Anticancer composition loaded with melphalan and carmustine
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A carmustine and composition technology, applied in the fields of anticancer compositions, sustained-release implants and sustained-release injections, can solve the problems of slow drug release, toxic reactions, and inability to effectively kill tumor cells, etc.
Inactive Publication Date: 2009-03-18
JINAN SHUAIHUA PHARMA TECH
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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 release drugs too slowly, which...
Method used
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Embodiment 1
[0106] Put 90, 90 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 10mg nimustine, 10mg melphalan, 10mg nimustine and 10mg melphalan respectively, shake up again and prepare 10% nimustine, 10% melphalan Phalan, and microspheres for injection with 10% nimustine 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
[0108] The method step of being processed into sustained release injection is the same as Example 1, but the difference is that the adjuvant used is the p(BHET-EOP / TC) of 50:50, containing anticancer active ingredient and its weight percentage is:
[0109] 5-30% nimustine or carmustine and 5-30% melphalan, cyclophosphamide, ifosfamide, 4H-peroxycyclophosphamide, norcantharidin, dephosphamide, A combination of malfosfamide or pefosfamide.
Embodiment 3
[0111] 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 carmustine, 30mg cyclophosphamide, 15mg carmustine and 15mg cyclophosphamide, re-shake and use spray drying method to prepare 30% carmustine, 30% cyclophosphamide, 15% carmustine Injectable microspheres of statin and 15% cyclophosphamide. 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 carrying melphalan and carmustine is a sustained release injection which consists of sustained release microspheres and a dissolvent, wherein, the sustained release microspheres comprise an anticancer active component and a sustained release adjuvant, and the dissolvent is a common dissolvent or a special dissolvent containing a suspending agent. The suspending agent has the viscosity of 100cp-3000cp (at the temperature of 20-30 DEG C) and is selected from sodium carboxymethyl cellulose and the like; the anticancer active component is a combination of a nitrosourea drug and an alkylating agent selected from the melphalan, ifosfamide, 4H-peroxycyclophosphamide or norcantharidin; the sustained release adjuvant is selected from copolymer of polyphosphate esters such as p(LAEG-EOP), p(DAPG-EOP) and the like, copolymer of the polyphosphate ester and polylactic acid, polifeprosan, dienoic fatty acid and sebacic acid, or copolymer or polyblend of poly(erucic acid dimmer-sebacic acid) or poly(fumaric acid-sebacic acid); the anticancer composition is also made into a sustained release implant, and injected into or placed inside or at the periphery of tumor to keep the effective drug concentration more than 60 days. The anticancer composition can also obviously reduce the general reaction of the drug, and selectively enhance the curative effects of non-operative therapies such as radiotherapy, chemotherapy and the like.
Description
(1) Technical field [0001] The invention relates to an anticancer composition containing nitrosourea drugs and an alkylating agent, belonging to the technical field of medicines. Specifically, the invention relates to a sustained-release preparation capable of stably releasing nitrosourea drugs and alkylating agents locally in solid tumors, mainly sustained-release implants and sustained-release injections, which can prolong the drug release time and Can 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 sud...
Claims
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Application Information
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