CN101129343A - Application of beta-caryophyllene alcohol in preparing medicament for codein and/or eliminating phlegm - Google Patents
Application of beta-caryophyllene alcohol in preparing medicament for codein and/or eliminating phlegm Download PDFInfo
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- CN101129343A CN101129343A CNA2007100255208A CN200710025520A CN101129343A CN 101129343 A CN101129343 A CN 101129343A CN A2007100255208 A CNA2007100255208 A CN A2007100255208A CN 200710025520 A CN200710025520 A CN 200710025520A CN 101129343 A CN101129343 A CN 101129343A
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- caryophyllenol
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Abstract
The invention belongs to the field of pharmacy and discloses the use of beta-caryophyllene alcohol in preparing medicaments for relieving cough and/or dispersing phlegm with evident effects and apparent amount-effect relationship.
Description
Technical field
The invention belongs to pharmaceutical field, relate to the application of β-caryophyllenol in preparation antitussive, expelling phlegm drugs.
Background technology
(β-carophyllenol) has another name called syringyl alcohol to β-caryophyllenol, be a kind of sesquiterpenoids alcohol, normally by plants essential oil, as the β-caryophyllene in Flos Caryophylli seed oil, oeum copaibae, Essential lavender oil, Oleum Folium Artemisiae Argyi and the Oleum Viticis Negundo after separate purifying, obtain by hydration reaction, also the back of the reaction earlier isolation technics of available optimization improves its purity and conversion ratio.
β-caryophyllenol has stronger physiologically active, and it has significant relexation to guinea pig tracheal smooth muscle, and the non-specific asthmatic guinea pigs due to acetylcholine-histamine is had remarkable antiasthmatic effect, can be used for treating asthma.But do not report β-caryophyllenol at present and have antitussive, expectorant effect.
Summary of the invention
The purpose of this invention is to provide the application of β-caryophyllenol in preparation antitussive and/or expelling phlegm drugs.
The inventor discovers that β-caryophyllenol has antitussive, expectorant effect, so propose the application of β-caryophyllenol in preparation antitussive and/or expelling phlegm drugs.
β-caryophyllenol can be prepared into appropriate dosage forms with the adjuvant that pharmaceutically allows, these preparations can be any one dosage forms that pharmaceutically allows, include but not limited to tablet, granule, pill, oral liquid, injection, membrane, capsule, liposome, spray etc., β-caryophyllenol can also be formed compound preparation with the medicine that its antitussive, phlegm-dispelling functions is not had antagonism.The consumption of β-caryophyllenol can be according to variations such as route of administration, patient age, body weight, body surface area, the disease type of being treated and the orders of severity, and its daily dose can be 80-2600mg, can use by one or many.
Beneficial effect of the present invention:
The present invention experiment shows that β-caryophyllenol has antitussive, phlegm-dispelling functions, and its antitussive, phlegm-dispelling functions is obvious and amount-result relation is clear and definite, can be used for preparing antitussive and/or expelling phlegm drugs, for the patient provides better choice.
Description of drawings
Fig. 1: β-caryophyllenol is to the influence of ammonia inducing mouse cough.Among the figure: * *: P<0.01, compare with matched group.
Fig. 2: β-caryophyllenol is to the phenol red excretory influence of airway of mice.Among the figure: * *: P<0.01, compare with matched group.
Fig. 3: β-caryophyllenol is to the influence of pigeon tracheal cilia motion.Among the figure: *: P<0.05; Compare with matched group *: P<0.01.
The specific embodiment
The invention will be further elaborated by the following examples.
General explanation:
Employed medicine, animal, instrument are in following examples:
One, medicine:
1, be subjected to the reagent thing: β-caryophyllenol, purity are provided by department of chemistry of Nanjing University more than 99%, and the purity that also can adopt market sale is at the β-caryophyllenol more than 99%.
2, other medicines and reagent:
2.1. codeine phosphate tablets: manufacturing enterprise: Industries, Inc of traditional Chinese medicines group Beijing Shunyi branch company, lot number: 061004, specification: the 30mg/ sheet, people's consumption: the 1/2-1 sheet/time, 1-3 sheet/day.
2.2. ammonia: manufacturing enterprise: Nanjing chemical reagent one factory, lot number: 060830476.
2.3. olive oil: manufacturing enterprise: Greece dust Lyme person of outstanding talent oil product company, standard code: Q/320623YK023-2005
2.4. ammonium chloride: manufacturing enterprise: Nanjing Chemistry Reagent Co., Ltd., lot number: 050610621.
2.5. it is phenol red: manufacturing enterprise: Chemical Reagent Co., Ltd., Sinopharm Group, lot number: F20070129.
Two, laboratory animal
1.ICR mice (cleaning level), body weight 18~22g, the male and female dual-purpose, Yangzhou University comparative medicine center provides licence: SCXK (Soviet Union) 2002-0009.
2. pigeon, body weight 300~350g, male and female are regardless of, Green Dragon mountain, Nanjing laboratory animal plant, licence: SCXK-2002 (Soviet Union)-0018.
