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38 results about "10-hydroxycamptothecin" patented technology
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Amphiphilic prodrug of 7- ethyl-10-hydroxycamptothecin and preparation method thereof
InactiveCN102060991AControl release speedPromote degradationOrganic chemistryPharmaceutical delivery mechanismSolubility7-ethyl-10-hydroxycamptothecin
The invention discloses an amphiphilic prodrug of 7- ethyl-10-hydroxycamptothecin, which is prepared by connecting hydroxyl at the site 10 and / or 20 site of the 7-ethyl-10- hydroxycamptothecin and a hydrophilic group through a scissionable chemical bond. The amphiphilic prodrug is self-assembled in water to form a micelle or vesicle structure. Therefore, on one hand, the solubility of SN-38 in water is greatly increased, and the stability of SN-38 lactone rings is improved; and on the other hand, the drug loading rate is high and the SN-38 can be quickly released in cells, consequently the defect of low drug loading rate of traditional drugs is overcame. Moreover, with the nano-micelles or the nano-vesicles of the prodrug, EPR (enhanced permeability and retention) effect targeted cancer tissues of tumors can be effectively utilized.
Owner:ZHEJIANG UNIV
Hydroxy camptothecin emulsion and its preparation method
InactiveCN1493289AChange distributionTissue-targetedOrganic active ingredientsEmulsion deliveryCurative effectTG - Triglyceride
A hydroxycamptothecin emulsion is prepared from hydroxycamptothecin 0.01-2.2 %, emulsifier 0.3-8%, triglyceride 2-30%, glycerine for injection 2.0-3.0 % and water for injection through dissolving the 10-hydroxycamptothecin in the oil phase containing triglyceride and emulsifier, adding water phase, mixing, and ultrasonic or homogeneous emulsifying. Its advantages are high curative effect and stability, and good target to tissue.
Owner:曹永强 +1
Method for separating camptothecin and 10-hydroxycamptothecin by adoption of rosin-based macromolecules
ActiveCN106565732ASmall expansionLarge specific surface areaIon-exchange process apparatusOrganic chemistryCross-linkMicrosphere
The invention discloses a method for separating camptothecin and 10-hydroxycamptothecin by the adoption of rosin-based macromolecules. According to the method, alpha-methacrylic acid (or methyl methacrylate) is used as a monomer, maleated rosin-[(2-acryloyloxy) ethyl] ester is used as a cross-linking agent, and an micro-suspension free radical polymerization method is adopted to prepare rosin-based macromolecule microspheres, wherein the microspheres are a spherical porous material, the article size distribution of the rosin-based macromolecule microspheres is 3-10 microns, the average pore size of the rosin-based macromolecule microspheres is 10-15 nm, the specific surface area of the rosin-based macromolecule microspheres is 90-120 m<2> / g, and the acid value of the rosin-based macromolecule microspheres is 50-150 mgKOH / g; wet column packing is conducted on the rosin-based macromolecule microspheres by the adoption of a column packing machine, so that a chromatographic column is prepared; HPLC separation is conducted on the camptothecin and the 10-hydroxycamptothecin, wherein the detecting wave length is 230-290 nm, the temperature is 30+ / -10 DEG C, the flow speed is 0.3-1.0 mL / min, and the separation degree of the camptothecin and the 10-hydroxycamptothecin is 1.80-2.15. By the adoption of the method for separating the camptothecin and the 10-hydroxycamptothecin by the adoption of the rosin-based macromolecules, a high separation degree of the camptothecin and the 10-hydroxycamptothecin is achieved, the selectivity is high, the method is high in sensitivity, easy to operate, rapid and efficient, and no secondary pollution to medicine, health care products and food is caused.
Owner:GUANGXI UNIV FOR NATITIES
Lignin and histidine drug-loaded nanoparticle with pH response and preparation method of lignin and histidine drug-loaded nanoparticle
InactiveCN108653238AWide variety of sourcesLow costOrganic active ingredientsPharmaceutical non-active ingredientsNanoparticle10-hydroxycamptothecin
The invention discloses a lignin and histidine drug-loaded nanoparticle with pH response and a preparation method of lignin and the histidine drug-loaded nanoparticle. The lignin and histidine drug-loaded nanoparticle is characterized in that a lignin and histidine comjugate is formed by chemically ligating imidized lignin with histidine by amido bonds; hydroxyls in histidine and lignin moleculesare used as hydrophilic ends; a benzene ring in a lignin structure is used as a hydrophobic end; the lignin and the histidine conjugate is self-assembled in an aqueous solution to entrap 10-hydroxycamptothecin to further form the drug-loaded nanoparticle.
