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Novel process and formulations

A preparation and tablet technology, applied in the field of sustained release tablet compositions

Inactive Publication Date: 2009-02-04
GLAXO GRP LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 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

[0171] 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

[0172] Granules (Platform Granule) for 1 mg and 5 mg tablets

[0173] Composition %w / w

[0174] Tosylate drugs 5.80

[0175] Microcrystalline Cellulose (Avicel PH101) 20.00

[0176] Lactose (regular monohydrate) 71.20

[0177] Kollidon (Povidone) 30 3.00

[0178] Appropriate amount of sterile water

[0179] Total 100.00

[0180] Granules for 5 mg to 10 mg tablets

[0181] Composition %w / w

[0182] Tosylate drugs 11.60

[0183] Microcrystalline cellulose (Avicel PH101) 18.73

[0184] Lactose (conventional monohydrate) 66.67

[0185] Kollidon 30 3.00

[0186] Appropriate amount of sterile water

[0187] Total 100.00

[0188] For 2.5mg tablet

[0189] Composition %w / w

[0190] Granules for 1mg to 5mg tablets 20.00

[0191] Lactose (anhydrous) 24.88

[0192] Microcrystalline cell...

Embodiment 2

[0236] 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

[0237] Backbone sheet with 30% polymer

[0238] The polymers used here are Methocel K 100LV or Hypromellose 2208

[0239] Component Quantity (mg / tablet) (% w / w):

[0240] 8-(2,6-difluorophenyl)-4-(4-fluoro-2-methyl

[0241] Phenyl)-2-{[2-hydroxy-1-(hydroxymethyl) 10.44mg / 6.96%w / w

[0242] Ethyl]amino}pyrido[2,3-d]pyrimidine

[0243] -7(8H)-Ketotosylate

[0244] Lactose (anhydrous) 71.01mg / 47.3%w / w

[0245] Microcrystalline Cellulose (Avicel PH200) 22.50mg / 15.0%w / w

[0246] Methocel KL00LV 45.00mg / 30.00%w / w

[0247] Magnesium Stearate 0.75mg / 0.50%w / w

[0248] Silica (anhydrous) 0.30mg / 0.20%w / w

[0249] 150mg total tablet weight (100%)

[0250] batch preparation method

[0251] The components were first weighed from bulk containers in the following qu...

Embodiment 3

[0256] 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

[0257] Backbone sheet with 40% polymer

[0258] The polymer is Methocel K 100LV or Hypromellose 2208

[0259] Component Quantity (mg / tablet) (%w / w)

[0260] 8-(2,6-difluorophenyl)-4-(4-fluoro-2-methyl

[0261] Phenyl)-2-{[2-hydroxy-1-(hydroxymethyl) 10.44mg / 6.96%w / w

[0262] Ethyl]amino}pyrido[2,3-d]pyrimidine

[0263] -7(8H)-Ketotosylate

[0264] Lactose (anhydrous) 39.26mg / 26.17%w / w

[0265] Microcrystalline Cellulose (Avicel PH200) 39.26mg / 26.17%w / w

[0266] Methocel K4M 60.00mg / 40.00%w / w

[0267] Magnesium Stearate 0.75mg / 0.50%w / w

[0268] Silica (anhydrous) 0.30mg / 0.20%w / w

[0269] 150mg total tablet weight (100%)

[0270] batch preparation method

[0271] These components were weighed from bulk containers in the above amounts and processed as...

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Abstract

The present invention provides for a novel process of making 6-carboxylic acid derivatives of pyrido[2,3- A61K 31 / 513 17 82 16 2006 / 11 / 15 101360497 2009 / 2 / 4 000000000 Glaxo Group Ltd. United Kasparec Jiri Spoors Paul G. Humphries Lesley Anne Abu Khalil As Ad Diederich Ann M. Blatcher Philip Vernon Lois E. Appleby John Robert George Lloyd Richard S. Taggart John J. zhang bengyuan 11105 United 2005 / 11 / 15 60 / 736,679 2008 / 7 / 15 PCT / US2006 / 060898 2006 / 11 / 15 WO2007 / 059500 2007 / 5 / 24 English

Description

technical field [0001] 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 [0002] 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 such dosage forms involves a matrix comprising a hydrophilic polymer in which the active agent is dispersed; the active agent is released in the gastrointestinal tract for a period of time ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/513
CPCC07D471/04A61K9/2054A61K31/513A61K9/2077A61P1/00A61P1/04A61P11/00A61P11/06A61P19/02A61P19/04A61P25/04A61P29/00A61P35/00A61P43/00A61P9/00A61P9/10Y02A50/30A61K9/20
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
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