70 results about "Ketorolac" patented technology

Disclosed herein is an injectable long-acting analgesic composition comprising:

(a) a ketorolac ester derivative of formula (I),  wherein

• •  R is a straight-chain or branched saturated or unsaturated C₁-C₂₀ aliphatic group optionally substituted with a C₆-C₁₀ aryl group; and (b) a pharmaceutically acceptable oil vehicle. The composition can provide a longer duration of action and, therefore, is suitable for use in the treatment of long-lasting pains and inflammations.

Topical alcoholic or aqueous alcoholic gels containing ibuprofen or other NSAIDs, such as, naproxen, in substantially neutral salt form, have enhanced penetration through skin and may provide rapid pain/inflammation relief by including in the formulation 2-n-nonyl-1,3-dioxolane or other hydrocarbyl derivative of 1,3-dioxolane-or 1,3-dioxane or acetal, as skin penetration enhancing compound. The amount of propylene glycol may be varied to adjust the initial flux of the NSAID through the skin, especially for ibuprofen, naproxen, and ketorolac.

The present invention relates to stable, preservative- and antioxidant-free liquid formulations of phenylephrine and ketorolac for injection.

The present invention provides a topical formulation containing NSAID, particularly diclofenac. The topical formulation is particularly useful for alleviating pain/inflammation associated with infection caused by herpes virus, especially herpes simplex virus (HSV) and varicella-zoster virus (VZV). Similar relief can be achieved where diclofenac is replaced with another non-steroidal anti-inflammatory drug (NSAID), which includes, without limitation, etodolac, ketorolac, bromfenac, diflunisal, ibuprofen, fenoprofen, ketoprofen, naproxen, suprofen, meclofenamate, mefenamic acid, piroxicam, meloxicam, indomethacin, sulindac, phenylbutazone, oxyphenbutazone, and tolmetin. The topical formulation is further characterized by its fast relief on pain and/or inflammation associated with infection caused by herpes virus, i.e., a complete relief in no more than seven (7) days after the application of the topical formulation on skins of patients.

This invention refers to the pharmaceutical combinations of Ketorolac salts and B-complex; to the methods used to make said combinations; and particularly, to ketorolac and B-complex synergic combinations useful in the treatment of patients that suffer from moderate to severe pain and neuralgias in different body sites.

The present invention provides for compositions and methods for accelerating the rate of delivery of ketorolac to the systemic circulation by sublingual spray administration under the tongue to provide a rapid response in the treatment of pain, especially acute pain associated with postoperative pain and migraine headache. Compositions of ketorolac formulated for sublingual delivery as liquid spray are provided. Also provided are methods of treatment and management of pain.

The invention provides a ketorolac implant and a preparation method thereof. The implant which contains ketorolac and a degradable carrier is prepared by using a hot melt extrusion method, can release drugs in a zero-level dynamic way within a preset drug release time and can be used for preventing or treating acute or chronic pain and inflammation. The ketorolac implant prepared by the invention is stable in release and free of burst release effect and has great advantages in clinic application.

The invention relates to applications of cytarabine or an analogue of cytarabine and ketorolac or an analogue of ketorolac in treating cachexia, and in particular provides a medicinal composition for treating cachexia. According to the scheme, for the first time, one or more of cytarabine or the analogue of cytarabine and ketorolac or the analogue of ketorolac are creatively adopted as the active ingredients of the composition for treating cachexia, and remarkable treatment effects are obtained in the animal experiment. Based on the severity degree of cachexia, the medicinal composition has the broad clinical application prospect.

The present invention relates to pharmaceutical compositions containing benfotiamine and one or more pharmaceutically active agents selected from the group consisting of analgesic acting substances, especially pharmaceutical compositions containing benfotiamine and one or more pharmaceutically active agents selected from the group consisting of gabapentin, pregabalin, XP13512, carbamacepin, amitryptilin, ketorolac, diclofenac, ibuprofen, flurpirtin, paracetamol and dexamethasone, the process for their preparation and their use for the treatment and prevention of conditions and diseases selected from the group consisting of pain conditions of neuropathic origin.

The novel positively charged pro-drugs of aryl- and heteroarylpropionic acids in the general formula (1) 'Structure 1' and general formula (2) 'Structure 2' were designed and synthesized. The compounds of the general formula (1) 'Structure 1' and general formula (2) 'Structure 2' indicated above can be prepared from functional derivatives of naproxen, suprofen, a- methyl-(p-chlorobenzoyl)-5-methoxy-2-methylindole 3-acetic acid, flurbiprofen, carprofen, pranoprofen, benoxaprofen, alminoprofen, tiaprofenic acid, pirprofen, zaltoprofen, bermoprofen, loxoprofen, indoprofen, fenclorac, oxaprozin, fenbufen, orpanoxin, ketorolac, clidanac, and related compounds, (for example acid halides or mixed anhydrides), by reaction with suitable alcohols, thiols, or amines. The positively charged amino groups of these pro-drugs not only largely increases the solubility of the drugs, but also bonds to the negative charge on the phosphate head group of membranes and pushes the pro-drug into the cytosol. The results suggest that the pro-drugs diffuses through human skin -100-130 times faster than do their parent drugs. It takes 2-4 hours for naproxen, suprofen, a- methyl-(p-chlorobenzoyl)-5-methoxy-2-methylindole 3-acetic acid, flurbiprofen, carprofen, pranoprofen, benoxaprofen, alminoprofen, tiaprofenic acid, pirprofen, zaltoprofen, bermoprofen, loxoprofen, indoprofen, fenclorac, oxaprozin, fenbufen, orpanoxin, ketorolac, clidanac, and related compounds to reach the peak plasma level when they are taken orally, but these prodrugs only took about 40-50 minutes to reach the peak plasma level when they are taken transdermally. In plasma, more than 90% of these pro-drugs can change back to the drug in a few minutes. The prodrugs can be used medicinally in treating any NS AIAs-treatable conditions in humans or animals. The prodrugs can be administered not only orally, but also transdermally for any kind of medical treatments.

