62 results about "Bufalin" patented technology

The invention discloses a 3-epi-bufalin 3-O-beta-D-glucoside and derivant, which inhibits cancer cell from growing rather than bufalin to make cardiotonic, local anesthesia, combat shock and tumour-resistant drug.

The invention relates to a traditional Chinese medicine venenum bufonis extract. A method for extracting the extract includes steps of extracting traditional Chinese venenum bufonis medical materials at the temperature ranging from 60 DEG C to 90 DEG C by ethanol water with volume percent of 60-95% in a backflow manner, separating extract liquid via silicagel columns after the extract liquid is concentrated, adopting petroleum ether and acetone with volume ratio of 1-8:1 as eluant to realize gradient elution, collecting parts of eluent, and filtering, concentrating and drying the eluent in a pressure reduction manner to obtain the traditional Chinese medicine vanenum bufonis extract containing mixture of three types of bufotalin including resibufogenin, cinobufagin and bufalin, wherein the sum of the weight percentages (calculated when three types of the bufotalin are dried) of the three types of the bufotalin is higher than or equal to 95%. The invention further provides the preparation method for the traditional Chinese medicine venenum bufonis extract. The sum of the weight percentages of the three types of the bufotalin in the traditional Chinese medicine venenum bufonis extract is higher than 95%, extraction transfer rate is high, the quantity of used solvent is lower, residual solvent is little, pollution degree is lower, operation is simple and convenient, and industrial production is realized easily.

The invention relates to a traditional Chinese medicine toad venom dissimlar extract and a preparation method thereof, and belongs to the technical field of drugs. The preparation method of the extract comprises the steps of crushing toad venom medicinal materials into middle power, and adding 4 to 10 times of water for grinding and dispersing; adding ethyl alcohol to carry out alcohol precipitation, and storing at a low temperature; adding sodium chloride into supernatant liquor for salting out at a low temperature; carrying out concentration under reduced pressure until block-shaped toad venom dissimlar extract is separated out, carrying out drying or concentration under reduced pressure until nearly dry, carrying out vacuum drying, and adding ethanol recrystallization, so as to obtain the toad venom dissimlar extract containing resibufogenin, cinobufagin venom toad and bufalin; the transfer rate of the mixture of three bufogenins is about 80%, and the sum of weight percentages of the three bufogenins is equal to or greater than 35%. The toad venom extracted by adopting the method has the advantages of high transfer rate and active ingredient content, no residual organic solvent, simple and convenient operation, low energy consumption, and easiness in controlling of product quality, and is suitable for industrializing production.

The present invention discloses the technology of purifying lipid bufogenin and cino-bufogenin in fresh toad cake. The purifying process includes grinding fresh toad cake, adding organic solvent through stirring to obtain toad cake solution, standing, filtering to obtain filtrate, concentrating and drying to obtain the product. The toad cake powder product has relatively high lipid bufogenin and cino-bufogenin content.

The invention provides a tumor targeted prodrug having an endosome escaping function; the tumor targeted prodrug is P (OEGMA-co-BUF-co-RGD)-g-P (DEA-co-BMA), wherein POEGMA is a water-soluble polymer having a long circulation function, BUF is chemotherapeutic bufalin having an antineoplastic activity, cRGD is polypeptide capable of targeting tumor tissues actively and P (DEA-co-BMA) is a polymer having an endosome escaping function. The invention also provides a method for preparing the tumor targeted prodrug, as well as a nano preparation and a preparation method of the tumor targeted prodrug having the endosome escaping function. The nano preparation can be used for effectively killing cancer cells with a relatively low dosage; and an effect of killing various cancer cells is obviously better than that of a free bufalin medicine.

The present invention discloses the application of toad venom extract containing more than 90% of bufolin, cinobufagin and cinobufagin in the preparation of medicines for treating human glioma. The content ratio of tobafagenin is 2:3:5, and the extract of toad venom is prepared into a nano-preparation. The bufagenin nano-preparation of the invention can increase the distribution of bufagenin in the brain and avoid being taken up by the heart, thereby improving the brain-targeting property of the drug and reducing cardiotoxicity. Compared with the common extract solution of bufogenin, the nano-preparation of bufogenin has a stronger therapeutic effect on glioma brain and less side effects, thus enhancing the use value of bufogenin and providing a new method for the treatment of glioma. new drug.

