Compounds and methods for lowering the abuse potential and...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C546S046000, C546S044000

Reexamination Certificate

active

10800898

ABSTRACT:
The abuse potential of a bioavailable drug such as an opiate analgesic agent is reduced and its duration of action is extended by converting it to a poorly absorbed ester prodrug or other prodrug derivative prior to formulation. Unlike many existing sustained release formulations of active pharmaceutical agents wherein an active pharmaceutical agent can be released by chewing, crushing, or otherwise breaking tablets or capsule beads containing the active pharmaceutical agent, such mechanical processing of tablets or capsule beads containing a prodrug of this invention neither releases the active drug nor compromises the controlled conversion of prodrug to drug. Moreover, tablets and capsule beads containing prodrugs of this invention or other drugs can be formulated with a sufficient amount of a thickening agent such as hydroxypropylmethylcellulose or carboxymethylcellulose to impede inappropriate intravenous and nasal administration of formulations that are not indicated for these modes of administration.

REFERENCES:
patent: 3299072 (1967-01-01), Bartels-Keith
patent: 3966940 (1976-06-01), Pachter et al.
patent: 4457933 (1984-07-01), Gordon et al.
patent: 4489065 (1984-12-01), Walton et al.
patent: 4661492 (1987-04-01), Lewis et al.
patent: 4769372 (1988-09-01), Kreek
patent: 4785000 (1988-11-01), Kreek et al.
patent: 5130126 (1992-07-01), Koyama et al.
patent: 5149538 (1992-09-01), Granger et al.
patent: 5176907 (1993-01-01), Leong
patent: 5194581 (1993-03-01), Leong
patent: 5236714 (1993-08-01), Lee et al.
patent: 6051576 (2000-04-01), Ashton et al.
patent: 6228863 (2001-05-01), Palermo et al.
patent: 6277384 (2001-08-01), Kaiko et al.
patent: 6375957 (2002-04-01), Kaiko et al.
patent: 6451806 (2002-09-01), Farrar
patent: 6475494 (2002-11-01), Kaiko et al.
patent: 2003/0022876 (2003-01-01), Ashton et al.
patent: 2004/0058946 (2004-03-01), Buchwald et al.
patent: 1 258 246 (2002-11-01), None
patent: 1 300 419 (1972-12-01), None
patent: WO 02/094254 (2002-11-01), None
patent: WO 03/072046 (2003-09-01), None
Agarwal, V. and Mishra, B.; “Design, Development, and Biopharmaceutical Properties of Buccoadhesive Compacts of Pentazocine;”Drug Dev. Ind. Pharm;Jun. 1999; 25 (6); 701-709.
Buckett, W. R.; “The Relationship Between Analgesic Activity, Acute Toxicity and Chemical Structure Inesters of 14-Hydroxycodeinone;”J Pharm Pharmacol;Dec. 1964; 16 Suppl-71T.
Buckett, W. R; Farquharson, M. E.; and Haining, C. G.; “The Analgesic Properties of Some 14-Substituted Derivatives of Codeine and Codeinone;”J Pharm Pharmacol;Mar. 1964; 16 174-182.
Okuda, T.; Tsuchiya, N.; Wakita, K.; Hatsuoka, K.; Koga, Y.; Ueda, S.; and Kaetsu, I.; “[Prolonged Antinociceptive Effect After Epidural Injection of Polyethylene Glycol-Morphine Composites in Rats];”Masui;May 1996; 45 (5); 571-575.
Nagase et al.; “The Facility of Formation of a Δ6Bond in Dihydromorphinone and Related Opiates;”J. Org. Chem.;1989, vol. 54; 4120-4125.
Hansen, H. C. and Spillum, A.; “Loss of Nitroglycerin During Passage Through Two Different Infusion Sets;”Acta Pharm Nord.;1991; 3 (3); 131-136.
Hosztafi, S.; Kohegyi, I.; Simon, C.; and Furst, Z.; “Synthesis and Analgetic Activity of Nicotinic Esters of Morphine Derivatives;”Arzneimittelforschung.;Nov. 1993; 43 (11); 1200-1203.
Hussain, M. A.; Aungst, B. J.; Koval, C. A.; and Shefter, E.; “Improved Buccal Delivery of Opioid Analgesics and Antagonists With Bitterless Prodrugs:”Pharm Res;Sep. 1988; 5 (9); 615-618.
Stinchcomb, A. L.; Paliwal, A.; Dua, R.; Imoto, H.; Woodard, R. W.; and Flynn, G. L.; “Permeation of Buprenorphine and Its 3-Alkyl-Ester Prodrugs Through Human Skin;”Pharm Res;Oct. 1996; 13 (10); 1519-1523.
Stinchcomb, A. L.; Swaan, P. W.; Ekabo, O.; Harris, K. K.; Browe, J.; Hammell, D. C.; Cooperman, T. A.; and Pearsall, M.; “Straight-Chain Naltrexone Ester Prodrugs: Diffusion and Concurrent Esterase Biotransformation in Human Skin;”J Pharm Sci;Dec. 2002; 91 (12); 2571-2578.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Compounds and methods for lowering the abuse potential and... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Compounds and methods for lowering the abuse potential and..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Compounds and methods for lowering the abuse potential and... will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-3873905

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.