108results about How to "Reduce cardiotoxicity" patented technology

The invention discloses a xiluomosi liposome freeze dried and making technique, which comprises the following steps: selecting liposome component, buffer, organic solvent, antioxidant and freeze-drying protective as raw material; adopting film diffusion method to make the liposome turbid liquor with xiluomosi through high-pressure or hypersonic dispersing method evenly; drying the liposome to improve the storage stability obviously; dispersing the freeze dried at random proportion in the water evenly without any sediment and impurity; making the packing rate of liposome at 96% with the grain size at 50-250nm; improving the drug effect greatly in comparison with oral agent; lengthening the circulating time in the blood; elevating the biological utility of drug.

The invention discloses an amphipathy block-polymer hydroxyethyl-starch-olylactic-acid copolymer and a preparing method and nanometer medicine loading system thereof. The method includes the steps that 4-dimethylaminopyridine serves as a catalyst, N-N'-dicyclohexylcarbodiimide serves as a dehydrating agent, carboxyl at the tail end of polylactic acid and hydroxyl on hydroxyethyl-starch sugar ring are subjected o an esterification reaction, hydrophobic polylactic acid is coupled on hydrophilic hydroxyethyl starch accordingly, and the amphipathy hydroxyethyl-starch-polylactic-acid block polymer is synthesized. Debydrochlorination adriamycin amycin is loaded to a hydrophobic core with the emulsified solvent evaporation method and the high pressure homogenization technology, evenly-distributed medicine loading polymer nanometer particles with the particle-size of about 140 nm are formed, and are applied in preparing antitumor medicine, the medicine in-vivo cycling time is prolonged, the toxic and side effects of the medicine are reduced, and the good antitumor effect is achieved.

The invention belongs to the technical field of medicines, relates to a paclitaxel medicinal composition and a preparation method thereof, and in particular relates to an injection paclitaxel nanocrystal preparation and a preparation method thereof as well as application of the preparation for preparing anti-tumor medicines. The paclitaxel nanocrystal belongs to a nano preparation, is small in grain diameter and good in stability, and cannot be easily separated, so that the dissolubility of paclitaxel is remarkably improved, and in-vivo studies prove that the paclitaxel nanocrystal has certain targeting performance, and can be used in anti-tumor treatment.

The invention relates to a tumor-targeted sound and light power medicine-carrying nanometer nano-micelle, and a preparation method and a purpose thereof. The medicine-carrying nanometer nano-micelle is structurally characterized in that porphyrins compounds and anthracyclines chemotherapeutic medicine form a nanometer composition through a pi-pi conjugation effect; and amphiphilic block copolymers with PEO (polyoxyethylene) or PEG (polyethylene glycol) hydrophilic segments cover nanometer compounds through the hydrophobic effect to form a hydrophilic case. The medicine-carrying nanometer nano-micelle is in a regular spherical form, and has the advantages of uniform distribution, stable property and high medicine carrying capacity; the medicine can be conveyed to the tumor focus in the targeted way and can be effectively enriched in the tumor tissue; under the ultrasound (illumination) condition, the treatment effect of the anthracyclines chemotherapeutic medicine on the tumor can be obviously enhanced; and the tumor drug resistance can be effectively reversed. Wide clinic application prospects can be realized in an aspect of combined tumor treatment by a sound (light) power therapy method and chemotherapy.

The invention provides therapeutically effective compounds for the prevention and treatment of cancer and pharmaceutical compositions containing these compounds as well as methods of using and administering these compounds. The invention also includes methods of activating a prodrug of these therapeutically effective compounds by the administration of a peptide-directed targeting construct that delivers a prodrug-activating enzyme to a target activation site.

A quinolone synthetic antibacterial agent and a therapeutic agent for an infection which exhibit broad spectrum and strong antibacterial activity for both Gram positive and Gram negative bacteria, and which are also highly safe are provided. The compound provided is represented by following formula (I):

wherein R¹ and R² represent hydrogen atom, or the like; R³ represents an alkyl group containing 1 to 6 carbon atoms, or the like; R⁴ and R⁵ independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like, with the proviso that R⁴ and R⁵ do not simultaneously represent hydrogen atom; or the substituents R⁴ and R⁵ together represent (a) a 3- to 6-membered cyclic structure including the carbon atom shared by R⁴ and R⁵ to form a spirocyclic structure with the pyrrolidine ring; R⁶ and R⁷ independently represents hydrogen atom, an alkyl group containing 1 to 6 carbon atoms, or the like; R⁸ represents a halogen-substituted alkyl group containing 1 to 6 carbon atoms, or the like; X¹ represents hydrogen atom or a halogen atom; A represents nitrogen atom or a moiety represented by formula (II):

Anaphylactic diseases comprising urticaria, papilla, subacute dermatitis, eczema, and the like, are skin diseases which seriously puzzle the human beings. In the invention, antihistamine, zinc salt and weak acid are prepared into a topical compound preparation, which not only reduces the untoward effect of drugs, avoids the first pass effect of the liver when feeding the drugs by mouth, avoids the blood concentration peak valley phenomenon caused by oral feeding, but also can improve the curative effect and is convenient for clinic application. Simultaneously pharmacological tests show that the topical compound preparation obtains excellent drug synergism to the anaphylactic skin diseases and has excellent effects on curing the anaphylactic diseases.

