186 results about "Sinomenine" patented technology

The invention aims at acid, alkali and heat labile features of sinomenine molecular structure, and provides an innovative structural reconstruction idea for new chemical synthesis of ring A, ring C, and ring D sinomenine derivatives. The chemical synthetic method includes amination and acylation of 1-position, C-C or C-O connection of 1 position, dicarbonylation and six-membered N heterocyclization of 3-position and 4-position, two molecule sinomenine adduction of connection of 4-hydroxyl and 1-amino, amination and acylation of 6-position, simultaneous amination and x-membered N heterocyclization of 6-position and 7-position, and opening of D ring and terminal amino group modification thereof. The method is novel and unique. The sinomenine derivatives have good antiinflammation activity and bioactivity evaluated by synovial membrane tumor cell (SW982), and can be used in drug and health products for resisting rheumatoid arthritis.

The invention provides a preparation method of sinomenine, comprising the process for preparing and refining a sinomenine crude product. The preparation method provided by the invention comprises the following steps of: wetting and percolating caulis sinomenii coarse powder with HCL (hydrochloric acid), and extracting and crystallizing the percolation liquid to obtain a sinomenine crude product; and adding ethanol or purified water in the sinomenine crude product and heating and refluxing till the sinomenine crude product is dissolved, adding active carbon for filtering, then cooling, crystallizing, filtering and cleaning a filter cake with ethanol till the filtrate is colorless, and thus obtaining the sinomenine. The preparation method is simple to operate, belongs to cold treatment completely without the need of needs heating in the extraction process; the yield is high, and mother liquid is treated simply; moreover, the preparation method is safe and reliable, causes low pollution and plays a positive effect on environmental protection because only inorganic acid and alkali and a mall amount of level-two toxicity solvent are used.

The invention provides a sinomenine injection special for intravenous administration. The sinomenine injection is an injection which comprises 0.005-0.3wt% of sinomenine and an aqueous solvent for injection, or an injection which comprises sterile injection powder or lyophilized injection powder used for preparation just before injection to cause the sinomenine concentration to be 0.005-0.3wt% in the injection and the aqueous solvent for injection. The sinomenine injection of the invention is used for treating rheumatism, chronic pain and other chronic inflammatory diseases. Compared with other existing injection forms, the sinomenine injection special for intravenous injection has lower drug adverse reaction, and the clinical curative effect is obviously improved.

The invention discloses a sinomenine or an enteric-coated controlled-release tablet of hydrochloride thereof. The prepared enteric-coated controlled-release tablet hardly releases the drug in artificial simulated gastric juice, but can slowly and smoothly release the drug in artificial simulated intestinal juice; the sustained release time of the drug can achieve more than 12 hours or even 24 hours; the enteric-coated controlled-release tablet is taken once or twice daily, the plasma drug concentration in vivo is smooth, and the peak-valley phenomenon of the plasma drug concentration is reduced; as the prepared enteric-coated controlled-release tablet hardly releases the drug in stomach, the contacted concentration of the drug with the gastric mucosa is small, the stimulation of the stomach caused by the drug is alleviated. As the prepared enteric-coated controlled-release tablet sustainedly slowly releases the drug in intestinal tract, the times of the drug administration are reduced, and the patient compliance is improved, thereby being applicable to the needs of the clinical development.

The invention discloses a sinomenine derivative and a synthesis method and aapplications thereof, wherein halogen, carbon-carbon double bond substituent and isoxazoline heterocyclic ring substituent are introduced to the 1-site of the sinomenine ring A. When the sinomenine derivative is prepared, sinomenine is used as the matrix and the synthesis technology containing microfluidic synthesis is adopted to perform Heck reaction and 1,3-dipolar cycloaddition reaction on the 1-site of sinomenine and generate the sinomenine derivative. The obtained compound has better anti-inflammatory activity and is potential to be used for curing arthritis and rheumatoid arthritis and used in the anti-inflammatory medicines thereof.

The invention discloses a sinomenine derivate and a preparation method and an application thereof. The preparation method comprises the following steps: carrying out a reaction on the sinomenine or hydrochloride thereof and paraformaldehyde to obtain a sinomenine benzyl alcohol midbody; carrying out an esterification reaction on the obtained sinomenine benzyl alcohol midbody and C2-4 carboxylic acid anhydride to prepare the product; or, carrying out a substitution reaction on the obtained sinomenine benzyl alcohol midbody with 1-bromo-C2-4 alkane to prepare the product. Applied to preparing the medicine with the anti-inflammatory and immune regulation effects, the obtained sinomenine derivate has transdermal performance better than sinomenine and has a certain anti-inflammatory activity. The derivate is expected to be applied to treating immune diseases such as rheumatic disease and rheumatoid disease.

