CN103417563A - Application of aurantiamarin to preparation of medicine for treating acute and chronic bronchitis - Google Patents
Application of aurantiamarin to preparation of medicine for treating acute and chronic bronchitis Download PDFInfo
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- CN103417563A CN103417563A CN2013103447099A CN201310344709A CN103417563A CN 103417563 A CN103417563 A CN 103417563A CN 2013103447099 A CN2013103447099 A CN 2013103447099A CN 201310344709 A CN201310344709 A CN 201310344709A CN 103417563 A CN103417563 A CN 103417563A
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Abstract
The invention discloses application of aurantiamarin to preparation of a medicine for treating acute and chronic bronchitis. The aurantiamarin has a good cough-relieving effect and not toxic or side effect and can treat acute and chronic bronchitis well. The aurantiamarin-containing medicine for treating acute and chronic bronchitis has a good cough-relieving and phlegm-reducing effect, can effectively treat diseases and symptoms such as acute and chronic bronchitis and cough accompanied by excessive phlegm, and has the characteristics of stable quality, low dose and the like.
Description
Technical field
The present invention relates to the application of natural product, particularly relate to the application of Hesperidin in the acute and chronic bronchitis medicine of preparation treatment.
Background technology
Bronchitis refers to the chronic nonspecific inflammation of trachea, bronchial mucosa and surrounding tissue thereof, is a kind of common respiratory system disease.Clinical manifestation is chronic bronchitis and acute bronchitis.The bronchitis Etiological has formed bronchial chronic nonspecific inflammation for the repeated infection of virus and antibacterial.When there's a sudden fall in temperature, under respiratory tract small blood vessel spasm ischemia, defense function, degradation can cause a disease; The chronic stimulations such as smog dust, atmosphere pollution also can be fallen ill; Also can cause bronchitis to allergy such as pollen.
For treat acute and chronic bronchitis with Chinese medicine, people have carried out more effort, such as cough-relieving tablets etc., now come into the market.Such medicine gone on the market at present has the many and inconvenient shortcoming of dosage.Therefore be necessary to continue to develop and take safety, curative effect and treat reliably acute and chronic bronchitic novel drugs.
Hesperidin (Hesperidins:Vitamin P), be a kind of flavonoid material extensively be present in citrus fruit, and its chemical structural formula is:
It has flavanone oxygen glycosides structure, is faintly acid, and extracting the crude product obtained is pale yellow powder.Sterling is white needle-like crystals, slightly bitter, is insoluble in water, be dissolved in hardly acetone, benzene, chloroform, be slightly soluble in methanol, hot glacial acetic acid, dissolve in Methanamide, diformamide, be soluble in dilute alkaline soln, the Hesperidin melting range that purity is 97% is 257～260 ℃, and molecular weight is 610.6.Hesperidin has the osmotic pressure of maintaining, and strengthens blood capillary toughness, shortens the bleeding time, reduce the effects such as cholesterol, for the auxiliary treatment of cardiovascular system diseases, can prepare the multiple medicine that prevents arteriosclerosis and myocardial infarction clinically, be one of primary raw material of patent medicine " beniol ".Hesperidin, as a kind of flavone compound extensively be present in rue fruit, can be used as the Natural antioxidant in food industry, also can be used for cosmetic industry etc.But, still do not report that Hesperidin has the application for the treatment of acute/chronic bronchitis aspect.
Summary of the invention
Based on this, the invention provides the application of Hesperidin in the acute and chronic bronchitis medicine of preparation treatment.
The present invention also provides a kind of acute and chronic bronchitic medicine for the treatment of, and described medicine is comprised of the Hesperidin as active component and pharmaceutically acceptable adjuvant, and the percentage by weight of described Hesperidin is 0.1-99.5%.The acute and chronic bronchitic medicine of above-mentioned treatment can be selected the conventional adjuvant of corresponding dosage form, and as the carrier of Hesperidin, excipient or medium, be prepared into the pharmaceutical preparation of required different dosage form.The adjuvant added can be solid, semisolid or liquid.