The invention belongs to the technical field of a tumor targeting deliverying and slow release administration system. The invention relates to a bufalin-loaded valine-arginine-glycine-aspartic acid-glutamic acid cyclopeptide (cRGD)-modified poly(oligo(ethylene glycol)methacrylate)-polycaprolactone (Ph PCL b P(OEGMA co RGD) bufalin) nanometer particle and a preparation method thereof. Ph-PCL-b-P(OEGMA-co-GMA) as a base material is modified through cRGD to form Ph-PCL-b-P(OEGMA-co-RGD) and bufalin is wrapped by micelle of the Ph-PCL-b-P(OEGMA-co-RGD) so that (Ph PCL b P(OEGMA co RGD) bufalin) nanometer particles are prepared. The nanometer preparation can effectively reduce toxic or side effect of bufalin and improve water solubility and tumor targeting ability. The bufalin is slowly released along with material degradation so that long-term treatment effects are obtained.

The invention provides medicine containing toad venom lipid-soluble substances and a preparation method thereof. According to the toad venom lipid-soluble substances, the weight sum of bufalin, cinobufagin and resibufogenin is larger than 50% of the total weight of the toad venom lipid-soluble substances. The preparation method of the toad venom lipid-soluble substances includes the steps that toad venom herbs are smashed, then absolute ethyl alcohol is added, the amount of the absolute ethyl alcohol is 5-50 times that of the herbs, heating reflux is performed on the mixture for 1 h in a water bath of 60 DEG C, then the mixture is cooled to indoor temperature, suction filtration is performed, dry extract is obtained after filtrate is evaporated to dryness, purified water is added into the extract for ultrasonic suspending, the amount of the purified water is 5-30 times that of the extract, and extracting is performed through chloroform, wherein the amount of chloroform is 5-50 times that of the mixture. The invention further provides a medicine composite and a preparation method thereof. The medicine composite is a toad venom extract lipid microsphere oral solution and is used for treating gastrointestinal tumors.

The invention discloses a lung cancer and breast cancer treatment compound preparation containing active ingredients of traditional Chinese medicine and a preparation method of the lung cancer and breast cancer compound preparation. The lung cancer and breast cancer treatment compound preparation is made from erianin, taxol, bufalin and bruceine D according to a certain weight ratio. According to the preparation method, liposomes are prepared according to an ethyl alcohol injection method or dropping pills are prepared by taking polyethylene glycol as a base material to obtain the lung cancer and breast cancer treatment compound preparation containing the active ingredients of the traditional Chinese medicine. The form of the compound preparation is compound liposomes and compound dripping pills. According to animal in-vivo anticancer pharmacological experiments, the lung cancer and breast cancer treatment compound preparation containing the active ingredients of the traditional Chinese medicine has obvious inhibiting effect on growth of lung cancer and breast cancer and has higher anticancer activity than chemotherapeutic drug 5-fluorouracil.

The invention relates to a dry powder inhalant, in particular to a Bufalin dry powder inhalant, the preparation method of the dry powder inhalant and the application in preparing drug for treating lung tumors. The Bufalin dry powder inhalant is characterized in that the Bufalin dry powder inhalant is composed of Bufalin and pharmaceutically acceptable auxiliary materials, wherein the mass ratio of the Bufalin to pharmaceutically acceptable auxiliary materials is (1:0.01)-(1:110). The dry powder inhalant by taking the Bufalin as the main drug can directly act on an affected part by aiming at the lung tumor to lower the possibility of toxic and side effect and improve the bioavailability. According to the Bufalin dry powder inhalant, the defects that the oral-administration preparation slowly takes effect, the preparation has low bioavailability and the like can be overcome, and the problems of low Bufalin content, inconvenient use, poor patient complicance and the like in the injectioncan be solved. Thus, the Bufalin is prepared into the dry powder inhalant, which has great prospect for developing new drug.