Owner:BEIJING FORESTRY UNIVERSITY
Process for promoting generation of 10-hydroxycamptothecin in the bud of camptotheca seed
InactiveCN1482129ASimple processEasy to operateOrganic chemistrySeed and root treatment10-hydroxycamptothecinBud
The present invention relates to the method of promoting the formation of 10-hydroxyl camptothecine in camptotheca seed sprout. The technological process includes water culture of camptotheca seed for sprouting, ultrasonic radiating sprouting camptotheca seed in an ultrasonic device with water, crushing and homogenating the seed sprout tissue in a homogenating machine, filtering to obtain filtrate of 10-hydroxyl camptothecine. The said process has the features of low cost and high yield of 10-hydroxyl camptothecine.
Owner:NORTHEAST FORESTRY UNIVERSITY +1
Method for efficient separation of camptothecin and 10-hydroxycamptothecin by core-shell SiO2@rosin-based polymer chromatographic column
The invention discloses a method for efficient separation of camptothecin and 10-hydroxycamptothecin by a core-shell SiO2@rosin-based polymer chromatographic column. The method includes: taking methacrylic acid or methyl methacrylate as the monomer, adopting maleopimaric acid ethylene glycol acrylate or acrylpimaric acid ethylene glycol acrylate as the cross-linking agent, fully mixing the substances with a free radical initiator, then coating a silica gel surface with the mixture, and then carrying out free radical polymerization reaction to obtain core-shell SiO2@rosin-based polymer microspheres, which have a particle size distribution of 2-50microm, a pore size distribution of 0.5-15nm and a specific surface area of 150-350m<2> / g; subjecting the core-shell SiO2@rosin-based polymer microspheres to wet packing to prepare a chromatographic column, using the prepared chromatographic column for HPLC separation on camptothecin and 10-hydroxycamptothecin, and setting the detection wavelength at 254nm, the temperature at 30+ / -10DEG C and the flow rate at 0.3-1.0mL / min, thus achieving a camptothecin and 10-hydroxycamptothecin separation degree of 2.45-3.47. The method provided by the invention has high separation degree and selectivity on camptothecin and 10-hydroxycamptothecin, and also has the advantages of high sensitivity, simple operation, high speed and efficiency, and environmental friendliness.
Owner:GUANGXI UNIV FOR NATITIES +1
Method of producing 10-hydroxy camptothein
InactiveCN1834097ALow costImprove efficiencyOrganic chemistryChemical recyclingSolubilityPurification methods
This invention discloses a method to produce 10-hydroxycamptothecin, that is, camptothecin adopted as raw materials is catalytic hydrogenised and oxidized in turn at pressures to obtain 10-hydroxycamptothecin. It has the characteristics that steps such as catalyst recycling are modified and that high-pressure liquid phase preparation column and recrystallization are combined for product purification. Conventional large-dosage and low-efficient column separation method or repeated acetic acid recrystallization method is abandoned and composite solvent with high solubility is adopted as mobile phase. The mixture is separated in high-pressure liquid phase column and the consequent substance is decolorized with active carbon and recrystallized by adding poor solvent. Compared to convention purification method, this method has the advantages of high yield, little pollution, simple procedure and economical solvent consumption. For the whole procedure, hydroxycamptothecin with a yield of over 60% and purity of over 99% can be obtained, and this method is suitable for large-scale industrial production.
Owner:JUNJIE BIOTECH SHANGHAI
Process for preparing Topotecan from 10-hydroxy-4-(S) camptothecin
The present invention relates to the use of dihalomethanes as reagents for the preparation of Topotecan{4-(S)-10(dimethylamino)-methyl-4-ethyl 4,9 dihydroxyl-H-pyrano[3'4':6,7]indolizino-[1,2-b]quinoline-3,14(4H,12H)dione} from 10-hydroxycamptothecin. The invention discloses the rationale use of dichloromethane under solid-liquid phase transfer catalysis, which can behave both as solvent and a reactant when it serves as a source for C-1 unit for amino-alkylation of 10-hydroxy-4-(S)camptothecin.
