WO2001049261A2 - Solution aqueuse stable de deoxyfructosazine - Google Patents
Solution aqueuse stable de deoxyfructosazine Download PDFInfo
- Publication number
- WO2001049261A2 WO2001049261A2 PCT/FR2001/000015 FR0100015W WO0149261A2 WO 2001049261 A2 WO2001049261 A2 WO 2001049261A2 FR 0100015 W FR0100015 W FR 0100015W WO 0149261 A2 WO0149261 A2 WO 0149261A2
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- solution according
- acid
- deoxyfructosazine
- solution
- pharmaceutically acceptable
- 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.)
- Ceased
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
Definitions
- the present invention relates to a stable aqueous solution of deoxyfructosazine in particular for its pharmaceutical use for oral administration.
- Deoxyfructosazine or (2 - [(1R, 2S, 3R) (1,2,3,4-tetrahydroxybutyl] -5- [2'S, 3'R) (2 ', 3', 4'-trihydroxybutylpyrazine)] is known for its anti-diabetic properties (WO97 / 28813).
- aqueous solutions and in particular those for oral administration must be physicochemically stable for several weeks or months and this, under conditions of variable temperature.
- the aqueous solutions of deoxyfructosazine must have a pH of 3 to 5 and preferably of 3.5 to 4.5 and more particularly of 4.
- the pH of the aqueous solution is obtained using a pharmaceutically acceptable acid or a pharmaceutically acceptable buffer system comprising an acid and a base.
- a pharmaceutically acceptable acid use may be made, for example, of citric acid, phosphoric acid, acetic acid and tartaric acid.
- the base of the buffer system it is possible to use, in particular, trisodium citrate, disodium phosphate, disodium tartrate, sodium acetate and sodium hydroxide.
- the aqueous solution of deoxyfructosazine is brought to the pH from 3 to 5 and, preferably from 3.5 to 4.5 and, more particularly, from 4 by means of a buffer system.
- citric acid and trisodium citrate or phosphoric acid and sodium hydroxide systems may be mentioned.
- the amount of deoxyfructosazine in the oral solution is from 1 to 150 mg / ml and, in particular from 10 to 100 mg / ml.
- a deoxyfructosazine solution (1 mg / ml) is prepared from an aqueous 0.05M phosphoric acid solution. Samples of the solution are adjusted to pH 2, 3, 4, 5, 6, 7, 8 and 9 by adding sodium hydroxide. The solutions thus obtained are stored in glass vials protected from light at 4 ° C (control solution), 25 ° C, 45 ° C and 60 ° C. After 2, 7 and 15 days, the samples are diluted 5 times with 20 mM phosphate buffer, pH7 and the stability is examined by high pressure liquid chromatography (HPLC).
- HPLC high pressure liquid chromatography
- FIG. 1 shows the percentages of the degradation products A and B formed at different pHs after storage of the aqueous solutions for 15 days at 45 ° C.
- FIG. 2 shows the percentages of the degradation products A and B formed at different pHs after storage of the aqueous solutions for 15 days at 60 ° C.
- FIG. 3 shows the variation in the formation of the degradation product A after storage of aqueous solutions at pH 2, 3 and 4 for 15 days at 25 ° C, 45 ° C and 60 ° C.
- FIG. 4 shows the variation in the formation of the degradation product B after storage of aqueous solutions at pH 2, 3 and 4 for 15 days at 25 ° C, 45 ° C and 60 ° C.
- FIG. 5 shows the variation in the formation of the degradation product A as a function of the storage time of the aqueous solutions at pH 2 to 4 of solutions at 45 and 60 ° C.
- FIG. 6 shows the variation in the formation of the degradation product B as a function of the storage time of the aqueous solutions at pH 5 to 9 of solutions at 45 ° C.
- FIG. 7 shows the variation in the formation of the degradation product B as a function of the storage time of the aqueous solutions at pH 5 to 9 of solutions at 60 ° C.
- Solutions for oral administration may contain buffers such as those mentioned above, diluents, for example ethanol, propylene glycol and glycerin, sweetening products such as sodium saccharin, cyclamate, thickeners such as sucrose (sucrose ), cellulose derivatives, Lycasin R and sorbitol, water-soluble flavorings, microbial preservatives such as sodium benzoate, benzoic acid and colorants. They can possibly be sterilized by any method known to those skilled in the art and which allows not to degrade the solution.
- diluents for example ethanol, propylene glycol and glycerin
- sweetening products such as sodium saccharin, cyclamate
- thickeners such as sucrose (sucrose ), cellulose derivatives, Lycasin R and sorbitol
- water-soluble flavorings such as sodium benzoate, benzoic acid and colorants.
