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CN106176693A - One is used for treating angina pectoris Neulized inhalation preparation - Google Patents

One is used for treating angina pectoris Neulized inhalation preparation Download PDF

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Publication number
CN106176693A
CN106176693A CN201610772974.0A CN201610772974A CN106176693A CN 106176693 A CN106176693 A CN 106176693A CN 201610772974 A CN201610772974 A CN 201610772974A CN 106176693 A CN106176693 A CN 106176693A
Authority
CN
China
Prior art keywords
neulized inhalation
nitroglycerin
preparation
inhalation preparation
anginal
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
CN201610772974.0A
Other languages
Chinese (zh)
Inventor
刘保林
凌敏燕
楼金芳
陆慧
张孝君
陈晓萍
曾智丽
傅华锋
胡富苗
宋博凡
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Hangzhou Baicheng Pharmaceutical Technology Co Ltd
Original Assignee
Hangzhou Baicheng Pharmaceutical Technology Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hangzhou Baicheng Pharmaceutical Technology Co Ltd filed Critical Hangzhou Baicheng Pharmaceutical Technology Co Ltd
Priority to CN201610772974.0A priority Critical patent/CN106176693A/en
Publication of CN106176693A publication Critical patent/CN106176693A/en
Pending legal-status Critical Current

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0078Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Dispersion Chemistry (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

The present invention is to treat angina pectoris Neulized inhalation preparation about preparation one, and this Neulized inhalation preparation comprises the nitroglycerin as active substance, solvent, stabilizer, and or pharmacologically acceptable carrier.The used administering mode of the present invention is simple to operation, it is prone to patient accept, when client need is saved oneself, medicinal liquid is placed in inhalation in atomising device, get final product fast and effeciently relief of symptoms, rescue for patient or send institute's treatment to provide sufficiently long slack time, thus improving the survival probability after angina pectoris morbidity.

