117results about How to "Improve drug activity" patented technology

Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided.

The invention relates to methods of promoting wound healing and reducing scar formation by administration of corticosteroids, and pharmaceutical compositions comprising corticosteroids.

The invention discloses a Chinese herbal microecological preparation for preventing and treating chicken Colibacillosis and a preparation method thereof. The Chinese herbal microecological preparation for preventing and treating chicken Colibacillosis is prepared by adding mixed bacterial liquid of bifidobacteria and bacillus subtilis with a total number of colonies of 0.5-1.0*10<8> CFU / ml into the extract of traditional Chinese medicines and carrying out hermetical anaerobic fermentation on an obtained mixture, wherein the traditional Chinese medicines comprise, by weight, 50 to 200 parts of coptis, 50 to 200 parts of phellodendron, 50 to 200 parts of rheum officinale, 50 to 200 parts of root of large-flowered skullcap, 50 to 200 parts of isatis root and 50 to 100 parts of licorice. The Chinese herbal microecological preparation for preventing and treating chicken Colibacillosis provided in the invention allows pharmaceutical activity of the compatible traditional Chinese medicines to be enhanced after fermentation treatment by using bacterial liquid of bifidobacteria and bacillus subtilis, reduces drug resistance exerted by the medicines on chicken on the basis of guaranteeing a good curative effect and maintains a good treatment effect after many times of administration.

Linkers for binding drugs to cell binding agents are modified to hydrophilic linkers by incorporating a polyethylene glycol spacer. The potency or the efficacy of the cell-binding agent-drug conjugates is surprisingly enhanced several folds in a variety of cancer cell types, including those expressing a low number of antigens on the cell surface or cancer cells that are resistant to treatment. A method for preparing maytansinoids bearing a thioether moiety and a reactive group which allows the maytansinoid to be linked to a cell-binding agent in essentially a single step is also provided.

The present invention relates to a novel ursolic acid derivative as an ursolic acid prodrug form, and to a method for preparing same, wherein the novel ursolic acid derivative as an ursolic acid prodrug can have excellent pharmacokinetic characteristics such as stability and oral absorptivity and exhibit excellent pharmaceutical activities by being converted into an ursolic acid in vivo, and. The ursolic acid derivative can be in an ester form in which C28 carboxylic acid in the ursolic acid is combined with a prodrug of a certain pharmaceutical compound.

The present invention discloses one kind of freeze dried polyene phosphatidylcholine powder for injection and its preparation process. It features that the preparation contains polyene phosphatidylcholine and solubilizer sodium deoxycholate, sodium dehydrocholate or sodium cholate in the weight ratio of 0.5-1.5.

A docetaxel inclusion complex having improved water-solubility (up to 15 mg / ml) and stability (stability constant Ka=2056M−1-13051M−1), comprises docetaxel and hydroxypropyl-beta-cyclodextrin and / or sulfobutyl-beta-cyclodextrin in a ratio of 1:10-150. The method includes steps as follows: docetaxel dissolved in ethanol is added into water solution of cyclodextrin via stirring, until docetaxel is completely dissolved; said solution is filtered in 0.2-04 μm microporous membrane then ethanol is removed through reduced pressure to obtain the inclusion complex in a liquid form; or ethanol, followed by water is removed through reduced pressure, then dried to obtain the inclusion complex in a solid form.

The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.

β-(1-6)-Glucanase treatment of glucan from yeast cells, pure or feed grade, especially yeast from the family Saccharomyces and particularly Saccharomyces cerevisiae, provides a novel glucan product suitable for use in enhancing the stimulation of host animal immune systems. Solubilization of such yeast cell glucan is further disclosed to extend the usefulness of yeast cell glucan as an adjuvant.

The invention discloses a preparation method and application of a cinnamaldehyde submicroemulsion for injection. The cinnamaldehyde submicroemulsion is prepared from the following components in percentage by weight-volume: 5.1-30.6 percent of oil, 0.5-3.0 percent of emulsifier, 1-4 percent of osmotic pressure regulator, 0.1-0.3 percent of stabilizer, 0.05-0.2 percent of antioxidant and the balance of distilled water. The submicroemulsion has excellent stability, biocompatibility and safety; the preparation method is simple, the quality is controllable, and industrial production is possible; the submicroemulsion can be used for treating tumors and other diseases.

