CN1923177A - Chlorhydric acid tranditerol aerosol - Google Patents
Chlorhydric acid tranditerol aerosol Download PDFInfo
- Publication number
- CN1923177A CN1923177A CN 200610047837 CN200610047837A CN1923177A CN 1923177 A CN1923177 A CN 1923177A CN 200610047837 CN200610047837 CN 200610047837 CN 200610047837 A CN200610047837 A CN 200610047837A CN 1923177 A CN1923177 A CN 1923177A
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- CN
- China
- Prior art keywords
- tranditerol
- chlorhydric
- chlorhydric acid
- aerosol
- acid
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Abstract
The invention provides a Tranditerol Hydrochloride aerosol, which comprises (by weight ratio) Tranditerol Hydrochloride 0.005-0.01 part, double solvent 5-10 parts, and propellant 90-95 parts.
Description
Technical field
The present invention relates to a kind of chlorhydric acid tranditerol aerosol.
Background technology
Chlorhydric acid tranditerol is a kind of brand-new β
2Receptor agonist, its chemistry is by name: 2-(3-chloro-4-amino-5-trifluoromethyl)-2-tert-butylamine base ethylate hydrochlorate, and have the following chemical structure:
Molecular formula: C
13H
18ClF
3N
2O.HCl is characterized in: high selectivity, only acts on β at low toxicity
2Receptor, and to β
1Receptor does not have effect, and cardiac toxicity is low, consumption little (in microgram), and oral effective, long action time (6～12 hours), may command asthma at night.But oral medication, medicine act on the bronchus position needs the long period, and it is slow to prove effective, and also gastrointestinal tract is had side effect; And can only for the heavier patient of asthma at night, can not in time play therapeutical effect every administration in 6 hours.
Summary of the invention
The objective of the invention is to solve the problems referred to above that prior art exists, provide a kind of and can treat asthma, make medicine directly reach effect or absorption site, drug distribution is even, it is fast, easy to use to prove effective, and can avoid the chlorhydric acid tranditerol aerosol of gastrointestinal side effect.
This chlorhydric acid tranditerol aerosol is made up of for 90～95 parts 0.005～0.01 part of chlorhydric acid tranditerol, 5～10 parts of double solventss and propellant according to the parts by weight meter.
Above-mentioned chlorhydric acid tranditerol aerosol, described double solvents are a kind of in ethanol, sorbester p37, the oleic acid acetic acid or two kinds, and when solvent was two kinds of components, the weight ratio of two kinds of components was 1: 2～2: 1.
Above-mentioned chlorhydric acid tranditerol aerosol, described propellant is meant a kind of in isceon, dichlorodifluoromethane, the dichlorotetra-fluoroethane or two kinds or three kinds, and the weight ratio of isceon, dichlorodifluoromethane, dichlorotetra-fluoroethane is 1～2: 2～4: 1～2.
Through pharmacodynamics test, the chlorhydric acid tranditerol medical instrument has following effect:
1, chlorhydric acid tranditerol causes the protective effect that Cavia porcellus pants to medicine
Childhood Cavia porcellus (body weight 150～250g), male and female are all used.Experiment is drawn to breathe heavily experiment the previous day, selects to draw and breathes heavily incubation period less than 120 seconds Cavia porcellus.During experiment Cavia porcellus is divided into 9 groups at random, promptly solvent matched group, albuterol 1,3,9mg/kg group and chlorhydric acid tranditerol 0.0625,0.125,0.25,0.5,1.0mg/kg organize, and said medicine is all made solution.After the administration 1 hour, it was the spray tank of 4L that animal is placed volume, with 2ml.min
-1Flow velocity sprays into 5 seconds of mixed liquor of 2% acecoline and 0.1% histamine.Experimental result shows, chlorhydric acid tranditerol and albuterol all can make by acetylcholine and histamine mixed liquor spray thing and cause significant prolongation incubation period that Cavia porcellus pants, this effect and matched group relatively have statistical significance (P＜0.05,0.01 or 0.001), the ED of its anti-asthmatic action
50Be respectively 0.15 ± 0.04 and 4.95 ± 0.48mg/kg, illustrate that the bronchiectatic activity of chlorhydric acid tranditerol when oral is strong 33 times than albuterol.
