CN1448131A - Medicine composition containing alpha-pinene and 1,8-eucalyptol fever-tree oil and use thereof - Google Patents
Medicine composition containing alpha-pinene and 1,8-eucalyptol fever-tree oil and use thereof Download PDFInfo
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Abstract
The composite medicine of the present invention contains tasmanian bluegum oil with alpha-pinene and 1,8-cineole as main components, medicinal diluent and medicinal additives. It may be administrated in solid form, semi-solid form or liquid form, and its preparation may be taken orally, intravenous injected or locally administrated. It is used in treating diseases of respiratory system, such as upper respiratory tract infection, acute and chronic bronchitis, chronic obstructive pneumonia, pulmonary tuberculosis, pneumosilicosis, etc.
Description
Affiliated technical field
The present invention relates to the pharmaceutical composition of Eucalyptus Globulus oil, relate in particular to and contain australene and 1, the medical composition and its use of the Eucalyptus Globulus oil of 8-eucalyptol is preferred for the expelling phlegm for arresting cough treatment of respiratory tract disease.
Background technology
Eucalyptus Globulus oil is mainly as spice.Pharmacopeia
[1]Contained Oleum Eucalypti derives from myrtle Eucalyptus globulus Labill Eucalyptus globulus Labill. canella Camphor tree or above-mentioned two sections belong to the volatile oil that other plant obtains through vapor distillation together, regulation eucalyptol (C
10H
18O) content must not be less than 70.0%.The effect of wind-expelling pain-stopping is arranged, be used for skin pruritus, neuralgia.The food such as the throat smoothing candy that contain Oleum Eucalypti contain the Chinese patent medicine compound recipe of Oleum Eucalypti in addition.Patent (publication number CN 1298699A) " pharmaceutical composition that comprises Oleum Eucalypti and orange oil " is the pharmaceutical composition of Oleum Eucalypti and orange oil, is used for the treatment of the respiratory system disease that microorganism causes.Morice etc.
[2]Report, the menthol inhalation in the Oleum Eucalypti is inhibited by the cough that citric acid (citric acid) causes to the normal person.Do not see both at home and abroad from Eucalyptus Globulus oil, make contain australene and 1, the preparation that the compositions of 8-eucalyptol is made is used for the report of expelling phlegm for arresting cough medicine.
Summary of the invention
The purpose of this invention is to provide a kind of australene and 1 contained, the Eucalyptus Globulus oil pharmaceutical composition of 8-eucalyptol, be to take from myrtle Eucalyptus globulus Labill Eucalyptus globulus Labill., through vapor distillation, again through redistillation, the volatile oil that obtains, through fractional distillation, collect 60～80 ℃ of fractions, mainly contain australene and 1, the Eucalyptus Globulus oil of 8-eucalyptol.
Eucalyptus Globulus oil pharmaceutical composition provided by the invention mainly contains australene and 1 in its Eucalyptus Globulus oil, the 8-eucalyptol also contains medicinal diluent and medical additive.
Eucalyptus Globulus oil pharmaceutical composition provided by the invention contains australene 5～30%, 1 in the Eucalyptus Globulus oil, the 8-eucalyptol is 30～80%.
Used diluent comprises ethanol, surfactant, carbohydrate and/or vegetable oil in the Eucalyptus Globulus oil pharmaceutical composition provided by the invention.
Eucalyptus Globulus oil pharmaceutical composition provided by the invention, its Eucalyptus Globulus oil and diluent ratio are between 0.1: 10 to 10: 0.1.
Eucalyptus Globulus oil pharmaceutical composition provided by the invention can solid or semi-solid form administration, comprises soft capsule, soft gelatin capsule, enteric coated capsule and liquid gelatin hard capsule, preferred soft hard gelatin capsule form.All right liquid form administration comprises suspensoid or Emulsion.
The preparation of Eucalyptus Globulus oil pharmaceutical composition provided by the invention, but oral administration, intravenous, topical, the preferred oral administration.
The preparation of Eucalyptus Globulus oil pharmaceutical composition provided by the invention wherein contains Eucalyptus Globulus oil by weight 1～80%, preferred 2～60%.
