CN1294902C - Cough and asthma relieving drop pills prepared using dahurian rhododendron leaf - Google Patents

Cough and asthma relieving drop pills prepared using dahurian rhododendron leaf Download PDF

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CN1294902C
CN1294902C CN 200410088415 CN200410088415A CN1294902C CN 1294902 C CN1294902 C CN 1294902C CN 200410088415 CN200410088415 CN 200410088415 CN 200410088415 A CN200410088415 A CN 200410088415A CN 1294902 C CN1294902 C CN 1294902C
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extract
polyethylene glycol
drop pill
cough
mixed
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CN1634435A (en
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曲韵智
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Beijing Chia Tai Green Continent Pharmaceutical Co Ltd
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Beijing Chia Tai Green Continent Pharmaceutical Co Ltd
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Abstract

The present invention discloses a medical composition, particularly a cough and asthma relieving drop pill which has the functions of cough relief, sputum reduction and asthma relief and is used for treating chronic bronchitis, cold, cough, etc. The present invention aims to supply the insufficiency of the existing oral medicine preparations which are used for treating chronic bronchitis, cold, cough, etc., and provides a cough and asthma relieving drop pill with the advantages of high living thing utilization, rapid medicine release, rapid effect taking, little toxic side effect, no pollution in the process of production, low production cost, convenient admission and portability. The cough and asthma relieving drop pill of the present invention is prepared by a specific technology after dahurian rhododendron leaf extracts are obtained through a general extraction technology by using pure Chinese medicine dahurian rhododendron leaf as raw materials.

Description

A kind of XIAOKECHUAN drop pill that adopts Folium Rhododendri Daurici to be prepared from
Technical field
The present invention relates to a kind of cough-relieving that has, society's expectorant, antiasthmatic effect is used for the treatment of the pharmaceutical composition of diseases such as chronic bronchitis and cold cough, be particularly related to Cheng Fangwei basis, change a social system a kind of drug composition oral preparation that forms through dosage form with pure Chinese medicine antitussive and antiasthmatic syrup.
Background technology
With the pure Chinese medicine Folium Rhododendri Daurici of single is the pharmaceutical composition that feedstock production forms, antitussive and antiasthmatic syrup and XIAOKECHUAN tablet etc. are arranged, be to be used for the treatment of the highly effective medicines of disease such as chronic bronchitis and cold cough, also be one of pure oral preparation of Chinese traditional medicinal commonly used clinically, but till to the greatest extent, still do not have the appearance of drop pills of dahurian rhododendron leaf dosage form.
Folium Rhododendri Daurici is the leaf of Cuculidae Cuculus polioephalus platymiscium Folium Cuculus polioephalus Rhododendron dauricum L., different name Rhododendron simsii Planch., Folium Rhododendri Mucronulati, beginning is stated from that " the Chinese herbal medicine handbook is used in northeast always, its property bitter cold, have cough-relieving, the effect of relievining asthma, eliminate the phlegm, be the traditional herbal medicine that is used for the treatment of chronic bronchitis, cough.The chemical constituent of having separated has flavones ingredient such as farrerol, Quercetin, kaempferol, Cuculus polioephalus second element and volatile ingredient germacrone, menthol, cadinol etc., also has liposoluble ingredient, Coumarins and toxic component; Introduction is write articles in mulberry honor in 1998 etc., has also therefrom isolated the triterpenes components oleanolic acid.
It is the antitussive and antiasthmatic syrup that forms of feedstock production and the drug standard of XIAOKECHUAN tablet with the Folium Rhododendri Daurici that drug standard WS3-B-0811-91 promulgated by the ministries or commissions of the Central Government and WS3-B-0812-91 have provided respectively.
Owing to reasons such as technologies of preparing, the oral formulations of most drug, exist all after taking that dissolve scattered time limit is long, dissolution is low, absorption is relatively poor, problem such as liver sausage first pass effect and bioavailability are lower, thereby influence the performance of drug effect, also directly affect therapeutic effect.And that oral syrup also exists medicament contg is low, and taking dose is big, and taking dose is inaccurate, takes inconvenience, also is not easy to go out to carry etc. not enough.
