68 results about "Mitoxantrone" patented technology

Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS-, HO- or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5'-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=-NH2, -OH, -COOH, -O-CO-R-COR*, -NH-CO-R-COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R* H, phenyl, alkyl with 1-6 carbon atoms.

A group of new compounds, N-(all-trans-Retinoyl)-L-cysteic acid, N-(13-cis-Retinoyl)-L-cysteic acid, N-(all-trans-Retinoyl)-L-cysteinesulfinic acid, N-(13-cis-Retinoyl)-L-cysteinesulfinic acid, N-(all-trans-Retinoyl)-L-homocysteic acid, N-(13-cis-Retinoyl)-L-homocysteic acid, and sodium salts of these compounds, including sodium salts of their esters and amides, is shown to exhibit therapeutic effects per se, and which compounds in combination with cytotoxic compounds, such as docetaxel, paclitaxel, doxorubicin and mitoxantrone, exhibit a synergistic effect. These compounds make it possible to manufacture new formulations of poorly soluble pharmaceutical compounds, and the present invention discloses a process of manufacturing water-soluble formulations of such compounds, exemplified by docetaxel, and paclitaxel, exhibiting enhanced pharmacological activity, and formulations of water-soluble pharmaceuticals exemplified by doxorubicin and mitoxantrone, exhibiting improved therapeutic efficacy.

Disclosed is a bangosome injection of mitoxantrone or and its preparing technique. The injection comprises of mitoxantrone, phospholipid, cholesterol, anti oxidant additive, organic acid, alkali, sugar, buffer and water for injection, the preparing technique includes preparation of lipid film, packaging medicine, homogenization of bangosome, purifying or solidifying bangosome, constant volume, degerming, subpackage and reposition and so on. The has remarkable stability, high ratio of packaging medicine, low cost, few poisonous side-effect and simple preparing technique.

This invention pertains to liposomal formulations of mitoxantrone and methods for their manufacture and use. The compositions of the present invention include liposomal formulations of mitoxantrone in which the liposome contains any of a variety of neutral or charged liposome-forming materials in addition to a compound that is thought to bind mitoxantrone, such as cardiolipin. The liposomal compositions can be used advantageously in conjunction with secondary therapeutic agents other than mitoxantrone, including antineoplastic, antifungal, antibiotic among other active agents. Methods are provided in which a therapeutically effective amount of the formulation is administered to a mammal, such as a human.

This invention pertains to liposomal formulations of mitoxantrone and methods for their manufacture and use. The compositions of the present invention include liposomal formulations of mitoxantrone in which the liposome contains any of a variety of neutral or charged liposome-forming materials in addition to a compound that is thought to bind mitoxantrone, such as cardiolipin. The liposomal compositions can be used advantageously in conjunction with secondary therapeutic agents other than mitoxantrone, including antineoplastic, antifungal, antibiotic among other active agents. Methods are provided in which a therapeutically effective amount of the formulation is administered to a mammal, such as a human.

The invention discloses a method for detecting mitoxantrone based on a molecularly imprinted polymer with quantum dot ratio fluorescence performance. The method comprises the following steps: preparing the mitoxantrone molecularly imprinted polymer with ratio fluorescence performance with a sol-gel method by taking red CdTe quantum dot@ SiO2 as a carrier, 3-aminopropyltriethoxysilane as a functional monomer, mitoxantrone as a template and tetraethoxysilane as a crosslinking agent in the presence of green CdTe quantum dots, wherein the polymer has holes being consistent with the sizes, shapes and functional groups of template molecules, and can be used for selectively recognizing mitoxantrone; implementing high-sensitivity detection of the mitoxantrone directly with a ratio fluorescence method. Compared with the original chromatography and electrochemical method, the detection method has the advantages that operation become easier, the detection speed becomes higher, the cost is lower, the analysis rate is increased greatly, and trace detection of the mitoxantrone can be realized.