Owner:COUNCIL OF SCI & IND RES
Method for treating abnormal cell growth
InactiveUS20050267140A1Ease of detectabilityEasy to prepareBiocideAnimal repellantsNitrocamptothecinSN-38
Therapeutic pharmaceutical compositions and methods of treatment of abnormal cell growth comprising a pyrimidine derivative or a pharmaceutically acceptable salt, solvate or prodrug thereof in combination with an oral camptothecin, an oral camptothecin derivative, an indolopyrrocarbazole derivative or a pharmaceutically acceptable salt, solvate or prodrug thereof for the treatment of cancer are described. In one embodiment of the present invention the oral camptothecin derivative is selected from the group consisting of 10-hydroxycamptothecin, 9-aminocamptothecin, 9-nitrocamptothecin, irinotecan, irinotecan salt, SN-38, CPT-11, and topotecan and the indolopyrrocarbazole derivative is edotecarin. In one embodiment the pyrimidine derivative is selected from the group consisting gemcitabine, MTA and capecitabine. In one preferred embodiment, the pyrimidine derivative is capecitabine and the camptothecin derivative is CPT-11.
Owner:PFIZER INC
High-efficient production method for 10-hydroxycamptothecine
InactiveCN1450067AReduce dosageSimple processOrganic chemistrySeed and root treatmentCavitationFiltration
The high-effective production method of 10-hydroxycamptothecin includes the following steps: making seed of camptotheca acuminate undergo the processes of negative pressure cavitation mixed-rotating wall-breaking, disinfecting, removing impurity, water culture and germination, mixing the seed sprout and extraction solvent, homogenization and solid-liquid extraction, filtration, negative pressure cavitation mixed-rotating solid-liquid extraction, filtration, concentration, negative pressure cavitation mixed-rotating liquid-liquid extraction, recrystallization or silicon gel column chromatography so as to obtain the 10-hydroxycamptothecin. Said invention raises its yield, can be substituted for traditional various extraction methods of drying material, pulverizing and heating process.
Owner:NORTHEAST FORESTRY UNIVERSITY +1
Water-soluble derivates containing 10-hydroxycamptothecin and preparation method
InactiveCN101397301AGood water solubilitySmall toxicityOrganic active ingredientsOrganic chemistrySolubilityOrganic group
The invention discloses a series of amino-acid ester with molecules internally containing 10-hydroxycamptothecin and derivatives thereof and also discloses water-soluble derivatives forming salts with acids, and a preparation method thereof. The water-soluble derivatives have the formula (I), wherein, A represents saturated hydrocarbons; D represents organic groups containing nitrogen atoms; HB represents the acids forming salt with the organic groups. The compounds have better water-solubility and the arylate can be easily hydrolyzed in the body of human and animals to release the 10-hydroxycamptothecin and the derivatives so as to play the role of anti-cancer.
Owner:重庆医科大学医药研究所
Targeted folic acid-polyethylene glycol-lignin conjugate medicine-carrying nano particles and preparation method thereof
The invention discloses targeted folic acid-polyethylene glycol-lignin conjugate medicine-carrying nano particles and a preparation method thereof. The particles are characterized in that a folic acid-polyethylene glycol-lignin conjugate is formed by chemically connecting folic acid, amidogen-polyethylene glycol-carboxyl and lignin, lignin is used as a framework material, amidogen-polyethylene glycol-carboxyl is used as a connection arm, folic acid is used as a targeted molecule, and the folic acid-polyethylene glycol-lignin conjugate is self-assembled in an aqueous solution and wraps 10-hydroxycamptothecin to form the targeted medicine-carrying nano particles. According to the medicine-carrying nano particles, the solubility, the stability, the permeability and the targeting performance of medicine can be effectively improved, the blood circulation time of the medicine can be effectively prolonged, and the particles have wide application prospects.
