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
View PDF8 Cites 0 Cited by
  • 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 ra

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Olaparib composition capsule
  • Olaparib composition capsule
  • Olaparib composition capsule

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0032] Preparation method of olaparib capsules:

[0033] Crush the pharmaceutical ingredients olaparib, starch, di-tert-butyl-p-cresol, sodium alginate, and glyceryl behenate respectively, pass through an 80 mesh sieve, mix uniformly, and send to a dry granulator for granulation, 18 mesh granulation , Capsule filling.

[0034] experiment method:

[0035] 1. Liquidity testing test:

[0036] The fluidity of a solid cannot be expressed by a single characteristic value, it is usually expressed by the angle of repose. Usually refers to the maximum 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 considered that the fluidity is good when θ≤30 degrees, and the fluidity requirements in the production process can be met when θ≤40 degrees. The fluidity of the powder has a greater impact on the weight difference and normal operation of granules, capsu...

Example Embodiment

[0042] Experimental example 1: Prescription screening experiment

[0043]

[0044]

[0045] Because olaparib is easy to absorb moisture and is unstable to heat and humidity, the dry granulation method is given priority to prevent the influence of moisture agent temperature on the raw and auxiliary materials. The specific preparation method is as follows: crush the raw and auxiliary materials separately, pass through an 80-mesh sieve, and send them evenly. Pour into dry granulator for granulation, 18 mesh whole granulation, and capsule filling.

[0046] There are too many screening experimental data. Only part of the important experimental data is listed here. After a large number of experimental screenings, 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 starch is used in combination, the fluidity is very poor, and the differenc...

Example Embodiment

[0047] Experimental example 2: Screening experiment on the dosage of glyceryl behenate and sodium alginate

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

[0049] The amount of disintegrant sodium alginate has a greater impact on the disintegration time and dissolution rate, and if the amount is too small, the disintegration and dissolution requirements cannot be met. Sodium alginate aqueous solution is a viscous disintegrant. The larger the amount, the slower the disintegration and dissolution rate. Therefore, the inventors selected the weight percentage of 14%-18% after a lot of experimental screening.

[0050] Table 2 Screening experiment of dosage of glyce...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap