Unlock instant, AI-driven research and patent intelligence for your innovation.

Regorafenib dispersing agent and preparation method thereof

A technology of regorafenib and dispersant, which is applied in the field of pharmaceutical preparations, can solve the problems of low dissolution rate of active ingredients, low bioavailability, difficult preparation of dosage forms, etc., and achieves simple preparation method, is conducive to the exertion of drug efficacy, and high efficiency. The effect of blood concentration

Inactive Publication Date: 2021-05-28
深圳市简一生物科技有限公司
View PDF8 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the limited solubility of regorafenib monohydrate (almost insoluble in common solvents), the existing dosage forms have low dissolution rate of active ingredients, low bioavailability, and difficulty in preparation of dosage forms. Therefore, it is necessary to provide A kind of regorafenib solid dispersion that can not only improve solubility or dissolution rate, but also have higher drug loading capacity, and can be further prepared for preparation and preparation method thereof

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
  • Regorafenib dispersing agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024]The present invention provides a technical solution: a Riggo non-dispersant and a preparation method thereof, including Ruigi Ni, carrier materials, and drug synergists;

[0025]The Riggo non-Ni, carrier materials and synergists are composed of 1: (2 to 15): (2 to 5);

[0026]The carrier material is composed of polymeridone and polyacrylamide in a mass ratio of 1: (1 to 5);

[0027]The drug synergist is composed of silica and sodium dodecyl sulfate in a mass ratio of 1: (1 to 2).

[0028]In the present embodiment, it is preferable that the synergist is a mass ratio of silica and sodium dodecyl sulfate in 1: 1.

[0029]In the present embodiment, it is preferable that the synergist is a mass ratio of silica and sodium dodecyl sulfate in 1: 1.

[0030]In the present embodiment, it is preferred that the Riggo non-Ni, carrier materials, and synergists consist of 1: 5: 1.

[0031]In the present embodiment, preferred, polymeridone is selected from one or more of the polymeridone K15, the polymeridone K25...

Embodiment 2

[0041]The present invention provides a technical solution: a Riggo non-dispersant and a preparation method thereof, including Ruigi Ni, carrier materials, and drug synergists;

[0042]The Riggo non-Ni, carrier materials and synergists are composed of 1: (2 to 15): (2 to 5);

[0043]The carrier material is composed of polymeridone and polyacrylamide in a mass ratio of 1: (1 to 5);

[0044]The drug synergist is composed of silica and sodium dodecyl sulfate in a mass ratio of 1: (1 to 2).

[0045]In the present embodiment, it is preferable that the synergist is a mass ratio of silica and sodium dodecyl sulfate in 1: 1.

[0046]In the present embodiment, it is preferable that the synergist is a mass ratio of silica and sodium dodecyl sulfate in 1: 1.

[0047]In the present embodiment, it is preferred that the Riggo non-Ni, carrier materials, and synergists consist of 1: 5: 1.

[0048]In the present embodiment, preferred, polymeridone is selected from one or more of the polymeridone K15, the polymeridone K25...

Embodiment 3

[0058]The present invention provides a technical solution: a Riggo non-dispersant and a preparation method thereof, including Ruigi Ni, carrier materials, and drug synergists;

[0059]The Riggo non-Ni, carrier materials and synergists are composed of 1: (2 to 15): (2 to 5);

[0060]The carrier material is composed of polymeridone and polyacrylamide in a mass ratio of 1: (1 to 5);

[0061]The drug synergist is composed of silica and sodium dodecyl sulfate in a mass ratio of 1: (1 to 2).

[0062]In the present embodiment, it is preferable that the synergist is a mass ratio of silica and sodium dodecyl sulfate in 1: 1.

[0063]In the present embodiment, it is preferable that the synergist is a mass ratio of silica and sodium dodecyl sulfate in 1: 1.

[0064]In the present embodiment, it is preferred that the Riggo non-Ni, carrier materials, and synergists consist of 1: 5: 1.

[0065]In the present embodiment, preferred, polymeridone is selected from one or more of the polymeridone K15, the polymeridone K25...

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

PropertyMeasurementUnit
concentrationaaaaaaaaaa
Login to View More

Abstract

The invention discloses a regorafenib dispersing agent and a preparation method thereof. The regorafenib dispersing agent comprises regorafenib, a carrier material and a drug synergist;the regorafenib, and the mass ratio of regorafenib to the carrier material to the synergist is 1:(2-15):(2-5); the carrier material is composed of povidone and polyacrylamide in a mass ratio of 1:(1-5); and the drug synergist is composed of silicon dioxide and lauryl sodium sulfate according to the mass ratio of 1:(1-2). The regorafenib is made into a solid dispersion with a polyacrylamide-regorafenib-povidone sandwich structure through a certain process, dissolution of the regorafenib is promoted from inside to outside, meanwhile, the aging phenomenon of the solid dispersion in the long-time storage process can be avoided, the stability is improved, the dissolution rate of the dispersing agent can be larger than or equal to 90% in 30 minutes; therefore, a relatively high blood concentration can be quickly achieved, the bioavailability of the regorafenib is effectively improved, and the drug effect is more favorably exerted.

Description

Technical field[0001]The present invention relates to the field of pharmaceutical preparations, and in particular, to a Riggo non-dispersant and a preparation method thereof.Background technique[0002]Riggo non-Ni Ni, the chemical name is: N ~ (4 ~ chloride ~ 3 ~ (trifluoromethyl) phenyl) ~ n '~ 2 ~ fluorine ~ (4 ~ (2 ~ (N ~ methyldinyl) ~ 4 ~ pyridyloxy) phenyl) urea, the structural formula is: is a new type of polyhase inhibitor, which can block a variety of enzymes that promote tumor growth, which is discovered and developed by Bayer, is an effective anti-cancer. And anti-angiogenic agents have various activity, including inhibitory activity against VEGFR, PDGFR, RAF, P38, and / or FLT to 3 kinase signals, and it can be used to treat various diseases and conditions, such as overprivified diseases. For example: cancer, tumor, lymphoid cancer, sarcoma and leukemia, mainly for the treatment of metastatic colorectal cancer, gastrointestinal tumor tumors. There is no hydrophilic group ...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/32A61K47/04A61K47/20A61K31/44A61P35/00A61P35/04
CPCA61K9/146A61K9/145A61K9/143A61K31/44A61P35/00A61P35/04
Inventor 邹情陈文青陈粮许倩彭惠慧
Owner 深圳市简一生物科技有限公司