Niraparib granules with high utilization efficiency and preparation method thereof

A granule and high-efficiency technology, applied in the field of highly utilized niraparib granule and its preparation, can solve the problems of short service life and inconvenient application of electronically controlled valves, and achieve the effects of maintaining medicinal effect, increasing concentration and reducing waste.

Active Publication Date: 2019-10-11
ANHUI HAIKANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Granules usually need to be packaged in separate bags with a granule packaging machine during preparation, while the existing impact packaging machines usually use the frequent opening and closing of the electric control valve at the discharge port to realize quantitative feeding, and the service life of the electric control valve is short ; The existing granule packaging machine immediately closes the electronically controlled valve when it detects that the remaining amount of granule is less than the preset value. The amount required for one bag, if you don’t want to waste the granule, you need to collect this part of the granule and return it to the storage box, which is inconvenient to use

Method used

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  • Niraparib granules with high utilization efficiency and preparation method thereof
  • Niraparib granules with high utilization efficiency and preparation method thereof
  • Niraparib granules with high utilization efficiency and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] A highly efficient niraparib granule, comprising the following components in parts by weight:

[0052] 5 parts nirapani;

[0053] 5 parts of carboxylesterase inhibitors;

[0054] 8 parts of glucose;

[0055] Vitamin C 2 parts;

[0056] 75 parts of filler;

[0057] 3 parts of disintegrant.

[0058] In this embodiment, the filler is pregelatinized starch.

[0059] In this embodiment, the disintegrating agent is a composition of sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose and croscarmellose sodium, and their mass ratio is 2:1:1.

[0060] The preparation method of the niraparib granule of above-mentioned efficient utilization comprises the steps:

[0061] S1. Soft material preparation: After making a thick paste from highly utilized niraparib granules, carboxylesterase inhibitors, glucose and vitamin C, mix it with a filler and a disintegrant to make a soft material;

[0062] S2. Making wet granules: turn on the swing granulator to preheat, a...

Embodiment 2

[0082] The difference between this embodiment and embodiment 1 is:

[0083] A highly efficient niraparib granule, comprising the following components in parts by weight:

[0084] Nirapani 6.5 parts;

[0085] 4.5 parts of carboxylesterase inhibitors;

[0086] Glucose 8.5 parts;

[0087] Vitamin C 2.5 parts;

[0088] 72 parts of filler;

[0089] 3.5 parts of disintegrant.

[0090] In this embodiment, the filler is a composition of lactose and microcrystalline cellulose, and their mass ratio is 2:5.

[0091] In this embodiment, the disintegrant is low-substituted hydroxypropyl cellulose.

[0092] In this embodiment, the mesh size of the oscillating granulator described in step S2 of the preparation method is 50 mesh, and the rotating speed of the drum of the oscillating granulator is 5 r / min.

[0093] In the present embodiment, according to a kind of highly utilized Nirapani granule according to claim 1, it is characterized in that the temperature of the hot air introduced...

Embodiment 3

[0096] The difference between this embodiment and embodiment 1 is:

[0097] A highly efficient niraparib granule, comprising the following components in parts by weight:

[0098] Nirapani 7.5 parts;

[0099] 4 parts of carboxylesterase inhibitor;

[0100] 9 parts of glucose;

[0101] Vitamin C 3 parts;

[0102] 70 parts of filler;

[0103] 4 parts of disintegrant.

[0104] In this embodiment, the filler is a composition of pregelatinized starch, lactose and microcrystalline cellulose, and their mass ratio is 3:1:2.

[0105] In this embodiment, the disintegrating agent is a composition of sodium carboxymethyl starch and croscarmellose sodium, and their mass ratio is 3:1.

[0106] In this embodiment, the mesh size of the oscillating granulator described in step S2 of the preparation method is 50 mesh, and the rotating speed of the drum of the oscillating granulator is 80 r / min.

[0107] In the present embodiment, according to claim 1, a highly efficient Niraparib granule is...

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Abstract

The invention discloses niraparib granules with a high utilization efficiency and a preparation method thereof, and belongs to the technical field of medicine production. The components of the niraparib granules include niraparib, glucose, vitamin C and a carboxylesterase inhibitor. A granule packaging machine adopted in the preparation method comprises a storage bin and a transparent upper discharge pipe, wherein the transparent upper discharge pipe penetrates through the storage bin, the two sides of the upper discharge pipe are provided with an infrared emitter and an infrared receiver respectively, the infrared emitter and the infrared receiver are capable of lifting and lowering, a turntable is arranged below the upper discharge pipe, a curved through hole is formed in the turntable,a retractable stop block with a proximity switch is arranged on one side of the turntable, and a curved groove is formed in the turntable. By adopting the niraparib granules, the amount of niraparib discharged along with excretion can be reduced, and the pharmacodynamic effect of the niraparib can be maintained; valve-related components of the granule packaging machine adopted in the preparation process of the niraparib granules have longer service life, it can be ensured that the amount of the material discharged each time is sufficient, the remaining granules with a remaining amount less than a set value are remained in the upper discharge pipe, and the application is convenient.

Description

technical field [0001] The invention relates to the technical field of medicine production, in particular to a highly utilized niraparib granule and a preparation method thereof. Background technique [0002] Niraparib (Niraparib) is an oral poly ADP-ribose polymerase (PARP) inhibitor, mainly targeting cancers with BRCA1 / 2 gene mutations, developed for ovarian cancer and breast cancer. Niraparib inhibits the repair of cells to DNA damage. For cancer cells with BRCA gene mutations, if PARP activity is further inhibited, a large amount of DNA damage will be generated when these cells divide, leading to the death of cancer cells. The chemical name of Nirapa is 2-[4-((3S)-3-piperidinyl)phenyl]-2H-indazole-7-carboxamide, which was developed by Merck and later transferred to American Biotechnology The company Tesaro, which announced the phase III clinical data of niraparib for advanced ovarian cancer, showed extremely good efficacy. [0003] According to research, after a single...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61J3/02B65B1/06B65B1/36B65B37/00
CPCA61J3/02A61J2200/42A61J2200/70B65B1/06B65B1/36B65B37/00
Inventor 张小顺
Owner ANHUI HAIKANG PHARMA
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