compositions will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2101019