WO2017101696A1 - Composition utilisée en médecine occidentale pour traiter la dyspnée aiguë et chronique et son procédé de préparation - Google Patents

Composition utilisée en médecine occidentale pour traiter la dyspnée aiguë et chronique et son procédé de préparation Download PDF

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Publication number
WO2017101696A1
WO2017101696A1 PCT/CN2016/108579 CN2016108579W WO2017101696A1 WO 2017101696 A1 WO2017101696 A1 WO 2017101696A1 CN 2016108579 W CN2016108579 W CN 2016108579W WO 2017101696 A1 WO2017101696 A1 WO 2017101696A1
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Prior art keywords
hydrochloride
medicine composition
western medicine
treating acute
racemic
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PCT/CN2016/108579
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English (en)
Chinese (zh)
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侯丽芳
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侯丽芳
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine

Definitions

  • the invention belongs to the field of medicines, and particularly relates to a western medicine composition for treating acute and chronic dyspnea and a preparation method thereof.
  • the existing treatment methods are antiviral, anti-shock, nutritional supplement or positive end-pressure oxygen delivery, but can not solve the basic cause of the patient's immune imbalance, although the use of glucocorticoids to suppress excessive inflammatory response, but excessive inhibition of inhibition, bone marrow Hematopoietic function is also inhibited, and progenitor cells and stem cells cannot be differentiated in time to transport cells that need to be replenished, which is the main reason for the difficulty in treating severe pneumonia.
  • Pneumoconiosis combined with pulmonary fibrosis is still the world's medical problem. The best way in recent years is to wash the lungs. The effect can remove some of the inhaled aerosols, but the operation is complicated and not suitable for all silicosis patients.
  • the present inventors believe that the above problems are caused by the loss of physiological balance of physiological functions, and it is urgent to effectively suppress or boost the imbalance state of certain functions, so that the physiological mechanism of the disorder is restored or reconstructed, and the serious shortage of existing treatment means is made up.
  • the present invention provides a western medicine composition for treating acute and chronic dyspnea and a preparation method thereof.
  • the technical scheme adopted by the invention is: a western medicine composition for treating acute and chronic dyspnea, the components thereof include racemic anisodamine hydrochloride, ephedrine hydrochloride and dioxpromazine hydrochloride.
  • Racemic racemic anisodamine, ephedrine hydrochloride and dioxpromazine hydrochloride are respectively ground into fine powder, and then the fine powder is separately sieved to obtain racemic anisodamine fine hydrochloride and hydrochloric acid.
  • Ephedrine fines and dioxpromazine hydrochloride fine are respectively ground into fine powder, and then the fine powder is separately sieved to obtain racemic anisodamine fine hydrochloride and hydrochloric acid.
  • step (2) each 4-15.3 mg of the finished product is divided into small packets.
  • the sieving described in the step (1) is a sieve having a size of 80-100 mesh.
  • a method for administering a western medicine composition for treating acute and chronic dyspnea is a method for administering a western medicine composition for treating acute and chronic dyspnea
  • Each dose can be taken at a body weight of 0.3 mg/kg.
  • dyspnea is a variety of physiological dysfunction induced by inflammation, such as autonomic dysfunction, resulting in excessive or insufficient secretion of immune factors, microvascular and microlymphatic dysfunction, red blood cells and platelet aggregation, bone marrow hematopoietic dysfunction.
  • the invention aims at a plurality of disorder mechanisms induced by the inflammatory reaction, and considers that the western medicines to be combined are essential drugs which are commonly used in clinical practice, safe and have few side effects. Selecting the same kind of drug in the same target, the effect is exact and stable, combined together can synergistic effect, and can mutually restrict each other This side effect is composed of the three monomeric western medicines retained in the clinical experiment to constitute the compounding agent of the present invention.
  • Inflammatory reactions whether rapid or slow, its secreted histamine and bradykinin are the main cytokines that cause secretion disorders and other physiological dysfunctions. Therefore, inhibition and prevention of excessive secretion is an important target, dioxazine hydrochloride. Not only is the efficacy of histamine bradykinin specific, but also indirectly blocks the cascade effect of other cytokines, while dioxypromethazine hydrochloride also plays an important role in regulating the respiratory center, and its side effects on central inhibition can be combined with this combination. Ephedrine hydrochloride partially offset.
  • Autonomic dysfunction mostly parasympathetic nerves dominate, relatively speaking sympathetic nerve deficiency.
  • the sympathetic innervation is low, and the immune cells, especially the non-specific innate immunity, are mainly dependent on sympathetic innervation. Therefore, various mechanisms of the respiratory system are disordered, which are all related to sympathetic deficit, especially chronic obstructive pulmonary disease, silicosis and lung fiber.
  • the sympathetic function is low.
  • the serous mucus hypersecretion of severe pneumonia is in the upper peak stage of parasympathetic innervation.
  • a variety of smooth muscle tension in the respiratory system is also a sympathetic nerve, which makes the parasympathetic god over-contracting smooth muscles an advantage. Therefore, it is necessary to supplement the sympathomimetic ephedra or pseudo-anesthetic sputum properly. At the same time, ephedra and edema can also eliminate edema.
  • the core of acute inflammation is the abnormal reaction process caused by abnormal stimulation.
  • This abnormal reaction can be reversed by effective multi-target regulation, and racemic hawthorn hydrochloride has a rapid biphasic adjustment effect on acute and chronic abnormalities of microvessels.
  • Excessive inflammatory stimulation changes the structure of vascular endothelial cells, and the distance between endothelial cells is increased. This is also the pathological basis of hemorrhagic exudation and edema, and also affects the ability of alveolar capillaries to exchange gas.
  • the microvascular damage in the lung tissue is the earliest and heaviest, so the first respiratory distress in critically ill patients is the current mainstream medical difficulty.
  • Existing treatments for input oxygen, interferon and glucocorticoids and escalating antibiotics including the application of artificial lungs, can have limited impact on the underlying causes of respiratory distress, when the ventilator or artificial lungs are withdrawn, eventually It also depends on the repair of the tissue damage of the lung itself and the normal functioning of the external respiratory function.
  • Racemic anisodamine hydrochloride is easily soluble in water, and it is absorbed quickly by oral administration, and plays an adjustment role from the part that enters the body. For example, blocking the parasympathetic over-excitation, relieving the smooth muscle spasm of the gastrointestinal tract, and absorbing the edema of the stagnation, which is reflected in the enhancement of the patient's appetite.
  • racemic anisodamine hydrolyzed the microvessels that were immersed in the sputum and returned to normal, changing the conformation of the endothelial cells that were exfoliated. Blood The accumulation of red blood cells and platelets is alleviated, blood viscosity is reduced, and blood flow rate is accelerated.
