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Pabociclib gastric floating tablet and preparation method thereof

A gastric floating tablet and tablet compression technology, which is applied in the field of palbociclib gastric floating tablet and its preparation, can solve the problems of low bioavailability and difficulty of palbociclib, and achieve reduced tablet weight and constant drug release Full, easy-to-swallow effect

Active Publication Date: 2017-12-01
上海润泰医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Aiming at the problem that palbociclib is extremely insoluble and has low bioavailability when the pH value is higher than 4, the present invention provides a palbociclib gastric floating tablet and a preparation method thereof

Method used

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  • Pabociclib gastric floating tablet and preparation method thereof
  • Pabociclib gastric floating tablet and preparation method thereof
  • Pabociclib gastric floating tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The prescription of palbociclib gastric floating tablet is:

[0040] Raw materials

g / 100 tablets

palbociclib

5

hypromellose

15

Bleach aid

17.5

Foaming agent

2

microcrystalline cellulose

10

Magnesium stearate

0.5

[0041] Described hypromellose, model is K4M.

[0042] The bleaching aid is fatty acid, and the fatty acid is stearic acid.

[0043] Described foaming agent is sodium bicarbonate.

[0044] Preparation method: crush palbociclib and pass through a 100-mesh sieve, hypromellose and bleaching aid pass through a 60-mesh sieve respectively, and then mix them evenly; Mesh sieve to prepare dry granules; add the prescribed amount of microcrystalline cellulose and magnesium stearate, mix well, and tablet.

Embodiment 2

[0046] The prescription of palbociclib gastric floating tablet is:

[0047] Raw materials

g / 100 tablets

palbociclib

20

hypromellose

20

Bleach aid

13.3

Foaming agent

4.7

microcrystalline cellulose

6.6

Magnesium stearate

2

[0048] Described hypromellose, model is K4M and K100M. Among them, hypromellose K4M is 6.7g, hypromellose K100M is 13.3g,

[0049] The bleaching aid is fatty alcohol, and the fatty alcohol is cetyl alcohol.

[0050] Described foaming agent is sodium carbonate.

[0051] Preparation method: crush palbociclib through a 100-mesh sieve, pass through a 60-mesh sieve for hypromellose, bleaching aid and microcrystalline cellulose respectively, and then mix them uniformly; wet granulate with 75% ethanol aqueous solution, Dry and sieve to obtain dry granules; mix the granules obtained above with a lubricant, and compress into tablets.

Embodiment 3

[0053] The prescription of palbociclib gastric floating tablet is:

[0054] Raw materials

g / 100 tablets

palbociclib

12.5

hypromellose

31.25

Bleach aid

12.5

Foaming agent

5.63

Magnesium stearate

0.63

[0055] Described hypromellose, model is K4M.

[0056] The bleaching aid is a fatty ester, and the fatty alcohol is glyceryl monostearate.

[0057] Described foaming agent is sodium citrate.

[0058] Preparation method: crush palbociclib and pass through a 100-mesh sieve, hypromellose and bleaching aid pass through a 60-mesh sieve respectively, and then mix them evenly; Mesh sieve to prepare dry granules; add the prescribed amount of magnesium stearate, mix evenly, and tablet.

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Abstract

The invention belongs to the technical field of medicine, and relates to a palbociclib gastric floating tablet and a preparation method thereof. The components of the gastric floating tablet and their mass percentages are: palbociclib 10%-30%, hydroxypropyl Methylcellulose 20%-50%, bleaching aid 20%-40%, foaming agent 2%-10%, microcrystalline cellulose 0%-25%, magnesium stearate 0.5-3%. The preparation process can adopt dry granulation or wet granulation process. The object of the present invention is to provide a palbociclib gastric floating tablet with high bioavailability, slow release tendency and effective reduction of total dosage. The unique advantage of the present invention is that two different mechanisms are used to prepare gastric floating tablets, the prepared tablets can maintain a floating time of more than 10 hours in gastric juice, and the drug can be continuously released in pH 1.2 hydrochloric acid solution, effectively avoiding the drug in the When the pH is higher than 4, it is extremely difficult to dissolve, resulting in low bioavailability, reducing the number of medications, reducing toxic and side effects, and effectively improving patient compliance.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a palbociclib gastric floating tablet and a preparation method thereof. Background technique [0002] Cyclin-dependent kinase 4 / 6 (cyclin-dependent kinase4 / 6, CDK4 / 6) inhibitor can inhibit the binding of serine / threonine kinase to cyclin D, and block the transition of cells from G1 phase to S phase. CDK4 / 6 inhibitors, as small molecule targeted drugs against tumors, have the advantages of: selectively inhibiting CDK4 / 6, and do not exhibit the cytotoxicity of "pan-CDK inhibitors", such as myelosuppression and intestinal reactions; The level of cyclin D is higher than that of normal cells, which increases the sensitivity of tumor cells to drugs, thereby increasing the targeting of drugs. [0003] Palbociclib (palbociclib) is a selective inhibitor of CDK4 / 6, chemical name: 6-acetyl-8-cyclopentyl-5-methyl-2-[[5-(piperazine-1- yl)pyridin-2-yl]amino]-8H-pyrido[2...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/46A61K9/20A61K31/519A61P35/00A61K47/38
Inventor 李勇刚李长军
Owner 上海润泰医药科技有限公司
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