Simultaneously, conventional peroral dosage form as tablet, capsule etc., because the technology of granulation is arranged, therefore can produce bigger dust pollution in preparation process, can staff's health be worked the mischief to a certain extent, also can cause certain pollution to environment simultaneously.
Summary of the invention
Purpose of the present invention, be to replenish the existing deficiency that is used for the treatment of the oral drug preparation of diseases such as chronic bronchitis and cold cough, a kind of bioavailability height is provided, release fast, quick produce effects, toxic and side effects is littler, and produces pollution-free, production cost is lower, and is convenient to the drug composition oral preparation XIAOKECHUAN drop pill taking and carry.
XIAOKECHUAN drop pill involved in the present invention is a raw material with pure Chinese medicine Folium Rhododendri Daurici, forms through specific prepared; Be prepared by the following technical solutions, can obtain XIAOKECHUAN drop pill involved in the present invention:
[preparation of Chinese crude drug]
It is some to get red autumnal leaves all over the mountain, calculates according to g or kg weight, adds 40% ethanol, airtight, flooded 7, (extraction temperature is 30-40 ℃), stir 2-3 every day, filter, the medicinal residues squeezing, press liquor and filtrate merge, and filter, be concentrated into relative density and be 1.2～1.5 thick paste, perhaps again with thick paste through decompression, dry, be ground into dry powder and promptly get (below be referred to as Rhododendron dahuricum extract).
Extraction process given here is conventional ethanol extraction technology, is not limited to this a kind of extracting method.
[drop pill prescription]
1. raw material: through above technology extract and Rhododendron dahuricum extract;
2. substrate: Polyethylene Glycol 2000,4000,6000,8000,10000,20000, one or more the mixture in pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac;
3. proportioning: with g or kg is unit, by weight, and Rhododendron dahuricum extract: substrate=1: 1～1: 9.
[preparation method]
1. according to the given ratio of prescription, accurately take by weighing Rhododendron dahuricum extract and substrate, be placed on heating while stirring in the heating container, standby until the fused solution that obtains containing active pharmaceutical ingredient and substrate and/or emulsion and/or suspension;
2. adopt homemade or general drop pill machine (as the TZDW-1 type drop pill machine of Changzheng Tianmin High Science ﹠ Technology Co., Ltd., Beijing's production), and the temperature control system of adjustment drop pill machine, make the water dropper temperature heating of drop pill machine and remain on (50～100) ℃, the temperature cooling of condensing agent also remains on (40～-5) ℃;
3. treating that the temperature of condensing agent in dropping-pill machine head and the condensation column is stable respectively is in above the 2nd step during desired state of temperature, the pharmaceutical composition mixed liquor that will contain Rhododendron dahuricum extract and substrate places in the water dropper storage vat of drop pill machine, splash in the condensing agent by water dropper with suitable speed, condensing agent can be any one in liquid paraffin, methyl-silicone oil, the vegetable oil;
4. will shrink the drop pill taking-up of molding by the outlet of drop pill machine, remove the surface condensation agent, be drying to obtain.Beneficial effect
With the pure Chinese medicine Folium Rhododendri Daurici of single is the pharmaceutical composition that feedstock production forms, antitussive and antiasthmatic syrup and XIAOKECHUAN tablet etc. are arranged, be to be used for the treatment of the highly effective medicines of disease such as chronic bronchitis and cold cough, also be one of pure oral preparation of Chinese traditional medicinal commonly used clinically, but till to the greatest extent, still do not have the appearance of drop pills of dahurian rhododendron leaf dosage form.
Drug standard WS promulgated by the ministries or commissions of the Central Government 3-B-0811-91 and WS 3It is the antitussive and antiasthmatic syrup that forms of feedstock production and the drug standard of XIAOKECHUAN tablet with the Folium Rhododendri Daurici that-B-0812-91 has provided respectively.