The invention discloses a medicine composition and gel for oral mucosa inflammatory pain and bacteriostasis and a preparation method. Bufalin, dyclonine, chitosan quaternary ammonium salt and epsilon-polylysine are used as the medicine composition to treat symptoms of oral ulcer and mucosa inflammatory pain, the medicine composition is a compound preparation according to the mechanism of pain on the surface of oral ulcer and pain causing base of inhibiting multiple microorganisms on the surface of the ulcer, the bufalin and the dyclonine are combined to quickly block pain conduction of exposednerve endings for a long time, food addition of non-western medicine antibiotics and combination of chitosan quaternary ammonium salt and epsilon-polylysine are adopted to effectively kill multiple pathogenic microorganisms on the surface of the ulcer, inflammatory irritation is further reduced, and the healing function of the wound ulcer is promoted.

The invention discloses a high purity bufonis veneum direct oral decoction piece and a preparation method thereof. The bufonis veneum direct oral decoction piece is in single dose package with a specification of 1-60mg, and the bufonis veneum powder particle size is smaller than or equal to 50 meshes. Calculated on a dry product, the total amount of bufalin, cinobufagin and resibufogenin contained in the direct oral decoction piece is not less than 6.5% (g/g), the total ash is not more than 5.0%, and the acid-insoluble ash does not exceed 2.0%. Salmonella (10g) is not detected in the product, and bile salt resistant gram-negative bacteria is less than 10000cfu (1g). The bufonis veneum direct oral decoction piece is produced in workshops conforming to the "good manufacture practice of drugs". The preparation method includes: (1) raw material inspection; (2) primary crushing; (3) processing with wine; (4) filtering; (5) drying; (6) second crushing; (7) inner packing; (8) outer packaging; and (9) finished product inspection. Specifically, the steps (2)-(7) are carried out in a D grade clean production area, and the step (8) is conducted in a general production area. The bufonis veneum direct oral decoction piece is in single dose package, has the advantages of accurate dosage, controllable production process, good safety, and qualified microbial limit, the product is in accordance with the quality standards of direct oral drugs, and is suitable for direct oral taking.

The invention discloses a method for microwave extracting fat-soluble toad venom by using skin of Bufo bufo gargarizans, which comprises the following steps: using ethanol as extraction solvent, using microwave to dispel, heat and extract, using ultrafiltration membrane to filter and then concentrating the extraction solvent, and using liquid chromatogram technique to conduct separation and purification, wherein the extraction temperature breaks through the convention, is relatively higher but is still controlled within the lowest denaturation temperature, and the extraction time is shorter and less than one hour. Therefore, the denaturation of the fat-soluble toad venom is less, and the extraction rate is relatively higher during the extraction process; when the liquid chromatogram conducts separation and purification, the retention time of bufalin, cinobufagin and resibufogenin are respectively 7.594min, 10.103min and 10.741min, thus being capable of better separating and obtaining various fat-soluble toad venoms; the obtained bufalin, cinobufagin and resibufogenin has high purity which can reach 99%, and the impurity is little, therefore the obtained various fat-soluble toad venoms are more stable, and not easy to generate denaturation; and the extraction rate of the fat-soluble toad venom is more than 17%, and the highest extraction rate can reach 40%.

The invention belongs to the technical field of medicines, relates to the novel medicinal application of the traditional Chinese medicinal preparation, namely, Bufalin, and in particular relates to applications of bufalin in preparing a preparation capable of realizing targeted inhibition on pancreatic cancer stem cells. The invention further provides a method for culturing Miapaca2/GEM by adopting a serum-free suspension culture method, and thus the stem cell spheres with a high proportion are obtained. According to the scheme, from the aspect of tumor stem cells, the experiment shows that in the application of preparing the preparation capable of realizing targeted inhibition on pancreatic cancer stem cells of the traditional Chinese medicinal preparation, namely, Bufalin, the preparation can inhibit the self-renewal of the tumor stem cells, particularly, the preparation can inhibit the proportion of the tumor stem cells in the pancreatic cancer drug resistant cell line Miapaca2/GEM, and thus the drug tolerance of pancreatic cancer is inverted.