Another object of the present invention is the purposes aspect the expelling phlegm for arresting cough of preparation when the cough of abundant expectoration such as respiratory tract disease such as acute upper respiratory tract infection, acute/chronic bronchitis, chronic obstructive pulmonary disease, pulmonary tuberculosis, pneumosilicosis of this pharmaceutical composition.
The present invention has the following advantages:
1. Eucalyptus Globulus oil is from containing that the myrtle Eucalyptus globulus Labill leaf extracts in the pharmaceutical composition of the present invention's extraction
Australene and 1, the Eucalyptus Globulus oil of 8-eucalyptol component.
2. Eucalyptus Globulus oil has expelling phlegm for arresting cough and antiinflammatory work through the pharmacodynamics proof in the pharmaceutical composition of the present invention's extraction
With;
3. pharmaceutical composition provided by the invention can be used for treating respiratory system disease such as acute upper respiratory tract sense
Dye, dispelling during abundant expectoration cough such as acute/chronic bronchitis, chronic obstructive pulmonary disease, pulmonary tuberculosis, pneumosilicosis
The treatment of the active chronic inflammation of phlegm and relieving cough treatment and respiratory system disease.
4. the pharmaceutical composition of the present invention's extraction has refrigerant sense as the expelling phlegm for arresting cough medicine after the use, feels comfortable;
5. the pharmaceutical composition toxicity extracted of the present invention is little, except that slight digestive tract reaction, does not have obviously that other is bad
Reaction.
The specific embodiment
The present invention will be described further in conjunction with specific embodiments, and these examples only are used for illustration purpose, and are not used in the restriction scope of the invention.
Embodiment 1 study of pharmacy
1. the process study steam distillation extracts volatile oil.Under normal pressure, fractional distillation, the Eucalyptus Globulus oil effective site (title Eucalyptus Globulus oil) of collecting 60～80 ℃ of fractions.Eucalyptus Globulus oil is colourless or little yellow oily liquid, and special fragrance is arranged, acrid in the mouth, cold.Relative density is 0.890～0.910, and index of refraction is 1.455～1.465.Adopt the GC method to measure, the content limit australene should be no less than 20.0%, cineole should be no less than 55.0%.Soft capsule preparation: the content limit australene should be no less than 12.0%, cineole should be no less than 28.0%.
2. chemical composition analysis
(1) the blue chemical composition analysis of pressing volatile oil
Adopt GC-MS to measure, mainly contain australene (α-pinene) 7.9～13.05%, p-p-Cymene (para-cymene), eucalyptol (1 through chemical composition analysis, 8-cineol) 41.5～46.85%, γ-terpinene (γ-terpinene), α-terpinenol (α-terpineol), globulol (globulol), white spirit layer alcohol (viriddiflorol), α, β, γ-eucalyptol (α, β, γ-eudesmol) etc., volatile oil has 48 peaks, and retention time is to 43min.
(2) Eucalyptus Globulus oil chemical composition analysis
Adopt GC-MS to detect, analysis result: main constituent has australene (α-pinene) 25～30%, p-p-Cymene (para-cymene), cineole (1,8-cineol) 66～70%, ((α-terpineol), globulol (globulol) etc. have 27 peaks to γ-terpinene, and chromatographic peak does not appear later in retention time 22.85min substantially for γ-terpinene), α-terpinenol.
Embodiment 2 pharmacodynamic studies:
1. Eucalyptus Globulus oil is to the influence of the phenol red excretion of airway of mice
Utilize phenol red mouse peritoneal injection rear section from the excretory characteristics of air flue, measure the phenol red excretion of airway of mice, be subjected to the influence of reagent, be subjected to the phlegm-dispelling functions of reagent with understanding air flue secretion liquid measure with judgement.
Method: mice, hunger is 16～18 hours before the experiment.Eucalyptus Globulus oil 30min before injection is phenol red irritates stomach, and lumbar injection 1% phenol red normal saline solution 0.2ml/10g injects back 30min and takes off neck execution then.Cut off skin of neck, separate trachea, insert trachea with thin plastic cement pipe, with 5% sodium bicarbonate 0.8ml, lavation bronchus gently three times amounts to 2.4ml.With wavelength 546nm colorimetric, compare with phenol red standard curve, calculate phenol red amount.