The invention belongs to the field of new auxiliary materials and new dosage forms of medicine preparations and relates to a chemotherapeutic drug-photosensitizer co-assembled nanoparticles and construction thereof. A chemotherapeutic drug is an anthracycline chemotherapeutic drug selected from mitoxantrone, doxorubicin or epirubicin; a photosensitizer is a porphyrin photosensitizer selected fromchlorine e6, hematoporphyrin monomethyl ether or a chlorophyll derivative, wherein the molar ratio of the chemotherapeutic drug to the photosensitizer is 3:1-1:3. A certain quantity of the chemotherapeutic drug and the photosensitizer or a mixture of the chemotherapeutic drug, the photosensitizer and PEG is dissolved in a proper quantity of organic solvent, and the solution is slowly dropwise added to water while stirring to form uniform nanoparticles spontaneously. The preparation process is simple, enlarged production is easy, particle size is small and uniform, and the nanoparticles can beenriched at tumor parts through a reinforced permeation retention effect; the nanoparticles have ultrahigh drug loading capacity and can reduce related toxicity of auxiliary materials; and surface modification is easy, and the circulation time of the nanoparticles in blood can be prolonged by PEG modification.

The invention discloses a biological self-assembly nanometer crystal injection agent composition with a lympha targeted function and an administration mode for targeting a lymphatic system by using a biological self-assembly nanometer crystal injection agent. A recipe composition is prepared from 0.05 to 5 percent of mitoxantrone and mitoxantrone salt, 0.1 to 10 percent of osmotic pressure regulating agents, 0.001 to 0.1 percent of buffer agents, 0.01 to 0.1 percent of antioxidants, 0.05 to 1 percent of adsorbents and 0 to 20 percent of filling agents. The administration mode is interstitial injection; after the passive lymphatic system targeting, the lymph gland can generate the macroscopic blue color. The problems of poor in vitro and vivo physical and chemical property, poor storage stability, preparation flow process complexity and high cost of the micro particle preparation with the lympha targeted function are solved.

The invention relates to the novel usage of an antimalarial medicine, in particular to the novel usage of hydroxychloroquine having sensitivity enhancing effect on various chemical anti-multiple myeloma medicaments. The novel usage is characterized in the application of hydroxychloroquine in treatment of multiple myeloma through chemotherapeutic medicaments. The hydroxychloroquine can obviously enhance the killing activity of chemotherapeutic medicines such as doxorubicine, epidoxorubicin, cis-platinum and mitoxantrone to multiple myeloma cells, and the killing activity thereof is realized by inhibiting the myeloma cell autophagy signals by hydroxychloroquine. Hydroxychloroquine can induce the quantity of the autophagy lysosomes of the multiple myeloma cells to be increased and the expression of the autophagy-associated albumen LC3-II to be increased.

A group of new compounds, N-(all-trans-Retinoyl)-L-cysteic acid, N-(13-cis-Retinoyl)-L-cysteic acid, N-(all-trans-Retinoyl)-L-cysteinesulfinic acid, N-(13-cis-Retinoyl)-L-cysteinesulfinic acid, N-(all-trans-Retinoyl)-L-homocysteic acid, N-(13-cis-Retinoyl)-L-homocysteic acid, and sodium salts of these compounds, including sodium salts of their esters and amides, is shown to exhibit therapeutic effects per se, and which compounds in combination with cytotoxic compounds, such as docetaxel, paclitaxel, doxorubicin and mitoxantrone, exhibit a synergistic effect. These compounds make it possible to manufacture new formulations of poorly soluble pharmaceutical compounds, and the present invention discloses a process of manufacturing water-soluble formulations of such compounds, exemplified by docetaxel, and paclitaxel, exhibiting enhanced pharmacological activity, and formulations of water-soluble pharmaceuticals exemplified by doxorubicin and mitoxantrone, exhibiting improved therapeutic efficacy.

