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Medicinal preparation of palbociclib and preparing method thereof

A technology for pharmaceutical preparations and tablets is applied in the field of pharmaceutical preparations and preparations of palbociclib, which can solve problems such as poor absorption of patients, and achieve the effects of increasing in vitro dissolution and increasing bioavailability

Active Publication Date: 2016-08-03
SHENZHEN PHARMACIN CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Poor absorption in some patients, likely due to the poorly soluble nature of the drug

Method used

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  • Medicinal preparation of palbociclib and preparing method thereof
  • Medicinal preparation of palbociclib and preparing method thereof
  • Medicinal preparation of palbociclib and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Preparation of dosage forms of acidic excipients and palbociclib dry granulated filling capsules

[0056] Take by weighing 1500 mg of palbociclib raw material, 345 mg of lactose, 1200 mg of tartaric acid, 840 mg of microcrystalline cellulose, 210 mg of sodium carboxymethyl starch, and 84 mg of silicon dioxide, mix for 15 minutes with a three-dimensional mixer, and then Add 21 mg of magnesium stearate, and mix for another 2 minutes with a three-dimensional mixer. After mixing, the materials were passed through a 40-mesh sieve, and compressed with a mechanical single-punch tablet press. The pressure of the compression was 5 MPa, and each tablet weighed 1050 mg. Break the pressed large pieces, pass through a 10-mesh sieve, and pack gelatin Capsules, each capsule contains 350 mg of medicine. The dissolution rate was measured at pH 6.0, and the selected time points were 5, 10, 15, 20, 30, 45 and 60 minutes.

[0057] At the same time, a comparative test without acidic exc...

Embodiment 2

[0060] Preparation of dry granulated filling capsules after mixing acidic materials with palbociclib and crushing

[0061] Weigh 1500 mg of palbociclib bulk drug that has been jet-milled, and then mix it with 1200 mg of tartaric acid, 345 mg of lactose, 840 mg of microcrystalline cellulose, 210 mg of sodium carboxymethyl starch, and 84 mg of silicon dioxide in a three-dimensional Mix in a mixer for 15 minutes. Add 21 mg of magnesium stearate, and mix for another 2 minutes with a three-dimensional mixer. After mixing, the materials were passed through a 40-mesh sieve, and compressed with a mechanical single-punch tablet press. The pressure of the compression was 5 MPa, and each tablet weighed 1050 mg. Break the pressed large pieces, pass through a 10-mesh sieve, and pack gelatin Capsules, each capsule contains 350 mg of medicine. Under the condition of pH 6.0, the dissolution rate was measured by basket method at 100 rpm, and the selected time points were 5, 10, 15, 20, 30,...

Embodiment 3

[0063] Preparation of solid dispersion of palbociclib and PVP-K30 after mixing with acidic materials

[0064] Weigh 100 mg of palbociclib crude drug and 200 mg of tartaric acid, put them into a 10-ml vial, add 2 ml of purified water, and dissolve with mixing. Add 200 mg of PVP-K30 (product of BASF, Germany, full name: povidone K30) to the above solution, and dissolve it by ultrasonic and hand shaking. In the fume hood, stir under heating conditions to help water evaporate; assist with nitrogen gas to help water evaporate. When the inside of the vial is gelatinous and there is no liquid loss, stop heating and stirring. Put it in a vacuum desiccator overnight at 40°C. It was taken out the next day and a solid dispersion was made.

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Abstract

The invention belongs to the field of pharmacy and particularly relates to a medicinal preparation of palbociclib and a preparing method thereof. The medicinal preparation comprises palbociclib, an acidic adjuvant and an optional hydrophily high-molecular material. Compared with a conventional preparation, the medicinal preparation has more excellent solubility and in-vitro dissolution property, and can be used for enhancing in-vivo adsorption and bioavailability of palbociclib.

Description

technical field [0001] The invention belongs to the field of pharmacy. More specifically, the present invention relates to a pharmaceutical preparation of palbociclib (also known as palbociclib, palbociclib, palbociclib, palbociclib, etc.) and a preparation method thereof. The palbociclib of the present invention may be palbociclib free base or any pharmaceutically acceptable salt thereof. Background technique [0002] Statistics from the World Health Organization show that breast cancer is the second leading cause of cancer death among women worldwide. The incidence of breast cancer has been increasing over the past few decades. It is estimated that by 2020, there will be more than 1.7 million new cases of breast cancer each year. In 2012, there were 1.67 million new cases of breast cancer worldwide, accounting for 25% of all new cancer cases. which developed nation 883,000 cases; developing nation There are 794,000 cases. developing nation new breast cancer cases a...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/519A61K47/12A61K47/04A61P35/00
CPCA61K9/4858A61K9/4866A61K31/519A61K47/02A61K47/12A61P35/00A61K9/2009A61K9/2013A61K9/485A61K9/146A61K9/145A61K9/48A61K47/26A61K47/32A61K47/36A61K47/38A61K9/10A61K9/1629A61K9/4808A61K9/1617A61K9/1652C07D471/04
Inventor 王泽人曲龙徐俊
Owner SHENZHEN PHARMACIN CO LTD
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