The result: Eucalyptus Globulus oil can increase the phenol red excretion of airway of mice.(seeing Table 1)
Table 1 Eucalyptus Globulus oil is to the influence of the phenol red excretion of airway of mice
The phenol red excretion μ of group n g/ml
Matched group 18 4.99 ± 0.98
Eucalyptus Globulus oil 300mg/kg 16 6.31 ± 1.98
+
100mg/kg 16 6.81±1.67
*
30mg/kg 17 6.58±1.92
*
10mg/kg 10 4.72±2.28
(with matched group comparison+p＜0.05, * p＜0.01 following table together)
Conclusion: Eucalyptus Globulus oil can increase the phenol red excretion of airway of mice and dilute sputum, plays phlegm-dispelling functions.
2. Eucalyptus Globulus oil is to the mucinous influence of Cavia porcellus air flue mucus
Tracheal mucus is mainly produced and secretion by cup cell and mucous gland cell, includes mucin, is made of mucopolysaccharide and protein.Measure mucinous content with of the influence of reflection Eucalyptus Globulus oil to air flue cup cell and mucous gland emiocytosis function.
Method: put to death Cavia porcellus, take out trachea and weigh, cut off trachea and get tracheal mucus with cotton rod, the mucus of taking-up washes with the 1.5ml distilled water, the centrifugal 15min of 3000rpm, and supernatant is stand-by.Measure mucinous content with the carbazole method.
The result: Eucalyptus Globulus oil can increase the mucinous content of Cavia porcellus air flue mucus, shows that Eucalyptus Globulus oil has facilitation to air flue cup cell and mucous gland emiocytosis.(seeing Table 2)
Table 2 Eucalyptus Globulus oil is to the mucinous influence of Cavia porcellus air flue mucus
Group n mucin content mg/ml matched group 10 1.69 ± 0.40 Eucalyptus Globulus oil 100mg/kg 7 2.43 ± 0.53
*
30mg/kg 8 2.51±1.23
Conclusion: Eucalyptus Globulus oil can promote air flue cup cell and mucous gland emiocytosis, shows that Eucalyptus Globulus oil has phlegm-dispelling functions.
3. Eucalyptus Globulus oil is to the influence of Columba livia tracheal cilia motion
Be covered with cilium from the tip bronchioles to top respiratory mucosa epithelium.Motion by cilium can make respiratory tract fluid, microgranule, expectorant etc. to the buccal direction motion, and this eliminating to respiratory tract foreign body plays an important role.Observe the influence of medicine, to understand the phlegm-dispelling functions of Eucalyptus Globulus oil to the motion of Columba livia tracheal cilia.
Method: Columba livia, body weight 250～350g, it is fixing not anaesthetize back of the body position, cuts along cervical midline, separates trachea, on trachea, carry out the labelling of 2cm, tracheostomize exposes tunica mucosa tracheae, stablize 10～15min after, granulated cork is put into the trachea that trachea 2cm entad holds, and the record granulated cork begins to walk the terminal required time to 2cm.Observe before the administration and the walking speed of 0.5h after the administration, write down the walking speed of 3～4 granulated corks at every turn, average.The drug port intracavitary administration.
The result: Eucalyptus Globulus oil can obviously speed Columba livia tracheal cilia movement velocity.(seeing Table 3)
Table 3. Eucalyptus Globulus oil is to the influence of Columba livia tracheal cilia motion
Ciliary movement speed (s/2cm)
Difference matched group (Tween 80) 8 158.2 ± 57.7 211.3 ± 102.7 53.5 ± 53.7 Eucalyptus Globulus oil 100mg/kg 8 161.6 ± 82.5 133.3 ± 48.7-28.4 ± 86.4 after the medication before the group n medication
+Eucalyptus Globulus oil 30mg/kg 8 170.9 ± 67.3 174.0 ± 80.1 3.2 ± 38.6
+Eucalyptus Globulus oil 10mg/kg 8 129.9 ± 27.5 146.8 ± 54.8 16.9 ± 53.4
Conclusion: Eucalyptus Globulus oil can speed Columba livia tracheal cilia movement velocity and promote foreign body to discharge, and shows that Eucalyptus Globulus oil has phlegm-dispelling functions.
