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Pharmaceutic preparation of palbociclib and preparation method of pharmaceutic preparation

一种药用盐、无定型的技术，应用在帕布昔利布的药物制剂及其制备领域，能够解决病人吸收差等问题，达到增加体外溶出、增加生物利用度的效果

Active Publication Date: 2018-12-25
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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  • Pharmaceutic preparation of palbociclib and preparation method of pharmaceutic preparation
  • Pharmaceutic preparation of palbociclib and preparation method of pharmaceutic preparation
  • Pharmaceutic preparation of palbociclib and preparation method of pharmaceutic preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Preparation of dosage forms of acidic excipients and palbociclib dry granulated filling capsules

[0057] Take by weighing 1500 mg of palbociclib bulk drug, 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, mixed 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.

[0058] At the same time, a comparative test without acidic excipients wa...

Embodiment 2

[0061] Preparation of dry granulated filling capsules after mixing acidic materials with palbociclib and crushing

[0062] 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 with a pressure of 5 MPa, and each tablet weighed 1050 mg. Break up 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, 20, 30, 45 and...

Embodiment 3

[0064] Preparation of solid dispersion of palbociclib and PVP-K30 after mixing with acidic materials

[0065] Take by weighing 100 mg of palbociclib bulk drug, 200 mg of tartaric acid, put into a 10 ml vial, add 2 ml of purified water, and mix and dissolve. 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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PUM

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Abstract

The invention belongs to the field of pharmacy, and particularly relates to a pharmaceutic preparation of palbociclib and a preparation method of the pharmaceutic preparation. The pharmaceutic preparation comprises the palbociclib, acidic auxiliary materials and an optional hydrophilic high polymer material. Compared with a conventional preparation, the pharmaceutic preparation of the palbociclibhas excellent solubility and an in-vitro dissolution property, and can be used for enhancing in-vivo absorption and bioavailability of the palbociclib.

Description

[0001] This application is a divisional application of the application number 201610187046.8 and the invention title "a pharmaceutical preparation of palbociclib and its preparation method" submitted on March 29, 2016. technical field [0002] The invention belongs to the field of pharmacy. More specifically, the present invention relates to a pharmaceutical preparation of palbociclib (also known as palbociclib, palbocoxib, 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 [0003] 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. There were 1.67 million ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K9/20A61K47/12A61K47/04A61K31/519A61P35/00
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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