CN106109427A - The application in preparation treatment asthmatic medicament of a kind of compound recipe puppet fiber crops U.S. sweet smell sheet - Google Patents
The application in preparation treatment asthmatic medicament of a kind of compound recipe puppet fiber crops U.S. sweet smell sheet Download PDFInfo
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- CN106109427A CN106109427A CN201610573981.8A CN201610573981A CN106109427A CN 106109427 A CN106109427 A CN 106109427A CN 201610573981 A CN201610573981 A CN 201610573981A CN 106109427 A CN106109427 A CN 106109427A
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- puppet
- fiber crops
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- sweet smell
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- 150000001875 compounds Chemical class 0.000 title claims abstract description 55
- 239000000835 fiber Substances 0.000 title claims abstract description 55
- 239000003205 fragrance Substances 0.000 title claims abstract description 51
- 241000556261 Sphenotoma Species 0.000 title claims abstract description 44
- 239000003814 drug Substances 0.000 title claims abstract description 32
- 208000006673 asthma Diseases 0.000 title claims abstract description 19
- 238000002360 preparation method Methods 0.000 title claims abstract description 19
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims abstract description 24
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims abstract description 16
- YQSHYGCCYVPRDI-UHFFFAOYSA-N (4-propan-2-ylphenyl)methanamine Chemical compound CC(C)C1=CC=C(CN)C=C1 YQSHYGCCYVPRDI-UHFFFAOYSA-N 0.000 claims abstract description 13
- 239000004375 Dextrin Substances 0.000 claims abstract description 13
- 229920001353 Dextrin Polymers 0.000 claims abstract description 13
- KWGRBVOPPLSCSI-UHFFFAOYSA-N d-ephedrine Natural products CNC(C)C(O)C1=CC=CC=C1 KWGRBVOPPLSCSI-UHFFFAOYSA-N 0.000 claims abstract description 13
- 235000019425 dextrin Nutrition 0.000 claims abstract description 13
- 229960003782 dextromethorphan hydrobromide Drugs 0.000 claims abstract description 13
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 claims abstract description 12
- 235000019359 magnesium stearate Nutrition 0.000 claims abstract description 12
- 229960003447 pseudoephedrine hydrochloride Drugs 0.000 claims abstract description 12
- BALXUFOVQVENIU-KXNXZCPBSA-N pseudoephedrine hydrochloride Chemical compound [H+].[Cl-].CN[C@@H](C)[C@@H](O)C1=CC=CC=C1 BALXUFOVQVENIU-KXNXZCPBSA-N 0.000 claims abstract description 12
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims abstract description 7
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims abstract description 7
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims abstract description 7
- 239000000203 mixture Substances 0.000 claims description 17
- -1 polyethylene pyrrole Pyrrolidone Polymers 0.000 claims description 5
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 2
- 229940050239 dextromethorphan hydrobromide 15 mg Drugs 0.000 claims description 2
- 239000011777 magnesium Substances 0.000 claims description 2
- 229910052749 magnesium Inorganic materials 0.000 claims description 2
- 229940021228 pseudoephedrine hydrochloride 30 mg Drugs 0.000 claims description 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 2
- ZPHQBFRCXUIIAZ-UHFFFAOYSA-N benzene;hydrochloride Chemical compound Cl.C1=CC=CC=C1 ZPHQBFRCXUIIAZ-UHFFFAOYSA-N 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 229920002554 vinyl polymer Polymers 0.000 claims 1
- 102000004016 L-Type Calcium Channels Human genes 0.000 abstract description 5
- 108090000420 L-Type Calcium Channels Proteins 0.000 abstract description 5
- 210000005090 tracheal smooth muscle Anatomy 0.000 abstract description 5
- 108091005462 Cation channels Proteins 0.000 abstract description 4
- 201000010099 disease Diseases 0.000 abstract description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract description 3
- 230000009471 action Effects 0.000 abstract description 2
- 239000004480 active ingredient Substances 0.000 abstract description 2
- 230000000903 blocking effect Effects 0.000 abstract description 2
- 229940127225 asthma medication Drugs 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 210000003437 trachea Anatomy 0.000 description 53
- 241000699670 Mus sp. Species 0.000 description 33
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 description 23
- 229960004373 acetylcholine Drugs 0.000 description 23
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 15
- 239000011575 calcium Substances 0.000 description 15
- 229910052791 calcium Inorganic materials 0.000 description 15
- 230000000694 effects Effects 0.000 description 12
- 229940079593 drug Drugs 0.000 description 10