4. Eucalyptus Globulus oil draws the influence of coughing test to mice ammonia
After mice sucks the zest chemical drugs, stimulate the respiratory tract sensor, reflexive causes cough.All medicines that can reduce breathing sensor sensitivity all have antitussive action.This laboratory observation Eucalyptus Globulus oil draws the antitussive action of coughing to mice ammonia.
Method: mice is put into bell jar, sucked ammonia 15 seconds, cough number of times in the record 2min with the ultrasound atomizer atomizing.
The result: Eucalyptus Globulus oil draws the cough number of times of coughing to mice ammonia the obvious suppression effect.(seeing Table 4)
Table 4 Eucalyptus Globulus oil to mice ammonia draw cough test influence group dosage cough number of times
(mg/kg) n (inferior/5min) contrast 25 11.2 ± 5.0 Eucalyptus Globulus oil 100mg/kg 26 6.1 ± 3.1
*
30mg/kg 25 8.9±4.6
10mg/kg 24 9.8 ± 6.1 codeine 30mg/kg 24 6.0 ± 2.7
*
The conclusion Eucalyptus Globulus oil draws the cough number of times of coughing to mice ammonia the obvious suppression effect, shows that Eucalyptus Globulus oil has antitussive effect.
5. Eucalyptus Globulus oil draws the influence of coughing test to the Cavia porcellus citric acid
With the citric acid soln spraying, stimulate Cavia porcellus respiratory mucosa sensor, reflexive causes cough.This laboratory observation Eucalyptus Globulus oil draws the antitussive action of coughing to the Cavia porcellus citric acid.
Method: Cavia porcellus is put into bell jar, suck 17.5% citric acid 1min, cough number of times in record 5min and the 10min with the ultrasound atomizer atomizing.
The result: Eucalyptus Globulus oil draws the cough number of times of coughing to the Cavia porcellus citric acid the obvious suppression effect.(seeing Table 5)
Table 5 Eucalyptus Globulus oil draws the influence of coughing test to the Cavia porcellus citric acid
Group dosage n cough number of times cough number of times
(mg/kg) (inferior/5min) (inferior/10min) contrast 14 14.93 ± 7.15 32.36 ± 13.64 Eucalyptus Globulus oil 100 15 10.80 ± 4.11 23.53 ± 5.96
+
30 16 10.19±5.11
+ 26.00±8.32
10 14 14.28 ± 4.70 30.07 ± 8.89 codeine 30 17 8.71 ± 6.05
+23.65 ± 12.44
Conclusion: Eucalyptus Globulus oil draws the cough number of times of coughing to the Cavia porcellus citric acid the obvious suppression effect, shows that Eucalyptus Globulus oil has antitussive effect.
6. Eucalyptus Globulus oil is to rat SO
2The influence of imbedibility chronic airway inflammation
Method: rat sucks SO in smoked case
2Gas (adds excessive concentrated sulphuric acid with the 5g sodium sulfite and reacts in retort, the SO of generation
2Mist feeds in the smoked case that volume is 45cm * 25cm * 10cm) 30min, 6d, totally 5 weeks weekly.Rat sucks SO
2Preceding 30min gastric infusion.In 5 weeks of modeling, after rat was put to death, lung was done pathological section usefulness on a bronchus crotch ligation left side, the capable bronchoalveolar lavage of right lung, bronchoalveolar lavage fluid after centrifugal, precipitation counting total cellular score and cell divide.
The result:
1. Eucalyptus Globulus oil is to rat SO
2Total cellular score and classification influences in the model control group bronchoalveolar lavage fluid (BALF) total white blood cells and neutrophilic granulocyte apparently higher than the normal control group among the BALF of imbedibility chronic airway inflammation, Eucalyptus Globulus oil medication group can obviously reduce total white blood cells and neutrophilic granulocyte number (seeing Table 6) among the BALF, shows that Eucalyptus Globulus oil is to SO
2The cell number of imbedibility chronic airway inflammation increases inhibitory action.
