Drug – bio-affecting and body treating compositions – Topical body preparation containing solid synthetic organic... – Anti-inflammatory or anti-irritant
Reexamination Certificate
2000-08-17
2002-09-17
Gitomer, Ralph (Department: 1623)
Drug, bio-affecting and body treating compositions
Topical body preparation containing solid synthetic organic...
Anti-inflammatory or anti-irritant
C424S449000, C514S605000
Reexamination Certificate
active
06451302
ABSTRACT:
The present invention relates to novel therapeutic non intensely coloured, water miscible injectable analgesic pharmaceutical compositions of Non-steroidal anti-inflammatory drugs and a process for the manufacture of such drugs. The analgesic injectable composition is very useful in mammals particularly in humans for the treatment of acute painful conditions like post operative trauma, pain associated with cancer, sports injuries, migraine headache, neurological pain, pain associated with sciatica and spondylitis. For these indications some modified route of administrations may also be construed.
BACKGROUND OF THE INVENTION
Non-steroidal anti-inflammatory drugs such as those belonging to the category of Cyclo-oxygenase-2 inhibitors including Nimesulide are highly hydrophobic compounds and readily precipitate even in the presence of minor amounts of water.
It is therefore very difficult to formulate Non-steroidal anti-inflammatory drugs which are inhibitors of Cyclo-oxygenase-2 as an injection for intramuscular or intravenous use.
In the past, efforts have been made to make an injectable composition of Nimesulide.
An injectable formulation of Nimesulide has been reported in the prior art PCT Patent No. WO 95/34533 which utilizes a salt form of Nimesulide with L-lysine which is in turn further complexed with cyclodextrins which may be dissolved in water to give an injectable preparation. The maximum solubility achieved by this injectable composition was reported to be 2.4 mg/ml which is not sufficient for intramuscular administration as it would require very large volumes to administer therapeutic doses. Moreover making a salt form of Nimesulide and then combining with Cyclodextrins not only makes the process cumbersome but also increases the cost of the formulations.
Another reference (Daffonchio. L et al. Inflammatory Research 45:259-264; 1995) wherein Nimesulide is dissolved in saline for intravenous administration for experimental studies in animals also describes only very dilute solutions which cannot deliver therapeutic doses in humans.
The disadvantages of WO 95/34533 and problems associated therewith were overcome by the invention described in U.S. Pat. No. 5,688,829 (Corresponding Korean Application No. 96-48013, Australian Application No. 67993/96 and Japanese Patent Application No. 8-290585, all pending) by the inventors of the present invention.
This invention utilizing solubilization techniques was able to achieve sufficiently high concentrations of Nimesulide suitable to deliver therapeutic doses in conveniently small volumes using a base which was oily in nature without using water and without any salt form or complexing agents of Nimesulide.
The present invention comprises a composition wherein all the ingredients of the base are hydrophilic. The hydrophilic base serves the advantage of better miscibility with body fluids, faster drug disposition and better compatibility with the tissue environment.
It is an objective of the present invention to provide an injectable analgesic hydrophilic composition of Non-steroidal anti-inflammatory drugs which are non-intensely coloured having better miscibility with body fluids. Such hydrophilic compositions described herein can be administered by intravenous routes also in addition to intramuscular route.
It is another objective of the present invention to provide a novel process for the preparation of a parenteral hydrophilic injectable composition of NSAIDs.
SUMMARY OF THE INVENTION
The invention comprises a novel injectable aqueous miscible composition of Cyclo-oxygenase-2 inhibitors such as Nimesulide which comprises:
1. Cyclooxygenase inhibitors
2. Alkyl amides/Alkyl sulphoxides or pyrrolidones
3. Glycols
4. 0 to 20% of water.
REFERENCES:
patent: 5716609 (1998-02-01), Jain et al.
patent: 1389/DEL/95 (1995-07-01), None
patent: 2046/DEL/95 (1995-11-01), None
patent: 2047/DEL/95 (1995-11-01), None
patent: 2048/DEL/95 (1995-11-01), None
patent: WO 99/41233 (1999-08-01), None
Jain Rajesh
Singh Amarjit
Akerman & Senterfitt
Gitomer Ralph
Khare Devesh
Panacea Biotec Limited
LandOfFree
Parenteral water-miscible non-intensely colored injectable... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Parenteral water-miscible non-intensely colored injectable..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Parenteral water-miscible non-intensely colored injectable... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2906096