Owner:BEIJING FORESTRY UNIVERSITY
Preparation method of novel water-soluble nanoparticles
InactiveCN105902518ADrug loading adjustableStrong targetingOrganic active ingredientsPharmaceutical non-active ingredientsBiocompatibility TestingUrsolic acid
The invention discloses a preparation method of novel water-soluble nanoparticles. The method comprises the following steps: pectin (PET) is used as a carrier; esterification is carried out between carboxyl of pectin and hydroxy of ursolic acid (UA) in order to form macromolecule micelle; self assembly is carried out in order to form nanoparticles PET-UA.NPs, a dihydroartemisinin hydrophobic medicament or 10-hydroxycamptothecin is enveloped during the process of self assembly, in order to form PET-UA(DHA).NPs or PET-UA(HCPT).NPs, and the nanoparticles with core-shell structures are formed. The water-soluble nanoparticles are used as a nanometer medicament with a slow release function, and the nanoparticles have the advantages of adjustable drug loading, good targeting ability, good stability, good biocompatibility, and low toxicity. The nanoparticles belong to the fields of biological pharmacy and nanometer technology, and the method has the advantages of simple preparation technology, operation convenience, and short period.
Owner:BEIJING FORESTRY UNIVERSITY
Implantation type antineoplastic drug of 10-hydroxycamptothecin dual-sustained-release particle formulation and preparation method thereof
InactiveCN101317823ARelease stabilityGood biocompatibilityOrganic active ingredientsPharmaceutical non-active ingredientsSolubilitySide effect
The invention discloses an implanted dual sustained-release granule preparation of 10-hydroxycamptothecine, an antitumor drug, and a preparation method thereof. The invention relates to pharmaceutical preparation and provides the dual sustained-release granule preparation of 10-hydroxycamptothecine that has long releasing time, stable releasing and high utilization ratio of the drug and the preparation method thereof. The preparation is administrated in the manner of implanting after the operation of tumor nidus, thus realizing local target administration to reduce toxic and side effects on the whole body and prevent the recurrence of the tumor. The ingredients of preparation are drug-loaded microspheres, chitosan, lecithin and collagen. The drug-loaded microspheres contain hydroxycamptothecine and polylactic acid that are dissolved in organic solvent in proportion. Initial latex is prepared by dialysis; deposit is collected by centrifugation; and the drug-loaded microsphere is obtained by freeze drying. Afterwards, the chitosan, the collagen and the lecithin with water solubility are added into acetic acid resolution in proportion; and the drug-loaded microsphere is mixed with the solution. After stamping and drying, solid strip preparation is obtained. And the preparation is cut up and stored according to the specifications of the preparation.
Owner:XIAMEN UNIV
Antitumor slow-release implantation agent and preparation method thereof
ActiveCN106236699AIncrease the area under the curveRapid drug actionOrganic active ingredientsInorganic non-active ingredientsWhole bodyTumor cells
The present invention belongs to the field of biomedicine, and particularly relates to an antitumor slow-release implantation agent, which comprises 10-hydroxycamptothecin, a degradable polymer and metal magnesium, and is obtained by a solution spraying or hot-melting extrusion process. According to the present invention, after the implantation agent is subjected to the surgical implantation, the slow release of the10-hydroxycamptothecin can be achieved, and compared with the traditional administration mode, the administration mode of the present invention has the following characteristics that the drug systemic toxicity can be substantially reduced in the premise of the effective maintenance of the local drug concentration of the tumor; the metal magnesium in the implantation agent can react with water in the body environment to generate magnesium hydroxide, such that the environment around the tumor can be adjusted to achieve the alkaline state so as to inhibit the tumor cell growth; and the implantation agent can be used alone or can be combined with other treatment methods to provide the treatment or tumor recurrence prevention effect.
Owner:THE FIRST HOSPITAL OF CHINA MEDICIAL UNIV +2
Chemical semi-synthetic process of 10-hydroxycamptothecin
ActiveCN101450949AControl activityNo overhydrogenationOrganic chemistryChemical recyclingHydrogenation reaction10-hydroxycamptothecin
The invention discloses a semisynthesis method for 10-hydroxycamptothecin, which takes camptothecin as a raw material to prepare the 10-hydroxycamptothecin through the combination of catalytic hydrogenation and oxidation. The method is characterized by realizing a process of the combination of hydrogenation and oxidation, saving operation steps, in particular improving a catalyst by using a Pd / C catalyst containing 5 to 10 percent of palladium and recycling the catalyst, improving the manageability of the reaction by changing high-temperature reaction to normal-temperature reaction, and improving the selectivity of oxidation by applying oxidizers such as 2-iodoxybenzoic acid during the oxidation reaction. Compared with the prior art, the method has the advantages of hydrogenation reaction which is simple and convenient in operation and is low in cost, oxidation reaction which is high in selectivity, total yield of the two reactions of the whole production process which is increased to more than 85 percent, and suitability for industrial production.
