GB2105988A - Anti-platelet aggregation dipyridamole with Al aspirin - Google Patents
Anti-platelet aggregation dipyridamole with Al aspirin Download PDFInfo
- Publication number
- GB2105988A GB2105988A GB08210802A GB8210802A GB2105988A GB 2105988 A GB2105988 A GB 2105988A GB 08210802 A GB08210802 A GB 08210802A GB 8210802 A GB8210802 A GB 8210802A GB 2105988 A GB2105988 A GB 2105988A
- Authority
- GB
- United Kingdom
- Prior art keywords
- dipyridamole
- platelet aggregation
- acid
- acetylsalycilic
- aluminium salt
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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
- A61K31/60—Salicylic acid; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- 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)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (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)
- Medicinal Preparation (AREA)
Abstract
A stabilised pharmaceutical composition for combatting platelet aggregation comprises dipyridamole and acetylsalycilic acid aluminium salt.
Description
SPECIFICATION
A pharmaceutical composition for combatting platelet aggregation
This invention relates to a pharmaceutical composition for combatting platelet aggregation. The active substances of the said composition are dipyridamole and acetylsalycilic acid aluminium salt.
Dipyridamole is the trivial name for 2,6 - bis (diethanolamino) - 4,8 - dipyperidinopyrimido - 4 - d) - pyrimidine.
The association of dipyridamole and acetylsalicilic acid is for combatting platelet aggregation and has a high pharmacological value in the preventive treatment of myocardial infarction and also in post-infarction treatment. The usual weight ratios of dipyridamole and acetylsalycilic acid used lie between 1/3 and 1/10.
From the point of view of pharmaceutical preparation, up to now it has not been possible simply to mix these substances, because of the hydrolysis that the acetylsalycilic acid undergoes in the presence of dipyridamole.
Several solutions have been investigated, among them: the association of a dipyridamoletablet inside a gelatine capsule containing the acetylsalycilic acid; modifications of the dipyridamoleformula with the formation of salts; the formation of granulates coated with inert products before mixing the two components.
A pharmaceutically stable composition of the said active substances has been found which is characterised by mixing the dipyridamole with the aluminium salt of acetylsalycilic acid.
The acetylsalycilic acid aluminium salt is the basic salt C18H1AlO9
having an 89% theoretical acetylsaiycilic acid content which, in practice, scarcely exceeds 75%, since polymerised products are formed in the majority of aluminium salts.
The hydrolysis of acetyisalycilic acid provides salycilic acid evidenced by an increase in the absorbance (around 308 nm) of the methanol-acetic solution thereof and by an increase in staining by ferric chloride, due to the presence of the phenol function.
With these two parameters, there may be studied the stability of the pharmaceutical composition according to the invention, after submitting it to accelerated stability tests at a temperature of 40"C for periods of time of two months.
With this stability criterion, there are offered several examples of pharmaceutical forms for a pharmacological association of dipyridamole and acetylsalycilic acid aluminium salt, at a rate of 113 to 1/10. These examples are given simply as illustrative and non-restrictive examples.
EXAMPLE 1
Tablet
A tablet was prepared with the following mixture by direct compression:
Dipyridamole 75 mg
Acetylsalycilic acid aluminium salt 419 mg
Starch 150mg Polyvinyl pyrrolidone 19 mg
Talc 32 mg
Alrosil 300 2 mg
Total 697 mg
After two months at 40"C, the pharmaceutical form contained the same level of acetylsalycilic acid.
EXAMPLE 2
Mixture for extemporaneous aqueous suspension
For a dose of 5 ml of liquid extemporaneous suspension, the following powder mix was prepared:
Dipyridamole 75 mg
Acetylsalycilic acid aluminium salt 420 mg
Citric acid 5 mg
Sodium benzoate 5 mg
Carboxy methyl cellulose 60 mg
Suchrose 2500 mg
Total 3065 mg
There was no evidence of hydrolysis of the acetylsalycilic acid after holding the powders for two months at 40"C.
After preparation of the suspension with the corresponding water addition, there was a hydrolysis inferior to 10% after eight days in a refrigerator.
EXAMPLE 3
Gelatine capsules
The following powder mix was prepared:
Dipyridamole 37.5 mg
Acetylsalycilic acid aluminium salt 210.0 mg
Starch 8.3 mg
Alrosil 300 1.2 mg
Total 257.0 mg and after mixing was placed in gelatine capsules.
After holding the capsule for two months at 40"C, there was no evidence of hydrolysis of the acety
Isalycilic acid.
