WO1995025511A1 - Low dosage ketoprofen - Google Patents
Low dosage ketoprofen Download PDFInfo
- Publication number
- WO1995025511A1 WO1995025511A1 PCT/US1995/003335 US9503335W WO9525511A1 WO 1995025511 A1 WO1995025511 A1 WO 1995025511A1 US 9503335 W US9503335 W US 9503335W WO 9525511 A1 WO9525511 A1 WO 9525511A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- ketoprofen
- low dosage
- pain
- dosage
- over
- Prior art date
Links
- DKYWVDODHFEZIM-UHFFFAOYSA-N ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 title claims abstract description 19
- 229960000991 ketoprofen Drugs 0.000 title claims abstract description 16
- 230000000202 analgesic effect Effects 0.000 claims abstract description 5
- 208000002193 Pain Diseases 0.000 claims description 12
- 206010037660 Pyrexia Diseases 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 230000001754 anti-pyretic effect Effects 0.000 abstract description 2
- 239000002221 antipyretic Substances 0.000 abstract description 2
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical compound CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 7
- 239000000902 placebo Substances 0.000 description 5
- 229940068196 placebo Drugs 0.000 description 5
- 229940079593 drug Drugs 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 229940080504 ketoprofen 12.5 mg Drugs 0.000 description 3
- 229960005489 paracetamol Drugs 0.000 description 3
- 229940082170 ibuprofen 200 mg Drugs 0.000 description 2
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 description 1
- 208000005171 Dysmenorrhea Diseases 0.000 description 1
- 206010013935 Dysmenorrhoea Diseases 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 description 1
- 208000008548 Tension-Type Headache Diseases 0.000 description 1
- 229960001138 acetylsalicylic acid Drugs 0.000 description 1
- 229940035676 analgesics Drugs 0.000 description 1
- 239000000730 antalgic agent Substances 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 229960001680 ibuprofen Drugs 0.000 description 1
- 238000011850 initial investigation Methods 0.000 description 1
- 229940080439 ketoprofen 25 mg Drugs 0.000 description 1
- 229940082560 naproxen sodium 275 mg Drugs 0.000 description 1
- 230000003637 steroidlike Effects 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 229940072651 tylenol Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
Definitions
- the field of the invention is analgesics for use in the over- the-counter market in general and is a particularly low dosage of ketoprofen for effective pain relief in the over-the-counter market in particular.
- Ketoprofen is a non-steroidal anti-inflammatory in the same chemical class as ibuprofen, is marketed for prescription use in the United States as ORUDIS by Wyeth-Ayerst.
- the product is available as 25, 50 and 75 mg capsules.
- the recommended daily dose of ORUDIS is 150 to 300 mg divided in three or four doses, ie approximately 50 to 100 mg per dose.
- the usual dose of ORUDIS recommended for mild to moderate pain and dysmenorrhea is 25 to 50 mg every 6 to 8 hours as necessary. It has been desired to make this analgesic available as an over-the-counter (OTC) medication by a mechanism known as an Rx to OTC switch.
- OTC dosage of a medication is lower than the Rx dosage because such medication could be purchased by individuals without the supervision of a physician. That dosage must be effective and yet safe for OTC analgesic use.
- ketoprofen at a dosage of 12.5 mg would be an effective analgesic and could be used for over-the-counter use.
- ketoprofen 12.5 mg and 25 mg results of a ketoprofen study in Europe utilizing a headache model indicated that there were no meaningful differences between ketoprofen 12.5 mg and 25 mg, ibuprofen 200 mg and naproxen sodium 275 mg to relieve tension-type headache two hours after administration in outpatients of general practitioners.
- ketoprofen 12.5 and 25 mg to acetaminophen 500 and 1000 mg Another dental pain study in Europe compared the efficacy of ketoprofen 12.5 and 25 mg to acetaminophen 500 and 1000 mg.
- general ketoprofen and acetaminophen provided similar results and both active drugs were significantly better than placebo.
- Both forms of ketoprofen provided a significantly greater amount of pain relief at one hour (“Time of Onset”) than placebo, while acetaminophen did not.
- ketoprofen 12.5 mg and TYLENOL 650 mg are both significantly more effective than placebo and not significantly different from each other.
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
It has been found that 12.5 mg ketoprofen is an effective analgesic and antipyretic. This low dosage is suitable for over-the-counter availability.
Description
LOW DOSAGE KETOPROFEN
FIELD OF THE INVENTION
The field of the invention is analgesics for use in the over- the-counter market in general and is a particularly low dosage of ketoprofen for effective pain relief in the over-the-counter market in particular.
BACKGROUND OF THE INVENTION
Ketoprofen, is a non-steroidal anti-inflammatory in the same chemical class as ibuprofen, is marketed for prescription use in the United States as ORUDIS by Wyeth-Ayerst. The product is available as 25, 50 and 75 mg capsules. The recommended daily dose of ORUDIS is 150 to 300 mg divided in three or four doses, ie approximately 50 to 100 mg per dose. The usual dose of ORUDIS recommended for mild to moderate pain and dysmenorrhea is 25 to 50 mg every 6 to 8 hours as necessary. It has been desired to make this analgesic available as an over-the-counter (OTC) medication by a mechanism known as an Rx to OTC switch. Generally the OTC dosage of a medication is lower than the Rx dosage because such medication could be purchased by individuals without the supervision of a physician. That dosage must be effective and yet safe for OTC analgesic use.
