39 results about "Cytisine" patented technology

The invention provides atomized liquid. The atomized liquid is prepared from nicotine, cytisine and a solvent. By using the cytisine which has a synergistic effect with the nicotine, on the premise that the dosage of the nicotine is not increased, the atomized liquid which is better in satisfaction and better in tobacco addiction relieving effect is provided.

The invention discloses an Escherichia coli mutant strain which is classified and named as Escherichia coli, the strain number is CR-TK01, and the preservation number is CGMCC (China General Microbiological Culture Collection Center) No.35554. The invention further discloses a preparation method of the Escherichia coli mutant strain. The Escherichia coli CR-TK01 with high yield of cytidine provided by the invention has the characteristics of high yield and stable high-yield character, glucose is used as a carbon source, the Escherichia coli CR-TK01 is used for fermentation production of cytidine under a certain fermentation condition, and the yield of cytidine is as high as 97.23 g / L; the strain is not degraded after passage for more than 20 generations, the performance of high-yield cytidine is maintained in the passage fermentation process, and the yield of cytidine in passage fermentation is improved. The method for producing cytidine through fermentation is simple in process, high in yield and suitable for industrialization.

The invention discloses application of a cytisine type alkaloid and a derivative thereof in preparation of a medicine for preventing or treating respiratory syncytial virus infection, and relates to the technical field of respiratory syncytial virus prevention and treatment. The research finds that the natural product cytisine shows good anti-respiratory syncytial virus infection activity in vivo and in vitro, and finds that the cytisine can obviously relieve lung injury caused by virus infection and reduce lung inflammation; the invention provides an experimental basis for developing an efficient and safe drug for resisting respiratory syncytial virus (RSV) infection. As a natural product, the cytisine reduces the social burden caused by treatment of respiratory syncytial virus infection and reduces the treatment cost.

Embodiments of the present application provide an atomization liquid. The atomization liquid comprises: nicotine, cytisine and a solvent. By using cytisine that acts synergistically with nicotine, the atomization liquid that provides better satisfaction and has a better tobacco addiction relief effect is provided without increasing the dosage of nicotine.

Provided herein is a pharmaceutical composition comprising cytisine and a nitrite scavenger, wherein, upon storage of the composition at about 60 ºC, the amount of N-nitrosocytisine relative to a total weight of cytisine is 4.2 ng / mg or less after about 30 days. A method of manufacturing a cytisine tablet is also provided.

The present invention discloses the use of cytisine-N-methylene-(5,7,4'-trihydroxy) isoflavone in the preparation of a drug for treating cerebral infarction. The invention relates to the fields of medicine, natural products, traditional Chinese medicine, and functional foods. The compound has both alkaloid and isoflavone structures, a novel structure, and good drugability. It also contains both flavonoid and alkaloid structural characteristics and is combined with any excipient or carrier acceptable in pharmaceutical, nutritional, and food science. The compound of the present invention can be used as an active ingredient in the treatment of cerebral infarction, inhibiting ischemic brain damage. It not only has a significant therapeutic effect on cerebral infarction, but also possesses multi-level, multi-target comprehensive pharmacological effects and targeted treatment of various pathological mechanisms.

To provide novel analogs of cytisine, and their use in medicine, for example in the treatment of addiction, as well as improved synthetic methods for the preparation of analogs of cytisine.SOLUTION: Disclosed are novel analogs of cytisine, a process for their preparation, pharmaceutical compositions containing them, and their use in the prevention of or treatment of CNS disorders including addictive disorders. The chemical structure of the novel cytisine analogs of the present invention is illustrated in the following chemical formula.SELECTED DRAWING: None

Methods for making compounds comprising a (S)-4,5-dihydro-1H-pyrazole ring are described. These methods include a chiral resolution step performed on an intermediate using a selected chiral resolution agent. For example, the chiral resolution agent can be selected from (-)-quinine, (R)-phenethylamine, (S)-phenethylamine, (S)-1-naphthylethylamine, (R)-(-)-2-amino-3-methyl-1-butanol, (-)-cinchonidine, (-)-cytisine, (R)-1-naphthylethylamine, D-arginine, L-lysine, (S)-(+)-2-pyrrolidinemethanol and (1R,2S)-(+)-cis-1-amino-2-indanol. #imgabs0#

Provided herein is a pharmaceutical composition comprising cytisine and a nitrite scavenger, wherein, upon storage of the composition at about 60° C., the amount of N-nitrosocytisine relative to a total weight of cytisine is 4.2 ng / mg or less after about 30 days. A method of manufacturing a cytisine tablet is also provided.