Owner:SHANGHAI LONGXIANG BIO MEDICINE DEV CO LTD
10-hydroxy camptothecin arginine salt, and its preparing method and use
InactiveCN1978447ALow toxicitySafe for clinical useOrganic active ingredientsPowder deliverySolubilityArginine
This invention relates to 10-hydroxycamptothecin arginine salt like the structure of formula (I). The preparation of this compound is in condition of water participating. 10-hydroxycamptothecin lactone is unfolded, of which carboxy group first bonds with amino-group of arginine to produce salt, then bonds with 10-phenolic hydroxyl group, then bonds with other arginine acid by hydrogen bond pattern. The quantity of adding arginine can be from 1 to 8 times of molar ratio. The water solubility of 10-hydroxycamptothecin arginine salt and its association object is obviously better than 10-hydroxycamptothecin. It overcomes flaws such as noxious property of camptothecin sodium is high, stability is bad. It provides a medicine of which curative effect is reliable, medication is safe and cost is low for tumor patient.
Owner:成都三康药物研究所
Pharmaceutical Formulation for Increasing Solubility of 10-Hydroxycamptothecin Compounds in Non-Aqueous Polar Solvents
InactiveUS20070254905A1Solubility in polar organic solvent can beImprove solubilityBiocideOrganic chemistrySolubility10-hydroxycamptothecin
The present invention relates to a pharmaceutical formulation for increasing the solubility of a 10-hydroxycamptothecin compound in non-aqueous polar solvent, comprising a 10-hydroxycamptothecin compound and an amine compound whose pKa value is 7.4 or more. By using the formulation according to the present invention, the solubility of the 10-hydroxycamptothecin compound for non-aqueous polar solvent is increased, while maintaining the active lactone form of 10-hydroxycamptothecin.
Owner:SAMYANG BIOPHARMLS CORP
10-hydroxy camptothecin arginine salt, and its preparing method and use
InactiveCN1978448ALow toxicitySafe for clinical useOrganic active ingredientsPowder deliverySolubilityArginine
This invention relates to 10-hydroxycamptothecin arginine salt like the structure of formula (I). The preparation of this compound is in anhydrous solvent. 10-hydroxycamptothecin arginine reacts with arginine, obtaining related arginine salt and its compound. The quantity of adding arginine can be from 1 to 10 times of molar ratio. The water solubility of 10-hydroxycamptothecin arginine salt and its association object is obviously better than 10-hydroxycamptothecin, and possessing conspicuous liver target. It overcomes flaws such as noxious property of camptothecin sodium is high, stability is bad. It provides a medicine of which curative effect is reliable, medication is safe and cost is low for tumor patient.
Owner:成都三康药物研究所
A method for separating camptothecin and 10-hydroxycamptothecin using rosin-based polymers
ActiveCN106565732BSmall expansionLarge specific surface areaIon-exchange process apparatusOrganic chemistryCross-linkMicrosphere
Owner:GUANGXI UNIV FOR NATITIES
Silica body loaded with 10-hydroxycamptothecin and its preparation method
ActiveCN104031080BImprove absorption rateReduce dosageSilicon organic compoundsPharmaceutical non-active ingredientsWater bathsIce water
Disclosed are a 10-hydroxycamptothecin-loaded silica body and a preparation method therefor. The method comprises the following steps: dissolving 10-hydroxycamptothecin in an acidic dichloromethane solution with the pH value of 2 to 4; adding siliceous lipid molecules into the acidic dichloromethane solution of the 10-hydroxycamptothecin under the ice water bath conditions by 3 to 10 batches, stirring for 10 to 120 minutes while continuing maintaining the ice water bath conditions, and removing the solvent in the reaction mixed solution; adding an ethanol / water solution into the solvent-removed solution, treating in a water bath at 50°C to 80°C for 10 to 240 minutes, and carrying out ultrasonic treatment on the solution for 1 to 20 minutes; and centrifugating the mixed solution subjected to the ultrasonic treatment, taking the supernate, and carrying out freeze-drying on the supernate to obtain the 10-hydroxycamptothecin-loaded silica body. By using the silica body, the encapsulation efficiency of the 10-hydroxycamptothecin is at least 75%, and the drug loading rate is at least 3%.
