IE54149B1 - Pharmaceutical compositions - Google Patents
Pharmaceutical compositionsInfo
- Publication number
- IE54149B1 IE54149B1 IE2152/82A IE215282A IE54149B1 IE 54149 B1 IE54149 B1 IE 54149B1 IE 2152/82 A IE2152/82 A IE 2152/82A IE 215282 A IE215282 A IE 215282A IE 54149 B1 IE54149 B1 IE 54149B1
- Authority
- IE
- Ireland
- Prior art keywords
- pharmaceutical composition
- inflammatory drug
- ranitidine
- drug
- inflammatory
- Prior art date
Links
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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
-
- 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
- A61K31/60—Salicylic acid; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Pharmaceutical compositions which contain a systemic steroid-free antiinflammatory agent together with the histamine H2 antagonist ranitidine or a physiologically suitable salt thereof are described. The histamine H2 antagonist reduces damage to the gastric mucosa caused by the antiinflammatory agent.
Description
Tills invention relates to improvements in the formulation of anti-inflammatory drugs.
Systemic non-steroidal anti-inflammatory drugs, such as aspirin, indomethacin and ibuprofen, are known Lo give rise Lo undesirable side effects. in partieular, they are known Lo be ulcerogenic and can thus, Iniexample, give rise to gastric ulceration when adminis-ere orally. This side effect may be further enhanced in combination with other factors such as stress. dilute in some treatments these compounds may have to be used for an extended period, such side effects can prove a serious disadvantage.
Ranitidine is the approved name for Χ-[2-'[ί/,i dimethyl amino )me thy! ]-2-l'uranyl ]iuethy 1 ] thio J e thyl ’ tg methyi-2-nitro-l,l-ethenediamine which is described ai.-i claimed in Patent Specification No. 45456. It is a potent iiistaiuj lie 11,,-nnLngoni s I, which may lie used 1:, Me 1 re.aiiiiont of conditions where there is ail advaiitare in lowering gastric acidity, particularly 111 gastric .uni peptic ulceration, and in Lhe treatment of aiitrgu and inflaminatory conditions where histamine is a Known mediator. it. lias now been discovered that, mucosal lesions or tne gastrointestinal tract caused by systemic non-steroiuat anti-inflammatory drugs can tie significant reduced by co-administerlng ranitidine.
The present invention provides a pharmaveutο·,η eompi·,-.ιLion comprising a sysiemic non-steroidal an:iinflaiiimatory drug and rani tidine or a physiological iy neccptable salt thereof.
Particularly useful pharmaceutical compositions according to tho invention are those in a form suiladle l or oral or rectal administration.
The systemic non-steroidal anti-inf lamina Lory drugs which may be employed iu the invention generally S 4 Ί 4 ί» - 3 also show analgesic activity and include, for example, aspirin, indornethac i η, ibuprofen, fenoprofen, ketoprofen, naproxen, me lenami c acid, diflunisal, benoryiate, azapropazone, diclofenac, fcnbufcn, feprazone, fencI οίenai, !iufenamic acid, flurbiprofen, oxyphenbutazone, phenylbutazone, piroxicam, sulindac and tolmetin. They may be used in the pharmaceutical compositions of the invention in their usual dosage amounts, e.g. 50mg - 1 g of aspirin, JO - lOOmg of indomethacin and 100 - 500mg of ibuprofen per dosage unit taken one or more times daily in accordance with the normal dosage regime for the drug in question.
It is preferred that ranitidine should be employed in Lht’ composition in the form of a physiologically acceptable salt. Such salts include salts of inorganic or organic acids such as the hydrochloride, hydrobromide, sulphate, acetate, maleate, succinate and fumarate salts. The hydrochloride salt is particularly preferred. The amount of ranitidine, preferably in the form o! a physiologically uiceptable salt, employed in the pharmaceutical composition ol hie iiiveiilion will be an amount sul fit ient to reduce Ihe gastrointestinal distress caused by the ant i - ί η f 1 anrr.a to r y drug and will preferably be in the range of 10 - 200mg per dosage unit.
The pharmaceutical compositions of the invention may be presented in a conventional manner with the aid ol it least one pharmaceutical carrier or excipient. The composition may take the form of, for example, tablets, capsules, powders, granules, solutions, syrups, suspensions, -- r suppos i t or ies p repar ed by conventional means with acceptable excipients. The composition may thus contain as excipients, for example, binding agents, compression aids, fillers, lubricants, disintegrants and wetting agents. If desired, other active ingredients may also be present in such compositions. Tablets may be coated in conventional manner, for example, with a suitable fiini— forming material such as methyl cellulose, ethyi cellulose and/or hydroxypropylmethyl cellulose or with sugar. preparations may also contain, io: example, j.jibt., oils such as peanut oil. Suppositories may eum.ain, for example, fat-soluble nr water miscible bases. 'i'he pharmaceutical compositions of the invention o way In; prepared according to conventional techniques well known in flu· pliaimaeeuti val industry. Thus, for example, fin; anti.-inflammatory drug and tlie ranitidine or rani tidine salt may be admixed together, if desired, with suitable excipients. Tablets may be prepared, for example, by lo direct compression of such a mixture. Capsules may be prepared by filling the blend along with suitable excipient; into gelatin capsules, using a suitable filling machine.
