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Novel process and formulations

一种衍射图、甲基苯基的技术，应用在抗炎剂、丸剂输送、医药配方等方向

Inactive Publication Date: 2011-04-27
GLAXO GRP LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] For immediate-release 8-(2,6-difluorophenyl)-4-(4-fluoro-2-methylphenyl)-2-{[2-hydroxyl-1-(hydroxymethyl )ethyl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one tablets are currently being studied on a twice-daily dosing regimen, but patients are more comfortable with a once-daily dosing regimen sex will improve

Method used

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  • Novel process and formulations
  • Novel process and formulations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0392] 8-(2,6-difluorophenyl)-4-(4-fluoro-2-methylphenyl)-2-{[2-hydroxy-1-(hydroxymethyl)ethyl]amino}pyrido [2,3-d]pyrimidin-7(8H)-one tosylate immediate release (IR) formulation

[0393] Granules (Platform Granule) for 1 mg and 5 mg tablets

[0394] Composition %w / w

[0395] Tosylate drugs 5.80

[0396] Microcrystalline Cellulose (Avicel PH101) 20.00

[0397] Lactose (regular monohydrate) 71.20

[0398] Kollidon (Povidone) 30 3.00

[0399] Appropriate amount of sterile water

[0400] Total 100.00

[0401] Granules for 5 mg to 10 mg tablets

[0402] Composition %w / w

[0403] Tosylate drugs 11.60

[0404] Microcrystalline cellulose (Avicel PH101) 18.73

[0405] Lactose (conventional monohydrate) 66.67

[0406] Kollidon 30 3.00

[0407] Appropriate amount of sterile water

[0408] Total 100.00

[0409] For 2.5mg tablet

[0410] Composition %w / w

[0411] Granules for 1mg to 5mg tablets 20.00

[0412] Lactose (anhydrous) 24.88

[0413] Microcrystalline cell...

Embodiment 2

[0457] 8-(2,6-difluorophenyl)-4-(4-fluoro-2-methylphenyl)-2-{[2-hydroxy-1-(hydroxymethyl)ethyl]amino}pyrido [2,3-d]pyrimidin-7(8H)-one tosylate sustained release (MR) formulation

[0458] Backbone sheet with 30% polymer

[0459] The polymers used here are Methocel K100LV or Hypromellose 2208

[0460] Component Quantity (mg / tablet) (% w / w):

[0461] 8-(2,6-difluorophenyl)-4-(4-fluoro-2-methyl

[0462] Phenyl)-2-{[2-hydroxy-1-(hydroxymethyl) 10.44mg / 6.96%w / w

[0463] Ethyl]amino}pyrido[2,3-d]pyrimidine

[0464] -7(8H)-Ketotosylate

[0465] Lactose (anhydrous) 71.01mg / 47.3%w / w

[0466] Microcrystalline Cellulose (Avicel PH200) 22.50mg / 15.0%w / w

[0467] Methocel KL00LV 45.00mg / 30.00%w / w

[0468] Magnesium Stearate 0.75mg / 0.50%w / w

[0469] Silica (anhydrous) 0.30mg / 0.20%w / w

[0470] 150mg total tablet weight (100%)

[0471] batch preparation method

[0472] The components were first weighed from bulk containers in the following quant...

Embodiment 3

[0477] 8-(2,6-difluorophenyl)-4-(4-fluoro-2-methylphenyl)-2-{[2-hydroxy-1-(hydroxymethyl)ethyl]amino}pyrido [2,3-d]pyrimidin-7(8H)-one tosylate sustained release (MR) formulation

[0478] Backbone sheet with 40% polymer

[0479] The polymer is Methocel K100LV or Hypromellose 2208

[0480] Component Quantity (mg / tablet) (%w / w)

[0481] 8-(2,6-difluorophenyl)-4-(4-fluoro-2-methyl

[0482] Phenyl)-2-{[2-hydroxy-1-(hydroxymethyl) 10.44mg / 6.96%w / w

[0483] Ethyl]amino}pyrido[2,3-d]pyrimidine

[0484] -7(8H)-Ketotosylate

[0485] Lactose (anhydrous) 39.26mg / 26.17%w / w

[0486] Microcrystalline Cellulose (Avicel PH200) 39.26mg / 26.17%w / w

[0487] Methocel K4M 60.00mg / 40.00%w / w

[0488] Magnesium Stearate 0.75mg / 0.50%w / w

[0489] Silica (anhydrous) 0.30mg / 0.20%w / w

[0490] 150mg total tablet weight (100%)

[0491] batch preparation method

[0492] These components were weighed from bulk containers in the above amounts and processed as indic...

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Abstract

The present invention provides for a novel process of making 6-carboxylic acid derivatives of pyrido[2,3-<d]pyrimidin-7-one's, as well as a novel process for making 8-(2,6-difluorophenyl)-4-(4-fluoro-2-methylphenyl)-2-{[2-hydroxy-l- (hydroxymethyl)ethyl]-amino}pyrido[2,3-d]pyrimidin-7(8H)-one, and salts thereof.

Description

[0001] This application is a divisional application of Chinese patent application No. 200680051105.3 (application date: November 15, 2006, invention name: new method and preparation). technical field [0002] The present invention relates to novel methods, tablet formulations, polymorphs, and sustained release tablet compositions for oral administration of pyrido[2,3-d]pyrimidin-7-one derivatives, the derivatives of which are exemplified by For 8-(2,6-difluorophenyl)-4-(4-fluoro-2-methylphenyl)-2-{[2-hydroxyl-1-(hydroxymethyl)-ethyl]amino} Water-soluble salts of pyrido[2,3-d]pyrimidin-7(8H)-one. Background technique [0003] Many active pharmaceutical agents, including drugs and prodrugs, have been formulated into orally administrable dosage forms that provide sustained release (or what is known as slow release, extended release) over a period of time. ) or modified release (modified release)) of the agent to allow once-daily dosing. A well-known system for formulating suc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04A61K31/519A61P29/00A61P19/04A61P1/00A61P9/10A61P25/04A61P11/00A61P11/06A61P35/00A61P43/00
CPCA61K9/2077A61K9/2054C07D471/04A61K31/513A61P1/00A61P1/04A61P11/00A61P11/06A61P19/02A61P19/04A61P25/04A61P29/00A61P35/00A61P43/00A61P9/00A61P9/10Y02A50/30A61K9/20
Inventor 约翰·R·G·阿普尔比莱斯利·A·汉弗莱斯菲利普·布拉彻阿萨德·阿布卡利尔吉里·卡斯帕雷克安·M·迪德里克洛伊丝·E·弗农约翰·J·塔格特理查德·S·劳埃德保罗·G·斯波尔斯
Owner GLAXO GRP LTD