β-(1-6)-Glucanase treatment of glucan from yeast cells, pure or feed grade especially yeast from the family Saccharomyces and particularly Saccharomyces cerevisiae, provides a novel glucan product suitable for use in enhancing the stimulation of host animal immune systems. Solubilization of such yeast cell glucan is further disclosed to extend the usefulness of yeast cell glucan as an adjuvant.

A pharmaceutical composition comprising cyclodextrin / paclitaxel inclusion, which consists of paclitaxel, cyclodextrin and a pharmaceutically acceptable excipient, wherein the mass ratio of the paclitaxel to cyclodextrin is 1:10-150, the said cyclodextrin is hydroxylpropyl-sulfobutyl-7-β-cyclodextrin, or sulfobutylether-7-β-cyclodextrin, or their mixture; the stability constant of the cyclodextrin / paclitaxel inclusion is Ka=5396M−1−1412M−1. The preparation method of the pharmaceutical composition is as follow: (a) A solution of cyclodextrin is added dropwise to a solution of paclitaxel in ethanol. (b) The resulting mixture is filtered through microporous membrane of 0.2-0.4 μm after being dissolved. (c) Ethanol is removed under reduced pressure to give a liquid inclusion which has the ethanol level of less than 2%, or alternatively water is also removed under reduced pressure, the resulting product is dried giving a solid inclusion.

The invention relates to a purely natural Chinese medicinal plant preparation, in particular to herbal tea for clearing liver and improving eyesight. The herbal tea improves and cures a series of physiological problems caused by fast pace of life, increment of work pressure, smoking, drinking, imbalanced diet, excessive eating and physiological function decline of organs. The herbal tea consists of the following raw materials in part by weight: 2 to 40 parts of black bean, 2 to 40 parts of Chinese magnoliavine fruit, 0.5 to 10 parts of cinnamomvine, 1 to 20 parts of chrysanthemum, 1 to 20 parts of mulberry, 1.5 to 30 parts of balsam pear, 1 to 15 parts of cassia seed, 1 to 30 parts of mulberry leaf and 1 to 20 parts of seabuckthorn leaf. The herbal tea has the effects of clearing liver, improving eyesight, promoting restoration of optic nerve function and blood vessel function, improving local blood circulation and eliminating local free radical. The herbal tea plays a role in adjusting eyesight function and hepatic and renal function, promoting health of eyesight, liver and kidney, enhancing immunologic function, improving quality of life and strengthening survival ability.

Provided are polyethylene glycol drug conjugates of general formula (I), (II) or (III) and pharmaceutical compositions and a use thereof. The conjugates are formed by combining low molecular weight polyethylene glycol with 2-4 drug molecules. The conjugates can interact with receptor dimers or polymers, thereby improving the in vivo distribution of the drug, changing the oil and water distribution coefficient, enhancing the pharmacological activity, reducing the blood-brain barrier permeability of the drug, and improving the bioavailability of the drug.

The invention provides a bilobalide A derivative and the use in pharmacy, wherein the bilobalide A derivative has a structural formula disclosed in the specification, R1 represents -X-Ar, -X-Z-Ar, -X-COOH, -CO-Ar, -SO2-Ar, -X-Het, X1-CO-X2-NR4R5 or -X-NR4R5, wherein X, X1, X2 represent C1-C8 alkylidene, Z represents C, O, S or N, Ar represents phenyl, pyridinyl, naphthyl, pyrimidinyl, or quinoline.

The invention relates to an absorbable magnesium alloy staple having antibiosis and anti-inflammation functions, and a making method thereof. The staple is composed of a pure magnesium or magnesium alloy wire core with the surface containing a porous ceramic layer, an intermediate functional layer loaded with anti-inflammation medicines and copper ions with gelatin as a carrier, and a degradable high-molecular external surface layer. The copper ions and the anti-inflammation medicines are effectively loaded on the surface of the wire with gelatin as the carrier by adopting an electrophoresis-electrodeposition process, and the external surface layer of the staple is a degradable high-molecular layer having a protection effect. The staple can slowly release the copper ions having a sterilizing effect and the anti-inflammation medicines having an anti-inflammation effect in the use process. Additionally, the synergistic effect between the intermediate functional layer with the gelatin as the carrier and the external degradable high-molecular layer realizes the effective control of the medicine release rate and the staple degradation speed. The staple can be widely applied to the stitching or inosculation of the intestine, the stomach and other human body different positions, and has a wide application prospect.