Table 6 Eucalyptus Globulus oil is to SO
2The influence of total white blood cells and classification among the BALF of imbedibility chronic airway inflammation
Group dosage total white blood cells macrophage % neutrophilic granulocyte % lymphocyte %
(mg/kg) 10
9/ L model control group 20.31 ± 8.27
#(9) 81.3 ± 6.3
#(10) 5.1 ± 2.6
#(10) 13.7 ± 4.6
#(10)
Eucalyptus Globulus oil 300 12.69 ± 3.88
+(8) 87.8 ± 5.8
+(8) 2.5 ± 2.3
+(8) 10.7 ± 6.9 (8)
Eucalyptus Globulus oil 100 17.61 ± 11.86 (8) 83.5 ± 12.0 (8) 1.9 ± 1.46 (8) 10.6 ± 1.8 (8)
Eucalyptus Globulus oil 30 19.19 ± 25.13 (5) 83.2 ± 7.0 (5) 3.8 ± 2.0 (5) 12.8 ± 4.8 (5) normal control groups 6.55 ± 3.63 (8) 90.1 ± 3.2 (8) 1.7 ± 1.5 (8) 8.1 ± 2.4 (8)
(with model control group comparison+p＜0.05 * p＜0.01; Compare #p＜0.05 with the normal control group; () number of animals; Following table together)
2. Eucalyptus Globulus oil is to rat SO
2The influence of imbedibility chronic airway inflammation pathological change
A. to rat SO
2The influence of the chronic bronchiolitis of imbedibility
The generation and the order of severity of model control group bronchiolitis, bronchiolitis cumulative number obviously increase than normal control group, and the generation of Eucalyptus Globulus oil medication group bronchiolitis, bronchiolitis cumulative number and the order of severity are than the obvious reduction of model control group (seeing Table 7).
Table 7 Eucalyptus Globulus oil is to rat SO
2The influence of the chronic bronchiolitis of imbedibility
The bronchiolitis bronchiolitis
Group n ++++++-u value cumulative number (%) model control group 10 4240 2.65
☆ ☆31.77 ± 12.30
#
Eucalyptus Globulus oil 300mg/kg 81061 1.98
*16.48 ± 14.83
*
Eucalyptus Globulus oil 100mg/kg 92034 1.97
*19.77 ± 25.95
Eucalyptus Globulus oil 30mg/kg 521200 16.36 ± 8.77
*Normal control group 80071 14.19 ± 7.04
(compare * p＜0.05 with model control group; Compare #p＜0.05.##p＜0.01 with the normal control group; The Ridit check
☆P＜0.05=1.96＜u＜2.58,
☆ ☆P＜0.01=u＞2.58; Following table together)
B. to rat SO
2The influence of the positive bronchioles number of imbedibility goblet cell
The positive bronchioles number of the goblet cell of model control group is apparently higher than the normal control group, and Eucalyptus Globulus oil 300mg/kg group can obviously reduce the positive bronchioles number (seeing Table 8) of goblet cell.
Table 8 Eucalyptus Globulus oil is to rat SO
2The influence of imbedibility chronic airway inflammation goblet cell
The goblet cell positive
Group n bronchioles number (%) model control group 10 15.23 ± 7.8
##Eucalyptus Globulus oil 300mg/kg 8 7.23 ± 3.96
*Eucalyptus Globulus oil 100mg/kg 9 10.65 ± 5.88 Eucalyptus Globulus oil 30mg/kg 5 18.37 ± 14.29
Normal control group 80 ± 0
Conclusion: SO
2The imbedibility chronic airway inflammation has typical cell number to increase and the inflammation pathological change, and Eucalyptus Globulus oil can obviously reduce total white blood cells and neutrophilic granulocyte number and the pathological change that improves airway inflammation among the BALF, shows that Eucalyptus Globulus oil has prevention SO
2Suck the formation and the effect of treatment chronic airway inflammation of wound model.
7. Eucalyptus Globulus oil is to the influence of the inductive airway inflammation of rat LPS
Method: the slight anesthetized rat of ether, insert aditus laryngis with otoscope, with the venous cannula pin, with breathing lipopolysaccharide (LPS) 0.2ml (200 μ g) that injects 1mg/ml when throat opens.Modeling Eucalyptus Globulus oil next day gastric infusion, 3 weeks of medication.3 weeks back execution rat, lung is done pathological section usefulness on a bronchus crotch ligation left side, the capable bronchoalveolar lavage of right lung, BALF is through centrifuged deposit counting cells sum and classification.