SUMMARY OF THE INVENTION
The applicant herein proposed, and it has since been proven, that ketoprofen at a dosage of 12.5 mg would be an effective analgesic and could be used for over-the-counter use.
DESCRIPTION OF THE CLINICAL SUPPORT FOR LOW DOSAGE KETOPROFEN Clinical studies have been conducted utilizing various pain models including dental pain and post-episiotomy pain. In addition, a clinical trial has been conducted to evaluate the efficacy of ketoprofen 12.5 mg as an antipyretic.
Results of a ketoprofen study in Europe utilizing a headache model indicated that there were no meaningful differences between ketoprofen 12.5 mg and 25 mg, ibuprofen 200 mg and naproxen sodium 275 mg to relieve tension-type headache two hours after administration in outpatients of general practitioners.
The results of one dental pain study indicated that both 12.5 mg of ketoprofen and 650 mg of aspirin are superior to placebo for pain relief but are not statistically significantly different from each other.
Another dental pain study in Europe compared the efficacy of ketoprofen 12.5 and 25 mg to acetaminophen 500 and 1000 mg. In " general ketoprofen and acetaminophen provided similar
results and both active drugs were significantly better than placebo. Both forms of ketoprofen provided a significantly greater amount of pain relief at one hour ("Time of Onset") than placebo, while acetaminophen did not.
Yet a third dental pain study indicated that ketoprofen 12.5 mg and TYLENOL 650 mg are both significantly more effective than placebo and not significantly different from each other.
Initial investigations assessing the efficacy of ketoprofen 12.5 and 25 mg when compared to ibuprofen 200 mg and placebo indicate that is effective at both dosage levels for dysmennorhea.
Claims
1. A method of treating pain with a 12.5 mg ketoprofen to provide safe and effective relief.
2. A method of treating symptoms of pain, discomfort and fever with a 12.5 mg ketoprofen to provide safe and effective relief.
3. An over-the-counter analgesic tablet, comprising 12.5 mg ketoprofen.
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU21218/95A AU2121895A (en) | 1994-03-18 | 1995-03-15 | Low dosage ketoprofen |
| EP95914079A EP0785779A1 (en) | 1994-03-18 | 1995-03-15 | Low dosage ketoprofen |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US21083294A | 1994-03-18 | 1994-03-18 | |
| US08/210,832 | 1994-03-18 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO1995025511A1 true WO1995025511A1 (en) | 1995-09-28 |
Family
ID=22784436
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US1995/003335 WO1995025511A1 (en) | 1994-03-18 | 1995-03-15 | Low dosage ketoprofen |
Country Status (4)
| Country | Link |
|---|---|
| EP (1) | EP0785779A1 (en) |
| AU (1) | AU2121895A (en) |
| CA (1) | CA2185805A1 (en) |
| WO (1) | WO1995025511A1 (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0871445A4 (en) * | 1995-12-07 | 2001-01-10 | Lilly Co Eli | Composition for treating pain |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3641127A (en) * | 1967-01-27 | 1972-02-08 | Rhone Poulenc Sa | (3-benzoylphenyl) alkanoic acids |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4962124A (en) * | 1987-11-17 | 1990-10-09 | Analgesic Associates | Onset-hastened/enhanced antipyretic response |
| US4868214A (en) * | 1987-11-17 | 1989-09-19 | Analgesic Associates | Onset-hastened/enhanced analgesia |
| US5331000A (en) * | 1992-03-09 | 1994-07-19 | Sepracor Inc. | Antipyretic and analgesic methods and compositions containing optically pure R(-) ketoprofen |
-
1995
- 1995-03-15 AU AU21218/95A patent/AU2121895A/en not_active Abandoned
- 1995-03-15 WO PCT/US1995/003335 patent/WO1995025511A1/en not_active Application Discontinuation
- 1995-03-15 CA CA 2185805 patent/CA2185805A1/en not_active Abandoned
- 1995-03-15 EP EP95914079A patent/EP0785779A1/en not_active Withdrawn
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3641127A (en) * | 1967-01-27 | 1972-02-08 | Rhone Poulenc Sa | (3-benzoylphenyl) alkanoic acids |
Non-Patent Citations (2)
| Title |
|---|
| HCA ABSTRACT, Volume 92, issued 1979, KUBOTA et al., "Studies on the Antiinflammatory, Analgesic and Antipyretic Effect of Ketoprofen (KP) After rectal Administration", Abstract No. 185851; & OYO YAKURI (JAPAN), 18(3), 449-53. * |
| See also references of EP0785779A4 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0871445A4 (en) * | 1995-12-07 | 2001-01-10 | Lilly Co Eli | Composition for treating pain |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2121895A (en) | 1995-10-09 |
| CA2185805A1 (en) | 1995-09-28 |
| EP0785779A4 (en) | 1997-07-30 |
| EP0785779A1 (en) | 1997-07-30 |
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