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A pharmaceutical preparation of palbociclib and its preparation method

A technology of solid preparations and solid dispersions, which is applied in the direction of drug combinations, pharmaceutical formulas, medical preparations of non-active ingredients, etc., can solve the problems of poor absorption by patients, and achieve the effect of increasing in vitro dissolution and increasing bioavailability

Active Publication Date: 2018-08-03
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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  • A pharmaceutical preparation of palbociclib and its preparation method
  • A pharmaceutical preparation of palbociclib and its preparation method
  • A pharmaceutical preparation of palbociclib and its preparation method

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 tablets, pass through a 10-mesh sieve, and pack in gelatin capsules, each capsule is loaded with 350 mg of medicine. Dissolution was measured at pH 6.0 at selected time points of 5, 10, 15, 20, 30, 45 and 60 minutes.

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

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 tablets, pass through a 10-mesh sieve, and pack in gelatin capsules, each capsule is loaded with 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,...

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 in particular relates to a pharmaceutical preparation of palbociclib and a preparation method thereof. The pharmaceutical preparation includes palbociclib, acidic excipients and optional hydrophilic polymer materials, which have better solubility and in vitro dissolution properties than conventional preparations, and can be used to enhance the in vivo absorption and absorption of palbociclib. bioavailability.

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. Among them, there are 883,000 cases in developed countries and 794,000 cases in developing countries. New breast cancer cases a...

Claims

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Application Information

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