Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Tipifarnib sustained-release implantation agent for treating solid tumors

A technology of tipifarnib and sustained-release preparations, which can be applied in the field of sustained-release implants or sustained-release injections, and can solve problems such as toxic reactions that limit clinical applications.

Inactive Publication Date: 2008-07-16
SHANDONG LANJIN PHARMA +1
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although it has a certain inhibitory effect on some tumors alone or in combination with other drugs, the toxicity caused by systemic administration greatly limits its clinical application.

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Put the weighed (80mg) sustained-release auxiliary material (polylactic acid (PLA) with a molecular weight of 20000-35000) into the container, add a certain amount of organic solvent to dissolve and mix (subject to complete dissolution), then add 20 mg of substitute Pifranil, shake again and dry in vacuo to remove organic solvents. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a slow-release implant containing 20% ​​tipifarnib. The release time of the slow-release implant in physiological saline in vitro is 18-24 days, and the release time in mouse subcutaneous is 20-25 days.

Embodiment 2

[0082] Sustained-release implants were made according to the method described in Example 1, but the anti-cancer active ingredients contained were one of the following:

[0083] (A) 1% tipifarnib and 99% polylactic acid;

[0084] (B) 5% tipifarnib and 95% polylactic acid;

[0085] (C) 10% tipifarnib and 90% polylactic acid;

[0086] (D) 15% tipifarnib and 85% polylactic acid;

[0087] (E) 20% tipifarnib and 80% polylactic acid.

Embodiment 3

[0089] Put the weighed (85mg) sustained-release excipient (PLGA with a molecular weight of 10000-20000, 50:50) into the container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), then add 15mg of tipine Farney, shake again and dry in vacuo to remove organic solvents. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a slow-release implant containing 15% tipifarnib. The release time of the sustained-release implant in physiological saline in vitro is 25-29 days, and the release time in mouse subcutaneous is 28-32 days.

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 a solid tumors-curing tipifarnib sustained-release implant, which is characterized in that the sustained-release implant contains effective anti-tumor dose of tipifarnib, sustained-release auxiliary material and a certain amount of sustained-release regulator. Solid tumors consist of lung cancer, esophageal cancer, gastric cancer, liver cancer, breast cancer, ovarian cancer, prostatic cancer, bladder cancer and colorectal cancer. The sustained-release auxiliary materials are mainly one or mixture of copolymer of glycolic acid and hydroxyacetic acid, polifeprosan, poly (L-lactide-co-ethyl phosphate) and poly (L-lactide-co-propyl phosphate). When the sustained-release auxiliary materials are degrading and absorbed, tipifarnib is slowly released into tumor part, thus while reducing toxic reaction of the whole body, the sustained-release auxiliary materials can sustain concentration of effective drug at the tumor part. Placing the anti-tumor sustained-release implant at the tumor part can not only reduce toxic reaction of the whole body of tipifarnib, but also improve drug concentration at the tumor part and enhance treatment effects of nonspecific treatments, such as chemotherapeutics, radiotherapy, etc.

Description

(1) Technical field [0001] The invention relates to a sustained-release agent for tipifarnib for treating solid tumors, which is a sustained-release implant or sustained-release injection, and belongs to the technical field of medicines. (2) Background technology [0002] The incidence of cancer is increasing year by year and tends to be younger. Statistics show that in less than 20 years, the incidence of cancer in my country has increased by 69%, and the mortality rate has increased by 29.4%. According to the latest statistics from the World Health Organization, the global cancer incidence rate will increase by 50% by 2020, and the number of patients will increase to 15 million. It is estimated that 4 million people will die of cancer every year in my country in 2020. Therefore, exploring an effective method or drug for treating cancer has become a hot research topic at present. [0003] Tipifanib is a farnesyltransferase inhibitor used in the treatment of acute myeloid l...

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): A61K9/00A61K31/4709A61K47/34A61P35/00
Inventor 孔庆忠丛波
Owner SHANDONG LANJIN PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com