The invention belongs to a field of medicament preparation, and relates to a pharmaceutical composition for treating cardiovascular disease and a preparation method thereof, especially to the pharmaceutical composition which contains drug-efficacy component groups capable of being absorbed into blood. The drug-efficacy component groups comprise: Japanese bufotaline, ginsenoside Re, ginsenoside Ra1, 1[beta]-hydroxy bufalin, ginsenoside Rb1, resibufogenin fine alcohol, ginsenoside Rc, ginsenoside Rb2, ginsenoside, ginsenoside Rd, bufalin, cholic acid, hyodeoxy cholic acid, cinobufagin, chenodeoxycholic acid and deoxycholic acid. The medicament has clear in vivo targets, has characteristics and advantages of multi-component multi-target effects, is good in protective effects for acute myocardial ischemia, and can reduce area of myocardial infarction and content of Lactate dehydrogenase and creatine kinase in serum.

The invention relates to the technical field of medicine, in particular to a bufalin (BUF)-carrying nano liposome modified by hyaluronic acid as well as a preparation method and application of the BUF-carrying nano liposome. A film dispersion method is combined with an ultrasonic method to prepare the liposome with a smaller particle size and dispersion uniformity, the hyaluronic acid is linked tothe DOPE phospholipid through chemical modification, and a dialysis bag method is used for purification. The solubility of the BUF can be improved, the tumor targeting effect can be enhanced, toxic and side effects can be reduced, the drug resistance of breast cancer cells to docetaxel (DCT) can be reversed, and new dosage form application is provided for the clinical application of the BUF.

The invention relates to the technology of traditional Chinese medicine extraction and discloses a preparation method of a venenum bufonis extract, by which the venenum bufonis extract being higher than 95% in comprehensive content of bufalin, cinobufagin and resibufogenin can be prepared. The invention also discloses an application of the venenum bufonis extract being higher than 95% in the comprehensive content of the bufalin, cinobufagin and resibufogenin in preparation of an anti-brain glioma medicine.

The invention relates to a preparation method for extracting a cinobufagin and bufalin mixture from venenum bufonis. The preparation method is characterized by comprising the following steps of: smashing the venenum bufonis into medium coarse powder, and then adding 70%-95% of ethanol for extraction; and carrying out silica gel column chromatography separation on an extracting solution to obtain the high-purity cinobufagin and bufalin mixture, wherein the content of the cinobufagin and bufalin mixture achieves more than 80%. The total content of the cinobufagin and bufalin mixture extracted by adopting the preparation method disclosed by the invention achieves more than 80%.

The invention provides a bufalin micelle nano-preparation. The bufalin micelle nano-preparation comprises bufalin, and a lipidized polypeptide micelle carrier which wraps the bufalin, and one moleculeof the lipidized polypeptide micelle carrier comprises one molecule of a hydrophilic unit and one molecule of a hydrophobic unit connected with the hydrophilic unit, wherein the hydrophilic unit is an asymmetric dendritic polypeptide polymer unit, the hydrophobic unit is a lipid unit, and the end of the dendritic polypeptide polymer unit carries a positive charge.

The present invention relates to medicine technology, and is nanometer granular bufalin-albumin preparation as one new preparation form of bufalin and its preparation process. Bufalin has excellent effects of treating tumor, reversing chemotherapeutic drug resistance, inhibiting hepatitis B virus copying, etc. but high toxicity and short intracorporeal half life, forming no medicine preparation up to now. The nanometer granular bufalin-albumin preparation of the present invention has round shape of nanometer grains, narrow grain size distribution in the range of 50-250 nm, average grain size of 102 nm, liver targeting and delayed releasing, so that it has increased concentration in target organ for long time action, raised curative effect and lowered toxic side effect and may be used in preparing medicine for treating liver cancer and hepatitis B.