Owing to reasons such as technologies of preparing, the oral formulations of most drug, exist all after taking that dissolve scattered time limit is long, dissolution is low, absorption is relatively poor, problem such as liver sausage first pass effect and bioavailability are lower, thereby influence the performance of drug effect, also directly affect therapeutic effect.And that oral syrup also exists medicament contg is low, and taking dose is big, and taking dose is inaccurate, takes inconvenience, also is not easy to go out to carry etc. not enough.
Simultaneously, conventional peroral dosage form as tablet, capsule etc., because the technology of granulation is arranged, therefore can produce bigger dust pollution in preparation process, can staff's health be worked the mischief to a certain extent, also can cause certain pollution to environment simultaneously.
XIAOKECHUAN drop pill involved in the present invention is compared with other XIAOKECHUAN oral formulations, has following beneficial effect:
1. XIAOKECHUAN drop pill involved in the present invention; utilize surfactant to be substrate; make solid dispersion with the Rhododendron dahuricum extract that contains active constituents of medicine; making medicine be molecule, colloid or microcrystalline state is scattered in the substrate; the total surface area of medicine increases, and substrate is hydrophilic, and medicine is had wetting action; can make that medicine is rapidly molten to loose into microgranule or solution, thereby make the dissolving of medicine and absorb and accelerate.Thereby improved bioavailability, brought into play efficient, quick-acting effects etc.
Compare with the administering mode of traditional oral formulations, exist essential distinction.Drop pill with the solid dispersion technology preparation can adopt oral and sublingual administration, and effective ingredient is fully contacted with mucomembranous surface, absorbs by mucomembranous epithelial cell, directly enters blood circulation.Owing to directly enter blood circulation without gastrointestinal tract and liver, avoided first pass effect effectively, also avoided gastrointestinal irritation, thereby it is rapid to have an onset, bioavailability height, characteristics such as side effect is little, and medication is convenient.
2. XIAOKECHUAN drop pill involved in the present invention contacts promptly with saliva and to dissolve rapidly, and is absorbed by oral mucosa, and is not only rapid-action, and the influence of not taken food, and promptly all can containing take after meal ante cibum.
3. production technology, the equipment of preparation drop pill are simple, easy to operate, the automaticity height, and labor intensity is low, the production efficiency height.Workshop does not have dust simultaneously, helps labor protection and environmental protection yet.
The active constituents of medicine of drop pill is uniformly dispersed in substrate, and dosage is accurate, and the ball method of double differences is different little than tablet, and production cost is usually with about 50% of other oral formulations of kind.
4. XIAOKECHUAN drop pill involved in the present invention mixes the Rhododendron dahuricum extract that contains active constituents of medicine mutually with molten matrix, splashes in the not miscible condensed fluid and makes.Therefore, the stability of drug height, not facile hydrolysis, oxidation, and the operation be under liquid state, to carry out, no dust pollution is not subject to the influence of crystal formation, thereby has guaranteed the quality of medicine, has increased stability.
In sum, make XIAOKECHUAN drop pill involved in the present invention have the advantage of triple effect (quick-acting, efficient, long-acting), three little (taking dose is little, toxicity is little, side effect little), five convenience (convenient for production, store convenience, convenient transportation, easy to carry, easy to use).
The specific embodiment
Now with the test and the result thereof of several groups of specific embodiments, be described further with regard to the preparation method of XIAOKECHUAN drop pill of the present invention.
First group: the test of single-matrix
[prescription]
1. Rhododendron dahuricum extract: it is some to get the Chinese medicine Folium Rhododendri Daurici, and the extraction process process that provides according to front [preparation of Chinese crude drug] joint is prepared respectively, can obtain containing the thick paste or the dry powder of Folium Rhododendri Daurici active constituents of medicine, and general designation is made Rhododendron dahuricum extract.
