WO2008098329A4 - Pharmaceutical composition, pharmaceutical product, obtaining processes of pharmaceutical compounds and use of such compounds for treating erectile dysfunction - Google Patents
Pharmaceutical composition, pharmaceutical product, obtaining processes of pharmaceutical compounds and use of such compounds for treating erectile dysfunction Download PDFInfo
- Publication number
- WO2008098329A4 WO2008098329A4 PCT/BR2008/000041 BR2008000041W WO2008098329A4 WO 2008098329 A4 WO2008098329 A4 WO 2008098329A4 BR 2008000041 W BR2008000041 W BR 2008000041W WO 2008098329 A4 WO2008098329 A4 WO 2008098329A4
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- pharmaceutical
- obtaining
- compounds
- pharmaceutical composition
- compound
- Prior art date
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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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
Abstract
The present invention generally relates to a process to obtain a compound and a standardized pharmaceutical product from parts of plants of genre Erythroxylum (Erythroxylum vacciniifolium Mart), in the form of isolated extracts, or enriched moieties, or pure compounds, or obtained by synthesis, used isolatedly or in mixture with other natural or synthetic products, in different ratios, comprising pharmaceutical compositions to be used by suitable routes (topic or oral) particularly presented in the form of tablets, capsules, dies, emulsions, W/O and 0/0 (creams and gels), liposomes, microcapsules, nanoparticles, sprays, slurries and the like, used for treating the erectile dysfunction.
Claims
1. Pharmaceutical composition comprising alkaloid compounds, in their free form or as salts pharmaceutically accepted, obtained by synthesis, isolated in mixtures or in the form of the extracts obtained from Erythroxylum vaccinifolium.
2. Pharmaceutical composition, according to claim 1, wherein such alkaloids are of the tropanic group.
3. Pharmaceutical composition, according to claim 1, wherein such compound has following the general chemical structure:
, which may contain one or more radicals R, wherein R1, R2, R3, R4, are the same or different, and each one is independently selected between H, OH, CH3, COCH3, metals alkaline, halogens, sugars, CO (CH2) nCH3, (CH2JnCH3 , which may also be: 38
N-pyrrol (Pc) 
N-methylpyπol (Mpc) Hdmb, 
in the free form or a pharmaceutically acceptable salt, wherein n varies from 2 to 16.
4. Pharmaceutical composition, according to claims 1 and 3, wherein the compounds are in the form of pharmaceutically acceptable salts as, for example, chlorates, sulphate or borates.
5. Pharmaceutical composition, according to claim 1, wherein the starting material comprises the species Erythroxylum vacciniifolium.
6. Pharmaceutical composition, according to claim 1, comprising 0.001 to 99% of the extract in weight of composition total weight.
7. Pharmaceutical composition, according to claim 1, comprising about 0.001 to about 5000 mg of the alkaloidic extract .
8. pharmaceutical composition, according to claim 1, wherein the compounds are used isolatedly or in mixtures thereof or combined with the extracts, fixed oils, essential oils, fragrances, powders or excipients from other natural or synthetic sources, or used under combined form with drug(s), vitamin (s), salt(s), sugar (s) or other pharmaceutically accepted excipients, suitable for oral, topic, injectable or inhalable application.
9. Pharmaceutical composition, according to claim 8, comprising.001% to 99.% of one or more compounds.
10. Pharmaceutical composition, according to claim 1, wherein said composition is encapsulated in hard gelatin capsule or in soft gelatin capsule.
11. Pharmaceutical product wherein said product is presented in the form of pure extract or combined, in the form of tablets, capsules, dies, syrups and the like or in the form of emulsions W/O and 0/0 (creams and gels) , liposomes, microcapsules, nanoparticles, aerosols, spray, slurries and the like, injectable liquids, powders, freeze- dried, patches, as well as formulations for controlled release implants, or the like used as adjuvants and other synthetic or natural pharmaceutically accepted carriers.