2, the influence that the overflow of rabbit lung is changed
Rabbit is divided into 5 groups at random, press chlorhydric acid tranditerol 27,9,3 μ g/kg, albuterol 80 μ g/kg dosed administrations or give isometric normal saline, in this experiment, chlorhydric acid tranditerol (27,9,3 μ g/kg) and albuterol (160 μ g/kg) all begin onset in the 3min after administration.But the chlorhydric acid tranditerol high dose group is shunk the suppression ratio that remains at about 45% to the rabbit air flue in whole 4 hours experimentation, the air flue dilating effect is obvious, by comparison, the albuterol action intensity a little less than, and effect is basic behind 120min disappears, 60,90,180 and the suppression ratio at four time point places of 240min there were significant differences with the chlorhydric acid tranditerol high dose group, and 90min time point place suppression ratio with chlorhydric acid tranditerol in the dosage group there were significant differences.
3, to the influence of rabbit lung mechanical function
Rabbit, body weight 1.6～2kg, the male and female dual-purpose is divided into 5 groups at random, in each treated animal through gastric infusion, chlorhydric acid tranditerol 80,40,20 μ g/kg, albuterol 160 μ g/kg, 1h after the administration presses 2ml.min with a ultrasonic nebulizer by surge flask
-1Flow velocity makes animal suck the normal saline solution 30s of 0.3% histamine, the situation of change of lung compliance and airway resistance when measuring spraying back 0.5,1,2,3,4,5min.Experimental result shows, descending all appears in each experimental group animal lung compliance, airway resistance is then in rising trend, and chlorhydric acid tranditerol behind duodenal administration 1h and albuterol all can after histamine sprays thing, make above-mentioned two indexs be improved significantly, and relatively have statistical significance with matched group.
4, healthy human body toleration and pharmacokinetics clinical research
This The effects healthy volunteer on an empty stomach single oral 25 μ g, 50 μ g and 100 μ g chlorhydric acid tranditerol tablets, the pharmacokinetics of full abdomen single oral 50 μ g and repeatedly oral 50 μ g chlorhydric acid tranditerol tablets.
Blood plasma Chinese medicine concentration is lower behind 30 the oral river of experimenter Ding Teluo tablets, may be more relevant with river Ding Teluo lipotropy, and the prototype medicine is drained percentage rate 2.8 ± 3.0 in the 48h from urine, on average eliminates half-life t
1/2Be 17.9 ± 6.1h, mean residence time is 7.7 ± 2.3h.
Behind experimenter's empty stomach single oral 25 μ g, 50 μ g and the 100 μ g chlorhydric acid tranditerol tablets, C
MaxBe respectively 0.0122 ± 0.0042,0.0200 ± 0.0043 and 0.0486 ± 0.0143ng/ml, AUC
0-tBe respectively 0.0805 ± 0.0430,0.1167 ± 0.0575 and 0.2157 ± 0.0645hr.ng/ml, healthy volunteer's single dose is described, and oral 25 μ g, 50 μ g and 100 μ g chlorhydric acid tranditerol tablets have linear pharmacokinetic characteristics on an empty stomach.
Show behind experimenter empty stomach single oral 50 μ g and the full abdomen single oral 50 μ g chlorhydric acid tranditerol tablets, food can shorten the peak time of chlorhydric acid tranditerol, but it is little to the influence of blood peak concentration of drug, food can reduce the absorbtivity of human body to river Ding Teluo simultaneously, the average A UC of full abdomen single oral 50 μ g river Ding Teluo tablets
0-tBe empty stomach single oral 50 μ g chlorhydric acid tranditerol tablet average A UC
0-t56.6%.
The repeatedly oral 50 μ g chlorhydric acid tranditerol tablets of experimenter, the preceding blood drug level of taking medicine reached stable state in the 8th day.The repeatedly oral 50 μ g chlorhydric acid tranditerol tablets of experimenter do not have tangible cumulative action.
Results of pharmacodynamic test shows: chlorhydric acid tranditerol is the β of a high selectivity
2Receptor stimulating agent, this medicine is at exciting β
2Behind the receptor, significantly expand airway smooth muscle, stablize mastocyte, strengthen air flue ciliary movement tension force, thus the effect of performance asthma.Because the relation of structure, the action time of chlorhydric acid tranditerol is longer, also because of to β
2Receptor-selective is strong, so it is little to cause the probability of relevant side effect, is a kind of active drug for the treatment of asthma.And being made aerosol, chlorhydric acid tranditerol has the following advantages:
One, can make medicine directly reach effect (or absorption) position, drug distribution is even, and it is fast to prove effective.
Two, medicine is loaded in airtight, the opaque container, avoids and is difficult for directly contacting with airborne oxygen or water, and is difficult by microbial contamination, helps to improve medicine stability and safety.
Three, easy to use, can avoid gastrointestinal side effect.
Four, can accurately control dosage with quantitative valve.