Owner:NORTHEAST FORESTRY UNIVERSITY
10-Hydroxycamptothecin Water-Soluble Macromolecular Conjugates for pH Sensitive Release, Preparation Method and Application
ActiveCN106750254BGood water solubilityGood pharmacokinetic propertiesOrganic active ingredientsPharmaceutical non-active ingredientsSolubilityControl release
The invention discloses a pH sensitive-released 10-hydroxycamptothecine water soluble macromolecular conjugate as well as a preparation method and application thereof. The conjugate is capable of greatly improving the water solubility of 10-HCPT through structural transformation; the pharmacokinetic property of 10-HCPT is improved; by means of the characteristic of a tumor microenvironment, a medicament is released in a pH responsive manner, so that the conjugate has a controlled-release effect; chemical bonds carry the drug with a high drug loading capacity and no drug leakage; a chemotherapeutic can be targeted to tumors and is left for a relatively long time, and the conjugate has a good targeting property.
Owner:ZHENGZHOU UNIV
A kind of anti-tumor sustained-release implant and preparation method thereof
ActiveCN106236699BIncrease the area under the curveRapid drug actionOrganic active ingredientsInorganic non-active ingredientsWhole bodyTumor cells
The present invention belongs to the field of biomedicine, and particularly relates to an antitumor slow-release implantation agent, which comprises 10-hydroxycamptothecin, a degradable polymer and metal magnesium, and is obtained by a solution spraying or hot-melting extrusion process. According to the present invention, after the implantation agent is subjected to the surgical implantation, the slow release of the10-hydroxycamptothecin can be achieved, and compared with the traditional administration mode, the administration mode of the present invention has the following characteristics that the drug systemic toxicity can be substantially reduced in the premise of the effective maintenance of the local drug concentration of the tumor; the metal magnesium in the implantation agent can react with water in the body environment to generate magnesium hydroxide, such that the environment around the tumor can be adjusted to achieve the alkaline state so as to inhibit the tumor cell growth; and the implantation agent can be used alone or can be combined with other treatment methods to provide the treatment or tumor recurrence prevention effect.
Owner:THE FIRST HOSPITAL OF CHINA MEDICIAL UNIV +2
10-Hydroxycamptothecin derivatives, synthesis method and application thereof
ActiveCN106588946BDecrease molecular polarityHigh speedOrganic active ingredientsOrganic chemistrySide effectSynthesis methods
The invention relates to the field of camptothecine drugs, in particular to a 10-HCPT (10-hydroxycamptothecine) derivative, a synthesis method and an application thereof. The 10-HCPT derivative is a derivative which is formed by esterifying a hydroxyl radical at site 10 in 10-HCPT and has an ester structure. The molecular polarity of the derivative is greatly reduced, the biological membrane crossing speed is remarkably increased, the speed and the number of drugs entering tumor cells are increased, the utilization of the drugs is increased, the better anti-tumor effect can be realized, and the toxic and side effects are reduced.
Owner:ZHENGZHOU UNIV
High-efficient production method for 10-hydroxycamptothecine
InactiveCN1172935CReduce dosageSimple processOrganic chemistrySeed and root treatmentCavitationFiltration
The high-effective production method of 10-hydroxycamptothecin includes the following steps: making seed of camptotheca acuminate undergo the processes of negative pressure cavitation mixed-rotating wall-breaking, disinfecting, removing impurity, water culture and germination, mixing the seed sprout and extraction solvent, homogenization and solid-liquid extraction, filtration, negative pressure cavitation mixed-rotating solid-liquid extraction, filtration, concentration, negative pressure cavitation mixed-rotating liquid-liquid extraction, recrystallization or silicon gel column chromatography so as to obtain the 10-hydroxycamptothecin. Said invention raises its yield, can be substituted for traditional various extraction methods of drying material, pulverizing and heating process.