- citric acid monohydrate 50 mg trisodium citrate dihydrate 20 mg sodium benzoate 5 mg sodium saccharin 2 ⁇ l pineapple flavoring 0.8 mg caramel 0.1 mg riboflavin demineralized water in sufficient quantity per 10 ml of solution
- the solutions according to the invention can be prepared by dissolving, with stirring, at a temperature in the region of 20 ° C, deoxyfructosazine and any excipients in distilled water and adjusting the pH using a pharmaceutically acid. acceptable. If a buffer system is used, it is also possible to dissolve the deoxyfructosazine and the possible excipients in distilled water containing a pharmaceutically acceptable acid and adjust the pH by means of the base of the buffer system.
Landscapes
- Health & Medical Sciences (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)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Saccharide Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
Description
Claims
Priority Applications (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CA002396180A CA2396180C (fr) | 2000-01-06 | 2001-01-03 | Solution aqueuse stable de deoxyfructosazine |
| AU31831/01A AU3183101A (en) | 2000-01-06 | 2001-01-03 | Stable aqueous deoxyfructosazine solution |
| DE60109889T DE60109889T2 (de) | 2000-01-06 | 2001-01-03 | Stabile wässrige lösung von deoxyfructosazine |
| AT01903860T ATE292474T1 (de) | 2000-01-06 | 2001-01-03 | Stabile wässrige lösung von deoxyfructosazine |
| EP01903860A EP1248652B1 (fr) | 2000-01-06 | 2001-01-03 | Solution aqueuse stable de deoxyfructosazine |
| JP2001549629A JP4898048B2 (ja) | 2000-01-06 | 2001-01-03 | 安定な水性デオキシフルクトサジン溶液 |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0000138A FR2803515B1 (fr) | 2000-01-06 | 2000-01-06 | Solution aqueuse stable de deoxyfructosazine |
| FR00/00138 | 2000-01-06 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2001049261A2 true WO2001049261A2 (fr) | 2001-07-12 |
| WO2001049261A3 WO2001049261A3 (fr) | 2002-03-07 |
Family
ID=8845670
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/FR2001/000015 Ceased WO2001049261A2 (fr) | 2000-01-06 | 2001-01-03 | Solution aqueuse stable de deoxyfructosazine |
Country Status (10)
| Country | Link |
|---|---|
| EP (1) | EP1248652B1 (fr) |
| JP (1) | JP4898048B2 (fr) |
| AR (1) | AR026805A1 (fr) |
| AT (1) | ATE292474T1 (fr) |
| AU (1) | AU3183101A (fr) |
| CA (1) | CA2396180C (fr) |
| DE (1) | DE60109889T2 (fr) |
| ES (1) | ES2238418T3 (fr) |
| FR (1) | FR2803515B1 (fr) |
| WO (1) | WO2001049261A2 (fr) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10030338B2 (en) | 2014-03-04 | 2018-07-24 | William P. Dempsey | Compositions and methods for pelletized recycled asphalt shingles |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2744365B1 (fr) * | 1996-02-06 | 1998-02-27 | Inst Malgache Rech Appl | Melanges isolables a partir de graines d'eugenia jambolana lamarck, leur preparation et l'utilisation de ces melanges et certains de leurs constituants comme medicaments |
-
2000
- 2000-01-06 FR FR0000138A patent/FR2803515B1/fr not_active Expired - Fee Related
-
2001
- 2001-01-03 DE DE60109889T patent/DE60109889T2/de not_active Expired - Lifetime
- 2001-01-03 WO PCT/FR2001/000015 patent/WO2001049261A2/fr not_active Ceased
- 2001-01-03 AT AT01903860T patent/ATE292474T1/de not_active IP Right Cessation
- 2001-01-03 JP JP2001549629A patent/JP4898048B2/ja not_active Expired - Fee Related
- 2001-01-03 AU AU31831/01A patent/AU3183101A/en not_active Abandoned
- 2001-01-03 CA CA002396180A patent/CA2396180C/fr not_active Expired - Fee Related
- 2001-01-03 ES ES01903860T patent/ES2238418T3/es not_active Expired - Lifetime
- 2001-01-03 EP EP01903860A patent/EP1248652B1/fr not_active Expired - Lifetime
- 2001-01-05 AR ARP010100055A patent/AR026805A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| FR2803515B1 (fr) | 2002-08-02 |
| WO2001049261A3 (fr) | 2002-03-07 |
| EP1248652B1 (fr) | 2005-04-06 |
| JP2003519170A (ja) | 2003-06-17 |
| JP4898048B2 (ja) | 2012-03-14 |
| AU3183101A (en) | 2001-07-16 |
| FR2803515A1 (fr) | 2001-07-13 |
| AR026805A1 (es) | 2003-02-26 |
| CA2396180A1 (fr) | 2001-07-12 |
| ATE292474T1 (de) | 2005-04-15 |
| ES2238418T3 (es) | 2005-09-01 |
| CA2396180C (fr) | 2009-06-16 |
| DE60109889T2 (de) | 2006-02-09 |
| EP1248652A2 (fr) | 2002-10-16 |
| DE60109889D1 (de) | 2005-05-12 |
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