Description

One is used for treating angina pectoris Neulized inhalation preparation
Technical field
The present invention is belonging to field of medicine preparations, relates to a kind of Neulized inhalation preparation, is used for treating the heart particularly to one The Neulized inhalation preparation of angor.
Background technology
Angina pectoris is a kind of due to coronary insufficiency, cause cardiac muscle drastically, temporary transient ischemia causes with anoxia With clinical syndrome that ictal chest pain or chest discomfort are main performance.Anginal direct pathogenic factor is blood supply of cardiac muscle Deficiency, and deficiency myocardial blood supply is mostly derived from coronary heart disease, other kinds of heart disease or hypertension out of control and the heart also can be caused to twist Bitterly.Anginal Clinical Manifestations is shirtfront paroxysmal, squeezing property pain, can be with other symptoms, and pain is predominantly located at breast Bone rear portion, can be radiated to pareordia and left upper extremity, work or excited often occur.Anginal very harmful, cardiac muscle stalk Extremely being belonging to one of common anginal harm performance, due to coronary artery acute occlusion, blood flow interrupts, cause sternness and Lasting IMN, clinical manifestation is that sudden, strong and lasting retrosternal pain, characteristic electrocardio dynamically spread out Become and the increasing of sero-enzyme;Angina pectoris is also easily caused heart failure, and heart weakens because of disease, overwork, ejection function, so that row Blood volume can not meet organ and anabolic needs;Patient with angina pectoris can occur the complication such as arrhythmia, shock, often can endanger And life.
Owing to angina pectoris is one of situation the most high-risk in heart disease symptom, if can not get giving treatment in time has the most very much May threat to life, emergency measures fast and effectively and send institute's treatment the most particularly important timely, but much patients It is in what it was rescued or sent to hospital by remoter place, the distance hospital inconvenient rescue personnel such as farther out in time during morbidity Situation, then be accomplished by patient and save oneself, by sucking or inject the medicine of certain relief of symptoms, strives for rescue time, Thus reduce the situation that severe complication is even dead.
The chemical formula of nitroglycerin is 1,2,3-glycerol trisnitrate:
Nitroglycerin, as the common drug for the treatment of heart disease, is to treat one of first-selected medicine of angina pectoris.Its mechanism Mainly by load before and after expansion peripheral blood vessel reduction heart, expansion coronary arteries reduces myocardial oxygen consumption and plays a role, and reaches Antianginal effect.Additionally, nitroglycerin also can make peripheral vascular resistance decline by expanding other tremulous pulsies, vein, thus Alleviate the burden of heart, increase heart blood discharge amount, improve the mechanisms play Antianginal effects such as heart and blood circulation.
At present, domestic listing nitroglycerin mainly has tablet, injection, aerosol, and nitroglycerin tablet can not be swallowed, This is because the nitroglycerin swallowed must pass through liver in absorption process, in liver, the nitroglycerin of the overwhelming majority is gone out Living, so that drug effect is substantially reduced, bioavailability is only 8%, and during sublingual administration, the blood capillary that medicine is enriched by oral cavity Pipe is directly absorbed into blood circulation rapidly, and bioavailability may be up to 80%.Owing to buccal tablets is short for action time, Sublingual contains Change only 1~4 minute half-life, be used for preventing angina pectoris attacks improper.Injection is rapid-action, but uses restricted, limitation ratio Relatively big, it is limited to the most to the greatest extent hospital's curing patient, patient can not oneself use.Aerosol need pressure vessel, valve system and Special production equipment, relatively costly;Aerosol has certain pressure, heat and after being impacted it may happen that blast and due to Containing propellant, there is certain toxicity, therefore be not suitable for cardiac and use as inhalation aerosol.
Summary of the invention
Therefore present invention mainly solves prior art problem, exploitation one treats angina pectoris Neulized inhalation preparation, and self The aerosol of the aerosolizable suction without propellant formed, has that atomizing effect is good, absorb fast, rapid-action feature.
For achieving the above object, the present invention adopts the following technical scheme that
A kind of being used for treats an anginal Neulized inhalation preparation, medicinal liquid be placed in atomising device and obtain, described medicinal liquid bag Include active constituents of medicine nitroglycerin, solvent and pharmaceutically acceptable carrier, wherein the concentration of nitroglycerin be 0.1~ 10mg/ml, described solvent can be water and or alcohol mixture, described pharmaceutically acceptable carrier includes stabilizer, isotonic Agent, PH regulator.
Described stabilizer be in propylene glycol, ethanol and glycerol one or more mixing, the concentration of stabilizer be 0.1~ 10mg/ml。
Described isotonic agent is one or more mixing in sodium chloride, potassium chloride, glucose, mannitol, and isotonic agent is dense Degree is 5~9mg/ml.
Described PH regulator is one or more in citric acid, sodium citrate, lactic acid, sodium lactate, hydrochloric acid, sodium hydroxide Mixing, pH value is adjusted to 3.5~5.5.
Described atomising device can be hand-held nebulizer, air compression type nebulizer, oxygen atomizer, metered dose atomization Device.
By the enforcement of above technical scheme, the present invention compared with prior art concrete advantages below:
The used administering mode of the present invention is simple to operation, it is easy to patient accepts.When client need is saved oneself, medicinal liquid is put Inhalation in atomising device, can fast and effeciently relief of symptoms, rescue for patient or send institute's treatment to provide sufficiently long Slack time, thus improve the survival probability after angina pectoris morbidity.And, the present invention treats angina pectoris Neulized inhalation system Agent in use, after medicinal liquid is sprayed by atomising device, forms the little molecule of medicinal liquid, then by the mucosa absorption of mouth and nose, has Absorb fast, rapid-action feature, win the more time for patient's first aid, improve the survival after angina pectoris morbidity several Rate.
Detailed description of the invention:
Now the present invention is described in more detail by following example of formulations, but limits the present invention never in any form.
Embodiment 1:
Nitroglycerin 0.5g
Propylene glycol 10.0g
Glucose 4.5g
Citric acid 0.1g
Pure water adds to 100ml
Technique: weigh nitroglycerin, propylene glycol, glucose, citric acid add in pure water heated and stirred to after being completely dissolved, pure Water purification is settled to full dose, is filtered by sterilizing filter by gained solution, then by liquid medicine filling in 2~5ml ampoule bottles, i.e. Obtain nitroglycerin Neulized inhalation preparation.
Embodiment 2:
Nitroglycerin 1.0g
Ethanol 10.0g
Sodium chloride 7.5g
Lactic acid 0.1g
Pure water adds to 100ml
Technique: weigh nitroglycerin, ethanol, sodium chloride, lactic acid add in pure water heated and stirred to after being completely dissolved, pure water It is settled to full dose, gained solution is filtered by sterilizing filter, then liquid medicine filling is pacified in 2~5ml Low Density Polyethylenes In small jar bottle, obtain nitroglycerin Neulized inhalation preparation.
Embodiment 3:
Nitroglycerin 0.1g
Ethanol 7.0g
Propylene glycol 20.0g
Glucose 4.5g
Citric acid 0.1g
Pure water adds to 100ml
Technique: weigh nitroglycerin, propylene glycol, ethanol, glucose, citric acid add in pure water heated and stirred to being completely dissolved After, pure water is settled to full dose, is filtered by sterilizing filter by gained solution, then by liquid medicine filling in 2~5ml low-density In polyethylene ampoule bottle, obtain nitroglycerin Neulized inhalation preparation.