- 150000003217 pyrazoles Chemical class 0.000 description 9
- 230000000638 stimulation Effects 0.000 description 9
- 206010049816 Muscle tightness Diseases 0.000 description 8
- 239000003795 chemical substances by application Substances 0.000 description 8
- HYIMSNHJOBLJNT-UHFFFAOYSA-N nifedipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1[N+]([O-])=O HYIMSNHJOBLJNT-UHFFFAOYSA-N 0.000 description 8
- 229960001597 nifedipine Drugs 0.000 description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 7
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 6
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 6
- 238000002474 experimental method Methods 0.000 description 6
- 239000001301 oxygen Substances 0.000 description 6
- 229910052760 oxygen Inorganic materials 0.000 description 6
- 239000011591 potassium Substances 0.000 description 6
- 229910052700 potassium Inorganic materials 0.000 description 6
- 230000036316 preload Effects 0.000 description 5
- 210000001519 tissue Anatomy 0.000 description 5
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M Potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 description 4
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 4
- 210000000621 bronchi Anatomy 0.000 description 4
- JBRBWHCVRGURBA-UHFFFAOYSA-N broxaterol Chemical compound CC(C)(C)NCC(O)C1=CC(Br)=NO1 JBRBWHCVRGURBA-UHFFFAOYSA-N 0.000 description 4
- 229950008847 broxaterol Drugs 0.000 description 4
- 210000002460 smooth muscle Anatomy 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- 241000699666 Mus <mouse, genus> Species 0.000 description 3
- 108090000312 Calcium Channels Proteins 0.000 description 2
- 102000003922 Calcium Channels Human genes 0.000 description 2
- UXVMQQNJUSDDNG-UHFFFAOYSA-L Calcium chloride Chemical compound [Cl-].[Cl-].[Ca+2] UXVMQQNJUSDDNG-UHFFFAOYSA-L 0.000 description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 description 2
- 235000016838 Pomo dAdamo Nutrition 0.000 description 2
- 244000003138 Pomo dAdamo Species 0.000 description 2
- 230000003504 ach effect Effects 0.000 description 2
- 239000001110 calcium chloride Substances 0.000 description 2
- 229910001628 calcium chloride Inorganic materials 0.000 description 2
- 239000003153 chemical reaction reagent Substances 0.000 description 2
- 239000000812 cholinergic antagonist Substances 0.000 description 2
- 210000002808 connective tissue Anatomy 0.000 description 2
- 230000008602 contraction Effects 0.000 description 2
- 230000007423 decrease Effects 0.000 description 2
- 230000003205 diastolic effect Effects 0.000 description 2
- DBLXOVFQHHSKRC-UHFFFAOYSA-N ethanesulfonic acid;2-piperazin-1-ylethanol Chemical compound CCS(O)(=O)=O.OCCN1CCNCC1 DBLXOVFQHHSKRC-UHFFFAOYSA-N 0.000 description 2
- 239000008103 glucose Substances 0.000 description 2
- 239000005556 hormone Substances 0.000 description 2
- 229940088597 hormone Drugs 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 230000007774 longterm Effects 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 230000003285 pharmacodynamic effect Effects 0.000 description 2
- 239000001103 potassium chloride Substances 0.000 description 2
- 235000011164 potassium chloride Nutrition 0.000 description 2
- 239000011780 sodium chloride Substances 0.000 description 2
- 230000001629 suppression Effects 0.000 description 2
- 238000013268 sustained release Methods 0.000 description 2
- 239000012730 sustained-release form Substances 0.000 description 2
- ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 description 2
- 241000271566 Aves Species 0.000 description 1
- 208000009079 Bronchial Spasm Diseases 0.000 description 1
- 208000014181 Bronchial disease Diseases 0.000 description 1
- 206010006482 Bronchospasm Diseases 0.000 description 1
- BHPQYMZQTOCNFJ-UHFFFAOYSA-N Calcium cation Chemical compound [Ca+2] BHPQYMZQTOCNFJ-UHFFFAOYSA-N 0.000 description 1
- 208000002177 Cataract Diseases 0.000 description 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 1
- 208000000059 Dyspnea Diseases 0.000 description 1
- 206010013975 Dyspnoeas Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 208000019025 Hypokalemia Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 208000008589 Obesity Diseases 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 208000037656 Respiratory Sounds Diseases 0.000 description 1
- 208000005392 Spasm Diseases 0.000 description 1
- 206010044565 Tremor Diseases 0.000 description 1
- 206010047924 Wheezing Diseases 0.000 description 1
- 150000001336 alkenes Chemical class 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 206010003119 arrhythmia Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 230000033228 biological regulation Effects 0.000 description 1
- 229910001424 calcium ion Inorganic materials 0.000 description 1
