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Palbociclib 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 Complete, compliance-enhancing effect

Active Publication Date: 2015-09-09
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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  • Palbociclib gastric-floating tablet and preparation method thereof
  • Palbociclib gastric-floating tablet and preparation method thereof
  • Palbociclib gastric-floating tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Raw materials g / 100 tablets palbociclib 5 hypromellose 15 Bleach aid 17.5 Foaming agent 2 microcrystalline cellulose 10 Magnesium stearate 0.5

[0040] Described hypromellose, model is K4M.

[0041] The bleaching aid is fatty acid, and the fatty acid is stearic acid.

[0042] Described foaming agent is sodium bicarbonate.

[0043] 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

[0045] Raw materials g / 100 tablets palbociclib 20 hypromellose 20 Bleach aid 13.3 Foaming agent 4.7 microcrystalline cellulose 6.6 Magnesium stearate 2

[0046] Described hypromellose, model is K4M and K100M. Among them, hypromellose K4M is 6.7g, hypromellose K100M is 13.3g,

[0047] The bleaching aid is fatty alcohol, and the fatty alcohol is cetyl alcohol.

[0048] Described foaming agent is sodium carbonate.

[0049] 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

[0051] Raw materials g / 100 tablets palbociclib 12.5 hypromellose 31.25 Bleach aid 12.5 Foaming agent 5.63 Magnesium stearate 0.63

[0052] Described hypromellose, model is K4M.

[0053] The bleaching aid is a fatty ester, and the fatty alcohol is glyceryl monostearate.

[0054] Described foaming agent is sodium citrate.

[0055] 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 palbociclib gastric-floating tablet comprises, by mass, 10%-30% of palbociclib, 20%-50% of hydroxypropyl methylcellulose, 20%-40% of bleaching auxiliaries, 2%-10% of foaming agents, 0%-25% of microcrystalline cellulose and 0.5%-3% of magnesium stearate. A dry granulating technology or a wet granulating technology can be used as the preparation technology. The palbociclib gastric-floating tablet is high in bioavailability, has a slow release tendency, and effectively lowers the total dosage. The palbociclib gastric-floating tablet and the preparation method thereof have the unique advantages that two different mechanisms are used for preparing the gastric-floating tablet, and accordingly the prepared tablet can keep floating in gastric juice by more than 10 hours and continuously release drugs in the hydrochloric acid solution with the pH being 1.2; the problem that the bioavailability is low due to the fact that drugs are extremely difficult to dissolve after the pH is higher than four is effectively solved; the medicine taking frequency is reduced; toxic and side effects are lightened; and the complaisance of a patient is effectively improved.

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 Applications(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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