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Tablet formulations and processes

A technology for pharmaceutical preparations and medicaments, which is applied in the directions of pill delivery, block delivery, etc.

Inactive Publication Date: 2009-03-25
WYETH LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The exact reason why the same compounds have cell-specific effects has not been elucidated, but it is thought that it may be due to differences in receptor configuration and / or being in the context of coordinating proteins

Method used

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  • Tablet formulations and processes
  • Tablet formulations and processes
  • Tablet formulations and processes

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0441] Preparation of anhydrate crystalline form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol

[0442] Dissolve the solid of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol (170 g, 0.627 mol) in ethyl acetate at 75-80°C ester (3946 g, 23 vol). The resulting solution was treated with charcoal (17 g) at 75-80°C. The filtrate was then concentrated to 7 volumes at atmospheric pressure, heptane (793 g, 6 volumes) was added to the slurry maintained at 75-80 °C, then cooled to 45-50 °C and maintained for 0.5 hours, followed by cooling to 0-5 °C and maintained for 1 hour. The solids were filtered off and dried at 55-65°C and 5-10 mg Hg to give 87% recovery with a product purity of 99.4%.

Embodiment 2

[0444]Preparation of monohydrate crystalline form of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol

[0445] Put 274 g of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol and 1375 ml of pre-filtered ethanol into a tank equipped with stir bar, condenser and temperature Probe inside a 3 L multi-neck flask. The mixture was heated to 75-80°C and a solution formed after 10 minutes. Water (688ml) was added to the solution during 0.5 hours at 75-80°C. The solution was cooled to 50°C over the course of 0.5 hours and then maintained at 50°C for 0.5 hours (crystallization started at about 74°C). The resulting suspension was then cooled to 0-5°C over the course of 0.5 hours and maintained at 0-5°C for 1 hour. The solid was collected by filtration and the filter cake was washed with 2 x 300 ml of ethanol:water (2:1 v / v) pre-cooled to 0-5°C. The washed filter cake was dried at 32-38°C and 20-25 mg Hg for 20 hours to yield 281.8 g (96.11% yield) of the final monohydrat...

Embodiment 3

[0447] Convert anhydrous to monohydrate crystalline form

[0448] pH method

[0449] Anhydrous 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol (71 mg) was added to 2 ml of water and at the time the solution started to become clear The pH was adjusted to pH 10 with 1N NaOH. After 2 hours, the solution turned cloudy pale yellow. The solution was centrifuged, the supernatant was removed, and the precipitate was air dried and then vacuum dried. The XRPD and TGA of this product were consistent with the monohydrate.

[0450] Solvent / anti-solvent method

[0451] Dissolve anhydrous 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol (about 100mg) in 3ml of ethanol, then slowly add 4ml of water until the solution becomes cloudy. The solution was centrifuged, the supernatant was removed, and the precipitate was air dried and then vacuum dried. The XRPD and TGA of this product were consistent with the monohydrate.

[0452] aqueous suspension method

[0453] Anhydro...

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Abstract

The present invention is directed to pharmaceutical formulations and tablet compositions of pharmacological active agents of Formula (I) that are estrogen receptor modulators, and preparative processes thereof.

Description

technical field [0001] The present invention relates to pharmaceutical formulations of pharmacologically active agents that are estrogen receptor modulators, and methods for their manufacture. The present invention further relates to pharmaceutical compositions comprising the pharmaceutical formulations of the present invention, and methods for their manufacture. Background technique [0002] The pleiotropic effects of estrogen in mammalian tissues have been well documented, and it is now recognized that estrogen can affect many organ systems [Mendelsohn and Karas, New England Journal of Medicine 340:1801-1811 (1999); Epperson et al., Psychosomatic Medicine 61: 676-697 (1999); Crandall, Journal of Women's Health & Gender Based Medicine 8: 1155-1166 (1999); Monk and Brodaty, Dementia & Geriatric Cognitive Disorders 11: 1-10 (2000); Hurn and Macrae, Journal Cerebral Blood Flow & Metabolism 20: 631-652 (2000); Calvin, Maturitas 34: 195-210 (2000); Finking et al., Zeitschrift f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/16
Inventor M·K·克利斯南R·W·卡森M·佛拉伯S·哈森S·K·辛夫A·S·纳吉
Owner WYETH LLC
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