- 230000002612 cardiopulmonary effect Effects 0.000 description 1
- 150000001768 cations Chemical class 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 210000000038 chest Anatomy 0.000 description 1
- 239000000460 chlorine Substances 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 229960000935 dehydrated alcohol Drugs 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 230000006806 disease prevention Effects 0.000 description 1
- 238000002224 dissection Methods 0.000 description 1
- 238000002651 drug therapy Methods 0.000 description 1
- 229960004756 ethanol Drugs 0.000 description 1
- 239000007789 gas Substances 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 230000003054 hormonal effect Effects 0.000 description 1
- 238000009169 immunotherapy Methods 0.000 description 1
- 150000002617 leukotrienes Chemical class 0.000 description 1
- 229940050906 magnesium chloride hexahydrate Drugs 0.000 description 1
- DHRRIBDTHFBPNG-UHFFFAOYSA-L magnesium dichloride hexahydrate Chemical compound O.O.O.O.O.O.[Mg+2].[Cl-].[Cl-] DHRRIBDTHFBPNG-UHFFFAOYSA-L 0.000 description 1
- 229940091250 magnesium supplement Drugs 0.000 description 1
- 230000028161 membrane depolarization Effects 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 235000020824 obesity Nutrition 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 230000036284 oxygen consumption Effects 0.000 description 1
- 230000010412 perfusion Effects 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 239000002574 poison Substances 0.000 description 1
- 231100000614 poison Toxicity 0.000 description 1
- 208000024896 potassium deficiency disease Diseases 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 229960003908 pseudoephedrine Drugs 0.000 description 1
- KWGRBVOPPLSCSI-WCBMZHEXSA-N pseudoephedrine Chemical compound CN[C@@H](C)[C@@H](O)C1=CC=CC=C1 KWGRBVOPPLSCSI-WCBMZHEXSA-N 0.000 description 1
- HNJBEVLQSNELDL-UHFFFAOYSA-N pyrrolidin-2-one Chemical compound O=C1CCCN1 HNJBEVLQSNELDL-UHFFFAOYSA-N 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 210000002027 skeletal muscle Anatomy 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229940126680 traditional chinese medicines Drugs 0.000 description 1
Classifications
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/485—Morphinan derivatives, e.g. morphine, codeine
-
- 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
-
- 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Emergency Medicine (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to the application in preparation treatment asthmatic medicament of a kind of compound recipe puppet fiber crops U.S. sweet smell sheet, described compound recipe puppet fiber crops U.S. sweet smell sheet is made up of pseudoephedrine hydrochloride, dextromethorphan hydrobromide, diphhydramine hydrochloride, low-substituted hydroxypropyl cellulose, polyvinylpyrrolidone, magnesium stearate and dextrin, described compound recipe puppet fiber crops U.S. sweet smell sheet is by blocking L-type calcium channel and non-selective cation channel and relaxed and comfortable tracheal smooth muscle, can be as a kind of Novel air pipe dilator, for the treatment of the diseases such as asthma.The sweet smell sheet pharmacological action of compound recipe of the present invention puppet fiber crops U.S. is good, active ingredient safety is high, provides a kind of novel, safe asthma medications for clinic.
Description
Technical field
The present invention relates to the application in preparation treatment asthmatic medicament of a kind of compound recipe puppet fiber crops U.S. sweet smell sheet, belong to medical science neck
Territory.
Background technology
Asthma is the disease of the high susceptibility of the trachea caused by some anaphylactogen existed in the external world or human body.By
In trachea, the tetchiness of stimulus object is reacted, cause trachea that reversibility spasm, narrow widely occurs.Clinical manifestation is outbreak
Property with the dyspnea of wheezing sound, last for several minutes to a few hours, through treatment or take a turn for the better voluntarily.
At present, treating asthma should take general treatment measures, including: avoid contact with anaphylactogen and other asthma trigger because of
Element, normalized Drug therapy, specific active immunotherapy and patient education.Its drug treatment includes controlling medicine and alleviation
Property medicine.Concrete medicine includes hormone, leukotrienes regulator, broxaterol, sustained-release theophyline, anti-IgE antibodies, imbedibility
Anticholinergic agents etc..Broxaterol, sustained-release theophyline, anticholinergic agents can pass through diastole bronchus smooth muscle, release and prop up
Tracheospasm thus alleviate symptoms of asthma.