Three, test instrument
1.T6 ultra-violet and visible spectrophotometer: the Beijing Puxi General Instrument Co., Ltd produces;
2.WM-2 type oil-free gas compressor: Bengbu medical college second instrument plant;
3. glass gas atomization pipe: instrument plant of Huaxi Medical Univ;
4.80-2 table-type low-speed centrifuge: Shanghai Medical Appliance (Group) Co., Ltd. Surgical Instruments Factory.
Effect embodiment 1: antitussive effect is tested the influence of a pair of ammonia inducing mouse cough
Experimental technique:
Press literature method
[1], get 60 of Kunming mouses, body weight 18~22g, male and female half and half are divided into 5 groups at random by body weight, 12 every group.β-caryophyllenol establishes 15.0,30.0, three dosage groups of 60.0mg/kg, grinds dissolving with olive oil.The positive matched group of codeine phosphate, dosage 4.0mg/kg grinds suspendible with 0.5%CMC-Na.Negative group waits capacity olive oil (10ml/kg).Above-mentioned respectively organize gastric infusion 1h after, draw ammonia (concentration 25%~28%) 0.2ml with the 1ml syringe, heavy cotton balls such as inject, with white mice together rapidly back-off in the 500ml beaker, write down in 3 minutes the animal number of times of coughing.Obviously be reduced to the antitussive effect index with the cough number of times.
Experimental result:
The results are shown in Table 1, Fig. 1.Result of the test shows, compare with matched group, β-caryophyllenol height (60.0mg/kg), in (30.0mg/kg) dosage group all can significantly suppress the cough number of times (P<0.01) of ammonia inducing mouse, low dose group (15.0mg/kg) also can reduce the cough number of times but with matched group no significant difference (P>0.05) relatively.
Be tangible linear relationship, regression equation between administration log10 dose and cough number of times: y=-21.927Logx+52.186 (r=0.9996) shows that dose-effect relationship is good.Administration log10 dose and cough also are tangible linear relationship, regression equation between suppression ratio: y=63.953Logx-52.193 (r=0.9997) can be regarded as to such an extent that suppression ratio reaches 50% dosage and is: 39.6 mg/kg.
Group | Dosage (mg/kg) | Number of animals | The cough number of times | Cough suppression ratio (%) |
Contrast | 12 | 34.3±14.8 | ||
Codeine phosphate | 4.0 | 12 | 11.2±4.8 ** | 67.3 |
β-caryophyllenol | 15.0 30.0 60.0 | 12 12 12 | 26.3±8.3 20.0±6.6 ** 13.1±7.7 ** | 23.3 41.7 61.8 |
*: P<0.01, compare with matched group
Cough suppression ratio (%)=(matched group cough number of times-administration group cough number of times) * 100% ÷ matched group cough number of times brief summary:
The antitussive effect result of the test of ammonia inducing mouse cough shows that β-caryophyllenol has tangible antitussive effect, can obviously reduce the cough number of times that ammonia causes mice, and amount-result relation is obvious, makes the dosage of cough number of times minimizing 50% be: 39.6mg/kg.
Effect embodiment 2: the phlegm-dispelling functions test
Experimental technique:
1. to the phenol red excretory influence of airway of mice
Press literature method
[2], get 60 of body weight 18~22g male mices, be divided into 5 groups at random, 12 every group, β-caryophyllenol establishes 15,30, three dosage groups of 60mg/kg, dissolves with olive oil respectively.Ammonium chloride is as positive control drug, dosage 50mg/kg.Negative group waits the olive oil of capacity.Behind each group difference gastric infusion 1h, the phenol red solution 0.5ml of lumbar injection 5% takes off cervical vertebra and puts to death behind the 30min, cut off skin of neck, separate trachea, take from the trachea section of thyroid cartilage place to the trachea crotch, it is soaked in 5% sodium bicarbonate solution, and fully vibration shakes up filtration.Measure absorbance (OD value) with T6 spectrophotometer 546nm place, the OD value is converted into phenol red content, and (regression equation: y (absorbance)=0.183x (phenol red content)-0.0036 r=0.9997), organizes result and negative control with each.Phlegm-dispelling functions is judged in increase with phenol red output.
2. the influence that the pigeon tracheal cilia is moved
Press literature method
[3], 24 of the pigeons of getting body weight 300~350g are divided into 5 groups at random, and 8 every group, the male and female dual-purpose.β-caryophyllenol establishes 12.5,25, three dosage groups of 50mg/kg, dissolves with olive oil respectively.Ammonium chloride is as positive control drug, dosage 50mg/kg.Negative group waits the olive oil of capacity.Behind the 1h, the Columba livia cervical region is pulled into the level position behind the gastric infusion, routine is separated trachea, injects Chinese prepared Chinese ink 0.02ml down by the proximal part inner surface of trachea, observes the distance (cm) of moving forward in the prepared Chinese ink 1min.Phlegm-dispelling functions is judged in increase with prepared Chinese ink displacement.
