41 results about "Nimustine" patented technology

The invention relates to anticancer sustained release injection which comprises sustained release microspheres and menstruum, wherein, the sustained release microspheres comprise anticancer active components and sustained release auxiliary material; the menstruum is special menstruum that contains suspending agent. The anticancer active components are fotemustine, nimustine, carmustine or combination of bendamustine and mitozolomide, docetaxel, etoposide, teniposide, vinblastine, anastrozole, tamoxifen, fluorouracil or mitomycin C; the sustained release auxiliary material is polylactic acid and polylactic acid copolymer, polyethylene glycol and polylactic acid copolymer of polyethylene glycol, terminal carboxyl group polylactic acid copolymer, EVAc, fatty acid and decanedioic acid copolymer, etc.; viscosity of the suspending agent is 100cp-3,000cp (at 25 DEG C-30 DEG C), and the suspending agent is selected from sodium carboxymethylcellulose, etc. The sustained release microspheres can also be made into sustained release implant; the injection or implant is injected or placed in or around tumor so as to reduce general reaction of the drug and selectively improve and keep local concentration for about 30-50 days. The anticancer sustained release injection can be used solely and can also promote anti-tumor effects of non-operative treatments, such as chemotherapy and/or radiotherapy, etc.

The invention relates to an anticancer slow-release gel injection and a preparation method thereof. The anticancer slow-release gel injection contains a taxane-like drug such as paclitaxel, docetaxel, hydroxypaclitaxel, epi-paclitaxel or deacetylpaclitaxel, a stine-like drug, an amphiphilic block polymer and a solvent. The composition exhibits the property of temperature-sensitive gelation, is a flowable liquid at the room temperature and turns into a stagnant and biodegradable water-insoluble gel in vivo in warm-blooded animals. The stine-like drug is selected from atrimustine, ambnmustine, nimustine, bendamustine, carmustine, elmustine, galamustine, fotemustine, estramustine, hesmustine, neptamustine, lomustine, semustine, ranimustine, semustine, tauromustine, tallimustine and spiromustine. The anticancer slow-release gel injection can release the drug slowly and locally around the tumor and retain the effective blood concentration for a plurality of weeks to a plurality of months, can not only kill tumor cells but also effectively inhibit tumor vessels, can reduce the general drug toxicity and can enhance the curative effect of chemotherapy particularly radioactive seed implantation.

Disclosed is slow release anticancer agent carrying both Nimustine and its synergistic agents, which comprises slow release auxiliary materials and active anticancer constituents, wherein the active anticancer constituents include Nimustine and its synergistic agents (such as Docetaxel, hydroxycamptothecin or 4-hydroperoxycyclophosphamide). The viscosity of the slow release injection is 10-650cp (at 20-30 deg C), and the active anticancer constituents can also be made into slow release implanting agent. The slow release subsidiary materials mainly comprise bio-compactable and degradable macromolecular polymers, when locally dispensed on the tumor, the composition not only can lower down the whole body toxicity reaction of the anti-cancer medicament, but also can selectively increase the tumor local medicinal concentration, the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can also be improved. The solid tumors include glioma, osteosarcoma, lymphoma, lung carcinoma, intestinal cancer and breast cancer.

A new anticarcinogenic sustained-release injection consists of sustained-release microballoon sphere and menstruum; wherein, the sustained-release microballoon sphere comprises anticarcinogenic active ingredient and sustained-release accessory material; the menstruum is special menstruum containing suspending agent. The anticarcinogenic active ingredient is the combination of cytotoxic drugs of fotemustine, bendamustine, tallimustine, carmustinum, nimustine, lomustine, semustine or ranimustine and adriamycin, epirubicin, melphalan, 4H peroxide cyclophosphamide, actinomycin D, vinorelbine or nolvadex, etc.; the sustained-release accessory material is selected from polylactic acid and the multipolymer or mixture thereof, mono-methyl polyethyleneglycol, polyethyleneglycol or polylactic acid multipolymer, EVAc, the multipolymer of fatty acid and decanedioic acid, etc.; the viscosity of the suspending agent is 100cp-3000cp (at the temperature of 25 DEG C-30 DEG C), the suspending agent is selected from sodium carboxymethyl cellulose, etc. The sustained-release microballoon sphere also can be made into sustained-release implant which can be injected and placed in tumor or around tumor and can release medicine at the local parts of the tumor for 30 to 40 days; therefore, the anticarcinogenic sustained-release injection can be separately united together with non-operativetreatment such as chemo-treatment and/or radiation treatment, etc. for application.