Either all there is untoward reaction in hormonal medicaments or broxaterol medicine, and Long-term Oral hormone can draw
Play osteoporosis, hypertension, diabetes, the suppression of hypothalmus-pituitary-adrenal axis, obesity, cataract etc.；
Needing interval to use during broxaterol Clinical practice, unsuitable use long-term, single, also unsuitable excess application, otherwise can cause
, there is certain drawback in the untoward reaction such as skeletal muscle trembles, hypokalemia, cardiac arrhythmia.Therefore, we are in the urgent need to exploitation one
Novel, safe asthmatic medicament.
Summary of the invention
It is an object of the invention to provide the purposes of a kind of compound recipe puppet fiber crops U.S. sweet smell sheet, be specifically related to compound recipe puppet fiber crops U.S. sweet smell sheet in system
Application in standby treatment asthmatic medicament.
Realization the technical scheme is that
The application in preparation treatment asthmatic medicament of a kind of compound recipe puppet fiber crops U.S. sweet smell sheet, the composition of described compound recipe puppet fiber crops U.S. sweet smell sheet
For pseudoephedrine hydrochloride, dextromethorphan hydrobromide, diphhydramine hydrochloride, low-substituted hydroxypropyl cellulose, polyvinylpyrrolidone,
Magnesium stearate, dextrin.
Preferably, the application in preparation treatment asthmatic medicament of compound recipe puppet fiber crops U.S. sweet smell sheet, every described compound recipe puppet fiber crops U.S. is fragrant
Sheet to consist of pseudoephedrine hydrochloride 30mg, dextromethorphan hydrobromide 15mg, diphhydramine hydrochloride 25mg, low substituted hydroxy-propyl fine
Dimension element 7.5mg, polyvinylpyrrolidone 4.5mg, magnesium stearate 3mg, dextrin 65mg.
The application in preparation treatment asthmatic medicament of compound recipe puppet fiber crops U.S. sweet smell sheet, described compound recipe puppet fiber crops U.S. sweet smell sheet preparation process
For:
(1) pseudoephedrine hydrochloride, dextromethorphan hydrobromide, diphhydramine hydrochloride, low-substituted hydroxypropyl cellulose, polyethylene
Ketopyrrolidine, magnesium stearate and dextrin are pulverized respectively, cross 40 mesh sieves；
(2) by pseudoephedrine hydrochloride, dextromethorphan hydrobromide, diphhydramine hydrochloride, low-substituted hydroxypropyl cellulose, poly-second
Alkene pyrrolidone and dextrin mix homogeneously；
(3) described magnesium stearate is added in the mixture of step (2), mix homogeneously；
(4) mixture tabletting step (3) obtained, obtains compound recipe puppet fiber crops U.S. sweet smell sheet, and tableting pressure is 8～10kg/
mm2。
Compared with prior art, the beneficial effects of the present invention is:
Pharmacodynamic experiment result shows, compound recipe puppet fiber crops U.S. sweet smell sheet leads to by blocking L-type calcium channel and non-selective cation
Road relaxes tracheal smooth muscle, can be as a kind of Novel air pipe dilator, for the treatment of the diseases such as asthma；Compound recipe puppet fiber crops U.S. is fragrant
Active ingredient pseudoephedrine hydrochloride, dextromethorphan hydrobromide and diphhydramine hydrochloride in sheet use for many years clinically, obtain
Clinical Laboratory, safety is high.
Detailed description of the invention
For making those skilled in the art can be better understood from the present invention and can be practiced, below in conjunction with being embodied as
The present invention is further elaborated for example.
The preparation of embodiment 1 compound recipe puppet fiber crops U.S. sweet smell sheet
(1) pseudoephedrine hydrochloride, dextromethorphan hydrobromide, diphhydramine hydrochloride, low-substituted hydroxypropyl cellulose, polyethylene
Ketopyrrolidine, magnesium stearate and dextrin are pulverized respectively, cross 40 mesh sieves；
(2) by pseudoephedrine hydrochloride 3g, dextromethorphan hydrobromide 1.5g, diphhydramine hydrochloride 2.5g, low substituted hydroxy-propyl
Cellulose 0.75g, polyvinylpyrrolidone 0.45g, dextrin 6.5g mix homogeneously；
(3) 3g magnesium stearate is added in the mixture of step (2), mix homogeneously；
(4) the mixture 10kg/mm that step (3) is obtained2Pressure tabletting, prepares 100 compound recipe puppet fiber crops U.S. sweet smell sheets.