The invention discloses an application of a novel liposome-entrapped mitoxantrone combined chemotherapeutic drug in antineoplastic treatment. According to the invention, a new liposome-entrapped mitoxantrone preparation containing components such as cardiolipin is prepared internationally, and is used for being combined with other clinical routine first-line chemotherapeutics for antineoplastic treatment. The invention expounds the preparation method and symptom research of the novel liposome preparation, the preparation has the characteristics of high entrapment rate, uniform particle size distribution, good stability, prolongation of chemotherapeutics half life, and reduction of toxic and side effect; compared with other treatment methods, in breast cancer and leukemia tumor animal models, antineoplastic curative effect of the new liposome-entrapped mitoxantrone preparation and other chemotherapeutics is more obvious.

The invention relates to the field of anti-tumor, and discloses a purpose of a mitoxantrone liposome preparation for preparation of medicine for treating a lymphoma, wherein the lymphoma is preferablya non-hodgkin lymphoma, is further preferably an invasive non-hodgkin lymphoma, is more further preferably a recurrent and refractory invasive lymphoma, and is more further preferably a diffuse largeB cell lymphoma or a peripheral T-cell lymphoma. The mitoxantrone liposome preparation is singly used, and is not applied in a way of being combined with other anti-tumor medicine.

Disclosed is an anticancer slow release agent which comprises slow release microspheres and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The anticancer antibiotics are selected from Idarubicin, Valtaxin, Pirarubicin and Mitoxantrone, The anti-metabolite drugs are selected from Pemetrexed, Carmustine, Tegafur, Zalcitabine, Emtritabine, Galocitabine, Ibacitabine, Ancitabine, Decitabine, Flurocitabine, Enocitabine, Imidazoletabine, Capecittabine, Gemcitabine, Fludrarbine, Raltitrexed, Dexrazoxane, Cladribine, Nolatrexed and folic acid, The slow release auxiliary materials are selected from EVAc, Polifeprosan, sebacylic acid copolymer, lactic acid, the viscosity of the suspension adjuvant is 100-3000cp (at 25-30 deg C), and is selected from sodium carboxymethylcellulose. The slow release microspheres can also be prepared into slow release implanting agent for injection or placement in or around tumor.

The present invention discloses a preparation method and uses of an anti-cancer drug estrogen targeting PEG-modified liposome. The liposome preparation method comprises: synthesizing estrone-pegylated phospholipid from activated estrone, taking 40-80 parts by weight of phospholipid, 5-45 parts by weight of cholesterol, and 5-40 parts by weight of pegylated phospholipid, dissolving in methanol, carrying out rotary evaporation, adding an ammonium sulfate aqueous solution, carrying out dialysis, adding 0.5-10 parts by weight of mitoxantrone, carrying out incubation, carrying out dialysis, adding 0.1-20 parts by weight of the estrone-pegylated phospholipid, carrying out incubation, and filtering with a membrane to obtain the liposome preparation. Compared with the liposome in the prior art, the obtained estrogen targeting PEG-modified liposome has characteristics of high encapsulation efficiency, uniform particle size, pharmacokinetics improving, anti-tumor efficacy enhancing, toxicity reducing, simple preparation process and easy scale-up production, and is expected to become the novel pharmaceutical preparation for cancer therapy. The uses are targeted treatments of breast cancer, leukemia and other cancers.

Novel lactones of polysaccharide carboxylic acids, and methods for the preparation of a variety of conjugates therefrom, as well as the novel conjugates, are provided. Conjugates include metallo-coordinated cisplatin (and carboplatin), as well as conjugates of ellipticinium, aminoglutethimide, mitoxantrone, mitoguazone, cis 3-hexen-1-ol, and other nucleophilic biologically effective agents. Also provided are conjugates via a coupling agent of biologically effective agents, such as Vitamin E, DTPA, TAXOL and TAXOTERE.