The result:
1. Eucalyptus Globulus oil is to the influence of total cellular score and classification among the BALF of the inductive airway inflammation of rat LPS
Total cellular score is apparently higher than the normal control group among the model control group BALF, and Eucalyptus Globulus oil medication group can obviously reduce total white blood cells among the BALF.Cell divide increases obviously with lymphocyte among the BALF, and Eucalyptus Globulus oil 300mg/kg group can make the lymphocyte cell number obviously reduce (seeing Table 9).Show that Eucalyptus Globulus oil has inhibitory action to total white blood cells and cell divide medium-sized lymphocyte rising among the inductive BALF of LPS.
What table 9 Eucalyptus Globulus oil was induced total cellular score and classification among the BALF of airway inflammation to LPS influences group mg/kg total white blood cells 10
9/ L macrophage % neutrophilic granulocyte % lymphocyte % model control group 34.38 ± 22.40
#(10) 78.2 ± 7.1
#(10) 6.5 ± 2.2
#(10) 15.6 ± 6.2
#(10)
Eucalyptus Globulus oil 300 18.13 ± 10.15
+(10) 86.4 ± 4.6
+(10) 4.5 ± 2.8 (10) 9.0 ± 4.1
+(10)
Eucalyptus Globulus oil 100 15.72 ± 7.62
+(10) 75.4 ± 5.7 (10) 6.4 ± 3.3 (10) 18.2 ± 6.6 (10)
Eucalyptus globulus Labill 30 14.44 ± 3.57
+(6) 74.0 ± 9.1 (9) 5.4 ± 6.5 (9) 20.6 ± 8.6 (9) normal control groups 6.79 ± 3.92 (9) 91.9 ± 3.1 (9) 0.9 ± 0.8 (9) 6.6 ± 3.4 (8)
2. Eucalyptus Globulus oil is respectively organized rat to the influence of the inductive airway inflammation pathological change of LPS all varying number, in various degree trachea, bronchus, bronchiolitis and interstitial pneumonia, inflammatory cell is many based on lymphocyte, and a small amount of plasma cell, neutrophilic granulocyte, acid granulocyte are arranged.Trachea, bronchus are not seen typical squamous metaplasia, also do not see pathological changes such as tangible papillary hyperplasia.Minority trachea, the visible columnar epithelium of bronchus come off.According to inflammation, exuviation degree inflammation is divided into " ,+, ++, +++" level Four, "-" promptly do not see obvious inflammatory cell infiltration, "+" a small amount of inflammatory cell infiltration, trachea structural integrity." +++" sees a large amount of inflammatory cell infiltrations, and can occur that tube wall destroys and (or) exuviation." ++ " boundary is between "+" and " +++".Bronchioles sum (whole tangent plane) in the counting lung, counting has the bronchioles number of inflammatory disorders simultaneously.Interstitial pneumonia by the degree of inflammatory cell infiltration around alveolar wall and the ductus arteriosus wall be divided into " ,+, ++, +++" level Four.
Pathological examination shows model control group and normal control group comparison trachea, bronchus, bronchiolar inflammation take place and the order of severity obviously increases and the bronchiolitis cumulative number also increases, trachea, bronchus, bronchiolar inflammation are taken place Eucalyptus Globulus oil and the order of severity has inhibitory action (to see Table 10,11), the bronchiolitis cumulative number obviously reduces (seeing Table 11), and the interstitial lung inflammation that LPS is caused also has inhibitory action (seeing Table 12).