The invention belongs to the field of medicine, which relates to Deferiprone and a novel medicated purpose of a Deferiprone preparation, in particular to Deferiprone (1,2- dimethyl-3-hydroxide radical-4-pyridine, Deferiprone) and the application of the Deferiprone preparation in the prevention and curing of Anthracycline medicine heart toxicity. The invention researches the preventing and curing function of the Deferiprone to bandicoot heart toxicity caused by Adriamycin from the cell level, the tissue level and the whole level and prepares biodegradable type Deferiprone implant, Deferiprone troche, capsule, oral liquor and injection that can release medicine continuously. An experimental result proves that the Deferiprone and the Deferiprone preparation can not only improves the cardiac muscle shrinkage functions and protects the myocardial cell organ structure, but also complexes free iron ions directly, reduces the heart toxicity and other side and toxic effects caused by the Anthracycline medicine obviously and the mortality rate caused by the Anthracycline medicine.

A 13-deoxy anthracycline and a taxane can be administered to a patient simultaneously, separately, sequentially, or consecutively to produce a therapeutic anticancer effect with reduced toxicity and side effect profile, compared to the administration of equieffective amounts of either compound alone. A composition or preparation of a 13-deoxy anthracyclines and a taxane for producing a potent anticancer therapeutic effect is also provided.

The present invention relates to methods of reducing cardiotoxicity and/or improving survival from treatment with anthracycline agents comprising administering a therapeutically effective amount of a composition comprising a vasopressin antagonist compound or a pharmaceutically acceptable salt thereof as an active ingredient, administered simultaneously or prior to the anthracycline administration.

The invention relates to astragalus polyose calcium phosphate nano taxol complex injection and a preparation method and the application thereof. 100 mL of injection comprises the following components: 0.01 to 1 g of astragalus polyose calcium phosphate nano to particles, 1.0 to 50 mg of taxol, 0 to 5.0 g of osmotic pressure regulator and appropriate amount of water. The pH value of the injection is 6.0 to 7.5. The preparation method comprises the following steps: blending the taxol with absolute ethyl alcohol to form taxol-absolute ethyl alcohol solution; blending the astragalus polyose with ultrapure water to form astragalus polyose solution; performing stirring and ultrasonic processing to the solution, rejecting the supernatant fluid after separation, and after depositing, drying and sterilizing, obtaining astragalus polyose calcium phosphate nano taxol complex granules used for injection, then adding the osmotic pressure regulator into the water for injection, and mixing with the astragalus polyose calcium phosphate nano taxol complex granules; after ultrasonic processing, astragalus polyose calcium phosphate nano taxol complex injection is formed. The complex injection can be used for the treatment or auxiliary treatment of tumor.

This invention relates to the discovery of prodrugs of substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the substituents have the meanings defined in claim 1 and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting the formation of blood platelets.

The invention belongs to the field of chemical synthesis, and in particular relates to a tilmicosin inclusion complex chitosan temperature-sensitive gel and a preparation method thereof. The preparation method comprises the following steps: dissolving chitosan in 0.1mol/L hydrochloric acid by weighing and fully stirring until Dissolve the sodium glycerophosphate in deionized water, add the sodium glycerophosphate solution dropwise into the chitosan solution, adjust the pH value of the mixed solution, and stir the resulting mixed solution at 4°C to obtain the chitosan thermosensitive gel, which is called Take a tilmicosin inclusion compound in a conical flask, add an appropriate amount of chitosan thermosensitive gel into the conical flask, and stir evenly with a magnetic stirrer at room temperature to obtain a tilmicosin inclusion complex thermosensitive gel. The invention has the advantages of low toxicity, high bioavailability and low injection irritation.

The invention provides an application of a dihydromyricetin composition in preparation of medicines for inhibiting adriamycin cardiotoxicity. The composition is composed of dihydromyricetin and adriamycin; as shown by in vivo and in vitro experimental studies, the dihydromyricetin can inhibit cell apoptosis activated by the adriamycin and dependent to mitochondrial membrane potential so as to reduce lethality caused by adriamycin cardiotoxicity, and the composition provided by the invention has excellent protection effect on cardiotoxicity induced by adriamycin. The composition provided by the invention can be used for preventing and alleviating the cardiotoxicity educed by adriamycin and has clinical practicability.

The present invention relates to a series of phosphoryl-containing steroidal compounds, a preparation method and an application thereof, in particular to the compounds as a formula I, an isomer, pharmaceutically acceptable salts or chemically protected forms thereof, the preparation method thereof, and the application of the compounds in preparation of a medicine for treating cancer-related diseases. The compounds of the present invention have the good activity for inhibiting malignant tumors such as melanoma and prostate cancer.

The invention discloses a histone deacetylase subtype inhibitor, namely a thioacetyl arylamine compound and application thereof. Pharmacological experiments show that the compound has a selective inhibition effect on HDAC6 enzyme, shows high anti-proliferative activity on various tumor cells, and is low in toxicity to normal cells and low in potential cardiotoxicity. Moreover, the compound has a protective effect on nerve cells, is ideal in pharmacokinetic characteristics, and has relatively high blood-brain barrier dredging characteristics. The compound disclosed by the invention has a deep development prospect as a high-efficiency low-toxicity anti-tumor or neurodegenerative disease therapeutic agent. The structural general formula of the histone deacetylase subtype inhibitor, namely thethioacetyl arylamine compound is as shown in the specification.

This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula shown below wherein the substituents have the meanings defined in claim 1: and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

A slow-release epidoxorubicin-polylactic acid microball is prepared through dissolving epidoxorubicin hydrochloride in DMF, adding triethylamine, adding polylactic acid, adding water, dialyzing in water while stirring and exchanging water every 1-3 hr, centrifugal dewatering, ultrasonic treating, water washing, removing uncoated epidoxorubicin, and freeze-drying of deposit.