The invention relates to a slow-release implant agent of nimustine, which is characterized in comprising amounts of nimustine, slow-release excipients and releasing regulatory agents in the slow-release implant agent. The excipients comprise macromolecules which are biologically compatible and degradable, mainly PLA and PLGA. The releasing regulatory agents are selected from one or more items from mannitol, sorbitol, xylitol, oligosaccharide, chitin, potassium salt, sodium salt, hyaluronic acid, collagen, chondroitin, gelatin and albumin. The slow-release implant agent slowly releases nimustine on the local tumor in the process of degradation and absorption, so the argent can evidently reduce the systemic toxicity and simultaneously apply to the effective drug concentration control on the local tumor. Therefore, the argent can be applied separately or combined with the non-surgical treatments such as chemotherapy drug and radiotherapy, which can also be widely used for tumor treatment of different phases, not only selectively improving the drug concentration on local tumor but also reinforcing the therapeutic effect of non-surgical treatments such as chemotherapy drug and radiotherapy.

Disclosed is a slow release injection containing platinum-group compounds and/or alkylating agents, which comprises slow release microspheres and dissolvent, the slow release microspheres include platinum-group compounds selected from Tegafur, Capecittabine, Pemetrexed, Carboplatin or Gemcitabine, and/or alkylating agent anticancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), copolymer or blend of polyphosphate ester with PLA, Polifeprosan, poly(dodecanedioic acid-tetradecanedioic acid) or poly(fumaric acid-sebacylic acid). The alkylating agent is selected from Carmustine, Nimustine, Fotemustine, Lomustine or bendamustine. The anticancer composition can also be prepared into slow release implanting agent, for injection or placement in or around tumor with a period of effective concentration maintenance over 60 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.

The invention relates to anticancer sustained release injection which comprises sustained release microspheres and menstruum, wherein, the sustained release microspheres comprise anticancer active components and sustained release auxiliary material; the menstruum is special menstruum that contains suspending agent. The anticancer active components are fotemustine, nimustine, carmustine or combination of bendamustine and mitozolomide, docetaxel, etoposide, teniposide, vinblastine, anastrozole, tamoxifen, fluorouracil or mitomycin C; the sustained release auxiliary material is polylactic acid and polylactic acid copolymer, polyethylene glycol and polylactic acid copolymer of polyethylene glycol, terminal carboxyl group polylactic acid copolymer, EVAc, fatty acid and decanedioic acid copolymer, etc.; viscosity of the suspending agent is 100cp-3,000cp (at 25 DEG C-30 DEG C), and the suspending agent is selected from sodium carboxymethylcellulose, etc. The sustained release microspheres can also be made into sustained release implant; the injection or implant is injected or placed in or around tumor so as to reduce general reaction of the drug and selectively improve and keep local concentration for about 30-50 days. The anticancer sustained release injection can be used solely and can also promote anti-tumor effects of non-operative treatments, such as chemotherapy and/or radiotherapy, etc.

A nimustine slow release injection for treating solid cancer comprises slow release finding and nimustine, or the combination of nimustine and relative booster (pidorubicin, osaliplatinum, adriablastina, amethopterin or the like). The viscidity of slow-release injection is 10-650cp (20-30Deg. C). The anti-cancer effective component can be made into slow release plant agent. The slow release finding substantially comprises macromolecule polymer with biological soluble degradable and absorb property, which can slow release the anti-cancer effective component to cancer part in the degradation process, significantly reduce general reaction and hold effective drug density on cancer. The anti-cancer compound can be arranged part of cancer to reduce the general toxicity reaction, selectively improve the drug density locally, and strengthen the effect of non-surgery treatments as chemotherapy, and radiation therapy or the like. The solid cancer comprises glioma, lung carcinoma, intestinal cancer, breast cancer or the like.

