Olaparib dissolution enhancing composition

A composition and drug technology, applied in the field of olaparib dissolution enhancement composition, can solve problems such as limitations in the development of high-dose preparations, difficulty in swallowing for patients with advanced cancer, limited stability or solubilization ability, etc.

Active Publication Date: 2021-09-07
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] 1) A kind of olaparib solid dispersion preparation is disclosed in WO2010041051 and CN102248945B. The olaparib solid dispersion of this invention is prepared with copovidone as the main material. The weight ratio of olaparib and copovidone is It is 1:2 to 1:4, and the proportion of the active agent is 20% to 30%. Since copovidone is difficult to dissolve after being pulverized and pressed into tablets, it needs to add 14.7% by weight of mannitol to dissolve effectively, and the amount of excipients is large. Difficulty swallowing for advanced cancer patients limits development of high-dose formulations
[0009] 2) CN104434809B discloses a solid dispersion of olaparib, the solid dispersion of olaparib of this invention is prepared with povidone as the main material, and the ratio range of olaparib and polymer is 25-100 parts Olaparib, 50-250 parts of povidone, the preparation of tablet needs to add disintegrant and a large amount of diluent, the amount of auxiliary material is large, and povidone has poor thermal stability when prepared by melt extrusion method, easy to Disadvantages of degradation and blackening
[0010] 3) EP3263095 discloses a solid dispersion preparation of olaparib. The solid dispersion of this invention is prepared from a hydrophilic polymer with a glass transition temperature of 40-100

Method used

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Examples

Experimental program
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Effect test

preparation Embodiment 1

[0060] Table 1

[0061]

[0062] Preparation method: Copovidone (PVP VA64, manufactured by BASF, Germany), dissolution accelerator (sulfobutyl-β-cyclodextrin (manufactured by Cyclolab Ltd., Hungary), hydroxypropyl-β-cyclodextrin (produced by Romano, France Gate company manufactures)), olaparib and colloidal silicon dioxide (Germany Evonik industrial group manufacture) are extruded with twin-screw extruder (screw diameter 11mm, ThermoScientific company) after mixing, obtain olaparib dissolution Enhanced composition.

[0063] Take the olaparib dissolution enhancing composition prepared in this example, after crushing, add the remaining excipients according to the prescription in Table 1 and mix evenly, and use a single-punch tablet press to form a preparation containing 150 mg of olaparib per tablet. Wherein sodium stearyl fumarate is manufactured by German JRS company), and PEG6000 is manufactured by U.S. Dow Chemical Company.

preparation Embodiment 2

[0065] Table 2

[0066]

[0067] Preparation method: dissolve copovidone (PVP VA64, manufactured by BASF, Germany), dissolution accelerators (sulfobutyl-β-cyclodextrin, hydroxypropyl-β-cyclodextrin) and olaparib in methanol / Acetone=1:4 solvent, the solvent was evaporated to obtain the olaparib dissolution enhancing composition.

[0068] Take the olaparib dissolution enhancing composition prepared in this example, after crushing, add the remaining excipients according to the prescription in Table 2 and mix evenly, and use a single-punch tablet machine to compress into a preparation containing 150 mg of olaparib per tablet.

preparation Embodiment 3

[0070] table 3

[0071]

[0072] Among them, sodium lauryl sulfate is manufactured by BASF of Germany, glyceryl behenate and labrasol are manufactured by Garfars of France, and Span 20 is manufactured by Nanjing Well Chemical Co., Ltd.

[0073] Preparation method: Copovidone, dissolution enhancer hydroxypropyl-β-cyclodextrin, olaparib, colloidal silicon dioxide, labrasol, sodium lauryl sulfate and Span 20 are mixed and extruded by twin-screw Machine extruded to obtain the olaparib dissolution enhancement composition.

[0074] Take the olaparib dissolution enhancing composition prepared in this embodiment, after crushing, add the remaining excipients (sodium stearyl fumarate and glyceryl behenate) according to the prescription in Table 3 and mix evenly, and use a single-punch tablet press Compressed into a preparation containing 150 mg olaparib per tablet. Wherein, the tablet obtained in prescription 12 is taken, and then the tablet is placed in a coating pan, and the tabl...

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PUM

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Abstract

The invention relates to an olaparib dissolution enhancing composition, a preparation method and application thereof, as well as a medicine containing the olaparib dissolution enhancing composition. The olaparib dissolution enhancing composition is prepared from the following components: olaparib, copovidone and a dissolution accelerator, wherein based on 100 parts by weight of olaparib, the copovidone is more than 100 parts by weight and less than 200 parts by weight, and the dissolution accelerator is 20-150 parts by weight. The olaparib dissolution enhancing composition and the medicine prepared from the olaparib dissolution enhancing composition have controllable stability, can be used for improving oral absorption of active ingredients, and can improve the medication convenience of patients since auxiliary dosage is reduced so as to facilitate industrial production.

Description

technical field [0001] The invention belongs to the technical field of olaparib preparations, and in particular, relates to a composition for enhancing the dissolution of olaparib, its preparation method and its use in the preparation of drugs for preventing or treating tumors, and the composition containing said olaparib A drug in a dissolution-enhancing composition. Background technique [0002] With the World Health Organization discussing tumor as a chronic disease that can be controlled and cured, in recent years, the concept of tumor treatment has changed from the traditional "survival without tumor" to "survival with tumor". Transition to Survival and Quality of Life. "Survival with tumor" significantly prolongs the survival period of patients compared with traditional chemotherapy (~5-10 years VS~1 year), and this "chronic treatment" method promotes the transformation of patients' medication from injection to oral administration, which is convenient for long-term us...

Claims

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Application Information

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IPC IPC(8): A61K31/502A61K9/20A61K47/32A61K47/40A61P35/00
CPCA61K31/502A61K9/2027A61K9/205A61P35/00
Inventor 甘勇郭仕艳安巍
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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