The invention relates to application of sinomenine as a medicament for preventing and treating pulmonary interstitial fibrosis. The medicament is prepared by sinomenine or pharmaceutically acceptable salt thereof and other adjuvants, wherein sinomenine or pharmaceutically acceptable salt thereof serves as an activating agent. The routes of administration of the medicament include intravenous drip, intramuscular injection, oral administration, transdermal absorption, atomization inhalation and bronchoalveolar lavage. Experiments show that sinomenine does not have obvious difference with the dexamethasone control group in the effect on inhibiting formation of bleomycin-induced pulmonary fibrosis in mice and prove that sinomenine can alleviate pulmonary alveolitis and fibrosis degrees of themice with bleomycin-induced pulmonary fibrosis and the mechanisms are probably realized by inhibiting expressions of TGF (transforming growth factor)-beta1 and alpha-SMA (smooth muscle actin) and thecontent of HYP (hydroxyproline).

The present invention relates to the preparation and pharmacological use of sinomenine derivatives of formula I . The approach disclosed herein is the modification of D ring by- substituting for R. Additional substitutions in the other rings are also provided herein. Several of the sinomenine derivatives have significantly greater anti-inflammation activity when compared with the parent compound.

The invention discloses sinomenine derivatives, and a preparation method and application thereof. The sinomenine derivatives are sinomenine derivative monomers or dimers formed by connecting the 4-position or 6-position carbon (C) of the frameworks of sinomenine and the conventional sinomenine derivatives with linker through X, wherein X is an ether bond, an ester bond, an amido bond, a sulfamide bond, or an amine bond and the like, and the linker is an aliphatic compound, an aromatic compound or polyethylene glycol and the like. The method for preparing the sinomenine derivatives is novel and unique, and simple and practicable; the prepared sinomenine derivatives have high purity and yield; when macrophages RAW264.7 in vitro are adopted to evaluate the NO inhibiting activity and anti-inflammatory action in rats, the sinomenine derivatives have high bioactivity, can be applied to preparing anti-inflammatory medicines for rheumatoid arthritis, rheumatic arthritis and the like, immunosuppressive agents and health products, have wide application range and good treatment effect, and have good social benefit.

The invention discloses a sinomenine vesicle and a preparation method thereof, a preparation containing the sinomenine vesicle and a preparation method of the preparation, which belong to the field of medicament preparations. The sinomenine vesicle is prepared from sinomenine, a nonionic surfactant and an additive. The sinomenine vesicle is preferably prepared into external gel. A sinomenine transdermal administration external preparation has a unique advantage to the medicament. Due to the application of a novel vesicle administration system, transdermal absorption of the medicament is improved, and a clinical curative effect is enhanced. The sinomenine vesicle can be used for treating rheumatism, rheumatoid arthritis, a glomerular disease, hyperosteogeny, spondylitis, arrhythmia, systemic lupus erythematosus, a heroin addict withdrawal symptom and the like.

The invention relates to a traditional Chinese medicine composition, and in particular relates to a compound pharmaceutical composition comprising a szechwan lovage rhizome extract and a caulis sinomenii extract, wherein the szechwan lovage rhizome extract is an extract containing more than 50% of ligustrazine, wherein the caulis sinomenii extract is an extract containing more than 50% of sinomenine; and the weight ratio of the szechwan lovage rhizome extract to the caulis sinomenii extract is (1-10):(1-10).

The invention discloses 14-hydroxyl sinomenine derivatives, a preparation method thereof and anti-inflammatory activity thereof. The 14-hydroxyl sinomenine derivatives are prepared from the raw materials of O-alkyl sinomenine and O-acyl sinomenine by a chemical method that reactions such as oxidation and hydroxylation are carried out at a 14-position. The compounds of the invention show excellent anti-inflammatory activity in in-vivo tests of animals and have an excellent application prospect.

The invention provides application of sinomenine to preparation of a medicament for treating human brain glioma. As proved by experiments, the sinomenine has a function of restraining human-derived glioma U87MG and SF767 cell strains, and the function is improved along with the increase of dose and time. Moreover, the sinomenine can induce the increase of autophagosomes, increase the quantity of autophagic vesicles, prompt the expression increase of human glioma cells LC3B-II, induce autophagic death of human glioma cells, and restrain the growth of U87MG cell xenograft tumors. The sinomenine is a novel and effective glioma-resisting medicament with a great potential, and can be used for preparing a human brain glioma medicament; by adopting the sinomenine, a new way is created for medical treatment of human brain glioma, and the medical application of the sinomenine is expanded.