The preparation of embodiment 2 compound recipe puppet fiber crops U.S. sweet smell sheet
(1) pseudoephedrine hydrochloride, dextromethorphan hydrobromide, diphhydramine hydrochloride, low-substituted hydroxypropyl cellulose, polyethylene
Ketopyrrolidine, magnesium stearate and dextrin are pulverized respectively, cross 40 mesh sieves；
(2) by pseudoephedrine hydrochloride 3g, dextromethorphan hydrobromide 1.5g, diphhydramine hydrochloride 2.5g, low substituted hydroxy-propyl
Cellulose 0.75g, polyvinylpyrrolidone 0.45g, dextrin 6.5g mix homogeneously；
(3) 3g magnesium stearate is added in the mixture of step (2), mix homogeneously；
(4) the mixture 8kg/mm that step (3) is obtained2Pressure tabletting, prepares 100 compound recipe puppet fiber crops U.S. sweet smell sheets.
The non-clinical pharmacodynamic study of embodiment 3 compound recipe puppet fiber crops U.S. sweet smell sheet
1. experiment material
1.1 laboratory animal
Sexual maturity and the male mouse of kunming of health, 8 weeks mean aves, be purchased from Disease Prevention Control Center, Hubei Prov.Little
Mus is raised in 20～25 DEG C of ambient temperature and 50～60% under humidity environment, and cycle light and dark interval time is 12 hours.
1.2 experimental apparatus and reagent
Compound recipe puppet fiber crops U.S.'s sweet smell sheet (making by oneself)；Dehydrated alcohol (traditional Chinese medicines chemical reagent company limited)；
Nifedipine (Sigma Co., USA)；Pyrazoles 3 (Sigma Co., USA)；
Acetylcholine (Sigma Co., USA)；
Stereomicroscope (Wuhan Ace pendant scientific instrument company limited)；
Ice machine (vitreous of another name for Sichuan Province, Chongzhou City work Co., Ltd)；
Conical flask (vitreous of another name for Sichuan Province, Chongzhou City work Co., Ltd)；
HV-4 type in vitro tissue organ constant temperature perfusion system (Chengdu TME Technology Co., Ltd.)；
Thermostatic water-circulator bath pot HW-1000 (Chengdu TME Technology Co., Ltd.)；
Biological functional system BL-420S (Chengdu TME Technology Co., Ltd.).
1.3 experimental solutions preparations
1.3.1 the preparation of high calcium solution
Take sodium chloride 7.889g, potassium chloride 0.3728g, glucose 1.982g, 4-hydroxyethyl piperazine ethanesulfonic acid 2.383g, chlorine
Change magnesium 0.2033g, calcium chloride 0.2296g, add sterilized water to 1000mL, then be that 0.5mol/L NaOH solution is adjusted to pH by concentration
7.4。
1.3.2 the preparation of High potassium solution
Take sodium chloride 135mM, potassium chloride 80mM, glucose 10mM, 4-hydroxyethyl piperazine ethanesulfonic acid 10mM, magnesium chloride hexahydrate
1mM, calcium chloride 2mM, add sterilized water to 1000mL, then be that 0.5mol/L NaOH solution is adjusted to pH7.4 by concentration.
1.3.3 the preparation of acetylcholine solution
Take acetylcholine 16.3mg, dissolve with high calcium solution and be diluted to 1000mL.
1.4 drug material
Compound recipe puppet fiber crops U.S. sweet smell sheet of Example 1 preparation, grinds to form powdery, weighs 0.3g in plastic tube, adds 3mL high
Calcium solution, is configured to the Experimental agents of 100mg/mL, standby.
2. experimental technique
The acquisition of 2.1 mice tracheas
Use cervical dislocation by sacrifice, then mice is fixed on dissection plate, sprays 75wt% ethanol, with disappearing
Cross poison shears along thorax scissors to cervical region, after exposing trachea, cut off at Adam's apple, gently carry Adam's apple with tweezers, shears is sideling
30 degree of connective tissues cutting off the right and left, are finally separating escape pipe and cardiopulmonary tissue, are immediately placed in the high calcium solution of pre-cooling.
Tissue is fixed in dissecting pan, removes the various connective tissues around trachea, then trachea upper end is cut to bronchus front end
Disconnected.