The invention discloses Carthamus tinctorius L. plant extract, a cosmetic additive adopting the same for realizing skin whitening, moisturizing and antioxidant activity and a combined application of the Carthamus tinctorius L. extract in cosmetics. The Carthamus tinctorius L. extract is ethanol extract of Carthamus tinctorius L. bee pollen or Carthamus tinctorius L. inflorescence or Carthamus tinctorius L. seed oil extract. The extract has good DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical cleaning capacity and is a good natural antioxidant. The Carthamus tinctorius L. extract has excellent skin cosmetic application potential in aspects of wrinkle resisting, whitening, sunscreen and the like in terms of skin care of a human body. With the effective utilization of Carthamus tinctorius L. which is the traditional medicinal plant in China, the Carthamus tinctorius L. extract with very high skin cosmetic activity is obtained, and the extract can be used for preparing a good tyrosinase activity inhibitor and a collagen secretion promoting active agent and is a good raw material for herbal cosmetics.

A pharmaceutical composition comprising cyclodextrin / paclitaxel inclusion, which consists of paclitaxel, cyclodextrin and a pharmaceutically acceptable excipient, wherein the mass ratio of the paclitaxel to cyclodextrin is 1:10-150, the said cyclodextrin is hydroxylpropyl-sulfobutyl-7-β-cyclodextrin, or sulfobutylether-7-β-cyclodextrin, or their mixture; the stability constant of the cyclodextrin / paclitaxel inclusion is Ka=5396M−1−1412M−1. The preparation method of the pharmaceutical composition is as follow: (a) A solution of cyclodextrin is added dropwise to a solution of paclitaxel in ethanol. (b) The resulting mixture is filtered through microporous membrane of 0.2-0.4 μm after being dissolved. (c) Ethanol is removed under reduced pressure to give a liquid inclusion which has the ethanol level of less than 2%, or alternatively water is also removed under reduced pressure, the resulting product is dried giving a solid inclusion.

Embodiments of the present disclosure provides a method of preparing an adipose tissue-targeting polypeptide-verbascoside-nanogold particle derivative, including: activating a carboxyl group of a cysteine residue at the C-terminus of an adipose tissue-targeting polypeptide to form an acyl chloride; reacting a verbascoside with a sodium hydroxide to obtain a sodium phenolate; esterifying the acyl chloride with the sodium phenolate to form an adipose tissue-targeting polypeptide-verbascoside derivative; and reacting the adipose tissue-targeting polypeptide-verbascoside derivative with PEG-modified nanogold particles. The present disclosure further discloses an adipose tissue-targeting polypeptide-verbascoside-nanogold particle derivative and the application of the adipose tissue-targeting polypeptide-verbascoside-nanogold particle derivative in preparing a drug for the treatment of obesity. The adipose tissue-targeting polypeptide-verbascoside-nanogold particle derivative has good biocompatibility, and capable of carrying drugs into the adipocytes, thereby greatly enhancing the availability of the drug and significantly improving the targeted anti-obesity activity of the drug.

Compounds represented by the formula: wherein R1 and R2 are hydrogen atom, a hydrocarbon group or a heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3- to 8-membered homocyclic or heterocyclic ring,W indicates(i) a group represented by the formula: wherein ring B indicates a 5- to 7-membered ring, or(ii) a group represented by the formula: wherein R4 indicates (1) an aliphatic hydrocarbon group, which may be substituted with an aromatic group, or (2) an acyl group containing an aromatic group, R5 is hydrogen atom, a C1-6 alkyl, or an acyl group, provided that, when W is Wa, R3 is hydrogen atom, a hydrocarbon group or a heterocyclic group, when W is Wb, R3 indicates a C6-14 aryl group, or salts thereof or prodrugs thereof have an excellent action to inhibit neurodegeneration and the like as well as an excellent brain penetrability and are low in the toxicity, thereby being useful as prophylactic or therapeutic drugs for nerve degenerative diseases and the like.