Result of the test:
1. to the phenol red excretory influence of airway of mice
The results are shown in Table 2, Fig. 2.Result of the test show and matched group relatively, β-caryophyllenol height (60.0mg/kg), in (30.0mg/kg), low (15.0mg/kg) dosage group all can significantly increase the phenol red drainage dawn of airway of mice (P<0.01).
Be tangible linear relationship, regression equation between administration log10 dose and phenol red air flue excretion: y=2.4419Logx-2.0066 (r=0.9966) shows that dose-effect relationship is good.Also be tangible linear relationship, regression equation between the phenol red drainage increment rate of administration log10 dose and air flue: y=740.03Logx-708.16 (r=0.9966) can be regarded as to such an extent that make the dosage of 1 times of the phenol red excretion increase of air flue be: 12.4mg/kg.
Table 2. β-caryophyllenol is to the phenol red excretory influence of airway of mice
Group | Dosage (mg/kg) | Number of animals | Air flue phenol red concentration (ug/ml) | Drain increment rate (%) |
Contrast | 12 | 0.33±0.17 | ||
Ammonia chloride | 50.0 | 12 | 3.08±1.24 ** | 833.3 |
β-caryophyllenol | 15.0 30.0 60.0 | 12 12 12 | 0.83±0.26 ** 1.67±0.55 ** 2.30±0.87 ** | 151.5 406.1 597.0 |
*: P<0.01, compare with matched group
Drain increment rate (%)=(administration group air flue phenol red concentration-matched group air flue phenol red concentration) * 100% ÷ matched group air flue phenol red concentration
2. the influence that the pigeon tracheal cilia is moved
The results are shown in Table 3, Fig. 3.Result of the test shows, compare with matched group, β-caryophyllenol height (50.0mg/kg), in (25.0mg/kg) dosage group all can significantly increase the move distance (P<0.01) of prepared Chinese ink in the pigeon air flue in 1 minute, show that ciliary movement speeds up, β-caryophyllenol has tangible phlegm-dispelling functions.
Be the better linearity relation between administration log10 dose and move distance, regression equation: y=0.7973Logx+0.0586 (r=0.9861), showing has dose-effect relationship.Also be the better linearity relation between administration log10 dose and move distance increment rate, regression equation: y=86.711Logx-93.689 (r=0.9861) can be regarded as to such an extent that make the dosage of move distance increase by 50% (showing that ciliary movement speed increases by 50%) be: 45.4mg/kg.
Table 3. β-caryophyllenol is to the influence of pigeon tracheal cilia motion
Group | Dosage (mg/kg) | Number of animals | Prepared Chinese ink move distance (cm/min) in the trachea | Move distance increment rate (%) |
Contrast | 8 | 0.92±0.12 | ||
Ammonia chloride | 50 | 8 | 1.42±0.22 ** | 54.3 |
β-caryophyllenol | 12.5 25.0 50.0 | 8 8 8 | 0.91±0.13 1.22±0.21 * 1.39±0.18 ** | -1.1 32.6 51.1 |
*: P<0.05;
*: P<0.01, compare with matched group
Move distance increment rate (%)=(administration group prepared Chinese ink move distance-matched group prepared Chinese ink move distance) * 100% ÷ matched group prepared Chinese ink move distance
Brief summary:
Airway of mice phenol red excretion test and pigeon tracheal cilia exercise test result show that all β-caryophyllenol has tangible phlegm-dispelling functions, can obviously increase phenol red excretion of airway of mice and quickening pigeon tracheal cilia movement velocity.Wherein, amount-result relation is obvious in the airway of mice phenol red excretion test, and the dosage that makes the phenol red excretion of air flue increase by 1 times is: 12.4mg/kg; Certain amount-effect dependency is also arranged in the pigeon tracheal cilia exercise test, make the dosage of ciliary movement speed increase by 50% in the trachea be: 45.4mg/kg.
List of references:
[1]. the Qi Chen chief editor. herbal pharmacology research methodology [M], People's Health Publisher, 1993:1639~6411.
[2]. the Qi Chen chief editor. herbal pharmacology research methodology [M], People's Health Publisher, 1994:1149~1521.
[3]. with [2].
Get β-caryophyllenol 10g, add the suitable adjuvant of oral liquid, become oral liquid by the oral liquid prepared.
Get β-caryophyllenol 10g, add the suitable adjuvant of capsule, become capsule by the capsule prepared.
Get β-caryophyllenol 10g, add the suitable adjuvant of tablet, become tablet by the tablet prepared.
Preparation embodiment
Get β-caryophyllenol 10g, add the suitable adjuvant of spray, become spray by the spray prepared.
Claims (1)
1. the application of β-caryophyllenol in preparation antitussive and/or expelling phlegm drugs.
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CNA2007100255208A CN101129343A (en) | 2007-08-02 | 2007-08-02 | Application of beta-caryophyllene alcohol in preparing medicament for codein and/or eliminating phlegm |
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CNA2007100255208A CN101129343A (en) | 2007-08-02 | 2007-08-02 | Application of beta-caryophyllene alcohol in preparing medicament for codein and/or eliminating phlegm |
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Open date: 20080227 |