2.2 tonotransducer pilot system debugging
Instrument is opened after row calibration oxygen valve, and regulation oxygen-supplying amount is in suitable scope, to ensure the basic of tissue
Oxygen consumption but not disturbed test baseline, then open tension force energy converting system, sample rate is set to 100HZ, opens thermostatic control system,
Ensureing that in vitro tissue temperature constant is 37 DEG C, each bath is equipped with 6mL high calcium solution, and instrument preheats 0.5 hour, standby.
The process of 2.3 tracheas and the sample loading of tonotransducer
Intercepted length is the trachea of 5mm, by mice trachea by hook linking tonotransducer pilot system, be placed in containing
6mL37 DEG C of high calcium solution also persistently leads to the constant temperature water bath of oxygen.Preload is set to 300mg, within every 15 minutes, changes one second highest
Calcium solution, continuous four times.After balancing 60 minutes, carry out pre-stimulation with 100 μm ol/L acetylcholine, make trachea be in optimal retraction
State, recovers to baseline after eluting.
2.4 compound recipe puppet fiber crops U.S.'s sweet smell sheet diastole pre-shrunk to acetylcholine effects
By mice trachea by hook linking tonotransducer pilot system, it is placed in containing 37 DEG C of high calcium solutions of 6mL and holds
The constant temperature water bath of continuous logical oxygen.Preload is set to 300mg, within every 15 minutes, changes a high calcium solution, continuous four times.Balance
After 60 minutes, carry out pre-stimulation three times with 100 μm ol/L acetylcholine, make tracheal muscle tension force reach more than 800mg, extensive after eluting
Multiple to baseline, add acetylcholine and make trachea preshrinking 15 minutes, then press Concentraton gradient 0.01mg/mL, 0.032mg/ successively
ML, 0.1mg/mL, 0.316mg/mL, 1mg/mL, 3.16mg/mL, 5.62mg/mL, 10mg/mL compound recipe puppet fiber crops U.S. sweet smell tries
Test, each mass action 12 minutes.
2.5 compound recipe puppet fiber crops U.S. sweet smell sheets nifedipine after preshrinking is blocked after diastole effect
By mice trachea by hook linking tonotransducer pilot system, it is placed in containing 37 DEG C of high calcium solutions of 6mL and holds
The constant temperature water bath of continuous logical oxygen.Preload is set to 300mg, within every 15 minutes, changes a high calcium solution, continuous four times.Balance
After 60 minutes, carry out pre-stimulation three times with 100 μm ol/L acetylcholine, make tracheal muscle tension force reach more than 800mg, extensive after eluting
Multiple to baseline, add acetylcholine and make trachea preshrinking 15 minutes, adding 3 μ L concentration is 10 μm ol/L nifedipine (L-type
Calcium ion channel blockor), adding Experimental agents to drug level after 15 minutes is 5.62mg/mL.
2.6 compound recipe puppet fiber crops U.S. sweet smell sheets pyrazoles after preshrinking 3 is blocked after diastole effect
By mice trachea by hook linking tonotransducer pilot system, it is placed in containing 37 DEG C of high calcium solutions of 6mL and holds
The constant temperature water bath of continuous logical oxygen.Preload is set to 300mg, within every 15 minutes, changes a high calcium solution, continuous four times.Balance
After 60 minutes, carry out pre-stimulation three times with 100 μm ol/L acetylcholine, make tracheal muscle tension force reach more than 800mg, extensive after eluting
Multiple to baseline, add acetylcholine and make trachea preshrinking 15 minutes, adding 3 μ L concentration is that 30 μm ol/L pyrazoles 3 are (non-selective
Cation channel blocker), adding Experimental agents to drug level after 15 minutes is 5.62mg/mL.
The pre-shrunk diastole effect that high potassium is induced by 2.7 compound recipe puppet fiber crops U.S. sweet smell sheets
By mice trachea by hook linking tonotransducer pilot system, it is placed in containing 37 DEG C of high calcium solutions of 6mL and holds
The constant temperature water bath of continuous logical oxygen.Preload is set to 300mg, within every 15 minutes, changes a high calcium solution, continuous four times.Balance
After 60 minutes, carry out pre-stimulation once with 100 μm ol/L acetylcholine, make tracheal muscle tension force reach more than 800mg, extensive after eluting
Multiple to baseline, add High potassium solution and make trachea preshrinking 15 minutes, then be that 5.62mg/mL compound recipe puppet fiber crops U.S. is fragrant with drug level
Act on mice trachea.