Methods of treating addictions and / or dependencies, methods of promoting abstraction of various addictions, such as smoking and / or vaporizing, and methods of promoting reduction of various addictions, such as smoking and / or vaporizing, the use of cytisine as an addiction abstraction treatment and dosage regimens therefor are provided.

Methods of assessing purity of cytisine using gradient chromatography at multiple wavelengths is provided herein.

The present invention relates to a stabilizing composition having significantly improved shelf stability. More specifically, the present invention relates to a stable liquid aqueous pharmaceutical composition comprising cytisine or a pharmaceutically acceptable salt thereof, at least one antioxidant selected from the group consisting of sulfite, bisulfite and pyrosulfite compounds. The invention also relates to the use of at least one antioxidant selected from the group consisting of sulfite, bisulfite and pyrosulfite compounds for the stabilization of a liquid aqueous pharmaceutical composition comprising cytisine.

A nicotine liquid preparation, and a preparation method therefor and the use thereof. The raw material components of the nicotine liquid preparation comprise nicotine, an additive capable of simulating the head-rush feeling of nicotine, an atomization solvent and an organic acid. The additive capable of simulating the head-rush feeling of nicotine is selected from at least one of cytisine, magnolol and 6-methylnicotine. The nicotine liquid preparation has a nicotine content of 10-20 mg / g.

The invention discloses a cytisine derivative as well as a preparation method and application thereof, and belongs to the technical field of cytisine derivatives. The structural general formula of the cytisine derivative is formula I: # imgabs0 #, wherein R1 is O or S; r2 is one of a heterocyclic ring, a substituted heterocyclic ring, an aryl group, a substituted aryl group and alkyl groups of C1, C3, C4 and C6; r3 and R5 are one of H, halogen and nitryl; and R4 is H. According to the invention, 35 compounds are successfully prepared by introducing a diurea bridge structure into the cytisine, the obtained compounds have certain inhibitory activity on lung cancer cell strains and show good inhibitory activity on various plant fungi, and the shown anti-tumor and plant fungus activities are obviously higher than those of the cytisine; the provided method is reasonable in design, the diurea bridge structure can be successfully introduced into the cytisine, the preparation condition is mild, high temperature and high pressure are not needed, and the yield is high.

The invention provides a green synthesis method of an alpha-aminoketone compound based on visible light catalytic oxidation amination reaction, and belongs to the technical field of organic chemical synthesizing.According to the method, aliphatic aldehyde and secondary amine which are low in price and easy to obtain serve as raw materials, oxygen serves as a green terminal oxidizing agent, and the alpha-aminoketone compound is synthesized under normal temperature and visible light irradiation. The alpha-aminoketone compound is efficiently synthesized in one step through oxidative amination reaction catalyzed by organic photosensitizers such as rhodamine 6G and anthraquinone. According to the method, a noble metal catalyst and a stoichiometric oxidant are abandoned, the reaction condition is mild (room temperature), the operation is simple and convenient, the substrate application range is wide, and the method shows excellent compatibility to functional groups including various complex cyclic secondary amines (such as natural product derivatives of nornicotine, cytisine and the like); compared with the prior art, the method has the advantages that important transformation from thermal activation to light activation is realized on the reaction mechanism, and a novel green way which is more economical and environment-friendly and is easy for large-scale production is provided for synthesis of alpha-aminoketone.

