38 results about "10-hydroxycamptothecin" patented technology

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 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 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 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.