3. experimental result
3.1 variable concentrations compound recipe puppet fiber crops U.S.'s sweet smell sheet diastole pre-shrunk to acetylcholine effects
Mice trachea carries out pre-stimulation three times with 100 μm ol/L acetylcholine, makes tracheal muscle tension force reach more than 800mg,
Recovering after eluting to baseline, add acetylcholine and make trachea preshrinking 15 minutes, mice trachea tension force is 11mN, then controls
Treat medicaments compound puppet fiber crops U.S. sweet smell sheet, measure the diastolic rate of mice trachea under each concentration item.The results are shown in Table 1.
Table 1 variable concentrations compound recipe puppet fiber crops U.S.'s sweet smell sheet diastole pre-shrunk to acetylcholine exercising result
The tracheal smooth muscle pulling force of mice trachea tension force (mN)=pulling force (mg)/trachea weight (mg), i.e. Unit Weight；
Diastolic rate (%)=(add medicine forward pull and add medicine backward pull)/(add acetylcholine backward pull to add
Enter acetylcholine forward pull) × 100%.
As shown in Table 1, along with constantly increasing of compound recipe puppet fiber crops U.S.'s sweet smell sheet concentration, mice trachea tension force constantly declines,
In concentration dependent in the range of 0.01～5.62mg/mL drug level.
When compound recipe puppet fiber crops U.S. sweet smell sheet concentration is 5.62mg/mL, mice trachea tension force is down to minimum 1mN, even if by compound recipe
The U.S. fragrant sheet concentration of pseudo-fiber crops improves to 10mg/mL, and mice trachea tension force the most no longer declines.Compound recipe puppet fiber crops U.S. sweet smell sheet energy diastole mice gas
Pipe smooth muscle, releases bronchospasm, it is achieved effect for the treatment of asthma.
3.2 compound recipe puppet fiber crops U.S. sweet smell sheets nifedipine after preshrinking is blocked after diastole effect
Mice trachea carries out pre-stimulation three times with 100 μm ol/L acetylcholine, makes tracheal muscle tension force reach more than 800mg,
Recovering after eluting to baseline, add acetylcholine and make trachea preshrinking 15 minutes, mice trachea tension force is 12mN.Add 3 μ
L concentration is 10 μm ol/L blocker nifedipines, and the contraction that after adding nifedipine, acetylcholine causes is suppressed significantly, little
Mus trachea tension force drops to 5mN, and adding Experimental agents to drug level after 15 minutes is 5.62mg/mL, under mice trachea tension force
Drop to 2mN.
After nifedipine blocks L-type calcium channel, after 5.62mg/mL Experimental agents acts on mice trachea, trachea is opened
Power declines 3mN, with do not use in 3.1 that nifedipine blocks compared with concentration experiment medicine mice trachea tension force decline 10mN,
Nifedipine significantly inhibits the diastole effect to trachea of compound recipe puppet fiber crops U.S. sweet smell sheet, and this explanation compound recipe puppet fiber crops U.S. sweet smell sheet has blocking-up L-
The effect of type calcium channel.
3.3 compound recipe puppet fiber crops U.S. sweet smell sheets pyrazoles after preshrinking 3 is blocked after diastole effect
Mice trachea carries out pre-stimulation three times with 100 μm ol/L acetylcholine, makes tracheal muscle tension force reach more than 800mg,
Recovering after eluting to baseline, add acetylcholine and make trachea preshrinking 15 minutes, mice trachea tension force is 11mN.Add 3 μ
L concentration is the blocker pyrazoles 3 of 30 μm ol/L, and the contraction that after adding pyrazoles 3, acetylcholine causes is suppressed, and mice trachea is opened
Power drops to 9mN, and adding Experimental agents to drug level after 15 minutes is 5.62mg/mL, and mice trachea tension force drops to 1mN.
After pyrazoles 3 blocks non-selective cation channel, after 5.62mg/mL Experimental agents acts on mice trachea, trachea is opened
Power declines 8mN, with do not use in 3.1 that pyrazoles 3 blocks compared with concentration experiment medicine mice trachea tension force decline 10mN, pyrazoles
The diastole effect to trachea of the 3 suppression compound recipe puppet fiber crops U.S. sweet smell sheets, this explanation compound recipe puppet fiber crops U.S. sweet smell sheet have the non-selective sun of blocking-up from
The effect of subchannel.