  • the western medicine composition for treating acute and chronic dyspnea mainly improves or relieves dyspnea caused by respiratory dysfunction, such as chronic obstructive pulmonary dyspnea, moderate to severe pneumonia caused by viral infection, pneumoconiosis and pulmonary fibrosis Difficulty breathing, central lung cancer, lung effusion and other breathing difficulties.
  • the symptoms of dyspnea are relieved, mainly to compensate for its low function, and to overreact and restore its basically stable dynamic balance.
  • the western medicine composition for treating acute and chronic dyspnea according to the invention can not only gradually degrade and remove dead mites, but also gradually lighten the fibrillated grid-like shadow, so that the patient with silicosis fibrosis does not wheezing and can breathe freely through the life of ordinary people. It improves the respiration and promotes the absorption of pleural effusion in advanced central lung cancer, and stabilizes the condition and improves the quality of life.
  • the beneficial effects of the invention are: the western medicine composition for treating acute and chronic dyspnea according to the invention can be made into a capsule or a powder, and the effect of inhibiting the over- and under-activation of the imbalance of the disease is exerted, and the disorder mechanism is restored to a regular dynamic. balance;
  • the western medicine composition for treating acute and chronic dyspnea mainly improves or relieves dyspnea caused by respiratory dysfunction, such as chronic obstructive pulmonary dyspnea, moderate to severe pneumonia caused by viral infection, pneumoconiosis and pulmonary fibrosis Sexual dyspnea, central lung cancer, pulmonary effusion and other dyspnea;
  • the western medicine composition for treating acute and chronic dyspnea according to the invention can not only gradually degrade and remove dead mites, but also gradually weaken the fibrotic gridded shadow; improve breathing and promote pleural effusion for advanced central lung cancer, stabilize the condition and improve the quality of life. , repeatability is excellent.
  • the invention relates to a western medicine composition for treating acute and chronic dyspnea, which is prepared by mixing racemic anisodamine hydrochloride, ephedrine hydrochloride and dioxpromazine hydrochloride at a weight ratio of 6:9:3.
  • a western medicine composition for treating acute and chronic dyspnea comprising the following materials:
  • the preparation method is
  • Milling Milled racemic anisodamine, ephedrine hydrochloride and dioxpromazine were separately ground into fine powder, and then the fine powder was passed through a 100 mesh sieve to obtain racemic anisodamine hydrochloride and hydrochloric acid. Ephedrine fines and dioxpromazine hydrochloride fine;
  • a western medicine composition for treating acute and chronic dyspnea comprising the following materials:
  • the preparation method is
  • Milling Milling of racemic anisodamine, ephedrine hydrochloride and dioxpromazine hydrochloride into fine powder, respectively, and then passing the fine mesh through a 100 mesh sieve to obtain racemic anisodamine hydrochloride and hydrochloric acid. Ephedrine fines and dioxpromazine hydrochloride fine;
  • a western medicine composition for treating acute and chronic dyspnea comprising the following materials:
  • the preparation method is
  • Milling Milling of racemic anisodamine, ephedrine hydrochloride and dioxpromazine hydrochloride into fine powder, respectively, and then passing the fine mesh through a 100 mesh sieve to obtain racemic anisodamine hydrochloride and hydrochloric acid. Ephedrine fines and dioxpromazine hydrochloride fine;
  • Test method the invention is added to the water twice and mixed uniformly, and the method of directly pouring medicine into the pig's mouth is used; the sick pigs are divided into 2 control groups, 2 low dose groups, and 10 medium dose groups; The control group was not fed the present invention, and the same dose of physiological saline was instilled as a blank control, and the low dose group was fed with 1 bag each time, 6 mg per pack, 3 times a day, and the medium dose group was fed 1.5 packs each time. , each package is 6mg, 3 times a day.
  • Porcine blue ear disease has been called “mysterious pig disease”, “new pig disease”, “porcine epidemic abortion and respiratory syndrome”, “porcine reproductive and respiratory syndrome”, “blue ear disease”, “pig plague”, etc. It belongs to animal respiratory diseases, and China lists it as a second-class infectious disease.
  • Typical cases of the human body are as follows:
  • Chronic obstructive pulmonary disease a chronic obstructive pulmonary disease, characterized by incomplete reversible airflow limitation; chronic obstructive pulmonary airflow limitation is often progressively aggravated with harmful particles or gases, as well as smoking and autoimmune disorders.
  • pulmonary fibrosis such as SARS pneumonia, severe influenza pneumonia, pneumoconiosis, etc., which are associated with different degrees of pulmonary fibrosis, which is also a medical problem in the world.
  • the western medicine composition for treating acute and chronic dyspnea according to the present invention has curative effect on pulmonary fibrosis.
  • Severe pneumonia in children is caused by viral infection, especially in children with pandemic influenza.
  • the incidence and mortality of bronchiolitis pneumonia are high, and the three-concave disease of the sick child is significantly improved after oral administration of the drug.
  • the breathing is improved, the oxygen supply is sufficient, the appetite spirit and physical strength are obviously improved, and the child resumes playing.
  • Acute viral pneumonia such as influenza although the virus has the ability to directly attack lung tissue cells, but this is not the main cause of death from pneumonia.
  • Excessive pulmonary inflammation or immune paralysis is the root cause of death from pneumonia.
  • More than 20% of patients with pan flu have systemic inflammatory response syndrome, and studies in the United States and China for different viral influenza have confirmed the above ratio, and it has been confirmed that controlling infection does not completely block the progression of systemic inflammatory response. It is urgent to address a variety of physiological mechanisms caused by the uncontrolled inflammatory response, and to quickly coordinate various mechanisms of disorder, especially pulmonary dysfunction, into the homeostasis of internal environment, which is the key point for cutting off multiple organ failure.
  • This product is aimed at the dysregulation of inflammatory response, and prevents and repairs lung tissue damage from multiple targets, such as repairing the damage of vascular endothelium and alveolar epithelial conformation and function, thus effectively preventing the further development of hemorrhagic edema and hemorrhage, improving microvascular and lymphatic vessels.
  • the body temperature does not decrease linearly, but gradually decreases after a certain period of stability.
  • the heat source such as toxins and immune complexes need to be gradually transformed and inactivated for a certain period of time, the body temperature is slowly decreasing, and the body temperature is generally not repeated after the decline.
  • the combination drug can not directly kill the virus, it can balance the disorder mechanism of the body, indirectly inhibit the virus replication, accelerate the virus inactivation, and prevent the virus from effluxing. It can help prevent infection and prevent the spread of the epidemic.
  • One week later. There were no new cases of the chicken farm epidemic. This is an effective way to cure and fight out the epidemic in order to solve the outbreak of influenza in remote areas.