2. substrate: Polyethylene Glycol 2000,4000,6000,8000,10000,20000, pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac;
3. proportioning: with g or kg is unit, by weight, and Rhododendron dahuricum extract: substrate=1: 1～1: 9;
4. the process that provides according to [preparation method] is prepared, and can obtain the XIAOKECHUAN drop pill of different size.
[result of the test]
Test 1: for observe the Rhododendron dahuricum extract that contains active constituents of medicine and different substrates when 1: 1 the proportioning prepared XIAOKECHUAN drop pill in qualitative difference, according to 1: 1 ratio, the Rhododendron dahuricum extract that will contain active constituents of medicine respectively with Polyethylene Glycol 2000, Polyethylene Glycol 4000, Polyethylene Glycol 6000, Polyethylene Glycol 8000, Polyethylene Glycol 10000, Polyethylene Glycol 20000, pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac matches, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 15 pharmaceutical compositions that Rhododendron dahuricum extract and different substrates constituted experiments that contain active constituents of medicine, and obtain 15 groups of different experimental results and see Table 1.
Test 2: for observe the Rhododendron dahuricum extract that contains active constituents of medicine and different substrates when 1: 3 the proportioning prepared XIAOKECHUAN drop pill in qualitative difference, according to 1: 3 ratio, the Rhododendron dahuricum extract that will contain active constituents of medicine respectively with Polyethylene Glycol 2000, Polyethylene Glycol 4000, Polyethylene Glycol 6000, Polyethylene Glycol 8000, Polyethylene Glycol 10000, Polyethylene Glycol 20000, pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac matches, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 15 pharmaceutical compositions that Rhododendron dahuricum extract and different substrates constituted experiments that contain active constituents of medicine, and obtain 15 groups of different experimental results and see Table 2.
Test 3: for observe the Rhododendron dahuricum extract that contains active constituents of medicine and different substrates when 1: 9 the proportioning prepared XIAOKECHUAN drop pill in qualitative difference, according to 1: 9 ratio, the Rhododendron dahuricum extract that will contain active constituents of medicine respectively with Polyethylene Glycol 2000, Polyethylene Glycol 4000, Polyethylene Glycol 6000, Polyethylene Glycol 8000, Polyethylene Glycol 10000, Polyethylene Glycol 20000, pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac matches, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 15 pharmaceutical compositions that Rhododendron dahuricum extract and different substrates constituted experiments that contain active constituents of medicine, and obtain 15 groups of different experimental results and see Table 3.
Second group: the test of mixed-matrix
[prescription]
1. Rhododendron dahuricum extract: it is some to get the Chinese medicine Folium Rhododendri Daurici, and the extraction process process that provides according to front [preparation of Chinese crude drug] joint is prepared respectively, can obtain containing the thick paste or the dry powder of Folium Rhododendri Daurici active constituents of medicine, and general designation is made Rhododendron dahuricum extract.
2. substrate:
2.1 Polyethylene Glycol---English name Macrogol,
2.2 polyoxyethylene stearate 40 esters---English name Polyoxyl (40) Stearate,
Molecular formula is with C 17H 35COO (CH 2CH 2O) nH represents that n is about 40,
2.3 poloxamer---English name Poloxamer, polyoxyethylene poly-oxygen propylene aether,
Molecular formula HO (C 2H 4O) a(C 3H 6O) b(C 2H 4O) cH,
2.4 carboxymethyl starch sodium---English name Carboxymethylstach Sodium, starch is at alkali condition
Down with the sodium salt of the starch carboxymethyl ester of monoxone effect generation,
2.5 betacyclodextrin---English name Betacyclodextrin, molecular formula C 6H 10O 5, this product is that ring dextrin glucosyl transferase acts on 7 glucoses that starch generates with α-1, the bonded cyclic oligosaccharide of 4-glycosidic bond;
3. (with g or kg is unit to proportioning, by weight)
3.1 the ratio of composite interstitial substance---polyoxyethylene stearate 40 esters: Polyethylene Glycol or poloxamer: Polyethylene Glycol or carboxymethyl starch sodium: Polyethylene Glycol or betacyclodextrin: Polyethylene Glycol=1: 1～1: 10,
3.2 Rhododendron dahuricum extract: mixed-matrix weight and=1: 1～1: 9.
4. the process that provides according to [preparation method] is prepared, and can obtain the XIAOKECHUAN drop pill of different size.
