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Olaparib composition capsules

A technology of composition and capsule, applied in the field of olaparib composition capsule, which can solve the problems of no further prompting, difficulty in quality control, aging, etc.

Inactive Publication Date: 2017-11-24
HUNAN QIWEI TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the solid dispersion preparation has the following disadvantages: (1) it is not suitable for large doses of medicines; (2) its carrier consumption is large, the stability of the drug dispersion state is not high, and long-term storage is prone to aging phenomenon, that is, the hardness of the solid dispersion Increased size, precipitation of crystals, or coarsening of crystals, thereby reducing the bioavailability of the drug
(4) The preparation process of solid dispersion preparations is complex, the requirements for carrier properties are relatively high, and quality control is relatively difficult
However, how to obtain a better dissolution rate through a suitable prescription and process, improve its fluidity and loading difference, reduce its moisture content, and further improve its stability, the prior art does not give further hints, in view of this, especially proposed this invention
[0010] The invention aims to overcome the problems of poor fluidity, low dissolution rate, obvious difference in filling capacity and high water content of the existing olaparib capsules, and the obtained olaparib capsules have high stability, good fluidity and low difference in filling capacity. , high dissolution rate, low moisture content, greatly improving the safety and effectiveness of medication

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0035] The preparation method of olaparib capsules:

[0036] The pharmaceutical ingredients olaparib and mannitol were crushed and sieved to 100 meshes, and then the pulverized materials, dextrin, potassium metaphosphate, polacrilin potassium, and acetylated monoglyceride were mixed evenly in a mixer, and sent into Granulated in a dry granulator, 18 mesh whole granules, filled in capsules.

[0037] experiment method:

[0038] 1. Liquidity test:

[0039] The fluidity of a solid cannot be expressed by a single characteristic value, and it is often expressed by the angle of repose. It usually refers to the largest angle formed by the free slope of the powder accumulation layer and the horizontal plane. The smaller the angle of repose, the smaller the friction, and the better the fluidity. It is generally believed that when θ≤30 degrees, the fluidity is good, and when θ≤40 degrees, it can meet the fluidity requirements in the production process. The fluidity of powder has a gr...

experiment example 1

[0045] Experimental Example 1: Prescription Screening Experiment

[0046]

[0047]

[0048] Because olaparib is easy to absorb moisture and is unstable to heat and humidity, the dry granulation method is preferred to prevent the influence of the temperature of the water agent on the raw and auxiliary materials. The specific preparation method is as follows: the pharmaceutical ingredients olaparib and mannitol are pulverized Sieve 100 mesh, then put crushed material and dextrin, potassium metaphosphate, polacrilin potassium, acetylated monoglyceride in a mixer and mix evenly, send it to dry granulator for granulation, 18 mesh granulation, Capsule filling.

[0049] There are too many screening experimental data, and only some important experimental data are listed here. After a large number of experimental screenings, the inventor found that when hydroxypropyl cellulose was combined with starch, mannitol, and dextrin, the dissolution rate was not good, especially the hydro...

experiment example 2

[0050] Experimental Example 2: Screening experiment of dosage of acetylated monoglyceride and polacrilin potassium

[0051] This experimental example is when preparing olaparib capsules, as the dosage screening experiment of acetylated monoglyceride and polacrilin potassium, the weight percentage content of each raw material is controlled: olaparib 23%, mannitol 40%, 25% dextrin and 0.5% potassium metaphosphate, on the basis of which the weight percent content of acetylated monoglyceride and polacrilin potassium is adjusted.

[0052] The dosage of disintegrant polacrilin potassium has great influence on the disintegration time and dissolution rate, and its dosage is too small to meet the requirements of disintegration and dissolution. The greater the dosage of polacrilin potassium, the slower the disintegration and dissolution rate. Therefore, the inventors selected 8.5%-10.5% by weight after a large number of experimental screenings.

[0053]

[0054] The above-mentioned...

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Abstract

The invention relates to the field of pharmaceutical preparations, and specifically discloses an olaparib composition capsule. The olaparib composition capsule of the present invention comprises olaparib, mannitol, dextrin, potassium metaphosphate, polacrilin potassium, and acetylated monoglyceride. The present invention preferably uses olaparib, mannitol, dextrin, potassium metaphosphate, polacrilin potassium, and acetylated monoglyceride as the composition of olaparib capsules, and the mutual synergy improves the stability of olaparib, Fluidity and dissolution rate, reducing water content, is conducive to the safe use and long-term storage of clinical drugs.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an olaparib composition capsule. 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-phenol is disclosed and exemplified in International Patent Application Publication No. WO2004 / 080976 (compound 168) Oxin-1-ones, which have the following structure: [0004] [0005] Olaparib is a drug with low solubility and low bioavail...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/502A61K47/26A61K47/36A61K47/02A61K47/32A61K47/14A61P35/00
CPCA61K9/1652A61K9/1611A61K9/1617A61K9/1623A61K9/1635A61K31/502
Inventor 朱社凤
Owner HUNAN QIWEI TECH CO LTD
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