A group of new compounds, N-(all-trans-Retinoyl)-L-cysteic acid, N-(13-cis-Retinoyl)-L-cysteic acid, N-(all-trans-Retinoyl)-L-cysteinesulfinic acid, N-(13-cis-Retinoyl)-L-cysteinesulfinic acid, N-(all-trans-Retinoyl)-L-homocysteic acid, N-(13-cis-Retinoyl)-L-homocysteic acid, and sodium salts of these compounds, including sodium salts of their esters and amides, is shown to exhibit therapeutic effects per se, and which compounds in combination with cytotoxic compounds, such as docetaxel, paclitaxel, doxorubicin and mitoxantrone, exhibit a synergistic effect. These compounds make it possible to manufacture new formulations of poorly soluble pharmaceutical compounds, and the present invention discloses a process of manufacturing water-soluble formulations of such compounds, exemplified by docetaxel, and paclitaxel, exhibiting enhanced pharmacological activity, and formulations of water-soluble pharmaceuticals exemplified by doxorubicin and mitoxantrone, exhibiting improved therapeutic efficacy.

The invention discloses a method for detecting mitoxantrone based on a luminous gold nanocluster. The method comprises the following steps: preparing the gold nanocluster, measuring fluorescence intensity of the gold nanocluster at a position with wavelength of 619 nm and recording as F0 under excitation of 469nm-wavelength light; after adding mitoxantrone with different weight in the step I, measuring the fluorescence intensity of the gold nanocluster containing the mitoxantrone with different concentrations and recording as F at the position with wavelength of 619 nm under excitation of 469nm-wavelength light, calculating out linear relation between change value of the fluorescence intensity of the gold nanocluster before and after adding the mitoxantrone and mitoxantrone concentration; adding a to-be-detected sample into the gold nanocluster, and testing the change value of the fluorescence intensity at the position with wavelength of 619 nm under excitation of 469nm-wavelength light before and after adding the mitoxantrone, calculating the weight or concentration of the added mitoxantrone to establish detection according to the obtained linear relation. The method has characteristics of being high in selectivity, high in sensitivity, simple and convenient, easy to implement, and the like.

The invention relates to a temperature-controlled sustained-release injection containing an anti-cancer drug, which consists of the anti-cancer drug and an amphiphilic block copolymer hydrogel and has the temperature-sensitive gelatinization feature, the temperature-controlled sustained-release injection is flowable liquid in the environment that is lower than the body temperature and can be automatically converted to the water-insoluble gel that can not flow and be biodegradable for absorption in an endotherm, thus allowing the drug to have the local sustained release in a tumor and maintain the effective drug concentration for a plurality of weeks to a plurality of months; the temperature-controlled sustained-release injection can be injected in the tumor or the tumor periphery or be arranged in the postoperative tumor cavity, thus significantly reducing the systemic reaction of the drug, strengthening the treatment effects of chemotherapy, radiotherapy and other non-surgical therapies, and being used for the treatment of the tumors in different stages. The anti-cancer drug can be vincristine, vinorelbine, navelbine, vindesine, vinleurosine, vinrosidine, cephalotaxine, bleomycin, daunomycin, aclarubicin, epirubicin, idarubicin, pirarubicin, valrubicin, mitomycin C, actinomycin D, losoxantrone, mitoxantrone, mitozolomide, temozolomide and so on.

An antineoplastic medicinal composition used to prepare the medicines for treating breast cancer and leukemia contains the epigallocatechin gallate and mitoxantrone in weight ratio of (1-2000): (1-5).

Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS-, HO- or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5'-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=-NH2, -OH, -COOH, -O-CO-R-COR*, -NH-CO-R-COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R*H, phenyl, alkyl with 1-6 carbon atoms.