The pre-shrunk diastole effect that high potassium is induced by 3.4 compound recipe puppet fiber crops U.S. sweet smell sheets
Mice trachea carries out pre-stimulation once with 100 μm ol/L acetylcholine, makes tracheal muscle tension force reach more than 800mg,
Recovering after eluting to baseline, add High potassium solution and make trachea preshrinking 15 minutes, mice trachea tension force is 11mN, adds experiment
Medicine to drug level is 5.62mg/mL, and mice trachea tension force drops to 3mN.
High potassium solution activates L-type calcium channel by depolarization, shrinks tracheal smooth muscle, and mice trachea tension force increases
To 11mN；When adding after Experimental agents, diastole bronchus smooth muscle, mice trachea tension force drops to 3mN, and compound recipe puppet fiber crops U.S. sweet smell be described
Sheet can suppress passage and then the diastole bronchus smooth muscle of L-type flow of calcium ions.
In sum, compound recipe puppet fiber crops U.S. sweet smell sheet has blocking-up L-type calcium channel and the effect of non-selective cation channel,
By two kinds of approach diastole mice tracheal smooth muscles, there is certain pharmacology advantage；Hydrochloric acid in compound recipe of the present invention puppet fiber crops U.S. sweet smell sheet
In clinical practice for many years, safety is high for pseudoephedrine, dextromethorphan hydrobromide and diphhydramine hydrochloride.
Claims (3)
1. the application in preparation treatment asthmatic medicament of compound recipe puppet fiber crops U.S. sweet smell sheet, consisting of of described compound recipe puppet fiber crops U.S.'s sweet smell sheet
Pseudoephedrine hydrochloride, dextromethorphan hydrobromide, diphhydramine hydrochloride, low-substituted hydroxypropyl cellulose, polyvinylpyrrolidone, hard
Fatty acid magnesium, dextrin.
The application in preparation treatment asthmatic medicament of compound recipe the most according to claim 1 puppet fiber crops U.S. sweet smell sheet, it is characterised in that
Every described compound recipe puppet fiber crops U.S. sweet smell sheet consist of pseudoephedrine hydrochloride 30mg, dextromethorphan hydrobromide 15mg, hydrochloric acid benzene sea are drawn
Bright 25mg, low-substituted hydroxypropyl cellulose 7.5mg, polyvinylpyrrolidone 4.5mg, magnesium stearate 3mg, dextrin 65mg.
The application in preparation treatment asthmatic medicament of compound recipe the most according to claim 1 puppet fiber crops U.S. sweet smell sheet, it is characterised in that
Described compound recipe puppet fiber crops U.S. sweet smell sheet preparation process is:
(1) pseudoephedrine hydrochloride, dextromethorphan hydrobromide, diphhydramine hydrochloride, low-substituted hydroxypropyl cellulose, polyvinyl pyrrole
Alkanone, magnesium stearate and dextrin are pulverized respectively, cross 40 mesh sieves；
(2) by pseudoephedrine hydrochloride, dextromethorphan hydrobromide, diphhydramine hydrochloride, low-substituted hydroxypropyl cellulose, polyethylene pyrrole
Pyrrolidone and dextrin mix homogeneously；
(3) described magnesium stearate is added in the mixture of step (2), mix homogeneously；
(4) mixture tabletting step (3) obtained, obtains compound recipe puppet fiber crops U.S. sweet smell sheet, and tableting pressure is 8～10kg/mm2。
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112617824A (en) * | 2020-12-09 | 2021-04-09 | 中南民族大学 | Ice drug addict detection method and system based on multichannel fNIRS signals |
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|---|---|---|---|---|
| CN1631358A (en) * | 2004-12-20 | 2005-06-29 | 李�杰 | Compound pseudoephedrine hydrochloric acid containing powder for treating cold, its prescription and preparation method |
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|---|---|---|---|---|
| CN1631358A (en) * | 2004-12-20 | 2005-06-29 | 李�杰 | Compound pseudoephedrine hydrochloric acid containing powder for treating cold, its prescription and preparation method |
| CN101180038A (en) * | 2005-03-23 | 2008-05-14 | 伊兰制药国际有限公司 | Nanoparticulate corticosteroid and antihistamine formulations |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| CN112617824A (en) * | 2020-12-09 | 2021-04-09 | 中南民族大学 | Ice drug addict detection method and system based on multichannel fNIRS signals |
| CN112617824B (en) * | 2020-12-09 | 2021-10-01 | 南京睿蜂健康医疗科技有限公司 | Ice drug addict detection system based on multichannel fNIRS signals |
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