The invention relates to phenylephrine ketorolac solution and a preparation method, and provides intraocular operation washing concentrated solution without a preservative, an antioxidant and a buffer system. The phenylephrine ketorolac solution is capable of preventing the intraoperative miosis and relieving the postoperation pain, and avoiding the side effects caused by the preservative, the antioxidant and the buffer system.

The present invention refers to pharmaceutical compositions based on ketorolac or one of its salts pharmaceutically acceptable, as well as the use of ketorolac or one of its salts acceptable from pharmaceutical viewpoint, for preparation of a pharmaceutical composition (tablets) for sublingual administration, with the purpose of accelerating the pharmacological response to ketorolac, without making use of the injectable via. On the other hand, a pharmaceutical composition is described encompassing, as one of its active principles, ketorolac or one of its salts acceptable from pharmaceutical viewpoint, representing from 10 to 15% by weight, in relation to the total weight of the compound and as the essential excipient, a ternary mixture of lactose/sorbitol/cellulose, eventually in a mixture with other excipients acceptable from pharmaceutical viewpoint.

Parenteral formulations comprising ketorolac, and a compound of formula II wherein R is hydrogen or lower alkyl. Such formulations are used for the treatment and prevention of pain.

The invention discloses a ketorolac impurity C and a preparation method and application thereof. According to the method, the ketorolac impurity C is prepared by taking pyrrole as an initial raw material through a series of reactions such as substitution, oxidation and alkaline hydrolysis, and the ketorolac impurity C is one of important impurities of ketorolac drugs or preparations thereof and can be used for toxicological and pharmacological researches such as in-vivo absorption and metabolism of ketorolac, and can also be applied to research on stability and quality control of ketorolac preparations. The preparation method of the ketorolac impurity C has the advantages of simplicity in operation, safety in reaction and high purity and yield, and can be widely applied to the fields of impurity analysis, toxicological research, safety detection, stability judgment and the like of ketorolac bulk drugs and preparations thereof.

The invention provides an application of a Rac1 activity inhibitor in preparation of drugs for treating an Alzheimer disease. The Rac1 activity inhibitor can be: at least one of EHop-016, CS7171, JKF-034, Secramine, AZD0530, NSC23766, MBQ-167, AZA1, AZA197, Compound 19, ZINC08010136, ZINC07949036, 69391, 1A-116, ITX3, ITX1, CPYPP, GGTase1inhibitor(P61A6, Statins), EHT1864, Compound 1, MLS000532223, R-Ketorolac, OSU-3012, FL172, FRAX597, Phox-11, 187-1 and Wiskostatin. The invention protects the discovery of a mechanism for treating AD by inhibiting the activity of a forgetting regulatory molecule Rac1, and protects the application of a small molecule compound capable of inhibiting Rac1 activity in treating AD.

Disclosed are non-steroidal analgesic and analgesic anti-inflammatory agents containing carboxyl including sodium, calcium, zinc, magnesium, N-n-octylgucamine, Arginine, Lycine or Trometamol salts of Loxoprofen, Ketoprofen, Pranoprofen, Tiaprofenic acid, Butibufen, Omolofen, epoxy indene acid, Lobuprofen, Clofenamic acid, Clonixin, Fenoprofen, Benorilate, Flurbiprofen, Alminoprofen, Bucloxic acid, Sulindac, Zidometacin, Acemetacin, Ketorolac, Risedronic acid, Sulindac, Lonaprofen, aspirin, Florfenicol, tiaprofenic acid, overall evaluation shows that trometamol salts are the best choice in terms of physicochemical properties, solvability, stability, local irritation, blood vessel irritation, and bioavailability for oral administration.

An analgesic/anti-inflammatory pharmaceutical dosage form which comprises an effective amount of an active ingredient selected from the group consisting of racemic 5-benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxylic acid, optically active forms thereof and pharmaceutically acceptable salts thereof, in combination with a pharmaceutically acceptable excipient or diluent, said dosage form being an intranasally administrable dosage form.

The present invention discloses the synthesis process of benzoyl pyrrole as the key intermediate for ketorolac trometamol. Benzoyl pyrrole is synthesized through the reaction of bis(trichloromethyl) carbonate and N, N-disubstituent amide to form one intermediate, adding pyrrole and reaction in organic solvent at 0-120 deg.c for 2-20 hr, and post-treatment of the resultant to obtain benzoyl pyrrole. The technological scheme of the present invention has reasonable production process, safe and reliable operation, high reaction yield, low cost and other advantages, and possesses broad industrial application foreground.