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Pharmaceutical composition containing ribose polymerase inhibitor

A technology of ribose polymerase and composition, applied in the field of pharmaceutical compositions containing olaparib nanoparticles and preparation thereof, can solve the problems of unfavorable industrialized production of preparations, narrow access routes, high safety production pressure, etc. Drug bioavailability, low content of impurities in preparations, and the effect of promoting absorption in vivo

Pending Publication Date: 2022-04-05
BEIJING TIDE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Two methods for preparing solid dispersions are disclosed in the prior art, one is to prepare solid dispersions by hot-melt extrusion, which involves high temperature during the preparation process, which easily leads to drug degradation and high impurity content; the other is to use solvents The volatilization method is used to prepare solid dispersions. The preparation process involves the use of organic solvents. Organic solvents are easy to remain. The requirements for environmental explosion protection are high, and the pressure of safe production is high.
At the same time, solid dispersion preparations have higher requirements on the properties of carrier and excipients. The marketed olaparib tablets have been screened by a large number of carriers, and copovidone is selected as the carrier. However, copovidone has a high cost and narrow acquisition channels, and has not been approved by the Chinese Pharmacopoeia. It is not conducive to the industrial production of preparations, and the amount of carrier used in the preparation of olaparib dispersion is large, the stability of the drug dispersion state is not high, and long-term storage is prone to crystallization and aging, thereby reducing the bioavailability of the drug Spend

Method used

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  • Pharmaceutical composition containing ribose polymerase inhibitor
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  • Pharmaceutical composition containing ribose polymerase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Preparation of Olaparib Nanoparticle Tablets

[0054]

[0055] 1) Add 400ml of water to sodium lauryl sulfate and stir to dissolve, then add the raw material of olaparib (manufacturer: Shanghai Yuang Chemical Co., Ltd.), and stir to form a coarse suspension;

[0056] 2) Transfer the coarse suspension to a nano grinder and grind until the average particle size is less than 300nm to obtain a nano suspension;

[0057] 3) Add lactose to 1000ml water and stir to dissolve, then mix with the nanosuspension evenly;

[0058] 4) Spray-dry the suspension obtained in step 3) to obtain a drug dry powder containing nanocrystals;

[0059] 5) After the dry powder is granulated by dry method, it is uniformly mixed with microcrystalline cellulose, crospovidone, micropowder silica gel, and magnesium stearate, and pressed into tablets to obtain the product.

[0060] Nanoparticle Size Analysis:

[0061] In order to further clarify the size of olaparib nanoparticles, take an appropriat...

Embodiment 2

[0067] Preparation of Olaparib Nanoparticle Tablets

[0068]

[0069] 1) Add 400ml of water to polysorbate 80 and stir to dissolve, then add the raw material of olaparib and stir to form a coarse suspension;

[0070] 2) Transfer the coarse suspension to a nano grinder and grind until the average particle size is less than 300nm to obtain a nano suspension;

[0071] 3) Add 1000ml of water to mannitol and stir to dissolve, then mix with the nanosuspension evenly;

[0072] 4) Spray-dry the suspension obtained in step 3) to obtain a drug dry powder containing nanocrystals;

[0073] 5) The dry powder is granulated by dry method, then mixed with calcium hydrogen phosphate, pregelatinized starch, micropowder silica gel, and sodium fumar stearate, and then pressed into tablets.

[0074] The nanosuspension in Example 2 was analyzed by a laser particle size analyzer, and its average particle size was 240.0nm. The dry drug powder containing nanocrystals could be quickly dispersed an...

Embodiment 3

[0076] Preparation of Olaparib Nanoparticle Tablets

[0077]

[0078] 1) Add 400ml of water to polysorbate 80 and stir to dissolve, then add the raw material of olaparib and stir to form a coarse suspension;

[0079] 2) Transfer the coarse suspension to a nano grinder and grind until the average particle size is less than 300nm to obtain a nano suspension;

[0080] 3) Add 1000ml of water to mannitol and stir to dissolve, then mix with the nanosuspension evenly;

[0081] 4) Spray-dry the suspension obtained in step 3) to obtain a drug dry powder containing nanocrystals;

[0082] 5) The dry powder is granulated by dry method, then mixed with microcrystalline cellulose, croscarmellose sodium, micropowder silica gel, and sodium fumarstearate, and then pressed into tablets to obtain the product.

[0083] The nanosuspension in Example 3 was analyzed by a laser particle size analyzer, and its average particle size was 198.3nm. The dry drug powder containing nanocrystals could be...

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Abstract

The invention provides a pharmaceutical composition containing a nanoparticle ribose polymerase inhibitor. The ribose polymerase inhibitor nanoparticle composition is prepared by adopting a grinding process. The drug nanocrystal particles in the composition are uniformly dispersed, so that the drug dissolution can be effectively promoted, the in-vivo absorption is promoted, and the bioavailability of the drug is improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a pharmaceutical composition containing a ribose polymerase inhibitor, in particular to a pharmaceutical composition containing olaparib nanoparticles and a preparation method thereof. Background technique [0002] Olaparib (Olaparib) is a poly ADP ribose polymerase inhibitor developed by AstraZeneca and is the world's first marketed RARP inhibitor drug for the treatment of women with advanced ovarian cancer associated with BRCA gene defects. As well as germline BRCA gene mutation, HER2-negative metastatic breast cancer, its curative effect is remarkable, with few adverse reactions, and the short-term tolerance of patients is good. [0003] Olaparib has poor water solubility and low bioavailability. The capsules that were first launched on the market use lauroyl macrogol glyceride as an excipient to improve the solubility of olaparib. Although capsules partially solve ...

Claims

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Application Information

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IPC IPC(8): A61K31/502A61K9/20A61K47/20A61K47/26A61P35/00A61P35/04
Inventor 张志兵卢迪徐义龙李显
Owner BEIJING TIDE PHARMA
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