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Cette invention concerne une composition utilisée en médecine occidentale pour traiter la dyspnée aiguë et chronique et son procédé de préparation, la composition étant préparée par pulvérisation de chlorhydrate de racéanisodamine, de chlorhydrate d'éphédrine et de chlorhydrate de dioxoprométhazine, puis mélange de ceux-ci.
PCT/CN2016/108579 2015-12-17 2016-12-05 Composition utilisée en médecine occidentale pour traiter la dyspnée aiguë et chronique et son procédé de préparation WO2017101696A1 (fr)

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CN201510955361.6 2015-12-17
CN201510955361.6A CN105412118B (zh) 2015-12-17 2015-12-17 治疗急慢性呼吸困难的西药组合物及其制备方法

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Cited By (1)

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CN113440524A (zh) * 2021-06-28 2021-09-28 成都第一制药有限公司 一种化合物用于制备具有改善肺纤维化作用的药物的用途

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Publication number Priority date Publication date Assignee Title
CN105412118B (zh) * 2015-12-17 2019-03-22 侯丽芳 治疗急慢性呼吸困难的西药组合物及其制备方法

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CN1491652A (zh) * 2002-10-25 2004-04-28 张善良 化学混合物及其应用
CN1478477A (zh) * 2003-07-04 2004-03-03 王鹏程 一种止咳药
CN101756946A (zh) * 2008-10-29 2010-06-30 天津金世制药有限公司 一种治疗慢性支气管炎的口服固体制剂
CN105412118A (zh) * 2015-12-17 2016-03-23 侯丽芳 治疗急慢性呼吸困难的西药组合物及其制备方法

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113440524A (zh) * 2021-06-28 2021-09-28 成都第一制药有限公司 一种化合物用于制备具有改善肺纤维化作用的药物的用途

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