Anticancer composition loaded with bortezomib and alkyl agent

A technology of bortezomib and alkylating agent, applied in boron compound active ingredient, drug combination, anti-tumor drug and other directions, can solve the problems of ineffective killing of tumor cells, slow drug release, toxic reaction, etc.

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

AI Technical Summary

Problems solved by technology

[0003] However, the sustained-release excipients used in the existing above-mentioned and other pharmaceutical preparations more or less cause sudden release or uneven release of the drug when the drug is released.
Some drugs are released too slowly, which is not enough to obtain effective drug concentration in the local area, so they cannot effectively kill tumor cells; some release drugs too fast, often causing burst release, which is likely to cause systemic toxic reactions like conventional injections

Method used

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  • Anticancer composition loaded with bortezomib and alkyl agent
  • Anticancer composition loaded with bortezomib and alkyl agent
  • Anticancer composition loaded with bortezomib and alkyl agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0109] Put 90, 90 and 80mg p(BHET-EOP / TC), BHET-EOP: TC is 80:20) copolymer into three containers of A, B and C respectively, and then add 100 ml of dichloromethane to each , after dissolving and mixing, add 10mg bortezomib, 10mg melphalan, 10mg bortezomib and 10mg melphalan respectively, shake up again and use spray drying method to prepare 10% bortezomib, 10% melphalan, and microspheres for injection with 10% bortezomib and 10% melphalan. 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 colon cancer is more than 60 days.

Embodiment 2

[0111] The method step of being processed into slow-release injection is identical with embodiment 1, but difference is that used auxiliary material is the p(BHET-EOP / TC) of 50: 50, containing anticancer active ingredient and weight percent thereof are:

[0112] 5-30% bortezomib with 5-30% melphalan, cyclophosphamide, ifosfamide, 4H-peroxycyclophosphamide, norcantharidin, desphosphamide, mafosfamide, or pefosfamide combination of amides.

Embodiment 3

[0114] 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 cyclophosphamide, 15mg bortezomib and 15mg cyclophosphamide, shake up again and use spray drying method to prepare 30% bortezomib, 30% cyclophosphamide, 15% bortezomib and 15 % cyclophosphamide injection microspheres. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. The release time of the sustained-release injection in physiological saline in vitro is 65-75 days, and the release time in mouse subcutaneous lung cancer is about 65 days.

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Abstract

An anticancer composition comprising bortezomib and an alkylating agent thereof is in form of a sustained-released injection and comprises sustained-released microspheres and a solvent. The sustained-released microspheres comprise an anticancer effective ingredient and a sustained-released adjuvant, and the solvent is a common solvent or a special solvent containing a suspending agent. The suspending agent has a viscosity of 100-3,000cp (20-30 DEG C) and is selected from sodium carboxymethyl cellulose, etc.; the anticancer effective ingredient is bortezomib and an alkylating agent selected from melphalan, iphosphamide, 4-hydro-peroxy-cyclophosphamide and norcantharidin; and the sustained-released adjuvant is a copolymer selected from poly(lactic acid), PLGA, p(LAEG-EOP), p(DAPG-EOP), polifeprosan, poly(erucic acid dimmer-sebacic acid), difatty acid-sebacic acid copolymer, poly(fumaric acid-sebacic acid), etc. or a mixture thereof. The anticancer composition can also be made into a sustained-released implant, which can sustain effective drug concentration for more than 60 days by intratumoral or peritumoral injection or placement, and can distinctly reduce the systemic reaction of the drug and selectively enhance the curative effect of non-operative treatments such as chemotherapy and radiotherapy.

Description

(1) Technical field [0001] The invention relates to an anticancer composition containing bortezomib and an alkylating agent, belonging to the technical field of medicines. Specifically, the invention relates to a sustained-release preparation capable of stably releasing bortezomib and an alkylating agent locally in solid tumors, mainly sustained-release implants and sustained-release injections, which can prolong drug release time and increase Drug sensitivity. (2) Background technology [0002] Local application of chemotherapeutic drugs, especially local sustained release, has become the current research direction and focus of solid tumor chemotherapy. 参见(中国专利申请号200510042234.3,03148624.X,200510042236.2,96116041.1,97107078.4,200510042260.6,200510042261.0,200510042262.5,200510042263.X;美国专利US5651986,RE37410)。 [0003] However, the sustained-release excipients used in the above-mentioned and other existing pharmaceutical preparations more or less cause sudden release or uneve...

Claims

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Application Information

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IPC IPC(8): A61K31/69A61K45/00A61K47/30A61P35/00A61K38/05
Inventor 侯洪春孙启明孙忠先
Owner 济南基福医药科技有限公司
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