The present invention relates to a transdermal therapeutic system (TTS) for transdermal administration of cytisine, the transdermal therapeutic system comprising a self-adhesive layer structure comprising a therapeutically effective amount of cytisine, such cytisine TTS for use in a method of treatment and a method for making such cytisine TTS.

Methods for the treatment of addiction and / or dependence are provided, methods to promote the cessation of various addictions, such as smoking and / or vaping, and methods to promote a reduction of various addictions, such as smoking and / or vaping, uses of cytisine as a treatment to quit addiction and dosage regimens for the above.

The present application relates to the technical field of electronic atomization, and specifically relates to a nicotine replacement liquid preparation, and a preparation method therefor and the use thereof. In the nicotine replacement liquid preparation provided in the present application, the raw material components of the nicotine replacement liquid preparation comprise an additive capable of simulating the throat-hit sensation of nicotine, an additive capable of simulating the head-rush sensation of nicotine, and an atomization solvent. The additive capable of simulating the throat-hit sensation of nicotine is selected from at least one of piperine and 6-methylnicotine; and the additive capable of simulating the head-rush sensation of nicotine is selected from at least one of cytisine, magnolol and 6-methylnicotine. The nicotine replacement liquid preparation of the present application simulates the head-rush sensation and throat-hit sensation brought about by nicotine, enhances the head-rush sensation and throat-hit sensation of a nicotine-free atomization preparation, and improves the sense of satisfaction of a user, thereby achieving the aim of relieving addiction physiologically. Moreover, the toxicity and addictiveness of the nicotine replacement liquid preparation are both much lower than nicotine, such that damages to health can be reduced.

The invention discloses a transdermal nicotine withdrawal soluble microneedle patch and a preparation method and application thereof.According to the transdermal nicotine withdrawal soluble microneedle patch, a drug-loaded compound formed by mixing a water-soluble polymer component, a smoking cessation active component and an auxiliary is added into a microneedle mold, and after low-temperature gradient drying, the transdermal nicotine withdrawal soluble microneedle patch is obtained. A porous target object capable of continuously and stably releasing smoking cessation active ingredients is formed. The soluble microneedle patch disclosed by the invention is obtained by combining a microneedle administration technology and a biocompatible material, so that the harm to the lung caused by smoking can be effectively avoided, and meanwhile, the soluble microneedle patch is directly administrated through the skin, so that a first-pass effect and a side effect possibly caused by an oral administration mode can be further avoided; according to the soluble microneedle patch disclosed by the invention, the cytisine or the analogue thereof is used as a main smoking cessation active ingredient, and the sodium hyaluronate or the analogue thereof is used as a matrix material, so that the soluble microneedle patch not only has enhanced solubility and biocompatibility, but also can help to adjust the release rate of the active ingredient.

Salts of cytisine have been prepared and incorporated in stable pharmaceutical compositions, including compositions comprising lactose. The salts are prepared by adding acid stock solutions to solutions of cytisine with heating, followed by cooling to ambient temperature. The salts and compositions are indicated in the treatment of nicotine addiction.

The present invention relates to a liquid pharmaceutical composition comprising cytisine, at least one inorganic pH regulator selected from the group consisting of inorganic acids, inorganic buffers, and salts of inorganic acids, and water, wherein the liquid pharmaceutical composition has a pH value between 3.0 and 7.5. The present invention also relates to the liquid pharmaceutical composition for use in the treatment of tobacco addiction and other forms of nicotine addiction. Additionally, the invention relates to a liquid pharmaceutical composition comprising cytisine for oral use in the treatment of tobacco addiction and other forms of nicotine addiction.

Methods of treating addictions and / or dependencies, methods of promoting abstraction of various addictions, such as smoking and / or vaporizing, and methods of promoting reduction of various addictions, such as smoking and / or vaporizing, the use of cytisine as an addiction abstraction treatment and dosage regimens therefor are provided.