Therein in embodiment, the percentage by weight 30-70% of described Hesperidin.
Therein in embodiment, the percentage by weight 50-70% of described Hesperidin.
In embodiment, the dosage form of described medicine is capsule, tablet, powder, medicated wine, suspensoid, Emulsion, syrup, aerosol or injection therein.
In embodiment, described medicine is in 0.1-500mg Hesperidin/kg body weight/day to the treatment acute/chronic bronchitis therein, and cough with copious phlegm has good curative effect.
In embodiment, the daily dose of described medicine is 1-100mg Hesperidin/kg body weight therein.
Hesperidin has good cough suppressing effect, have no toxic and side effects, can well treat acute/chronic bronchitis, contain acute and chronic bronchitic medicine of being used for the treatment of of Hesperidin, effect with good relieving cough and resolving phlegm, can effectively treat the diseases such as acute/chronic bronchitis, cough with copious phlegm, and there are the characteristics such as steady quality, dose be little.
The specific embodiment
Below in conjunction with specific embodiment, the present invention is further elaborated.
The dextromethorphan hydrobromide tablets of using in embodiment is produced by Guangzhou Guanghua Pharmaceutical Co., Ltd, lot number: T24006.
The Hesperidin of using in following examples (purity is more than 95%) refers to from the various medical materials containing Hesperidin, extract Hesperidin crude product or the Hesperidin monomer obtained in various medical materials such as Fructus Aurantii Immaturus, Fructus Aurantii, orange, Hesperidin both can be synthetic by conventional chemical method prepare, the approach that also can extract by conventional plant obtains, or can buy and obtain.
The extraction of embodiment 1 Hesperidin
According to prior art, according to the conventional extracting method of Hesperidin, can be extracted in such a way:
By pulverizing medicinal materials, process water or alcohol extraction 1-4 time, filter merging filtrate;
Filtrate is condensed into extractum, and extractum is upper prop or the direct upper prop of extractum after precipitate with ethanol, carries out the post separation, the organic solvent eluting;
Eluent volatilizees after dry solvent, obtains the Hesperidin crude product, through recrystallization repeatedly, obtains Hesperidin monomer (sterling).
The Hesperidin monomer extracted is through nuclear magnetic resonance chemical analyser (Switzerland Bruker company, VANCE AV400MHz) and mass spectrograph (Agilent1200/MSD) evaluation, and what obtain is the Hesperidin monomer
The cough-relieving pharmacological experiment of embodiment 2 Hesperidins
1, test animal used: the NIH mice, male and female half and half, clean grade standard, totally 45, by the sequence of body weight size, select the healthy mice of body weight 18～22g, be divided at random three groups, 15 every group.
2, establish negative control group, positive controls and Hesperidin sample sets.
3, sample source and preparation
(1), Hesperidin sample sets: get Hesperidin monomer (purity is more than 95%) appropriate, with the normal saline standardize solution, in volumetric flask, the concentration of preparation Hesperidin is 2.0mg/mL.
(2), positive controls is dextromethorphan hydrobromide: Nycoff, the content of dromethan is the 15mg/ sheet.Get 2 and be dissolved in 20 ml physiological salines, make suspension, concentration is 3mg/mL, and dosage is the 30mg/kg body weight.
(3), negative control group is normal saline: sodium chloride injection, the mass percent of sodium chloride is 0.9%.
4, experimental technique
Adopt the strong aqua ammonia nebulization, mouse stomach, after 1 hour, is started to accept the strong aqua ammonia spraying.Spray 30 seconds, spraying finishes, and takes out immediately mice, observes and has or not the cough reaction.Observe the cough number of times of mice in a minute, if occur typical case's cough action (abdominal muscle shrinks or the contracting breast, magnifies mouth, sometimes can cough sound) person more than 3 times in 1 minute simultaneously, count " cough ", otherwise count " without cough ".