[result of the test]
Test 4: for observe the Rhododendron dahuricum extract that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared XIAOKECHUAN drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 1 mixed evenly as mixed-matrix, the Rhododendron dahuricum extract that will contain active constituents of medicine according to 1: 1 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that Rhododendron dahuricum extract and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 4.
Test 5: for observe the Rhododendron dahuricum extract that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared XIAOKECHUAN drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 1 mixed evenly as mixed-matrix, the Rhododendron dahuricum extract that will contain active constituents of medicine according to 1: 3 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that Rhododendron dahuricum extract and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 5.
Test 6: for observe the Rhododendron dahuricum extract that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared XIAOKECHUAN drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 1 mixed evenly as mixed-matrix, the Rhododendron dahuricum extract that will contain active constituents of medicine according to 1: 9 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that Rhododendron dahuricum extract and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 6.
Test 7: for observe the Rhododendron dahuricum extract that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared XIAOKECHUAN drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 5 mixed evenly as mixed-matrix, the Rhododendron dahuricum extract that will contain active constituents of medicine according to 1: 1 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that Rhododendron dahuricum extract and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 7.
Test 8: for observe the Rhododendron dahuricum extract that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared XIAOKECHUAN drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 5 mixed evenly as mixed-matrix, the Rhododendron dahuricum extract that will contain active constituents of medicine according to 1: 3 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that Rhododendron dahuricum extract and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 8.
Test 9: for observe the Rhododendron dahuricum extract that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared XIAOKECHUAN drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 5 mixed evenly as mixed-matrix, the Rhododendron dahuricum extract that will contain active constituents of medicine according to 1: 9 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that Rhododendron dahuricum extract and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 9.
Test 10: for observe the Rhododendron dahuricum extract that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared XIAOKECHUAN drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 10 mixed evenly as mixed-matrix, the Rhododendron dahuricum extract that will contain active constituents of medicine according to 1: 1 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that Rhododendron dahuricum extract and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 10.
Test 11: for observe the Rhododendron dahuricum extract that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared XIAOKECHUAN drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 10 mixed evenly as mixed-matrix, the Rhododendron dahuricum extract that will contain active constituents of medicine according to 1: 3 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that Rhododendron dahuricum extract and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 11.
Test 12: for observe the Rhododendron dahuricum extract that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared XIAOKECHUAN drop pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 10 mixed evenly as mixed-matrix, the Rhododendron dahuricum extract that will contain active constituents of medicine according to 1: 9 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that Rhododendron dahuricum extract and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 12.