The invention discloses nano-scale mesoporous silicon dioxide-methotrexate-mitoxantrone nanoparticles. Its preparation method is disclosed, that is, amino functionalized mesoporous silica nanoparticles (MSNN) are prepared by modifying amino groups on the surface of mesoporous silica nanoparticles, and then the amino groups of MSNN are covalently combined with MTX to form methotrexate ‑Amino-modified mesoporous silica nanoparticles (MSNN‑MTX), and finally load mitoxantrone into the nanopores of MSNN‑MTX to obtain nanoscale mesoporous silica‑methotrexate / mitoxantrone Quinone nanoparticles (MSNN‑MTX / MIT). Its antitumor effect is disclosed. Compared with the combined application of conventional MTX and MIT, MSNN‑MTX / MIT significantly prolongs the survival time of S180 mice, improves the curative effect and reduces systemic toxicity. Therefore, the present invention discloses the application of MSNN-MTX / MIT in the preparation of antitumor drugs combined with MTX and MIT. The MSNN-MTX / MIT of the present invention has a good clinical application prospect.

The present invention describes the use of radio-labeled antitumor drugs in the treatment of solid tumors by the method of administering a radio-labelled anticancer drug to a patient and imaging at least a part of the patient using Positron Emission Tomography imaging. The method is used to monitor delivery of antitumor drugs to tumors and may be used to predict the effectiveness of therapy with a particular antitumor drug or combination of antitumor drugs, to assess the effectiveness of modulators of cellular accumulation, to individualize therapy and to evaluate the effectiveness of antitumor drugs with respect to particular cancers. Particularly preferred drugs are labeled taxanes, e.g., 11C-paclitaxel and 11C-docetaxel, labeled anthracyclines, e.g., 11C-doxorubicin and 11C-epirubicin, and other radio-labeled drug, e.g. 11C-topotecan and 11C-mitoxantrone. The invention further describes antitumor drugs labeled with the radioactive label 11C and methods of preparing radio-labeled drugs.

The present invention relates to the technical field of medicine and particularly relates to an antitumor lymphatic metastasis function of mitoxantrone and a pharmaceutical preparation of the mitoxantrone. The mitoxantrone is administered locally, such as intratumoral administration and peritumoral and tumor subcutaneous administration. The mitoxantrone can be prepared into the clinically acceptable pharmaceutical preparation with a pharmaceutically acceptable carrier. The pharmaceutical preparation is a parenteral administration preparation. The parenteral administration preparation is selected from a solution, a liposome, a dendritic macromolecule, a nanoparticle, a nanocrystal, a microcrystal, a microsphere and a gel agent. The mitoxantrone is used for local chemotherapy to increase anti-tumor activity, reduces toxic and side effects, targets a lymphatic system, inhibits tumor lymphatic metastasis, can reduce tumor volume and is convenient for subsequent surgical resection when usedfor neoadjuvant chemotherapy, can also kills tumor cells metastasized in lymphatic vessels, reduces risks of postoperative tumor recurrence, and improves quality of life of patients.

A double sustained release anticancer gel sustained release injection consists of anticancer medicine and amphiphilic block copolymer hydrogel, wherein the anticancer medicine comprises vincristine, vinorelbine, vinblastine, daunomycin, mitoxantrone, mitozolomide and temozolomide, etc., and exists in sustained release preparation injection in the forms of sustained release microsphere, microsphere or micropowder, i.e. the anticancer medicine in anticancer useful quantity is partly or completely wrapped inside the sustained release microsphere. Sustained release gel has temperature-sensitive gelling characteristics and is in the state of fluxible liquid in an environment with the temperature lower than body temperature; moreover, the sustained release gel can be automatically converted into non-flowing water-insoluble gel capable of biodegradation and absorption inside the body of a warm blood so as to slowly release medicine inside part of a tumor; the sustained release microsphere is propitious to release medicine smoothly and slowly, and double sustained release is propitious to control tumor cells entering a dormancy stage; moreover, the medicine which exists in the sustained release gel in the form of micropowder is propitious to release the medicine relatively faster and to control cells in faster proliferation. The double sustained release anticancer gel sustained release injection can used together with radiotherapeutic particle, etc.

