38 results about "10-hydroxycamptothecin" patented technology

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.

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.

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.

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.

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%.

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.

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.

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.

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.

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.

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.

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.

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.