The present invention relates to a kind of 1-substituted amine methyl sinomenine derivative and its preparation method. Said invention also provides its chemical structure formula and detailed description.

The invention relates to a method for separating and preparing tetrandrine and hanfangchin through ion exchange and column chromatography on silica gel. Fourstamen stephania root is dried root of a menispermaceae stephania plant stephania tetrandra, an effective ingredient of the fourstamen stephania root is sinomenine, main effective ingredients of sinomenine are tetrandrine and hanfangchin, and the sinomenine has anti-myocardial ischemia, anti-arrhythmia, blood pressure lowering, anti-inflammatory, anti-silicosis, anti-cancer and analgesic effects. When in drug use, the purity requirement of the tetrandrine and hanfangchin reaches more than 99%, and extraction and purification are important reasons limiting the drug use of the tetrandrine and hanfangchin. At present, a technology for extracting and purifying the tetrandrine and hanfangchin applies massive toxic and expensive chloroform and strong base, and the chloroform has great toxic effect on human and the environment and is also strong corrosive on equipment for enlarged production; besides, sample purity is not high, and a technological process is complex. At the current situation, the invention develops a method for obtaining high-purity tetrandrine and hanfangchin through rapid separation and purification by applying ion exchange resin and a C18 bonded silica gel column chromatography and also discloses a method for recrystallizing and purifying the tetrandrine and hanfangchin by utilizing ethyl alcohol. The method provided by the invention has the advantages that a preparation technology does not apply any toxic reagent, column chromatography filler can be recycled, and ethyl alcohol can be recycled.

The invention discloses a sinomenine derivative and salt acceptable by pharmacy, and a sinomenine-containing derivative and a drug synthesis of salt acceptable by pharmacy and application thereof. The sinomenine derivative and the salt acceptable by pharmacy are prepared through a chemical synthesis method with sinomenine as a parent compound, have remarkable effects on analgesia, anti-inflammation and relieving cough, are obviously superior to sinomenine, and can be used for curing related diseases.

The invention discloses a compound matrine and diversine nano-emulsion preparation which comprises 0.10-10.00 percent of matrine, 0.10-4.00 percent of diversine, 20.00-38.73 percent of surfactant, 1.64-8.28 percent of oil phase, 0.10-10.00 percent of cosurfactant, 1.00-8.00 percent of azone and 44.00-77.06 percent of distilled water. The compound matrine and diversine nano-emulsion preparation isa transparent oil-in-water nano-emulsion, has the liquid drop grain diameter of 1-100nm, has good stability, improves the solubility and the stability of a medicament, has good skin affinity, enablesthe medicament to faster enter systemic circulation through the skin, avoids the hepatic first pass effect and the gastrointestinal side reaction of the medicament, everlastingly provides the steady flow of the medicament, improves the bioavailability of the medicament, enhances the curative effect of the medicament, is easy to prepare and store and has low production cost and broad market prospects in the medical field.

The sinomenine osmotic pump type control-released preparation capable of releasing a certain quantity of medicine at a constant releasing speed mainly is formed from main core, coating membrane and medicine-releasing hole, and its tablet core is composed of sinomenine hydrochloride, osmosis agent, filling agent and other medicinal auxiliary material, and the coating membrane is a cellulose acetate semi-permeable membrane, and is made up through the processes of pulverizing, sieving, coating and drying. The obtained control-release preparation uses the osmotic pressure difference between interior and exterior of the membrane as medicine-releasing power, and possesses the advantages of blood concentration equilibration, small side effect and long duration of drug effect, etc.

An orally applied slow-releasing micropill of tuduranine or its salt is composed of core and coated layer. Said core is prepared from tuduranine hydrochloride powder and fillers. Said coated layer is prepared from ethyl cellulose.

The invention relates to novel medicinal application of sinomenine, in particular to application of the sinomenine to the preparation of an analgesic drug and belongs to the field of Chinese medicines. When the sinomenine and pharmaceutically-acceptable salts thereof are used for preparing the analgesic drug, pharmaceutically-general excipients such as bonding agent, disintegrating agent, filling agent, lubricating agent, preservative, solubilizing agent, flavoring agent, solvent, emulsifying agent, and the like can be added. The sinomenine and pharmaceutically-acceptable salts thereof can be combined with other compatible treatment drugs to prepare medicament when being used for preparing the analgesic drug.