The invention discloses a preparation method of lentinan. The preparation method comprises the following steps: 1) pre-treating; 2) breaking cell walls and pulping; 3) extracting with clean water; 4)carrying out alcohol precipitation to obtain crude polysaccharide; 5) filling the crude polysaccharide on ion exchange resin and collecting an eluting solution to obtain a de-colored polysaccharide solution; 6) carrying out micro-filtration and ultra-filtration, and concentrating to obtain a concentrated solution; 7) freezing and drying the concentrated solution obtained by step 6) to obtain a lentinan product. According to the preparation method provided by the invention, the obtained lentinan product has high extraction rate and high purity; meanwhile, the lentinan has excellent pharmaceutical activity and prominent advantages.

The invention relates to methods of promoting wound healing and reducing scar formation by administration of corticosteroids, and pharmaceutical compositions comprising corticosteroids.

The invention discloses curcumin-containing aryl metal complexes which can effectively improve bioavailability of curcumin and have good phototoxicity, anti-cancer activity, angiogenesis inhibiting capacity and antibacterial activity. The invention further discloses a synthetic method of the curcumin-containing aryl metal complexes. The method adopts simple technical process, is easy to operate and high in yield. The invention finally discloses an application of the curcumin-containing aryl metal complexes to preparation of anti-cancer drugs, anti-cancer drug components, anti-tumor metastasisdrugs, anti-tumor metastasis drug components, antibacterial agents and antibacterial agent components.

The invention belongs to the field of traditional Chinese medicines and particularly relates to an application of traditional Chinese medicine composition and a preparation thereof in preparation of adrug for treating ALI (acute lung injury). The traditional Chinese medicine composition is prepared from raw materials such as rhizoma paridis, radix scutellariae, thunberg fritillary bulb, common dayflower herbs, rhizoma anemarrhenae, gypsum, dried tangerine or orange peel, fructus aurantii, fructus xanthii, bitter almond kernels, radix platycodonis, cablin potchouli herbs, folium perillae and prepared liquorice roots. Study results show that the traditional Chinese medicine composition can reduce the water content and the permeability index of the lung of a model rat with ALI and reduce thelevel of cell inflammatory factors, improve change of ALI lung histopathology, has a remarkable treatment effect on ALI and is suitable for clinical popularization and application.

The invention provides a brand new anilinoquinazoline compound of the structure in the formula (I). The anilinoquinazoline compound has a tyrosine kinase inhibiting effect. Real-time fluorogenic quantitative PCR measurement results indicate that the VEGF expression quantity is reduced by 1000 times or more through the target compound, the inhibiting effect on VEGF expression is quite obvious, and the inhibiting activity is far higher than that of vandetanib. Further experiments indicate that the target compound has the better antineoplastic activity compared with vandetanib under the anoxia condition and is expected to be the medicine for treating tumors.

Compounds represented by the formula: wherein R1 and R2 are hydrogen atom, a hydrocarbon group or a heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3- to 8-membered homocyclic or heterocyclic ring, W indicates (i) a group represented by the formula: wherein ring B indicates a 5- to 7-membered ring, or (ii) a group represented by the formula: wherein R4 indicates (1) an aliphatic hydrocarbon group, which may be substituted with an aromatic group, or (2) an acyl group containing an aromatic group, R5 is hydrogen atom, a C1-6 alkyl, or an acyl group, provided that, when W is Wa, R3 is hydrogen atom, a hydrocarbon group or a heterocyclic group, when W is Wb, R3 indicates a C6-14 aryl group, or salts thereof or prodrugs thereof have an excellent action to inhibit neurodegeneration and the like as well as an excellent brain penetrability and are low in the toxicity, thereby being useful as prophylactic or therapeutic drugs for nerve degenerative diseases and the like.

The invention relates to the technical field of pesticides and pharmaceuticals and particularly relates to the application of four compounds in preparation of nematicidal medicines. The four compoundsdisclosed by the invention are safe and reliable, are capable of effectively controlling nematodiasis agriculturally and expelling nematoid parasites medicinally, do not have any toxic and / or side effects or drug dependence to the human body, are better than existing pesticides and pharmaceuticals, and can be widely applied to the preparation of nematicidal medicines.