5, experimentation
Obtain with sequential method (upper purgation) spray time (EDT that causes the half mouse cough
50).Calculate the R value, if the R value is greater than 130%, illustrate that medicine has antitussive action.If the R value is greater than 150%, show to have significant antitussive action.Computing formula is as follows:
EDT
50=log
-1C/n, in formula, n is number of animals, the summation that c is r value and x value, the number of animals that r is every dosage group, the logarithm that x is dosage (being spray time).The computing formula of R is:
By statistics, each sample sets half Cough length and cough suppressing effect are in Table 1.
Table 1 each sample sets half Cough length and cough suppressing effect
As known from Table 1, the Hesperidin oral administration, to stimulating mice to cause the tolerance time of cough, compares with negative control group, and significant prolongation is arranged, and there were significant differences statistically; With positive controls, compare, tolerance time extends, and dose is little, and curative effect is remarkable than dextromethorphan hydrobromide.Therefore, Hesperidin has good therapeutic effect to acute and chronic bronchitis, and cough suppressing effect is good.
The toxicological experiment of embodiment 3 Hesperidins
Be 24 ℃ in temperature, under the condition that humidity is 60 ± 5%, choose 30 of healthy clean level NIH mices, male and female half and half, body weight is at 18-22g.By feedstuff and water sterilization, before test and in the observation period of test, all by normal feedstuff condition, raise.
Hesperidin is dissolved in 0.5wt% sorbitan monooleate polyoxyethylene ether (Tween80), and concentration is 900mg/mL, and by this liquid oral administration mice, dosage is the 0.2mL/20g Mouse Weight.Observe Isosorbide-5-Nitrae after administration, 8,12 hours, within later every 12 hours, observe once.Observe the dead mouse situation, record Mouse Weight variation and other symptom every day.The 10th day, disconnected neck was put to death mice, gets each organ and carries out pathologic finding.
At the 10th day, whole mouse survivals, the Hesperidin that mice takes 900mg/kg dosage has no toxic reaction.Each organ pathologic finding of mice is normal, does not find pathological changes, and in 10 days, Mouse Weight has no and alleviates.Therefore, illustrate that Hesperidin has no toxicity when the oral administration animal.
Above-mentioned experimental results show that, Hesperidin not only has the acute and chronic bronchitis of good treatment, the curative effect of cough with copious phlegm, and almost do not show toxicity in mouse animal experiment, when the Hesperidin oral administration animal of 900mg/kg dosage, animal also has no toxic reaction.
4 one kinds of capsules for the treatment of acute and chronic bronchitis medicine of embodiment
A kind of capsule that is used for the treatment of acute and chronic bronchitis medicine, active component is Hesperidin, comprises following component:
Hesperidin 100g (66.7%)
Dry starch 40g (26.7%)
Micropowder silica gel 10g (6.6%)
The capsule of the acute and chronic bronchitis medicine of above-mentioned treatment, its preparation method is:
Dry starch, micropowder silica gel are mixed homogeneously with Hesperidin, in the transparent capsule of packing into, obtain being used for the treatment of the capsule of acute and chronic bronchitis medicine.Loading amount is: the 150mg/ capsule.
5 one kinds of tablets for the treatment of acute and chronic bronchitis medicine of embodiment
A kind of tablet that is used for the treatment of acute and chronic bronchitis medicine, active component is Hesperidin, comprises following component:
The tablet of the acute and chronic bronchitis medicine of above-mentioned treatment, its preparation method is:
Hesperidin is evenly mixed with starch, add starch slurry continuation stirring and make into soft material, granulate by 10 order nylon mesh, 80-90 ℃ of aeration-drying, dry granular adds magnesium stearate, through 12 mesh sieve granulate, mixes, and is pressed into tablet.Be total to obtain 5000, every sheet heavily is about 0.3g.
6 one kinds of capsules for the treatment of acute and chronic bronchitis medicine of embodiment
A kind of powder that is used for the treatment of acute and chronic bronchitis medicine, active component is Hesperidin, comprises following component:
Hesperidin 45g (30%)
Dry starch 70g (46.7%)
Micropowder silica gel 35g (23.3%)
The capsule of the acute and chronic bronchitis medicine of above-mentioned treatment, its preparation method is:
Dry starch, micropowder silica gel are mixed homogeneously with Hesperidin, in the transparent capsule of packing into, obtain being used for the treatment of the capsule of acute and chronic bronchitis medicine.Loading amount is: the 150mg/ capsule.