Disclosed is a slow release injection containing antimetabolites and/or alkylating agents, which comprises slow release microspheres and dissolvent, the slow release microspheres include antimetabolites selected from Tegafur, Capecittabine, Pemetrexed, Carmofur or Gemcitabine, and/or alkylating agent anticancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), copolymer or blend of polyphosphate ester with PLA, Polifeprosan, poly(dodecanedioic acid-tetradecanedioic acid) or poly(fumaric acid-sebacylic acid). The alkylating agent is selected from Carmustine, Nimustine, Fotemustine, Lomustine or bendamustine. The anticancer composition can also be prepared into slow release implanting agent, for injection or placement in or around tumor with a period of effective concentration maintenance over 50 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.

A sustained-release gel injection comprises angiogenesis inhibitor and/or carmustine or nimustine, amphiphilic block copolymer and solvent, wherein the angiogenesis inhibitor is selected from SU5416, SU6668, alemtuzumab, axitinib, ibritumomab, bevacizumab, sutent, dasatinib, tarceva, vandetanib, gefitinib, lapatinib, lapatinib, sunitinib, sorafenib, endostatain, engiostatin, tositumomab, tipifarnib, sirolimus, cetuximab, ematinib, lenalidomide and thalidomide. The mixture of amphiphilic block copolymer and solvent has temperature sensitive gelatinization characteristic, is fluid liquid at room temperature, and automatically becomes non-flowing biodegradable water insoluble gel in warm-blooded animals. The preparation can locally slowly release at tumor foci and maintain effective drug concentration for several weeks to several months; and has effects on killing tumor cells, effectively inhibiting tumor angiogenesis, reducing systemic toxicity of drug, and enhancing the treatment effect of chemotherapy and radiotherapy (particularly radioactive particles).

A new anticarcinogenic sustained-release injection consists of sustained-release microballoon sphere and menstruum; wherein, the sustained-release microballoon sphere comprises anticarcinogenic active ingredient and sustained-release accessory material; the menstruum is special menstruum containing suspending agent. The anticarcinogenic active ingredient is the combination of cytotoxic drugs of fotemustine, bendamustine, tallimustine, carmustinum, nimustine, lomustine, semustine or ranimustine and adriamycin, epirubicin, melphalan, 4H peroxide cyclophosphamide, actinomycin D, vinorelbine or nolvadex, etc.; the sustained-release accessory material is selected from polylactic acid and the multipolymer or mixture thereof, mono-methyl polyethyleneglycol, polyethyleneglycol or polylactic acid multipolymer, EVAc, the multipolymer of fatty acid and decanedioic acid, etc.; the viscosity of the suspending agent is 100cp-3000cp (at the temperature of 25 DEG C-30 DEG C), the suspending agent is selected from sodium carboxymethyl cellulose, etc. The sustained-release microballoon sphere also can be made into sustained-release implant which can be injected and placed in tumor or around tumor and can release medicine at the local parts of the tumor for 30 to 40 days; therefore, the anticarcinogenic sustained-release injection can be separately united together with non-operativetreatment such as chemo-treatment and/or radiation treatment, etc. for application.

An anti-cancer composition comprises anti-cancer effective ingredient selected from tyrosine kinase inhibitor and/or nimustine and sustained release adjuvant, and can be made into sustained release injection and sustained release implant agent. Sustained release injection also comprises special dissolvent containing suspending agent. The Suspending agent has a viscocity of 100cp-3000cp (at 20deg.C-30deg.C) and is selected from sodium carboxymethylcellulose, and so on. the sustained release adjuvant is selected from p(LAEG-EOP), p(DAPG-EOP), p(BHET-EOP/TC), p(BHET-EOP/TC), p(BHDPT-EOP/TC), p( BHDPT-EOP/TC), p(CHDM-HOP) or p(CHDM-EOP).Slow releasing injection and implantable agent can keep high medicinal concentration in tumour part through slow releasing for over 60 days after being injected or implanted in or around tumour. The anticancer composition may also be prepared into sustained-release implant. It can reduce systemic toxic reaction of anticancer drugs, and also selectively improve the therapeutic effect of non-operative therapy such as chemotherapy.

Disclosed is slow release anticancer agent carrying both Nimustine and its synergistic agents, which comprises slow release auxiliary materials and active anticancer constituents, wherein the active anticancer constituents include Nimustine and its synergistic agents (such as Vinblastine, Goserelin or Carmofur). The viscosity of the slow release injection is 10-650cp (at 20-30 deg C), and the active anticancer constituents can also be made into slow release implanting agent. The slow release subsidiary materials mainly comprise bio-compactable and degradable macromolecular polymers, when locally dispensed on the tumor, the composition not only can lower down the whole body toxicity reaction of the anti-cancer medicament, but also can selectively increase the tumor local medicinal concentration, the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can also be improved. The solid tumors include glioma, osteosarcoma, lymphoma, lung carcinoma, intestinal cancer, and breast cancer.