Claims (6)

1. for the anginal Neulized inhalation preparation for the treatment of, medicinal liquid it is placed in atomising device and obtains, it is characterised in that Described medicinal liquid includes active constituents of medicine nitroglycerin, solvent and pharmaceutically acceptable carrier, wherein nitroglycerin Concentration is 0.1~10mg/ml, described solvent can be water and or alcohol mixture, described pharmaceutically acceptable carrier includes Stabilizer, isotonic agent, PH regulator.
The most according to claim 1 for treating anginal Neulized inhalation preparation, it is characterised in that described stabilizer For one or more mixing in propylene glycol, ethanol and glycerol, the concentration of stabilizer is 0.1~10mg/ml.
The most according to claim 1 for treating anginal Neulized inhalation preparation, it is characterised in that described isotonic agent For one or more mixing in sodium chloride, potassium chloride, glucose, mannitol, isotonic agent concentration is 5~9mg/ml.
The most according to claim 1 for treating anginal Neulized inhalation preparation, it is characterised in that described PH regulator For in citric acid, sodium citrate, lactic acid, sodium lactate, hydrochloric acid, sodium hydroxide one or more mixing, pH value be adjusted to 3.5~ 5.5。
The most according to claim 1 for treating anginal Neulized inhalation preparation, it is characterised in that described atomising device Can be hand-held nebulizer, air compression type nebulizer, oxygen atomizer, metered dose nebulizer.
The most according to claim 1 for treating anginal Neulized inhalation preparation, it is characterised in that described in preparation 100ml Medicinal liquid use following prescription: nitroglycerin 0.5g, propylene glycol 10.0g, glucose 4.5g, citric acid 0.1g, add with pure water To 100ml;And use following preparation method to prepare: weigh nitroglycerin, propylene glycol, glucose, citric acid add pure In water, heated and stirred is to after being completely dissolved, and pure water is settled to full dose, is filtered by sterilizing filter by gained solution, then will Liquid medicine filling, in 2~5ml ampoule bottles, obtains nitroglycerin Neulized inhalation preparation.
CN201610772974.0A 2016-08-31 2016-08-31 One is used for treating angina pectoris Neulized inhalation preparation Pending CN106176693A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201610772974.0A CN106176693A (en) 2016-08-31 2016-08-31 One is used for treating angina pectoris Neulized inhalation preparation

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN201610772974.0A CN106176693A (en) 2016-08-31 2016-08-31 One is used for treating angina pectoris Neulized inhalation preparation

Publications (1)

Publication Number Publication Date
CN106176693A true CN106176693A (en) 2016-12-07

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ID=58089040

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Application Number Title Priority Date Filing Date
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021227540A1 (en) * 2020-05-10 2021-11-18 王安 Healthcare device for tonifying vitality of human body

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102389609A (en) * 2011-06-29 2012-03-28 田中枢 Portable heart disease first aid administration device
CN202289115U (en) * 2011-10-29 2012-07-04 王志萍 Nitroglycerin nasal spraying device
CN102924302A (en) * 2012-11-07 2013-02-13 陕西合成药业有限公司 Injection-grade ambroxol hydrochloride and solution for inhalation of injection-grade ambroxol hydrochloride

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102389609A (en) * 2011-06-29 2012-03-28 田中枢 Portable heart disease first aid administration device
CN202289115U (en) * 2011-10-29 2012-07-04 王志萍 Nitroglycerin nasal spraying device
CN102924302A (en) * 2012-11-07 2013-02-13 陕西合成药业有限公司 Injection-grade ambroxol hydrochloride and solution for inhalation of injection-grade ambroxol hydrochloride

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
南京药学院: "《药剂学》", 31 March 2016 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021227540A1 (en) * 2020-05-10 2021-11-18 王安 Healthcare device for tonifying vitality of human body

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Application publication date: 20161207

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