EXAMPLE 4
Single dose in sachets
The following powder mix was prepared for placement in sachets:
Dipyridamole 75 mg
Acetylsalycilic acid aluminium salt 419 mg
Starch 2506 mg
Total 3000 mg
After holding the mixture at a temperature of 40"C for two months, there was no evidence of hydrolysis of the acetylsalycilic acid.
Claims (4)
1. Pharmaceutical composition for combatting platelet aggregation, characterised in that it comprises dipyridamole and acetylsalycilic acid aluminium salt.
2. The composition of claim 1, characterised in that the weight ratio of dipyridamole and acetylsalycilic acid aluminium salt is from 1/3 to 1/10.
3. A pharmaceutical composition substantially as hereinbefore described in any one of Examples 1 to
4.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR8117659A FR2513118A1 (en) | 1981-09-18 | 1981-09-18 | PHARMACEUTICAL COMPOSITION BASED ON DIPYRIDAMOL AND ALUMINUM SALT OF ACETYLSALICYLIC ACID TO COMBAT PLATELET AGGREGATION |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| GB2105988A true GB2105988A (en) | 1983-04-07 |
| GB2105988B GB2105988B (en) | 1985-05-30 |
Family
ID=9262274
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| GB08210802A Expired GB2105988B (en) | 1981-09-18 | 1982-04-14 | Anti-platelet aggregation dipyridamole with al aspirin |
Country Status (6)
| Country | Link |
|---|---|
| JP (1) | JPS5862114A (en) |
| CH (1) | CH651207A5 (en) |
| DE (1) | DE3230834A1 (en) |
| FR (1) | FR2513118A1 (en) |
| GB (1) | GB2105988B (en) |
| IT (1) | IT1157271B (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4850489A (en) * | 1986-07-11 | 1989-07-25 | Hoechst Aktiengesellschaft | Dispensing packs containing pharmaceutical combinations for sequential administration |
| WO1998057643A1 (en) * | 1997-06-16 | 1998-12-23 | Janssen Pharmaceutica N.V. | Use of draflazine-analogues for treating pain |
| EP1061908A1 (en) * | 1998-03-13 | 2000-12-27 | Merck & Co., Inc. | Combination therapy and composition for acute coronary ischemic syndrome and related conditions |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3627423A1 (en) * | 1986-08-13 | 1988-02-18 | Thomae Gmbh Dr K | MEDICINAL PRODUCTS CONTAINING DIPYRIDAMOL OR MOPIDAMOL AND O-ACETYLSALICYL ACID OR THEIR PHYSIOLOGICALLY COMPATIBLE SALTS, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE FOR COMBATING THROMBUS FORMATION |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2368280A1 (en) * | 1976-10-20 | 1978-05-19 | Theramex | Aspirin and dipyridamole salt compsn. - having blood platelet aggregation inhibitory activity |
| LU77353A1 (en) * | 1977-05-16 | 1979-01-19 |
-
1981
- 1981-09-18 FR FR8117659A patent/FR2513118A1/en active Pending
-
1982
- 1982-04-14 GB GB08210802A patent/GB2105988B/en not_active Expired
- 1982-05-06 IT IT21120/82A patent/IT1157271B/en active
- 1982-05-21 JP JP57085043A patent/JPS5862114A/en active Pending
- 1982-05-25 CH CH3208/82A patent/CH651207A5/en not_active IP Right Cessation
- 1982-08-19 DE DE3230834A patent/DE3230834A1/en not_active Withdrawn
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4850489A (en) * | 1986-07-11 | 1989-07-25 | Hoechst Aktiengesellschaft | Dispensing packs containing pharmaceutical combinations for sequential administration |
| WO1998057643A1 (en) * | 1997-06-16 | 1998-12-23 | Janssen Pharmaceutica N.V. | Use of draflazine-analogues for treating pain |
| US6403589B1 (en) | 1997-06-16 | 2002-06-11 | Janssen Pharmaceutica N.V. | Method of treating pain with draflazine-analogues |
| EP1061908A1 (en) * | 1998-03-13 | 2000-12-27 | Merck & Co., Inc. | Combination therapy and composition for acute coronary ischemic syndrome and related conditions |
| EP1061908A4 (en) * | 1998-03-13 | 2007-01-24 | Merck & Co Inc | Combination therapy and composition for acute coronary ischemic syndrome and related conditions |
Also Published As
| Publication number | Publication date |
|---|---|
| IT8221120A0 (en) | 1982-05-06 |
| DE3230834A1 (en) | 1983-03-31 |
| JPS5862114A (en) | 1983-04-13 |
| IT1157271B (en) | 1987-02-11 |
| FR2513118A1 (en) | 1983-03-25 |
| GB2105988B (en) | 1985-05-30 |
| CH651207A5 (en) | 1985-09-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PCNP | Patent ceased through non-payment of renewal fee |