The invention relates to a drug combination, namely, a slow-release injection, carrying nimustine and a synergistic agent thereof at the same time, which consists of slow-release accessories and active anti-cancer ingredients. The active anti-cancer ingredients comprise the nimustine and the synergistic agent thereof (vinorelbine, melphalan or mitomycin C) respectively. The viscosity of the slow-release injection is 10cp to 650cp (at the temperature of 20 DEG C to 30 DEG C). The active anti-cancer ingredients can also be prepared into a slow-release implant. The slow-release accessories are mainly biological soluble and degradable macromolecular polymerizers that can be absorbed. During the process of degradation and adsorption, the macromolecular polymerizers can slowly release the active anti-cancer ingredients to parts of tumors, thus obviously reducing the toxic reaction of the whole body as well as maintaining the concentration of effective drugs at the parts of the tumors. Putting the anti-cancer drug combination at the parts of the tumors can not only reduce the toxic reaction of the whole body active against cancer, but also selectively raise the drug concentration of the parts of the tumors and enhance the curative effect of nonspecific treatment, such as chemotherapy drugs and radiotherapy treatment, and the like. Solid tumors include glioma, osteoma sarcomatosum, lymphoma, lung cancer, intestinal cancer, oophoroma, and the like.

A slow-release injection or implant containing the nitrosourea-type medicines (nimustine, carmustine, etc) and topostine as the active anticancer components is composed of the slow-release microballs containing said active anticancer components and the slow-release auxiliary chosen from p(LAEG-EOP), p(DAPG-EOP), etc, and the solvent which may be ordinary solvent or a special solvent containing suspending aid.

The invention provides a sustained-release injection which is an anti-tumor composite containing nitrosoureas drug and bortezomib. The sustained-release injection comprises a sustained-release microsphere and a solution medium, wherein the sustained-release microsphere comprises effective anti-tumor ingredient and sustained-release excipient, the solution medium is a common solution medium or a special solution medium containing a suspending drug. The suspending drug has the viscosity between 100cp and 3000cp (under twenty centi degrees to thirty centi degrees) and is selected from sodium carboxymethylcellulose and others; the nitrosoureas drug is selected from nimustine,bendamustine,carmustine,galamustine,fotemustine,ranimustine,samustine or lomustine; the sustained-release excipient is selected from polyphosphonate copolymer like p(LAEG-EOP)or p(DAPG-EOP), PLA, PLGA, polyphosphonate with PLA, polifeprosan, the polymer or blending polymer of ( erucic acid dipolymer-sebacic acid) or poly(boletic acid-sebacic acid); the anti-tumor composite can also be prepared to be a sustained-release implant which can maintain the effective concentration of drug over forty days for intratumor or tumor circumference injection or placement, can also reduce general reaction obviously and enhance the treatment effect of non-operative therapeutics such as chemotherapy and radiotherapy.

The invention relates to novel sustained-release injection for cancer therapy. The sustained-release injection comprises sustained-release microspheres and dissolvent, wherein the sustained-release microspheres comprise active ingredients for cancer therapy and sustained-release auxiliary materials, and the dissolvent is special dissolvent containing suspending agent. The active ingredients for cancer therapy are combination of fotemustine, bendamustine, tallimustine, carmustine, nimustine, lomustine, semustine or ranimustine with cytotoxic drug of adriacin, epidoxorubicin, melphalan, 4H- cyclophosphamide peroxide, actinomycin D, vinorelbine or tamoxifen; the sustained-release auxiliary materials comprise polylactic acid and the copolymer or mixture thereof, monomethyl polyethylene glycol, polyethylene glycol/polylactic copolymer, EVAc, fatty acid and decanedioic copolymer; the viscocity of the suspending agent is 100cp to 3000cp (at 25 to 30 DEG C), and the suspending agent is selected from sodium carboxymethyl cellulose; the sustained-release microspheres can also be produced into sustained-release implant, and by injecting or positioning the sustained-release agent in tumor or tumor margin, drug release in local part of tumor can be performed for approximately 30 to 40 days; therefore, the sustained-release injection can be applied in combination with non-operative treatment such as chemical treatment and/or radiation treatment.

