AR080678A1 - NEW POLYMORPHIC FORMS OF AGOMELATIN, ITS OBTAINING PROCEDURES AND PHARMACEUTICAL COMPOSITIONS - Google Patents
NEW POLYMORPHIC FORMS OF AGOMELATIN, ITS OBTAINING PROCEDURES AND PHARMACEUTICAL COMPOSITIONSInfo
- Publication number
- AR080678A1 AR080678A1 ARP110100740A ARP110100740A AR080678A1 AR 080678 A1 AR080678 A1 AR 080678A1 AR P110100740 A ARP110100740 A AR P110100740A AR P110100740 A ARP110100740 A AR P110100740A AR 080678 A1 AR080678 A1 AR 080678A1
- Authority
- AR
- Argentina
- Prior art keywords
- agomelatine
- crystalline form
- compound
- ray diffraction
- diffraction pattern
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 2
- YJYPHIXNFHFHND-UHFFFAOYSA-N agomelatine Chemical compound C1=CC=C(CCNC(C)=O)C2=CC(OC)=CC=C21 YJYPHIXNFHFHND-UHFFFAOYSA-N 0.000 abstract 12
- 229960002629 agomelatine Drugs 0.000 abstract 12
- 150000001875 compounds Chemical class 0.000 abstract 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 4
- 238000002441 X-ray diffraction Methods 0.000 abstract 3
- 238000001816 cooling Methods 0.000 abstract 2
- 238000001914 filtration Methods 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 2
- 239000007787 solid Substances 0.000 abstract 2
Landscapes
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
La presente se relaciona con polimorfos de agomelatina, los cuales se denominan en la presente como formas cristalinas a y b. La presente se relaciona, además, con procedimientos para preparar las formas cristalinas a y b de agomelatina y las composiciones farmacéuticas que los comprenden. Reivindicacion 1: Un compuesto, el cual es la forma cristalina a de agomelatina, el cual tiene, de manera sustancial, el mismo patron de difraccion de rayos X que se muestra en la figura 1. Reivindicacion 2: El compuesto de la reivindicacion 1, que tiene un patron de difraccion de rayos X que comprende picos a 16.85, 18.30, 18.70, 19.63, 19.73, 20.12, 20.91, 21.80, 23.75, 23.87, 24.94, 25.59 y 33.68 +- 0.1 grados 2q. Reivindicacion 4: Un procedimiento para preparar la forma cristalina a de agomelatina, que comprende las etapas de: a) disolver agomelatina en 2 volumenes / peso de agua a 98 - 100sC, b) enfriar gradualmente la solucion resultante hasta 25sC y c) filtrar los solidos resultantes, lavarlos con agua y secarlos a 45sC, durante 1 hora, bajo presion reducida. Reivindicacion 5: Un compuesto, el cual es la forma cristalina b de agomelatina el cual tiene, de manera sustancial, el mismo patron de difraccion rayos X que se muestra en la figura 3. Reivindicacion 6: El compuesto de la reivindicacion 5, que tiene un patron de difraccion de rayos que comprende los picos a 10.55, 17.85, 19.37, 20.07, 23.39, 24.96 y 26.11 +- 0.1 grados 2q. Reivindicacion 8: Un procedimiento para preparar la forma cristalina b de agomelatina, el cual comprende las etapas de: a) disolver agomelatina en 10 volumenes / pesos de agua a 100 - 103sC, b) enfriar gradualmente la solucion resultante hasta 25sC, c) filtrar los solidos resultantes, lavarlos con agua y secarlos a 50 - 55sC, durante 1 hora, bajo presion reducida. Reivindicacion 9: Una composicion farmacéutica de agomelatina que comprende la forma cristalina a de agomelatina y excipientes farmacéuticamente aceptables. Reivindicacion 10: Una composicion farmacéutica de agomelatina que comprende la forma cristalina b de agomelatina y excipientes farmacéuticamente aceptables.This is related to agomelatine polymorphs, which are referred to herein as crystalline forms a and b. This also relates to methods for preparing the crystalline forms a and b of agomelatine and the pharmaceutical compositions comprising them. Claim 1: A compound, which is the crystalline form a of agomelatine, which has substantially the same X-ray diffraction pattern as shown in Figure 1. Claim 2: The compound of claim 1, which has an X-ray diffraction pattern that includes peaks at 16.85, 18.30, 18.70, 19.63, 19.73, 20.12, 20.91, 21.80, 23.75, 23.87, 24.94, 25.59 and 33.68 + - 0.1 degrees 2q. Claim 4: A process for preparing the crystalline form a of agomelatine, comprising the steps of: a) dissolving agomelatine in 2 volumes / weight of water at 98-100sC, b) gradually cooling the resulting solution to 25sC and c) filtering the solids resulting, wash them with water and dry at 45sC, for 1 hour, under reduced pressure. Claim 5: A compound, which is the crystalline form b of agomelatine which substantially has the same X-ray diffraction pattern shown in Figure 3. Claim 6: The compound of claim 5, which has a ray diffraction pattern comprising the peaks at 10.55, 17.85, 19.37, 20.07, 23.39, 24.96 and 26.11 + - 0.1 degrees 2q. Claim 8: A process for preparing the crystalline form b of agomelatine, which comprises the steps of: a) dissolving agomelatine in 10 volumes / weights of water at 100-103sC, b) gradually cooling the resulting solution to 25sC, c) filtering the resulting solids, wash them with water and dry them at 50-55sC, for 1 hour, under reduced pressure. Claim 9: A pharmaceutical composition of agomelatine comprising the crystalline form a of agomelatine and pharmaceutically acceptable excipients. Claim 10: A pharmaceutical composition of agomelatine comprising the crystalline form b of agomelatine and pharmaceutically acceptable excipients.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN3249CH2010 | 2010-11-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR080678A1 true AR080678A1 (en) | 2012-05-02 |
Family
ID=46160731
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100740A AR080678A1 (en) | 2010-11-29 | 2011-03-10 | NEW POLYMORPHIC FORMS OF AGOMELATIN, ITS OBTAINING PROCEDURES AND PHARMACEUTICAL COMPOSITIONS |
Country Status (1)
| Country | Link |
|---|---|
| AR (1) | AR080678A1 (en) |
-
2011
- 2011-03-10 AR ARP110100740A patent/AR080678A1/en unknown
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