7 one kinds of capsules for the treatment of acute and chronic bronchitis medicine of embodiment
A kind of powder that is used for the treatment of acute and chronic bronchitis medicine, active component is Hesperidin, comprises following component:
Hesperidin 105g (70%)
Dry starch 30g (20%)
Micropowder silica gel 15g (10%)
The capsule of the acute and chronic bronchitis medicine of above-mentioned treatment, its preparation method is:
Dry starch, micropowder silica gel are mixed homogeneously with Hesperidin, in the transparent capsule of packing into, obtain being used for the treatment of the capsule of acute and chronic bronchitis medicine.Loading amount is: the 150mg/ capsule.
The above embodiment has only expressed several embodiment of the present invention, and it describes comparatively concrete and detailed, but can not therefore be interpreted as the restriction to the scope of the claims of the present invention.It should be pointed out that for the person of ordinary skill of the art, without departing from the inventive concept of the premise, can also make some distortion and improvement, these all belong to protection scope of the present invention.Therefore, the protection domain of patent of the present invention should be as the criterion with claims.
Claims (5)
1. the application of Hesperidin in the acute and chronic bronchitis medicine of preparation treatment.
2. the acute and chronic bronchitic medicine for the treatment of, is characterized in that, described medicine is comprised of the Hesperidin as active component and pharmaceutically acceptable adjuvant, and the percentage by weight of described Hesperidin is 0.1-99.5%.
3. the acute and chronic bronchitic medicine for the treatment of according to claim 2, is characterized in that, the percentage by weight 30-70% of described Hesperidin.
4. the acute and chronic bronchitic medicine for the treatment of according to claim 3, is characterized in that, the percentage by weight 50-70% of described Hesperidin.
5. according to the acute and chronic bronchitic medicine of the described treatment of claim 2-4 any one, it is characterized in that, the dosage form of described medicine is capsule, tablet, powder, medicated wine, suspensoid, Emulsion, syrup, aerosol or injection.
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107569504A (en) * | 2016-07-04 | 2018-01-12 | 珠海同源药业有限公司 | A kind of ambroxol hydrochloride dispersible tablet and preparation method |
| WO2021222987A1 (en) * | 2020-05-08 | 2021-11-11 | Gretals Australia Pty Ltd | Compositions and methods for the prophylaxis and treatment of fibrotic and inflammatory conditions |
| CN115990179A (en) * | 2022-12-16 | 2023-04-21 | 中山大学 | Application of hesperidin in preparation of medicine for treating chronic obstructive pulmonary disease |
-
2013
- 2013-08-08 CN CN2013103447099A patent/CN103417563A/en active Pending
Non-Patent Citations (2)
| Title |
|---|
| 汤青云 等: "柑橘皮中橘皮油、果胶、橙皮苷的提取与利用", 《湖南城市学院学报（自然科学）》 * |
| 王戈然: "消喘宁颗粒质量标准研究", 《时珍国医国药》 * |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107569504A (en) * | 2016-07-04 | 2018-01-12 | 珠海同源药业有限公司 | A kind of ambroxol hydrochloride dispersible tablet and preparation method |
| CN107569504B (en) * | 2016-07-04 | 2020-06-09 | 珠海同源药业有限公司 | Ambroxol hydrochloride dispersible tablet and preparation method thereof |
| WO2021222987A1 (en) * | 2020-05-08 | 2021-11-11 | Gretals Australia Pty Ltd | Compositions and methods for the prophylaxis and treatment of fibrotic and inflammatory conditions |
| CN115990179A (en) * | 2022-12-16 | 2023-04-21 | 中山大学 | Application of hesperidin in preparation of medicine for treating chronic obstructive pulmonary disease |
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Application publication date: 20131204 |