The invention relates to a TOP medicament resistant cell line human ovarian cancer, with a accession number of CGMCC No 1217, which is selecting human ovarian cancer cell line as parental cell, putting the cell into RPMI1640 culture medium containing 15% calf serum, putting into incubator with 5% CO2 and 37 DEG C to culture; acquiring cells in logarithmic growth phase, counting after digesting with 0.25% pancreatin, inoculating 5*105 / ml into culture bottle according to amount of 5ml in each bottle, when cells adheres to wall after 24 hours, reacting for 2 hours with a TOP final content of 2160ng / ml, discarding culture medium, washing by phosphate buffer for 3 times, replacing fresh culture medium, second impulsing after growing is resumed, and repeatedly operating, until it is impulsed with medicament for 13 times. The cell line is constructed for 10 months, medicament resistance of cell is 10.67 per cell, P<0.01 comparing with sensitive cell, has cross resistance to mitoxantrone, camptothecin, vincristine besides resistance to TOP.

The invention discloses a preparation method and application of a polycarbonate drug-loaded nano chemosensitizer based on nitric oxide. The sensitizer is prepared by self-assembling a polycarbonate block copolymer containing a nitric oxide donor and a small molecule chemotherapeutic drug. The polycarbonate drug-loaded nano chemosensitizer based on nitric oxide has the advantages of good water solubility, small toxic and side effects, good stability in a normal physiological environment and the like, and effectively solves the problems of poor water solubility, large toxic and side effects and the like of indissolvable chemotherapeutic drugs such as adriamycin, mitoxantrone and the like in clinical use. The polycarbonate drug-loaded nano chemosensitizer based on nitric oxide also has the features that the drug-loading capacity is high, the tumor targeting property is remarkable, the tumor microenvironment can be regulated and controlled, the ideal chemotherapy sensitization effect is achieved, and tumor recurrence is reduced.

The invention relates to an improved mesenchymal stem cell (MSC) culture medium, bone marrow mesenchymal stem cells (BMSCs) and a culture method and application of the BMSCs. The improved MSC culturemedium comprises a base culture medium, a first component and melatonin, wherein the first component is selected from at least one of coenzyme Q10 and mitoxantrone mesylate, the working concentrationof the first component is 1-20 [mu]M, the working concentration of the melatonin is 1-20 [mu]M, and the molar ratio of the first component to the melatonin is 1: (0.2-10). The improved MSC culture medium can improve mitochondrial activity and mitochondrial quantity in MSCs.

The invention belongs to the field of antiviral drugs, and discloses an application of a DNA topoisomerase inhibitor in preparation of medicines for preventing and / or treating novel coronavirus infection, and the DNA topoisomerase inhibitor comprises mitoxantrone, doxorubicin or pharmaceutically acceptable salts of above small molecule compounds. DNA topoisomerase inhibitors such as mitoxantrone and doxorubicin can extremely strongly inhibit the synthesis of novel coronavirus virus SARS-CoV-2 replicon RNA and reduce the RNA copy amount of wild novel coronavirus virus SARS-CoV-2 in cells, so that the replication of novel coronavirus SARS-CoV-2 is inhibited, and the effect of preventing and / or treating novel coronavirus SARS-CoV-2 infection is achieved.

The invention relates to a method and a kit for detecting breast cancer resistance protein (BCRP) gene mutation related to treatment effect of molecular targeted anti-cancer medicines, in particular to a fluorescence quantitative polymerase chain reaction (PCR) detection method and a kit for detecting mutation in a BCRP genic mutation hotspot region, and application thereof. By the invention, the mutation of a specific BCRP gene locus is detected, the treatment effects of anti-tumor medicines such as mitoxantrone MX, adriamycin, daunorubicin, etoposide, topotecan, Irinotecan, CPT-11, cis-platinum, taxol, vinblastine and the like are predicted, and guidance is provided for clinical individualized medication schemes for patients suffering from tumors.