Table 10 Eucalyptus Globulus oil is to inductive tracheitis of LPS and bronchitic influence
The tracheitis bronchitis
Group mg/kg n ++++++-the u value ++++++-u value model matched group 10 1810 3.58
☆ ☆3700 3.72
☆ ☆
Eucalyptus Globulus oil 300 10 424002341 1.84
Eucalyptus Globulus oil 100 10 2260 1.49 2332 1.84
Eucalyptus Globulus oil 30 10 00 10 0 3.87
##2170 2.38
#Normal control group 10 01270127
Table 11 Eucalyptus Globulus oil influences group bronchiolitis bronchiolitis cumulative number (%) to the inductive bronchiolitis of LPS
N ++++++-u value model matched group 10 7210 3.40
☆ ☆46.17 ± 15.57
##Eucalyptus Globulus oil 300mg/kg 10 0181 3.58
##19.93 ± 10.63
*Eucalyptus Globulus oil 100mg/kg 10 4141 1.67 34.13 ± 10.89
*Eucalyptus Globulus oil 30mg/kg 10 2260 2.44
#50.05 ± 28.69 normal control groups 10 1027 5.49 ± 9.57
Table 12 Eucalyptus Globulus oil is to the influence of the inductive interstitial lung inflammation of rat LPS
The scorching group N of interstitial lung ++++++-u value model matched group 10 5320 3.69
☆ ☆Eucalyptus Globulus oil 300mg/kg 10 1162 2.63
##Eucalyptus Globulus oil 100mg/kg 10 0640 2.03
#Eucalyptus Globulus oil 30mg/kg 10 2350 1.56 normal control groups 10 0037
Conclusion: splash in the LPS trachea and can cause that cell number increases and the inflammation pathological change among the BALF, Eucalyptus Globulus oil can reduce increasing of total white blood cells and cell divide medium-sized lymphocyte among the BALF, and the inflammation pathological change is had inhibitory action.Show that Eucalyptus Globulus oil can prevent the generation of the inductive airway inflammation of LPS and suppress the order of severity.
Embodiment 3 toxicological studies
Eucalyptus Globulus oil mice LD
50Be 1.716 ± 0.148g/kg, the 95% credible 1.5746～1.8707g/kg that is limited to.According to the classification of WHO acute toxicity, the oral LD of mice
50501～5000mg/kg belongs to low toxicity, and Eucalyptus Globulus oil belongs to low cytotoxic drug, and the people of low cytotoxic drug may lethal dose 250g.
Embodiment 4 preparations
Eucalyptus Globulus oil pharmaceutical composition provided by the invention contains australene, 1, and 8-eucalyptol, diluent and medical dressing wherein contain australene 5～30%, 1, and 8-eucalyptol 30～80% preferably contains australene and is not less than 20%, 1, and the 8-eucalyptol is not less than 55%.
Contain australene and 1, the Eucalyptus Globulus oil of 8-eucalyptol can be through intravenous, topical, but is preferred with the oral administration, is used for expelling phlegm for arresting cough.This medicine is preferably with soft hard gelatin capsule form, or with liquid or semi-solid form administration.With the soft capsule is example: with gelatin, glycerol, water is the capsule material, and ethyl hydroxybenzoate is an antiseptic.Eucalyptus Globulus oil is a volatile oil, and softgel shell is had transudation, therefore, adds diluent (refined plant oil), and the proportioning of Eucalyptus Globulus oil and refined plant oil can be 1: 5 to 5: 1, the optimum ratio Eucalyptus Globulus oil: refined plant oil is 3: 2, no transudation.Each capsule includes Eucalyptus Globulus oil 50～350mg, optimised quantity 300mg.Day dosing 10～30mg/kg body weight.
Eucalyptus Globulus oil can also be equipped with the mixture of ethanol, surfactant, carbohydrate or these materials, is prepared into suspensoid or Emulsion.Its amount that contains Eucalyptus Globulus oil is by weight 1～30%, and is best 2～3%, suspension, and every ml contains 30mg, each 10ml, day dosing 30ml.Emulsion, every 100ml contains 2g, intravenous injection 100ml, every day 1 time.
The partial reference document that the present invention relates to:
1. Pharmacopoeia of People's Republic of China version (an one) in 2000; P227
2.Morice?AH.et?al.Thorax，1994，49(10)：1024
Claims (9)
1. one kind contains australene and 1, and the Eucalyptus Globulus oil medical composition and its use of 8-eucalyptol is characterized in that: mainly contain australene and 1 in the Eucalyptus Globulus oil, the 8-eucalyptol also contains medicinal diluent and medical additive.
2. Eucalyptus Globulus oil pharmaceutical composition as claimed in claim 1 is characterized in that: contain australene 5～30%, 1 in the Eucalyptus Globulus oil, the 8-eucalyptol is 30～80%.