12. Pharmaceutical product, comprising a pharmaceutical composition, according to claim 1, which is a phytotherapic, or synthetic medicament.
13. Process for obtaining a phytotherapic composition wherein said compound may be obtained by the following ways: (a) from standardized extracts, moieties or molecules of plants of species E. vacciniifolium; (b) by semi-synthesis from the extracts of plants of species E. vacciniifolium; (c) by semi-synthesis from scopolamine, (d) by synthesis from 3-hydroxy-tropanol, or 3, 6-dihydroxy- tropanol, 3, 7-dihydroxy-tropanol, or 3,6,7- trihydroxytropanol and (and) by semi-synthesis from 6β- hydroxy-hiosciamine .
14. Process for obtaining the pharmaceutical compound, according to claim 13, comprising in items (a) and (b) the following steps:
(a) Spraying, or grinding, or slicing or branning one or more parts of plants of genre Erythroxylum, as well as, roots, stems, skins, and leaves; green or dried;
(b) Extraction of the compounds by percolation, or maceration, or Soxlet, or using gases in supercritical state, using basic or acid media, or in aqueous media, or using organic solvents, alone or mixtures thereof.
15. Process for obtaining the pharmaceutical compound, according to claim 14, wherein the extraction in step (b) is achieved with strong or weak, diluted or concentrated acids, as in mixtures, as, for example, the acetic acid, the hydrochloridic acid, the formic acid and the base used in the extraction process comprises concentrated or diluted bases, alone or in mixtures as for example, the ammonium hydroxide (NH4OH) and sodium carbonate (Na2CO3) .
16. Process for obtaining the pharmaceutical compound, according to claim 14, wherein the extraction in step (b) uses an organic solvent comprising halogenated compounds, alcohols, aldehydes, ethers, esters, ketones, alkane, cycloalkane, phenolic compounds, benzenes and derivatives, alone or mixtures thereof.
17. Process for obtaining the pharmaceutical compound, according to claim 13 wherein the concentration of the organic solution is performed by means of a system at reduced pressure, or spray-dryer, or at room temperature. 41
18. Process for obtaining the pharmaceutical compound, according to claim 17, wherein inlet and outlet temperatures, of the process of concentration by spray- dryer, is between 150-1900C and 80-90°C respectively.
19. Process for obtaining the pharmaceutical compound, according to claim 17, wherein the temperature of the system at reduced pressure is from 25-100°C.
20. process for obtaining the pharmaceutical compound, according to claim 13, wherein organic partition containing the tropanic alkaloids, in processes (b) , (c ) , (d) , and (e) , is subjected to the a reaction of esterification with N-methylpyrrol acid or methylpyrrol acid chlorides and then pyridine and N-methylpyrrol acid chloride are added under stirring in inert atmosphere.
21. Process for obtaining the pharmaceutical compound, according to claim 13, wherein scopolamine and ββ- hydroxy-hiosciamine, in processes (c) and (e) respectively, are solved in an acid solution at pH 1.0-3.5.
22. Process for obtaining the pharmaceutical compound, according to claim 13, wherein 3-hydroxytropanol, or 3, 6-dihydroxy-tropanol, 3, 7-dihydroxy-tropanol or 3,6,7- trihydroxytropanol, in item (d) , are solved in an anhydrous organic solvent.
23. Process for obtaining the pharmaceutical composition, according to claim 13, comprising in processes (b) , (c) and (and) , a step of hydrolysis under reflux.
24. Process for obtaining the composition pharmaceutical, according to claim 23 wherein reflux temperature is between 50° and 1000C. 42
25. Process for obtaining the pharmaceutical compound, according to claim 13, wherein the solution which contains the tropanic alkaloids, in processes (b) and (e) , is basified to neuter pH using a concentrated or diluted basic solution.