Alternatively, the pharmaceutical compositi*.us of the invention may be presented in a suitable controlled >.5 release form so that the ranitidine or its salt is rapidlymade available for absorption and the non-steroidal antiinflammatory drug is released more slowly. The pliarmavcuttcal compositions may Unis be presented for oral or rectal, administration in a conventional manner associated l!.i will: control Jed release forms.
The pharmaceutical compositions of the invention may be used in tlie treatment of inflammatory conditions, particularly acute and chronic muscuio-skeletaJ inflammatory conditions such as rheumatoid and osteo21 arthritis und ankylosing spondylitis, and for analgesia in conditions such as dysmenorrhoea, especially where the use of tho anti-inflammatory drug is limited by- gas tre intestinal side-effects.
In order that the invention may be more fulIv pi understood, the following Exiunpies are given by way oi i J 1 us (..ration only.
Example 1 - TAJIhETS \a) mg/tabI d.
Ranitidine hydrochloride ibuprofen Lactose i 68. (JO* hid). On ,87. t io mg/tab Ic t Hydroxypropyl metliyiecilulose 7.0() Sodium starch glyool'late 30.00 Magnesium stearate 10.00 Compression weight 1000.00 ^'Equivalent to 1J0 mg ranitidine hase The ranitidine hydrochloride and ibuprofen are sieved through a 250 pm sieve and blended with the lactose. This mix is granulated with a solution of the hydroxypropyl 1.0 methylcellulose. The granules are dried, screened and blended with the sodium starch glycollate and the magnesium stearate. Tlie lubricated granules are compressed into tablets using 12.5mm punches. (b) ing/tahint ilani Udine hydrochloride it>s. 00 Indomc l.linci n 50.00 Microerystailine celluJose 79.00 Magnesium stearate 5.00 Compression weight 300.00 The i-anitidine hydrochloride and indomethacin are blended with the microcrystalline cellulose and magnesium stearate and compressed using 9.5mm punches.
Example 2 - CAPSULES (a) capsuI <; Itani Udine hydroch l ori dc 108.00 Ibuprofen 000.00 Starch 1500 ** 228.00 Magnesium stearate 0.00 Fill weight •SCO. 00 ** A (.'oi'jn ul' directly compressible starch supplied hy CoJorcon Ltd, Orpington, Kent.
The ranitidine hydrochloride and ibuprofen are sieved through a 250 pm sieve and blended with tin· Starch .1500 and magnesium stearate. The resultant mix is filled into size 0 hard gelatin capsules using a suitable filling machine. ϊ ’ 4 S (h) mg/capsul ο Raniti dine hydrochl0 r i de 166.00 Indoinethaein 50.00 Starch 1500 so. 50 Magnesium stearate .1.50 Fili weight 500.00 Tlie ranitidine hydrochloride and indoiaethacin are sieved through a 250 pm sieve and blended with ihe Starch 1500 and magnesium stearate. The resultant mix Ju ia filled into size 2 hard gelatin capsules using a .suitable filling machine.
Claims (25)
1. A pharmaceutical composition comprising a systemic non-steroidal anti-inflammatory drug and ranitidine or a physiologically acceptable salt thereof.
2. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is indomethacin.
3. A pharmaceutical composition as claimed in Claim 2 which contains 10 - 100 mg of indomethacin and 100 - 200 mg of ranitidine or a physiologically acceptable salt thereof per unit dose.
4. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is ibuprofen.
5. A pharmaceutical composition as claimed in Claim 4 which contains 100 - 500 mg of ibuprofen and 10 - 200 mg of ranitidine or a physiologically acceptable salt thereof per unit dose.
6. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is aspirin.
7. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is fenoprofen. S. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is ketoprofen. S. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is naproxen.
8. 10. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is mefenamic acid. 5 -11 4 S
9. 11. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is diflunisal.
10. 12. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is benorylate. 5
11. 13. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is azapropazone.
12. 14. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is diclofenac.
13. 15. A pharmaceutical composition as claimed in Claim 1 10 in which the anti-inflammatory drug is fenbufen.
14. 16. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is feprazone.
15. 17. A pharmaceutical composition as claimed in Claim I in which the anti-inflammatory drug is fenclofenac. 15
16. 18. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is flufenamic acid.
17. 19. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is flurbiprofen.
18. 20. A pharmaceutical composition as claimed in Claim 1 20 in which the anti-inflammatory drug is oxyphenbutazone.
19. 21. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is phenylbutazone.
20. 22. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is piroxicam.
21. 23. A pharmaceutical composition as claimed in claim 1 in which the anti-inflammatory drug is sulindac.
22. 24. A pharmaceutical composition as claimed in Claim 1 in which the anti-inflammatory drug is tolmetin. 5
23. 25. A pharmaceutical composition as claimed in any of Claims 1 to 24 also including at least one pharmaceutical carrier or excipient.