3. as claim 1 and 2 described Eucalyptus Globulus oil pharmaceutical compositions, it is characterized in that: used diluent comprises ethanol, surfactant, carbohydrate and/or vegetable oil.
4. as claim 1 and 3 described Eucalyptus Globulus oil pharmaceutical compositions, it is characterized in that: Eucalyptus Globulus oil and diluent ratio are between 0.1: 10 to 10: 0.1.
5. as claim 1 and 2 described Eucalyptus Globulus oil pharmaceutical compositions, it is characterized in that: pharmaceutical composition can be made into solid or semi-solid form administration, comprises soft capsule, soft gelatin capsule, enteric coated capsule and liquid gelatin hard capsule, preferred soft hard gelatin capsule form.
6. as claim 1 and 2 described Eucalyptus Globulus oil pharmaceutical compositions, it is characterized in that: pharmaceutical composition can be made into the liquid form administration, comprises suspensoid or Emulsion.
7. as claim 5 and 6 described Eucalyptus Globulus oil pharmaceutical compositions, it is characterized in that: but pharmaceutical composition oral administration, intravenous, topical, the preferred oral administration.
8. Eucalyptus Globulus oil pharmaceutical composition as claimed in claim 1 is characterized in that: the amount that contains Eucalyptus Globulus oil in the pharmaceutical composition is by weight 1～80%, and preferred 2～60%.
9. Eucalyptus Globulus oil pharmaceutical composition as claimed in claim 1 is characterized in that: the purposes of pharmaceutical composition aspect the expelling phlegm for arresting cough of respiratory tract disease.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03116764 CN1228048C (en) | 2003-04-28 | 2003-04-28 | Medicine composition containing alpha-pinene and 1,8-eucalyptol fever-tree oil and use thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 03116764 CN1228048C (en) | 2003-04-28 | 2003-04-28 | Medicine composition containing alpha-pinene and 1,8-eucalyptol fever-tree oil and use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1448131A true CN1448131A (en) | 2003-10-15 |
| CN1228048C CN1228048C (en) | 2005-11-23 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 03116764 Expired - Fee Related CN1228048C (en) | 2003-04-28 | 2003-04-28 | Medicine composition containing alpha-pinene and 1,8-eucalyptol fever-tree oil and use thereof |
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| Country | Link |
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| CN (1) | CN1228048C (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103156924A (en) * | 2013-04-01 | 2013-06-19 | 金华牧之家动物药业有限公司 | Chinese medicinal suppository for treating mammal endometritis and preparation method thereof |
| CN109464428A (en) * | 2018-12-29 | 2019-03-15 | 北京远大九和药业有限公司 | A kind of transdermal penetration patch and preparation method thereof containing terpenes |
| CN113368219A (en) * | 2021-06-28 | 2021-09-10 | 广东工业大学 | Application of Globullol |
| CN114601866A (en) * | 2020-12-08 | 2022-06-10 | 北京远大九和药业有限公司 | Composition for treating or preventing viral influenza and application thereof |
-
2003
- 2003-04-28 CN CN 03116764 patent/CN1228048C/en not_active Expired - Fee Related
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103156924A (en) * | 2013-04-01 | 2013-06-19 | 金华牧之家动物药业有限公司 | Chinese medicinal suppository for treating mammal endometritis and preparation method thereof |
| CN109464428A (en) * | 2018-12-29 | 2019-03-15 | 北京远大九和药业有限公司 | A kind of transdermal penetration patch and preparation method thereof containing terpenes |
| CN114601866A (en) * | 2020-12-08 | 2022-06-10 | 北京远大九和药业有限公司 | Composition for treating or preventing viral influenza and application thereof |
| CN113368219A (en) * | 2021-06-28 | 2021-09-10 | 广东工业大学 | Application of Globullol |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1228048C (en) | 2005-11-23 |
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Address after: Shenzhen City, Guangdong Province, 518040 Shennan Road No. 6009 Che Kung Temple Green Plaza building 37 layer Patentee after: Shenzhen Salubris Pharmaceuticals Co., Ltd. Address before: 1901 room 518040, exhibition center, 6007 Shennan Road, Shenzhen, Futian District Patentee before: Shenzhen Salubris Pharmaceuticals Co., Ltd. |
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