Palbociclib pharmaceutical composition and preparation method thereof

A composition and drug technology, applied in the field of medicine, can solve the problems of low dissolution rate, the raw material cannot be fully absorbed, and the curative effect is reduced, and achieves the effects of good content uniformity, good dissolution effect, and improved curative effect.

Inactive Publication Date: 2017-05-17
HENAN RUNHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the existing palbociclib capsules generally have the problem of low dissolution rate, which leads to the inability of the raw material to be fully absorbed and reduces the curative effect.

Method used

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  • Palbociclib pharmaceutical composition and preparation method thereof
  • Palbociclib pharmaceutical composition and preparation method thereof
  • Palbociclib pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] The palbociclib pharmaceutical composition of the present embodiment is made up of the following components by mass percentage: palbociclib 27.78%, lactose 21.74%, microcrystalline cellulose 43.48%, carboxymethyl starch sodium 5% (granule Intragranular 3%, extragranular 2%), silicon dioxide 0.5%, magnesium stearate 1.5% (intragranular 1.0%, extragranular 0.5%).

[0032] The above pharmaceutical composition is made into capsules, specification: 75 mg active ingredient / capsule; batch size: 10,000 capsules. The preparation method of the palbociclib pharmaceutical composition capsule of the present embodiment comprises the following steps (technical process such as figure 1 shown):

[0033] 1) Pass the palbociclib raw material through a 65-mesh sieve and set aside; pass lactose (TABLETTOSE 80) through a 80-mesh sieve and set aside; pass microcrystalline cellulose (TYPE 101), sodium carboxymethyl starch, stearin Magnesium acid and silicon dioxide are respectively passed th...

Embodiment 2

[0041] The palbociclib pharmaceutical composition of the present embodiment is made up of the following components by mass percentage: palbociclib 27.78%, lactose 21.74%, microcrystalline cellulose 43.48%, carboxymethyl starch sodium 5% (granule Intragranular 3%, extragranular 2%), silicon dioxide 0.5%, magnesium stearate 1.5% (intragranular 1.0%, extragranular 0.5%).

[0042] The above pharmaceutical composition is made into capsules, specification: 100 mg active ingredient / capsule; batch size: 10,000 capsules. The preparation method of the palbociclib pharmaceutical composition capsule of the present embodiment comprises the following steps:

[0043] 1) Pass the palbociclib raw material through a 65-mesh sieve and set aside; pass lactose (TABLETTOSE 80) through a 80-mesh sieve and set aside; pass microcrystalline cellulose (TYPE 101), sodium carboxymethyl starch, stearin Magnesium acid and silicon dioxide are respectively passed through a 50-mesh sieve for subsequent use; ...

Embodiment 3

[0051] The palbociclib pharmaceutical composition of the present embodiment is made up of the following components by mass percentage: palbociclib 27.78%, lactose 21.74%, microcrystalline cellulose 43.48%, carboxymethyl starch sodium 5% (granule Intragranular 3%, extragranular 2%), silicon dioxide 0.5%, magnesium stearate 1.5% (intragranular 1.0%, extragranular 0.5%).

[0052] The above pharmaceutical composition is made into capsules, specification: 125 mg active ingredient / capsule; batch size: 10,000 capsules. The preparation method of the palbociclib pharmaceutical composition capsule of the present embodiment comprises the following steps:

[0053] 1) Pass the palbociclib raw material through a 65-mesh sieve and set aside; pass lactose (TABLETTOSE 80) through a 80-mesh sieve and set aside; pass microcrystalline cellulose (TYPE 101), sodium carboxymethyl starch, stearin Magnesium acid and silicon dioxide are respectively passed through a 50-mesh sieve for subsequent use; ...

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Abstract

The invention relates to a palbociclib pharmaceutical composition and a preparation method thereof and belongs to the technical field of medicines. The pharmaceutical composition is prepared from the following components in percentage by mass: 27.00 percent to 28.50 percent of palbociclib, 21.00 percent to 22.5 percent of lactose, 42.50 percent to 44.00 percent of microcrystalline cellulose, 4.5 percent to 5.5 percent of sodium carboxymethyl starch, 0.5 percent to 0.8 percent of silicon dioxide and 1.2 percent to 2.0 percent of magnesium stearate. In the pharmaceutical composition, the palbociclib is used as an active component, the lactose and the microcrystalline cellulose are used as a filling agent, the sodium carboxymethyl starch is used as an efficient disintegrating agent, the silicon dioxide is used as a flow aid and the magnesium stearate is used as a lubricant; main and auxiliary materials have good compatibility and the medicine has good stability; all the components are matched with one another and have a coordinating effect; the obtained pharmaceutical composition has a good dissolution effect and a high dissolution degree, and can be sufficiently absorbed so that the curative effect is improved.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular to a palbociclib pharmaceutical composition, and also to a preparation method of the palbociclib pharmaceutical composition. Background technique [0002] Palbociclib (Palbociclib), Chinese chemical name: 6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperazin-1-yl)pyridin-2-yl] Amino}-pyrido[2,3-d]pyrimidin-7(8H)-one, English chemical name: 6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperazin-1-yl )pyridin-2-yl]amino}-pyrido[2,3-d]pyrimidin-7(8H)-one, its structural formula is as shown in formula (I): [0003] [0004] Palbociclib is an inhibitor of cyclin-dependent kinases 4 and 6 (CDK4 / 6). Cyclin D1 and CDK4 / 6 are downstream molecules of signaling pathways that lead to cell proliferation. In vitro, palbociclib can prevent the transition of the cell cycle from the growth phase (G1 phase) to the DNA replication phase (S1 phase), thereby reducing or slowing down the estrogen receptor E...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/519A61K47/38A61K47/36A61K47/26A61K47/12A61K47/04A61P35/00
CPCA61K9/485A61K9/4858A61K9/4866A61K31/519
Inventor 杨婷高志亮郭强
Owner HENAN RUNHONG PHARMA
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