Olaparib composition capsule

A composition and capsule technology, applied in the field of olaparib composition capsules, can solve the problems of high water content, large amount of carrier, and no further prompts are given.

Active Publication Date: 2017-12-15
SHANDONG YUXIN PHARMA 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

[0032] The preparation method of olaparib capsules:

[0033] Separately pulverize the drug ingredients olaparib, starch, di-tert-butyl-p-cresol, sodium alginate, glyceryl behenate, pass through a 80-mesh sieve, mix them evenly and send them to a dry granulator for granulation, 18-mesh granulation , Capsule Filling.

[0034] experiment method:

[0035] 1. Liquidity test:

[0036] 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 great influence on the weight difference and normal operation of granules, capsu...

experiment example 1

[0042] Experimental Example 1: Prescription Screening Experiment

[0043]

[0044]

[0045] Since 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 moisture agent on the raw and auxiliary materials. Put it into a dry granulator for granulation, 18-mesh granulation, and capsule filling.

[0046] There are too many screening experimental data, and here are only some important experimental data. After a large number of experimental screening, the inventor found that when hydroxypropyl cellulose is combined with starch or lactose, the dissolution rate is not good, especially when hydroxypropyl cellulose is combined with starch or lactose. When the starch is combined and applied, the fluidity is very poor, and the difference in loading is obvious; when the lubricant is changed to glyceryl behenate, the fluidity is significantly improved, but the dissolution rate ...

experiment example 2

[0047] Experimental Example 2: Screening experiment of dosage of glyceryl behenate and sodium alginate

[0048] This experimental example is used as a dosage screening experiment of glyceryl behenate and sodium alginate when preparing olaparib capsules, and the weight percentage of each raw material is controlled: olaparib 30%-35%, starch 50.4% -53.5%, di-tert-butyl-p-cresol 0.1%-0.3%, on this basis, adjust the weight percent content of glyceryl behenate and sodium alginate.

[0049] The amount of disintegrating agent sodium alginate has a great influence on the disintegration time and dissolution rate, and if the amount is too small, it cannot meet the requirements of disintegration and dissolution. Sodium alginate aqueous solution is a viscous disintegrating agent, the larger the dosage, the slower the disintegration and dissolution rate. Therefore, the inventors selected 14%-18% by weight after a large number of experimental screenings.

[0050] Table 2 The amount screeni...

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Abstract

The invention relates to the field of medicinal preparations, and particularly discloses an olaparib composition capsule. The olaparib composition capsule comprises olaparib, starch, di-tert-butyl p-cresol, sodium alginate and glyceryl behenate. The olaparib, the starch, di-tert-butyl p-cresol, sodium alginate and glyceryl behenate are preferably selected to form a composition of the olaparib capsule, and through a mutual synergistic effect, the stability, the fluidity and the dissolution rate of the olaparib are improved and the water content is reduced, so that the safe use and long-term storage of a clinical medicine are facilitated.

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- Phenazin-1-one, which has the following structure: [0004] [0005] Olaparib is a drug with low solubility and low bioavailability. The conventional preparation method has poor dissolution effect, poor quality stability and low bioavaila...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/502A61K47/36A61K47/14A61K47/10A61P35/00
CPCA61K9/1617A61K9/1652A61K31/502
Inventor 刘振腾孙逸威王立标公文举
Owner SHANDONG YUXIN PHARMA CO LTD
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