26. Process for obtaining the pharmaceutical compound, according to claim 13, wherein separation and purification of the compounds are performed by chromatographic techniques with or without pressure, as for example, chromatography at atmospheric pressure, chromatography at low, medium or high pressure, using normal stationary phase as silica gel or reverse phase as C-8 or C- 18, or liquid/liquid partition as upstream chromatography, or the centrifugal partition, or using ion exchange resins or filtration membranes. ς
27. , Process for obtaining the pharmaceutical compound, according to claim 26, wherein said process results in at least one of the alkaloids in free form or in the form of salts, of chemical structure I, containing one or more radicals R1, R2, R3, R4, being the same or different and each one being independently selected from H, OH, CH3, COCH3, alkaline metals, halogens, monosaccharides, disaccharides or polysaccharides, CO (CH2) nCH3, (CH2) nCH3 and also N-pyrrol (Pc), N-methylpyrrol (Mpc) , COCH2Ph-3-OH and Hdmb.
28. Process for obtaining the pharmaceutical compound, according to claim 13, wherein starting compounds, in processes (c) , (d) and (e) , are in their free form or in the form of salts. 43
29. Pharmaceutical composition used in the treatment of erectile dysfunction comprising one or more compounds obtained by one or more of the processes of claim 13, in their free form or salts pharmaceutically accepted.
30. Use of a pharmaceutical composition isolated or in mixture thereof at different ratios or in mixture with other natural or synthetic products, in different ratios, wherein said composition integrates pharmaceutical compositions to be used by suitable routes (topic, oral, injectable) particularly presented in the form of tablets, capsules, dies, emulsions, The/The and The/The (creams and gels), liposomes, microcapsules, nanocapsules, sprays, slurries and the like, used for treating the erectile dysfunction.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| BRPI0705772-5A BRPI0705772A (en) | 2007-02-13 | 2007-02-13 | pharmaceutical composition, pharmaceutical product, processes for obtaining pharmaceutical compounds and use of such compounds for the treatment of erectile dysfunction |
| BRPI0705772-5 | 2007-02-13 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| WO2008098329A2 WO2008098329A2 (en) | 2008-08-21 |
| WO2008098329A8 WO2008098329A8 (en) | 2008-10-23 |
| WO2008098329A3 WO2008098329A3 (en) | 2009-02-05 |
| WO2008098329A4 true WO2008098329A4 (en) | 2009-03-26 |
Family
ID=39690569
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/BR2008/000041 WO2008098329A2 (en) | 2007-02-13 | 2008-02-13 | Pharmaceutical composition, pharmaceutical product, obtaining processes of pharmaceutical compounds and use of such compounds for treating erectile dysfunction |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR065339A1 (en) |
| BR (1) | BRPI0705772A (en) |
| WO (1) | WO2008098329A2 (en) |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2001322941A (en) * | 2000-05-15 | 2001-11-20 | Kose Corp | Skin care preparation |
| WO2006021930A2 (en) * | 2004-08-25 | 2006-03-02 | Femi-X A/S | Aphrodisiac herbal composition for a female comprising epimedium grandiflorum, turnera diffusa var. aphrodisiaca, ilex paraguariensis and smilax spp |
| CN101016283B (en) * | 2007-03-07 | 2010-07-28 | 福州聚英医药有限公司 | Preparation of yanhuning |
-
2007
- 2007-02-13 BR BRPI0705772-5A patent/BRPI0705772A/en not_active Application Discontinuation
-
2008
- 2008-02-13 AR ARP080100622A patent/AR065339A1/en unknown
- 2008-02-13 WO PCT/BR2008/000041 patent/WO2008098329A2/en active Application Filing
Also Published As
| Publication number | Publication date |
|---|---|
| WO2008098329A2 (en) | 2008-08-21 |
| BRPI0705772A (en) | 2008-09-30 |
| WO2008098329A8 (en) | 2008-10-23 |
| WO2008098329A3 (en) | 2009-02-05 |
| AR065339A1 (en) | 2009-06-03 |
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