24. 26. A pharmaceutical composition as claimed m any of Claims 1 to 25 in a form suitable for oral or rectal 10 administration.
25. 27. A pharmaceutical composition as claimed in any of Claims 1 to 26 in which the ranitidine is used in the form of the hydrochloride salt.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB8126786 | 1981-09-04 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IE822152L IE822152L (en) | 1983-03-04 |
| IE54149B1 true IE54149B1 (en) | 1989-07-05 |
Family
ID=10524316
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IE2152/82A IE54149B1 (en) | 1981-09-04 | 1982-09-03 | Pharmaceutical compositions |
Country Status (15)
| Country | Link |
|---|---|
| JP (1) | JPS5865215A (en) |
| AU (1) | AU564018B2 (en) |
| BE (1) | BE894285A (en) |
| CH (1) | CH652304A5 (en) |
| DE (1) | DE3232830C2 (en) |
| FR (1) | FR2512342B1 (en) |
| HK (1) | HK91387A (en) |
| IE (1) | IE54149B1 (en) |
| IT (1) | IT1208432B (en) |
| KE (1) | KE3739A (en) |
| MY (1) | MY8700560A (en) |
| NL (1) | NL193821C (en) |
| SE (1) | SE8205034L (en) |
| SG (1) | SG59387G (en) |
| ZA (1) | ZA826477B (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8516083D0 (en) * | 1985-06-25 | 1985-07-31 | Glaxo Group Ltd | Heterocyclic compounds |
| JPH01197444A (en) * | 1986-03-04 | 1989-08-09 | Bristol Myers Co | Effect of combination of beta-adrenergic agent to damage of digestive tract generated by non-steroidal anti-inflammatory composition and certain kind of histamine h1-and/or h2-receptor blocker |
| FR2636532B1 (en) * | 1988-09-20 | 1993-11-19 | Glaxo Group Ltd | PHARMACEUTICAL COMPOSITIONS |
| EP1171161A1 (en) * | 1999-04-19 | 2002-01-16 | Richard Weisbart | Treatment of adult rheumatoid arthritis by oral administration of pooled human immunoglobulin and an antacid |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2360306A1 (en) * | 1976-08-03 | 1978-03-03 | Huguet Georgette | Analgesic and antibacterial agents - esp. for dental application contg. a salicylic acid deriv. and a nitro-furan |
| GB1565966A (en) * | 1976-08-04 | 1980-04-23 | Allen & Hanburys Ltd | Aminoalkyl furan derivatives |
-
1982
- 1982-09-02 BE BE0/208936A patent/BE894285A/en not_active IP Right Cessation
- 1982-09-03 DE DE3232830A patent/DE3232830C2/en not_active Expired - Lifetime
- 1982-09-03 SE SE8205034A patent/SE8205034L/en unknown
- 1982-09-03 FR FR8215042A patent/FR2512342B1/en not_active Expired
- 1982-09-03 ZA ZA826477A patent/ZA826477B/en unknown
- 1982-09-03 NL NL8203457A patent/NL193821C/en not_active IP Right Cessation
- 1982-09-03 IE IE2152/82A patent/IE54149B1/en not_active IP Right Cessation
- 1982-09-03 JP JP57153791A patent/JPS5865215A/en active Pending
- 1982-09-03 CH CH5245/82A patent/CH652304A5/en not_active IP Right Cessation
- 1982-09-03 AU AU87997/82A patent/AU564018B2/en not_active Expired
- 1982-09-03 IT IT8249071A patent/IT1208432B/en active
-
1987
- 1987-07-10 KE KE3739A patent/KE3739A/en unknown
- 1987-07-22 SG SG593/87A patent/SG59387G/en unknown
- 1987-12-03 HK HK913/87A patent/HK91387A/en not_active IP Right Cessation
- 1987-12-30 MY MY560/87A patent/MY8700560A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MY8700560A (en) | 1987-12-31 |
| HK91387A (en) | 1987-12-11 |
| SE8205034D0 (en) | 1982-09-03 |
| FR2512342A1 (en) | 1983-03-11 |
| NL193821C (en) | 2000-12-04 |
| SG59387G (en) | 1987-10-23 |
| SE8205034L (en) | 1983-03-05 |
| NL8203457A (en) | 1983-04-05 |
| KE3739A (en) | 1987-09-04 |
| JPS5865215A (en) | 1983-04-18 |
| BE894285A (en) | 1983-03-02 |
| DE3232830A1 (en) | 1983-03-24 |
| IT1208432B (en) | 1989-06-12 |
| IT8249071A0 (en) | 1982-09-03 |
| CH652304A5 (en) | 1985-11-15 |
| FR2512342B1 (en) | 1986-09-05 |
| AU564018B2 (en) | 1987-07-30 |
| AU8799782A (en) | 1983-03-10 |
| NL193821B (en) | 2000-08-01 |
| IE822152L (en) | 1983-03-04 |
| ZA826477B (en) | 1984-04-25 |
| DE3232830C2 (en) | 1994-12-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MK9A | Patent expired |