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

Sustained-released injection containing bortezomib and topology enzyme inhibitor

A sustained-release injection, bortezomib technology, applied in the field of medicine, can solve problems such as treatment failure and increased tolerance

Inactive Publication Date: 2009-01-07
济南基福医药科技有限公司
View PDF11 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The latter often leads to increased resistance of tumor cells to anticancer drugs, with consequent treatment failure

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
  • Sustained-released injection containing bortezomib and topology enzyme inhibitor
  • Sustained-released injection containing bortezomib and topology enzyme inhibitor
  • Sustained-released injection containing bortezomib and topology enzyme inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0112] Put 80, 80 and 80 mg of p(BHET-EOP / TC) (BHET-EOP: TC is 80: 20) copolymers into three containers of A, B and C respectively, and then add 100 ml of dichloromethane to each , after dissolving and mixing, add 20mg bortezomib, 20mg camptothecin, 10mg bortezomib and 10mg camptothecin respectively, shake up again and prepare 20% bortezomib, 20% camptothecin, And 10% bortezomib and 10% camptothecin microspheres for injection. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. The release time of the sustained-release injection in physiological saline in vitro is 60-70 days, and the release time in mouse subcutaneous is more than 65 days.

Embodiment 2

[0114] The method step of being processed into sustained-release injection is the same as that of Example 1, but the difference is that the adjuvant used is p(BHET-EOP / TC) of 50:50, containing anticancer active ingredients and their weight percentages: 5-40% Bortezomib or a combination of bortezomib and 1-20% camptothecin or hydroxycamptothecin.

Embodiment 3

[0116] Put 70 mg of p(LAEG-EOP) with a peak molecular weight of 10,000-25,000 into three containers of A, B, and C, respectively, and then add 100 ml of dichloromethane to each, dissolve and mix well, and pour into the three containers respectively Add 30mg bortezomib, 30mg camptothecin, 25mg bortezomib and 5mg camptothecin, shake up again and use spray drying method to prepare 30% bortezomib, 30% camptothecin, 25% bortezomib and 5 % camptothecin microspheres for injection. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The drug release time of the sustained release injection in physiological saline in vitro is 65-70 days, and the drug release time in mice subcutaneous is about 70 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

PropertyMeasurementUnit
Molecular weightaaaaaaaaaa
Login to View More

Abstract

The invention relates to a slow-release injection containing bortezomib and topoismerase inhibitors. The slow-release injection is composed of slow-release microspheres and a solvent, wherein the slow-release microsphere contains an anticancer effective component selected from bortezomib and topoismerase inhibitor and a slow-release adjuvant, and the solvent is a common solvent or a special solvent containing suspending agent. The viscosity of the suspending agent is in the range from 100cp to 3000cp at a temperature ranging from 20 DEG C to 30 DEG C. The suspending agent is preferably sodium carboxymethylcellulose. The slow-release adjuvant is selected from a copolymer of poly(phosphate ester) (such as p(LAEG-EOP) and p(DAPG-EOP)) or a copolymer or a blend of poly(phosphate ester) and PLA or polifeprosan or PLGA or poly(erucic acid dipolymer-sebacic acid). The topoismerase inhibitor is selected from camptothecin, hydroxycamptothecine, topoteean, lurtotecan, irinotecan, etoposide and teniposide. The anticancer composition is also formulated as slow-release implant. After the intratumoral or peritumoral injection or implantation, the effective blood concentration lasts more than 60 days. Additionally, the slow-release injection can significantly reduce the general drug reaction and selectively enhance the chemotherapeutic effect, particularly the effect of non-operative treatment such as local radiotherapy. The slow-release injection is used for the treatment of various solid tumors.

Description

(1) Technical field [0001] The invention relates to a sustained-release injection containing bortezomib and a topoase inhibitor and a preparation method thereof, belonging to the technical field of medicines. (2) Background technology [0002] As commonly used chemotherapeutic drugs, topoase inhibitors and bortezomib have been widely used in the treatment of various malignant tumors, and the effect is relatively obvious. However, its significant toxicity greatly limits the wide application of this class of drugs, and it is easy to develop tolerance when used alone. [0003] Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all higher than those of the surrounding normal tissues. Therefore, it is difficult for conventional chemotherapy to form an effective drug concentration in the tumor. In addition, blood vessels, connective tissue, matrix proteins, fibrin, and c...

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): A61K9/00A61K9/08A61K31/69A61K45/00A61K47/30A61P35/00A61K38/05
Inventor 毛海婷王明华陈颖
Owner 济南基福医药科技有限公司
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