The invention provides a novel application of cytisine, and belongs to the field of medicines. The invention provides application of cytisine in preparation of a medicine for treating pulmonary heart disease. Compared with the cytisine, the cytisine-polypeptide coupling compound (PDC medicine) prepared by coupling the cytisine and the polypeptide has the advantages that the dosage is obviously reduced, the effect is better, the right heart dysfunction can be improved, the myocardial fibrosis is reduced, the right heart remodeling is alleviated, and a new choice is provided for clinically treating the pulmonary heart disease.

Topical formulations have been developed which have been demonstrated to reduce ultraviolet ("UV")-induced cyclobutane pyrimidine dimer ("CPD") formation in a human clinical trial. The formulation includes all natural, non-toxic compounds which can be utilized in sunscreens, cosmetics and hair conditioners to protect from ultraviolet radiation. A preferred embodiment of the formulation contains 10% Ferulic Acid, 10% Diosmin, 5% Cytisine and 5% Resveratrol. A method of screening for compounds that are safe and effective to reduce UV-induced CPD formation also has been developed.

A unit dosage comprising a succinate salt of cytisine formulated as a pharmaceutical composition further comprising a pharmaceutically acceptable excipient, and use in treating a nicotine addiction.

The invention relates to the technical field of electronic atomization, in particular to a nicotine substitute liquid preparation and a preparation method and application thereof. The invention provides a nicotine substitution liquid preparation. The nicotine substitution liquid preparation comprises the following raw material components: a nicotine throat hitting feeling simulation additive, a nicotine head feeling simulation additive and an atomization solvent, the nicotine throat hitting feeling simulation additive is selected from at least one of piperine and 6-methyl nicotine; the nicotine head feeling simulation additive is selected from at least one of cytisine, magnolol and 6-methyl nicotine. The nicotine replaces a liquid preparation to simulate the feeling of feeling on the head and the feeling of hitting the throat caused by the nicotine, the feeling of feeling on the head and the feeling of hitting the throat of the nicotine-free atomized preparation are improved, the satisfaction of a user is improved, the aim of physiologically relieving addiction is achieved, meanwhile, the toxicity and addiction of the nicotine-free atomized preparation are far lower than those of the nicotine, and health damage can be reduced.

The embodiment of the invention belongs to the technical field of buccal substances, and relates to a buccal substance and a preparation method thereof. The component of the buccal substance comprises cytisine. The cytisine is a quinolizidine alkaloid mainly existing in seeds of leguminous pomacea plants, and can have high binding affinity with a nicotine acetylcholine receptor. Therefore, the nicotine-dependent nicotine receptor can selectively act on the human brain to regulate the nicotine-dependent nicotine receptor, the purpose of reducing the nicotine withdrawal symptom is achieved, and the smoking impulse of a user is relieved. However, the buccal substance disclosed by the embodiment of the invention contains the cytisine, so that when the user takes the buccal substance, the tobacco addiction can be relieved by virtue of the cytisine component, and the effect of abstinging the tobacco is further achieved.

The invention relates to the technical field of electronic atomization, in particular to a nicotine liquid preparation and a preparation method and application thereof. The nicotine liquid preparation provided by the invention is prepared from the following raw material components: nicotine, a nicotine head feeling simulation additive, an atomizing solvent and organic acid, the nicotine head feeling simulation additive is selected from at least one of cytisine, magnolol and 6-methyl nicotine; the content of nicotine in the nicotine liquid preparation is 10-20 mg / g. According to the nicotine liquid preparation formed by compounding the head feeling simulation additive and the nicotine on the specific nicotine, under the synergistic effect of all the components, the satisfaction of a user on the low-nicotine-content liquid preparation is improved, and under the condition of the same experience feeling, the toxicity and addiction are reduced, and health damage is reduced.

The application provides an antitumor delphinine alkaloid in Caesalpinia minax, a core skeleton of angustifoline type, and provides an extraction method and application, and compound 3 is used for preparation of an antitumor drug. The natural delphinine with a new angustifoline type structural skeleton is obtained by separation and extraction, wherein compound 3 has a significant inhibitory effect on multiple tumor cell strains, and can be used for preparation of an antitumor drug.