Owner:NORTHEAST FORESTRY UNIVERSITY +1
Ganoderma lucidum polysaccharide-based conjugate drug-loaded nano particle with pH/redox dual response and preparation method thereof
ActiveCN110179993AExtend cycle timeAvoid damageOrganic active ingredientsPharmaceutical non-active ingredientsDual responseRutin
The invention discloses a ganoderma lucidum polysaccharide-based conjugate drug-loaded nano particle with pH / redox dual response. The ganoderma lucidum polysaccharide-based conjugate drug-loaded nanoparticle is characterized in that the ganoderma lucidum polysaccharide-based conjugate is prepared by chemically linking rutin, phenylboronic acid, ganoderma lucidum polysaccharide, dithiodipropionicacid and dihydroartemisinin to form rutin-phenylboronic acid-ganoderma lucidum polysaccharide-dithiodipropionic acid-dihydroartemisinin. The ganoderma lucidum polysaccharide is a hydrophilic segment,the rutin and dihydroartemisinin are hydrophobic segments, and the rutin-phenylboronic acid-ganoderma lucidum polysaccharide-dithiodipropionic acid-dihydroartemisinin conjugate self-assembles and entraps 10-hydroxycamptothecin in an aqueous solution to form the drug-loaded nanoparticle.
Owner:BEIJING FORESTRY UNIVERSITY
Implantation type antineoplastic drug of 10-hydroxycamptothecin dual-sustained-release particle formulation and preparation method thereof
InactiveCN101317823BRelease stabilityGood biocompatibilityOrganic active ingredientsPill deliverySolubilitySide effect
The invention discloses an implanted dual sustained-release granule preparation of 10-hydroxycamptothecine, an antitumor drug, and a preparation method thereof. The invention relates to pharmaceutical preparation and provides the dual sustained-release granule preparation of 10-hydroxycamptothecine that has long releasing time, stable releasing and high utilization ratio of the drug and the preparation method thereof. The preparation is administrated in the manner of implanting after the operation of tumor nidus, thus realizing local target administration to reduce toxic and side effects on the whole body and prevent the recurrence of the tumor. The ingredients of preparation are drug-loaded microspheres, chitosan, lecithin and collagen. The drug-loaded microspheres contain hydroxycamptothecine and polylactic acid that are dissolved in organic solvent in proportion. Initial latex is prepared by dialysis; deposit is collected by centrifugation; and the drug-loaded microsphere is obtained by freeze drying. Afterwards, the chitosan, the collagen and the lecithin with water solubility are added into acetic acid resolution in proportion; and the drug-loaded microsphere is mixed with the solution. After stamping and drying, solid strip preparation is obtained. And the preparation is cut up and stored according to the specifications of the preparation.
Owner:XIAMEN UNIV
Pharmaceutical composition of baicalein and 10-hydroxycamptothecin and its application
ActiveCN103961353BGood curative effectSignificant synergyOrganic active ingredientsAntineoplastic agentsSide effect10-hydroxycamptothecin
The invention relates to a medicine composition which contains 10-hydroxycamptothecine and baicalein. The medicine composition has obvious synergetic effects on treating stomach cancer, breast cancer, liver cancer and the like, reduces the dose of the medicine, improves the curative effect of the medicine, and reduces the generation of side effects.
Owner:DALIAN UNIV OF TECH
Amphiphilic prodrug of 7- ethyl-10-hydroxycamptothecin and preparation method thereof
InactiveCN102060991BImprove hydrophobicityImprove solubilityOrganic chemistryPharmaceutical delivery mechanismSolubility7-ethyl-10-hydroxycamptothecin
The invention discloses an amphiphilic prodrug of 7- ethyl-10-hydroxycamptothecin, which is prepared by connecting hydroxyl at the site 10 and / or 20 site of the 7-ethyl-10- hydroxycamptothecin and a hydrophilic group through a scissionable chemical bond. The amphiphilic prodrug is self-assembled in water to form a micelle or vesicle structure. Therefore, on one hand, the solubility of SN-38 in water is greatly increased, and the stability of SN-38 lactone rings is improved; and on the other hand, the drug loading rate is high and the SN-38 can be quickly released in cells, consequently the defect of low drug loading rate of traditional drugs is overcame. Moreover, with the nano-micelles or the nano-vesicles of the prodrug, EPR (enhanced permeability and retention) effect targeted cancer tissues of tumors can be effectively utilized.
Owner:ZHEJIANG UNIV
A kind of preparation method of water-soluble nanoparticles
InactiveCN105902518BDrug loading adjustableStrong targetingOrganic active ingredientsPharmaceutical non-active ingredientsUrsolic acidBiocompatibility Testing
Owner:BEIJING FORESTRY UNIVERSITY
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