Pharmaceutical preparation containing cyclin inhibitor, and preparation method thereof

A drug and composition technology, applied in the field of pharmaceutical preparations and preparations of cyclin inhibitors, can solve the problems of high incidence and slow progress of the disease, and achieve the effects of excellent dissolution behavior and good bioavailability in vivo

Inactive Publication Date: 2016-06-01
JIANGSU HANSOH PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Breast cancer is one of the most common malignant tumors in women. It has a high incidence rate and is quite aggressive, but the course of the disease progresses slowly

Method used

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  • Pharmaceutical preparation containing cyclin inhibitor, and preparation method thereof
  • Pharmaceutical preparation containing cyclin inhibitor, and preparation method thereof
  • Pharmaceutical preparation containing cyclin inhibitor, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] 1.1 Unit prescription composition

[0046]

[0047]

[0048] Note: " / " means not added.

[0049] 1.2 Preparation

[0050] Put the above-mentioned 1,000 tablets of the formula I compound and other excipients except magnesium stearate into the hopper mixer and mix evenly, add a wetting agent to moisten the granules, dry on a fluidized bed at 45°C for 10 minutes, and sieve the granules with a size of 1.0 mm. Add magnesium stearate and mix for 10 minutes, control the content in the middle, and fill the capsules. Or compressed into tablets.

[0051] 1.3 Dissolution data

[0052]

Embodiment 2

[0054] 2.1 Composition of unit prescription

[0055]

Prescription 9

Prescription 10

Prescription 11

Prescription 12

Formula I compound

75

75

100

125

microcrystalline cellulose

38.7

10.8

93.9

117.3

lactose

54.3

18.8

49.7

65.7

Hypromellose

/

/

/

17.5

Povidone

10.5

3.5

14

/

Carboxymethyl Starch Sodium

/

10.5

14

17.5

Croscarmellose Sodium

21

/

/

/

Sodium dodecyl sulfate

2.1

/

2.8

/

Talc powder

2.1

0.7

2.8

3.5

[0056] Magnesium stearate

2.1

0.7

2.8

3.5

weight

210

120

280

350

[0057] Note: " / " means not added.

[0058] 2.2 Preparation

[0059] Put the above 1000 tablets of formula Ⅰ compound and other excipients except magnesium stearate into the hopper mixer for mixing, use a roller p...

Embodiment 3

[0063] 3.1 Unit prescription composition

[0064]

Prescription 13

Prescription 14

Prescription 15

Formula I compound

75

75

75

microcrystalline cellulose

71.8

/

50

lactose

35.9

25.8

15.7

Hypromellose

10.5

6.0

9.0

Carboxymethyl Starch Sodium

10.5

6.0

5.0

Crospovidone

/

3.0

4.0

Sodium dodecyl sulfate

2.1

/

2.1

Talc powder

2.1

2.1

2.1

Magnesium stearate

2.1

2.1

2.1

weight

210

120

165

[0065] Note: " / " means not added.

[0066] 3.2 Preparation

[0067] Put the above 1000 tablets of the formula I compound and excipients into the hopper mixer and mix evenly, control the content in the middle, and fill the capsules. Or compressed into tablets.

[0068] 3.3 Dissolution data

[0069]

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PUM

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Abstract

The present invention discloses a pharmaceutical preparation containing a cyclin inhibitor, and a preparation method thereof, and particularly relates to a pharmaceutical preparation adopting 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazine-1-yl-pyridine-2-yl-amino)-8H-pyrido[2,3-d]pyrimidine-7-one represented by a formula I or a salt thereof as an active component, wherein the salt comprises a hydrochloride and an isethionate, and the dosage form of the pharmaceutical preparation comprises tablets and capsules, and has good stability and excellent dissolution behavior. The formula I is defined in the specification.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a pharmaceutical preparation for cell cycle protein inhibitors and a preparation method thereof. Background technique [0002] Cyclin-dependent kinase (CDK) has a total of 13 members, all of which belong to the serine / threonine protein kinase family, relying on the combination with cyclin to promote cell cycle phase transition, initiate DNA synthesis and regulate cell transcription and other key functions. [0003] CDKs play a key role in the proliferation and death of all cells, including healthy and tumor cells. Broad-spectrum CDK inhibitors, especially for patients who have not undergone genetic screening, are difficult to show a high therapeutic window. A large dose is too toxic, and a small dose has no medicinal effect. So selectively inhibiting some CDKs becomes extremely important. Of course, because most CDK subtypes have relatively similar chemical structure...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K9/28A61K9/48A61P35/00
CPCA61K9/2018A61K9/2054A61K9/4858A61K31/519A61K9/28A61K9/48A61P35/00A61P43/00A61K9/2009A61K9/2059A61K9/485A61K9/4866
Inventor 曾金王瑞军王小雷
Owner JIANGSU HANSOH PHARMA CO LTD
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