The specific embodiment
Embodiment 1:
This chlorhydric acid tranditerol aerosol is made up of for 90～95 parts 0.005～0.01 part of chlorhydric acid tranditerol, 5～10 parts of double solventss and propellant in parts by weight, described double solvents is ethanol or sorbester p37 or oleic acid acetic acid or ethanol and span or ethanol and oleic acid acetic acid or sorbester p37 and oleic acid acetic acid, and when double solvents was two kinds of components, the weight ratio of two kinds of components was 1: 2～2: 1.
Described propellant is meant isceon (F
11) or dichlorodifluoromethane (F
12) or dichlorotetra-fluoroethane (F
114) or isceon (F
11) and dichlorodifluoromethane (F
12) or isceon (F
11) and dichlorotetra-fluoroethane (F
114) or dichlorodifluoromethane (F
12) and dichlorotetra-fluoroethane (F
114) or isceon (F
11), dichlorodifluoromethane (F
12) and dichlorotetra-fluoroethane (F
114), and the weight ratio of isceon, dichlorodifluoromethane, dichlorotetra-fluoroethane is 1～2: 2～4: 1～2.
Chlorhydric acid tranditerol is added above-mentioned double solvents, stir and to make the chlorhydric acid tranditerol dissolving, this medicinal liquid is packed in the aerosol container, the above-mentioned propellant of filling promptly gets chlorhydric acid tranditerol aerosol.
Embodiment 2
Get 0.5～1 milligram of chlorhydric acid tranditerol
Ethanol or sorbester p37 or oleic acid acetic acid 0.5～1 gram
Isceon (F
11) or dichlorodifluoromethane (F
12) or dichlorotetra-fluoroethane (F
114) 9～9.5 grams
Wherein ethanol or sorbester p37 or oleic acid acetic acid are double solvents, isceon (F
11) or dichlorodifluoromethane (F
12) or dichlorotetra-fluoroethane (F
114) be propellant.
Chlorhydric acid tranditerol is added above-mentioned double solvents, stir and to make the chlorhydric acid tranditerol dissolving, this medicinal liquid is packed in the aerosol container (10ml), the filling propellant promptly gets chlorhydric acid tranditerol aerosol.
Embodiment 3
Get 0.5～1 milligram of chlorhydric acid tranditerol
Ethanol or sorbester p37 or oleic acid acetic acid 0.5～1 gram
Isceon (F
11) and dichlorodifluoromethane (F
12) or dichlorotetra-fluoroethane (F
114) and dichlorodifluoromethane (F
12) 9～9.5 grams
Wherein ethanol or sorbester p37 or oleic acid acetic acid are double solvents, isceon (F
11) and dichlorodifluoromethane (F
12) or dichlorotetra-fluoroethane (F
114) and dichlorodifluoromethane (F
12) be propellant, and isceon (F
11) or dichlorotetra-fluoroethane (F
114) and dichlorodifluoromethane (F
12) weight ratio be 1～2: 2～4.
Chlorhydric acid tranditerol is added above-mentioned double solvents, stir and to make the chlorhydric acid tranditerol dissolving, this medicinal liquid is packed in the aerosol container (10ml), the filling propellant promptly gets chlorhydric acid tranditerol aerosol.
Embodiment 4:
Get 0.5～1 milligram of chlorhydric acid tranditerol
Ethanol or sorbester p37 or oleic acid acetic acid 0.5～1 gram
Isceon (F
11) and dichlorotetra-fluoroethane (F
114) 9～9.5 grams
Wherein ethanol or sorbester p37 or oleic acid acetic acid are double solvents, isceon (F
11) and dichlorotetra-fluoroethane (F
114) be propellant, and isceon (F
11) and dichlorotetra-fluoroethane (F
114) weight ratio be 1～2: 2～1.
Chlorhydric acid tranditerol is added above-mentioned double solvents, stir and to make the chlorhydric acid tranditerol dissolving, this medicinal liquid is packed in the aerosol container (10ml), the filling propellant promptly gets chlorhydric acid tranditerol aerosol.
Embodiment 5:
Get 0.5～1 milligram of chlorhydric acid tranditerol
Ethanol or sorbester p37 or oleic acid acetic acid 0.5～1 gram
Isceon (F
11), dichlorodifluoromethane (F
12) and dichlorotetra-fluoroethane (F
114) 9～9.5 grams
Wherein ethanol or sorbester p37 or oleic acid acetic acid are double solvents, isceon (F
11), dichlorodifluoromethane (F
12) and dichlorotetra-fluoroethane (F
114) be propellant, and isceon (F
11), dichlorodifluoromethane (F
12) and dichlorotetra-fluoroethane (F
114) weight ratio be 1～2: 2～4: 1～2.
