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Preparation method of olaparib solid dispersoid and product thereof

A technology of solid dispersion and compound, applied in the field of preparation of olaparib solid dispersion, can solve the problems of low reproducibility, complicated process, residual organic solvent, etc., to achieve continuous large-scale production and simple and easy process , the effect of improving the dissolution rate

Inactive Publication Date: 2017-05-24
江苏开元医药有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method has the following disadvantages: (1) the static electricity produced by the micronized bulk drug is large, and the bulk drug is easy to gather, which affects the dissolution of the drug; Stability; (3) The molten mixture of raw materials and excipients is difficult to fill, and liquid hard capsule filling machines are needed, but it has not been prepared in China so far, and imported equipment is still required, and the cost of equipment is high
[0006] Traditional solid dispersion preparation methods include melting method, solvent method and grinding method, but these methods have problems such as complex process, low reproducibility, organic solvent residue, etc., and it is difficult to promote industrialization

Method used

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  • Preparation method of olaparib solid dispersoid and product thereof
  • Preparation method of olaparib solid dispersoid and product thereof
  • Preparation method of olaparib solid dispersoid and product thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Embodiment 1: Preparation of olaparib solid dispersion and capsules.

[0028] Olaparib (50g) and copovidone VA64 (950g) were passed through a 60-mesh sieve respectively, and the sieved olaparib and copovidone VA64 were mixed uniformly to obtain a mixture of raw and auxiliary materials (1000g).

[0029] Set the extrusion temperature of the twin-screw extruder to 150°C. After reaching the temperature, add the above-mentioned mixture of raw and auxiliary materials into the extruder, melt and extrude, and finally extrude in strips to obtain strips. Extrudate (960 g).

[0030] The strip-shaped extrudate was cooled to room temperature, crushed and passed through a 20-mesh sieve to obtain a granular olaparib solid dispersion (960 g).

[0031] According to the filling amount of 50 mg solid dispersion / particle, the above-mentioned granular olaparib solid dispersion is packed into a hard capsule shell to obtain the corresponding capsule.

[0032] According to the second method ...

Embodiment 2

[0034] Embodiment 2: Preparation of olaparib solid dispersion and capsules.

[0035] Olaparib (100g) and povidone K30 (900g) were passed through a 70-mesh sieve respectively, and the sieved olaparib and povidone K30 were mixed uniformly to obtain a mixture of raw and auxiliary materials (1000g).

[0036] Set the extrusion temperature of the twin-screw extruder to 180°C. After reaching the temperature, add the above-mentioned mixture of raw and auxiliary materials into the extruder, melt and extrude, and finally extrude in strips to obtain strips. Extrudate (955 g).

[0037] The strip-shaped extrudate was cooled to room temperature, crushed and passed through a 40-mesh sieve to obtain a granular olaparib solid dispersion (945 g).

[0038] According to the filling amount of 50 mg solid dispersion / particle, the above-mentioned granular olaparib solid dispersion is packed into a hard capsule shell to obtain the corresponding capsule.

[0039] According to the second method of ap...

Embodiment 3

[0041] Embodiment 3: Preparation of olaparib solid dispersion and capsules.

[0042] Olaparib (150g) and povidone K30 (850g) were passed through an 80 mesh sieve respectively, and the sieved olaparib and povidone K30 were mixed uniformly to obtain a mixture of raw and auxiliary materials (1000g).

[0043] Set the extrusion temperature of the twin-screw extruder to 200°C. After reaching the temperature, add the above-mentioned mixture of raw and auxiliary materials into the extruder, melt and extrude, and finally extrude in strips to obtain strips. Extrudate (960 g).

[0044] The strip-shaped extrudate was cooled to room temperature, crushed and passed through a 50-mesh sieve to obtain a granular olaparib solid dispersion (940 g).

[0045] According to the filling amount of 50 mg solid dispersion / particle, the above-mentioned granular olaparib solid dispersion is packed into a hard capsule shell to obtain the corresponding capsule.

[0046] According to the second method of a...

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Abstract

The invention belongs to the field of pharmaceutical preparations and relates to a preparation method of an olaparib solid dispersoid and a product thereof. The preparation method comprises the following steps: 1) sieving olaparib and a hydrophilic high-molecular compound respectively and uniformly mixing the sieved olaparib and the sieved hydrophilic high-molecular compound at a ratio, so as to obtain a raw auxiliary material mixture; 2) adding the raw auxiliary material mixture into an extruding machine achieving the extruding temperature, and fusing and extruding the raw auxiliary material mixture, so as to obtain strip extrudate; 3) cooling, smashing and sieving the strip extrudate, so as to obtain the olaparib solid dispersoid. The solid dispersoid prepared with the method can effectively improve the dissolving-out speed of drugs, the crude drugs do not needs to be micronized, and no special equipment is required to be used, therefore, the process is simple and easy, the cost is low, the energy consumption is less, no solvent residue exists, other impurities are not introduced in the whole process, and continuous mass production is realized easily.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a preparation method of olaparib solid dispersion and a product thereof. Background technique [0002] Olaparib (Olaparib), the chemical name is 1-(cyclopropylformyl)-4-[5-[(3,4-dihydro-4-oxophthalazin-1-yl)methyl]-2 -Fluorobenzoyl]piperazine, an oral polyadenylate diphosphate ribosyltransferase (PARP) inhibitor indicated for the treatment of BRCA-mutated advanced ovarian cancer, has low permeability, low solubility, and low bioavailability. [0003] [0004] At present, the common preparation method of olaparib is to add micronized drug substance into molten excipients, and increase the solubility of the drug through surfactants. However, this method has the following disadvantages: (1) the static electricity produced by the micronized bulk drug is large, and the bulk drug is easy to gather, which affects the dissolution of the drug; Stability; (3) The molten mixtur...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/14A61K9/48A61K47/32A61K31/502A61P35/00
CPCA61K9/1635A61K9/146A61K9/4866A61K31/502
Inventor 燕立波董静金永华
Owner 江苏开元医药有限公司
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