Disclosed is a slow release injection for treating solid tumors which comprises slow release auxiliary materials and active anticancer constituents, wherein the active anticancer constituents include Nimustine or the combination of Nimustine and its synergists (such as adriamycin, Carboplatin or Amethopterin). The viscosity of the slow release injection is 10-650cp (at 20-30 deg C), and the active anticancer constituents can also be made into slow release implanting agent. The slow release subsidiary materials mainly comprise bio-compactable and degradable macromolecular polymers, when locally dispensed on the tumor, the composition not only can lower down the whole body toxicity reaction of the anti-cancer medicament, but also can selectively increase the tumor local medicinal concentration, the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can also be improved. The solid tumors include glioma, osteosarcoma, lymphoma, lung carcinoma, intestinal cancer, and breast cancer.

Disclosed is a slow release injection for treating solid tumors which comprises slow release auxiliary materials and active anticancer constituents, wherein the active anticancer constituents include Nimustine or the combination of Nimustine and its synergists (such as Paclitaxe, camptothecine or cytophosphanel). The viscosity of the slow release injection is 10-650cp (at 20-30 deg C), and the active anticancer constituents can also be made into slow release implanting agent. The slow release subsidiary materials mainly comprise bio-compactable and degradable macromolecular polymers, when locally dispensed on the tumor, the composition not only can lower down the whole body toxicity reaction of the anti-cancer medicament, but also can selectively increase the tumor local medicinal concentration, the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can also be improved. The solid tumors include glioma, osteosarcoma, lymphoma, lung carcinoma, intestinal cancer, and breast cancer.

Disclosed is a Nimustine slow release injection for treating solid tumors, which comprises effective anticancer dose of Nimustine or the combination of Nimustine and its synergists (such as 5-FU, cisplatin or 06-benzyl guanine). The solid tumors include osteosarcoma, lymphoma, gastric carcinoma, cancer of pancreas, lung carcinoma, bladder carcinoma, hepatic carcinoma, breast cancer, esophagus cancer, intestinal cancer, thyroid carcinoma, and glioma. The viscosity of the slow release injection is 10-650cp (at 20-30 deg C), and the active anticancer constituents can also be made into slow release implanting agent. The slow release subsidiary materials mainly comprise bio-compactable and degradable macromolecular polymers, when locally dispensed on the tumor, the composition not only can lower down the whole body toxicity reaction of Nimustine, but also can selectively increase the tumor local medicinal concentration, the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can also be improved.

Disclosed is a slow release injection containing nitrosourea drugs and/or topoisomerase depressant, which comprises slow release microspheres and dissolvent, the slow release microspheres include nitrosourea drugs selected from Nimustine, Carmustine, and/or topoisomerase depressant anticancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), copolymer or blend of polyphosphate ester with PLA, Polifeprosan, PLGA and poly(dodecanedioic acid-tetradecanedioic acid), the topoisomerase depressant is selected from camptothecine, monohydric camptothecine, Topotecan, Lartotecan, Irinotecan, Etoposide or Teniposide, the anticancer composition can also be prepared into slow release implanting agent for injection or placement in or around tumor with a period of effective concentration maintenance over 60 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.

Disclosed is a slow release injection agent of anticancer composition containing nitrosourea drugs and alkaloid drugs, which comprises slow release microspheres and dissolvent, wherein the slow release microspheres comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being conventional dissolvent or specific dissolvent containing suspension adjuvant. The viscosity of the suspension adjuvant is 100-3000cp (at 20-30 deg C), and is selected from sodium carboxymethylcellulose, the nitrosourea drugs are selected from Carmustine, Nimustine, Fotemustine, Lomustine or Bendamustine, the alkaloid drugs include Vincristine, Vinblastine, Vinorelbine, Vindesine and Vinrosidine, the slow release auxiliary materials are selected from polyphosphate ester copolymers such as p(LAEG-EOP), p(DAPG-EOP), copolymer or blend of polyphosphate ester with polylactic acid, Polifeprosan, sebacylic acid and PLGA. The anticancer composition can also be prepared into slow release implanting agent, for injection or placement in or around tumor with a period of effective concentration maintenance over 60 days, as well as the treatment effect of appreciably lowering general reaction of the drugs, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.