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Olaparib solid dispersion preparation and preparation method thereof

A solid dispersion and tablet technology, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, pill delivery, etc., can solve the impact of the stability of olaparib preparations, narrow access, lack of Safety and other issues, to achieve the effect of ensuring the dissolution effect, bioavailability and stability, which is conducive to industrial production and has a wide range of sources

Active Publication Date: 2015-03-25
BEIJING COLLAB PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] However, this patent uses copovidone as a matrix polymer, but copovidone has a relatively high cost and narrow acquisition channels, which is not conducive to large-scale industrial production. At the same time, copovidone is not commonly used in preparations. The 2010 edition " The Chinese Pharmacopoeia is not included in the Pharmacopoeia, lacking certain security
Compared with copovidone, povidone not only has a wide source and low cost, and is included in the 2010 edition of "Chinese Pharmacopoeia", but there is a fatal defect in preparing solid dispersions with povidone as the matrix polymer, namely Under accelerated test conditions, the dissolution rate gradually decreases with time, and a specific crystal form appears. Table 12 and paragraph 0217 on page 28 of the patent CN102238945A disclose the defect of povidone, which affects the stability of olaparib preparations. It has caused an impact, which is not conducive to the preservation of the preparation

Method used

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  • Olaparib solid dispersion preparation and preparation method thereof
  • Olaparib solid dispersion preparation and preparation method thereof
  • Olaparib solid dispersion preparation and preparation method thereof

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preparation example Construction

[0053] According to the preparation scheme of the present invention, those skilled in the art can choose the melt extrusion method, spray drying method and solvent evaporation method that have been matured in the art to prepare the olaparib solid dispersion, and can also be prepared according to the three methods described in the present invention. A kind of preparation scheme is prepared, and the method is as follows:

[0054] 1. Melt extrusion method

[0055] Take the prescribed amount of olaparib and povidone, add part of the lubricant, mix well, and put the mixture in a twin-screw extruder to extrude the mixture. During the extrusion process, apply a vacuum to the extrusion barrel to remove the melt The extrudate is calendered by passing it through two counter-rotating calender rolls, followed by cooling before grinding to obtain a solid dispersion.

[0056] 2. Spray drying method

[0057] Dissolve the Olaparib and povidone in the prescribed amount in an organic solvent ...

Embodiment 1

[0061] Embodiment 1: Olaparib solid dispersion tablet

[0062] prescription:

[0063] components

mg / tablet

olapani

25

Povidone K30

125

Microcrystalline Cellulose pH102

40

Croscarmellose Sodium

8

Sodium dodecyl sulfate

1

Magnesium stearate

1

Sheet weight

200

[0064] Preparation process: solvent evaporation method

[0065] Dissolve the prescribed amount of Olaparib and Povidone K30 in a solvent of acetone:methanol (1:3), volatilize under reduced pressure in a water bath at 60°C, vacuum degree 0.07-0.08MPa, and recover organic matter under reduced pressure. After the solvent becomes viscous, continue vacuum drying under reduced pressure for 1 hour, transfer to a vacuum drying oven, dry at 40°C for 48 hours, and pass through an 80-mesh sieve to pulverize to obtain a solid dispersion.

[0066] Add the prepared solid dispersion to the prescription amount of microcrystalline cellulos...

Embodiment 2

[0067] Embodiment 2: Olaparib solid dispersion tablet

[0068] prescription:

[0069] components

mg / tablet

olapani

25

[0070] Povidone K30

75

Microcrystalline Cellulose pH102

60

Crospovidone

6

Sodium dodecyl sulfate

1

Talc powder

2

Sheet weight

169

[0071] Preparation process: solvent evaporation method

[0072] Take Olaparib and povidone K30 in the prescribed amount, dissolve them in methanol:dichloromethane (4:1) solvent, put them in a water bath at 60°C, vacuum 0.07-0.08MPa, recover the organic solvent under reduced pressure, wait for After becoming viscous, continue vacuum drying under reduced pressure for 1 hour, transfer to a vacuum drying oven, dry at 40°C for 48 hours, and pass through an 80-mesh sieve to pulverize to obtain a solid dispersion.

[0073] The prepared solid dispersion is added into the prescribed amount of microcrystalline cellulose pH102, cros...

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Abstract

The invention relates to the field of a pharmaceutical preparation, and in particular discloses an olaparib solid dispersion preparation and a preparation method thereof. The olaparib solid dispersion preparation consists of olaparib, povidone, a special lubricating agent, a special disintegrating agent and a thinner. According to the olaparib solid dispersion preparation disclosed by the invention, povidone, replacing the existing copovidone, is used as a matrix polymer, and appropriate auxiliary materials are added, so that the povidone, as the matrix polymer of the olaparib solid dispersion preparation, is wide in source, low in cost and clear in quality standard in accordance with Chinese Pharmacopoeia; meanwhile, the dissolution effect, bioavailability and stability of the preparation are guaranteed; and the industrial production of the olaparib solid dispersion preparation is facilitated.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an olaparib solid dispersion preparation and a preparation method thereof. Background technique [0002] Olaparib, chemically known as 4-[3-(4-cyclopropanecarboxy-piperazine-1-carboxy)-4-fluoro-benzyl]-2H-phenazin-1-one, can be used to provide poly- ADP-ribose polymerase (PARP) inhibition. This effect can be used in the treatment of cancers, such as breast or ovarian cancer, which can be particularly effective in the treatment of cancers whose cells are defective in the homologous recombination (HR)-dependent DNA double bond break (DSB) repair pathway, such as BRCA1+ and / or BRCA2+ve cancer. [0003] 4-[3-(4-cyclopropanecarboxy-piperazine-1-carboxy)-4-fluoro-benzyl]-2H- Phenazin-1-one, which has the following structure: [0004] [0005] Olaparib is a drug with low solubility and low bioavailability. Ordinary preparations cannot improve the dissolution rate and b...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/16A61K9/20A61K9/48A61K31/502A61K47/32A61P35/00
Inventor 申超邱敦有王珂赵大龙邹德超
Owner BEIJING COLLAB PHARMA
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