Chlorhydric acid tranditerol is added above-mentioned double solvents, stir and to make the chlorhydric acid tranditerol dissolving, this medicinal liquid is packed in the aerosol container (10ml), the filling propellant promptly gets chlorhydric acid tranditerol aerosol.
Embodiment 6:
Get ethanol, sorbester p37 or ethanol, oleic acid acetic acid or sorbester p37, oleic acid acetic acid as double solvents, total amount is 0.5～1 gram, and the weight ratio of ethanol, sorbester p37 or ethanol, oleic acid acetic acid or sorbester p37, oleic acid acetic acid is 1: 2～2: 1, and other is with embodiment 2～embodiment 5.
Embodiment 7:
Get chlorhydric acid tranditerol 0.5mg, add ethanol 1g, stir and make the chlorhydric acid tranditerol dissolving, this medicinal liquid is packed in the aerosol container (10ml), filling propellant 9g promptly gets chlorhydric acid tranditerol aerosol.
Embodiment 8:
Chlorhydric acid tranditerol 1mg is dissolved in the 1.5g ethanol, in the aerosol container of packing into (18ml), filling propellant isceon (F
11) 4g and dichlorodifluoromethane (F
12) 10g, promptly get chlorhydric acid tranditerol aerosol.
Embodiment 9:
Get 1 milligram of chlorhydric acid tranditerol
Oleic acid acetic acid 0.5 gram
Sorbester p37 0.5 gram
Isceon (F
11) 2 grams
Dichlorodifluoromethane (F
12) 8 grams
Dichlorotetra-fluoroethane (F
114) 2 grams
Wherein oleic acid acetic acid and sorbester p37 are double solvents, isceon (F
11), dichlorodifluoromethane (F
12) and dichlorotetra-fluoroethane (F
114) be propellant.Chlorhydric acid tranditerol is added double solvents, stir and to make the chlorhydric acid tranditerol dissolving, this medicinal liquid is packed in the aerosol container (14ml), the filling propellant promptly gets chlorhydric acid tranditerol aerosol.
Concentration of alcohol among the foregoing description 1～embodiment 9 is 95～100%.
Claims (3)
1, a kind of chlorhydric acid tranditerol aerosol is characterized in that, is made up of for 90～95 parts 0.005～0.01 part of chlorhydric acid tranditerol, 5～10 parts of double solventss and propellant according to the parts by weight meter.
2, chlorhydric acid tranditerol aerosol according to claim 1 is characterized in that, described solvent is a kind of in ethanol, sorbester p37, the oleic acid acetic acid or two kinds, and when solvent was two kinds of components, the weight ratio of two kinds of components was 1: 2～2: 1.
3, chlorhydric acid tranditerol aerosol according to claim 1, it is characterized in that, described propellant is a kind of in isceon, dichlorodifluoromethane, the dichlorotetra-fluoroethane or two kinds or three kinds, and the weight ratio of isceon, dichlorodifluoromethane, dichlorotetra-fluoroethane is 1～2: 2～4: 1～2.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006100478377A CN100431535C (en) | 2006-09-18 | 2006-09-18 | Chlorhydric acid tranditerol aerosol |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2006100478377A CN100431535C (en) | 2006-09-18 | 2006-09-18 | Chlorhydric acid tranditerol aerosol |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1923177A true CN1923177A (en) | 2007-03-07 |
| CN100431535C CN100431535C (en) | 2008-11-12 |
Family
ID=37816121
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB2006100478377A Active CN100431535C (en) | 2006-09-18 | 2006-09-18 | Chlorhydric acid tranditerol aerosol |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN100431535C (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112451509A (en) * | 2020-12-19 | 2021-03-09 | 沈阳药科大学 | Chuangbuterol powder inhalation and preparation method thereof |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1118277C (en) * | 2000-07-06 | 2003-08-20 | 中国药科大学 | Medicinal aerosol for curing respiratory system disease |
| CN1276911C (en) * | 2001-09-30 | 2006-09-27 | 沈阳药科大学 | New phenyl ethyl amine compounds having beta 2-receptor excitation and its producing method |
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2006
- 2006-09-18 CN CNB2006100478377A patent/CN100431535C/en active Active
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112451509A (en) * | 2020-12-19 | 2021-03-09 | 沈阳药科大学 | Chuangbuterol powder inhalation and preparation method thereof |
| CN112451509B (en) * | 2020-12-19 | 2023-03-07 | 沈阳药科大学 | Chuangbuterol powder inhalation and preparation method thereof |
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| Publication number | Publication date |
|---|---|
| CN100431535C (en) | 2008-11-12 |
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