The group practices of table 1 Rhododendron dahuricum extract and single-matrix
(Rhododendron dahuricum extract: substrate=1: 1)
The substrate title Effective ingredient (%) Rounding rate (%) Dissolve scattered time limit (minute) The ball method of double differences different (%) Hardness
Polyethylene Glycol 2000 50.0 61 ＜30 ＞10 +
Polyethylene Glycol 4000 50.0 74 ＜30 ＞10 ++
Polyethylene Glycol 6000 50.0 80 ＜30 ＞10 +++
Polyethylene Glycol 8000 50.0 82 ＜30 ＞10 +++
Polyethylene Glycol 10000 50.0 82 ＜30 ＞10 +++
Polyethylene Glycol 20000 50.0 80 ＜30 ＞10 +++
Polyoxyethylene stearate 40 esters 50.0 71 ＜30 ＞10 ++
Betacyclodextrin 50.0 63 ＞30 ＞10 +
Poloxamer 50.0 72 ＜30 ＞10 +++
Carboxymethyl starch sodium 50.0 70 ＜30 ＞10 ++
Sodium lauryl sulphate 50.0 69 ＜30 ＞10 +
Stearic acid 50.0 53 ＞30 ＞10 +
Sodium stearate 50.0 53 ＞30 ＞10 +
Glycerin gelatine 50.0 48 ＞30 ＞10 +
Lac 50.0 43 ＞30 ＞10 +
The group practices of table 2 Rhododendron dahuricum extract and single-matrix
(Rhododendron dahuricum extract: substrate=1: 3)
The substrate title Effective ingredient (%) Rounding rate (%) Dissolve scattered time limit (minute) The ball method of double differences different (%) Hardness
Polyethylene Glycol 2000 25.0 79 ＜30 ＞10 ++
Polyethylene Glycol 4000 25.0 87 ＜30 ＜10 +++
Polyethylene Glycol 6000 25.0 91 ＜30 ＜10 +++
Polyethylene Glycol 8000 25.0 93 ＜30 ＜10 +++
Polyethylene Glycol 10000 25.0 92 ＜30 ＜10 +++
Polyethylene Glycol 20000 25.0 93 ＜30 ＜10 +++
Polyoxyethylene stearate 40 esters 25.0 86 ＜30 ＜10 +++
Betacyclodextrin 25.0 84 ＜30 ＜10 ++
Poloxamer 25.0 87 ＜30 ＜10 +++
Carboxymethyl starch sodium 25.0 78 ＜30 ＞10 ++
Sodium lauryl sulphate 25.0 69 ＜30 ＞10 ++
Stearic acid 25.0 63 ＜30 ＞10 ++
Sodium stearate 25.0 64 ＞30 ＞10 ++
Glycerin gelatine 25.0 61 ＞30 ＞10 ++
Lac 25.0 58 ＞30 ＞10 ++
The group practices of table 3 Rhododendron dahuricum extract and different substrates
(Rhododendron dahuricum extract: substrate=1: 9)
The substrate title Effective ingredient (%) Rounding rate (%) Dissolve scattered time limit (minute) The ball method of double differences different (%) Hardness
Polyethylene Glycol 2000 10.0 88 ＜30 ＜10 ++
Polyethylene Glycol 4000 10.0 91 ＜30 ＜10 +++
Polyethylene Glycol 6000 10.0 93 ＜30 ＜10 +++
Polyethylene Glycol 8000 10.0 93 ＜30 ＜10 +++
Polyethylene Glycol 10000 10.0 94 ＜30 ＜10 +++
Polyethylene Glycol 20000 10.0 92 ＜30 ＜10 +++
Polyoxyethylene stearate 40 esters 10.0 93 ＜30 ＜10 +++
Betacyclodextrin 10.0 87 ＜30 ＜10 ++
Poloxamer 10.0 91 ＜30 ＜10 +++
Carboxymethyl starch sodium 10.0 89 ＜30 ＜10 +++
Sodium lauryl sulphate 10.0 86 ＜30 ＜10 +++
Stearic acid 10.0 74 ＜30 ＞10 ++
Sodium stearate 10.0 77 ＜30 ＞10 ++
Glycerin gelatine 10.0 72 ＞30 ＞10 ++
Lac 10.0 76 ＞30 ＞10 ++
The group practices of table 4 Rhododendron dahuricum extract and mixed-matrix
(Rhododendron dahuricum extract: mixed-matrix=1: 1)
The substrate title Effective ingredient (%) Rounding rate (%) Dissolve scattered time limit (minute) The ball method of double differences different (%) Hardness
Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 1 50 83 ＜30 ＞10 ++
Poloxamer: Polyethylene Glycol=1: 1 50 80 ＜30 ＞10 ++
Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 50 78 ＜30 ＜10 ++
Betacyclodextrin: Polyethylene Glycol=1: 1 50 62 ＜30 ＞10 +
The group practices of table 5 Rhododendron dahuricum extract and mixed-matrix
(Rhododendron dahuricum extract: mixed-matrix=1: 3)
The substrate title Effective ingredient (%) Rounding rate (%) Dissolve scattered time limit (minute) The ball method of double differences different (%) Hardness
Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 1 25 88 ＜30 ＜10 +++
Poloxamer: Polyethylene Glycol=1: 1 25 89 ＜30 ＜10 +++
Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 25 84 ＜30 ＜10 ++
Betacyclodextrin: Polyethylene Glycol=1: 1 25 81 ＜30 ＞10 ++
The group practices of table 6 Rhododendron dahuricum extract and mixed-matrix
(Rhododendron dahuricum extract: mixed-matrix=1: 9)
The substrate title Effective ingredient (%) Rounding rate (%) Dissolve scattered time limit (minute) The ball method of double differences different (%) Hardness
Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 1 10 92 ＜30 ＜10 +++
Poloxamer: Polyethylene Glycol=1: 1 10 91 ＜30 ＜10 +++
Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 10 90 ＜30 ＜10 +++
Betacyclodextrin: Polyethylene Glycol=1: 1 10 86 ＜30 ＜10 +++
The group practices of table 7 Rhododendron dahuricum extract and mixed-matrix
(Rhododendron dahuricum extract: mixed-matrix=1: 1)
The substrate title Effective ingredient (%) Rounding rate (%) Dissolve scattered time limit (minute) The ball method of double differences different (%) Hardness
Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 5 50 86 ＜30 ＜10 +++
Poloxamer: Polyethylene Glycol=1: 5 50 87 ＜30 ＜10 +++
Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 50 87 ＜30 ＜10 ++
Betacyclodextrin: Polyethylene Glycol=1: 5 50 83 ＜30 ＞10 ++
The group practices of table 8 Rhododendron dahuricum extract and mixed-matrix
(Rhododendron dahuricum extract: mixed-matrix=1: 3)
The substrate title Effective ingredient (%) Rounding rate (%) Dissolve scattered time limit (minute) The ball method of double differences different (%) Hardness
Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 5 25 90 ＜30 ＜10 +++
Poloxamer: Polyethylene Glycol=1: 5 25 91 ＜30 ＜10 +++
Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 25 88 ＜30 ＜10 +++
Betacyclodextrin: Polyethylene Glycol=1: 5 25 86 ＜30 ＜10 ++
The group practices of table 9 Rhododendron dahuricum extract and mixed-matrix
(Rhododendron dahuricum extract: mixed-matrix=1: 9)
The substrate title Effective ingredient (%) Rounding rate (%) Dissolve scattered time limit (minute) The ball method of double differences different (%) Hardness
Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 5 10 93 ＜30 ＜10 +++
Poloxamer: Polyethylene Glycol=1: 5 10 92 ＜30 ＜10 +++
Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 10 90 ＜30 ＜10 +++
Betacyclodextrin: Polyethylene Glycol=1: 5 10 90 ＜30 ＜10 +++
The group practices of table 10 Rhododendron dahuricum extract and mixed-matrix
(Rhododendron dahuricum extract: mixed-matrix=1: 1)
The substrate title Effective ingredient (%) Rounding rate (%) Dissolve scattered time limit (minute) The ball method of double differences different (%) Hardness
Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 10 50 90 ＜30 ＜10 +++
Poloxamer: Polyethylene Glycol=1: 10 50 89 ＜30 ＜10 ++
Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 50 87 ＜30 ＜10 ++
Betacyclodextrin: Polyethylene Glycol=1: 10 50 84 ＜30 ＞10 ++
The group practices of table 11 Rhododendron dahuricum extract and mixed-matrix
(Rhododendron dahuricum extract: mixed-matrix=1: 3)
The substrate title Effective ingredient (%) Rounding rate (%) Dissolve scattered time limit (minute) The ball method of double differences different (%) Hardness
Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 10 25 93 ＜30 ＜10 +++
Poloxamer: Polyethylene Glycol=1: 10 25 92 ＜30 ＜10 +++
Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 25 90 ＜30 ＜10 +++
Betacyclodextrin: Polyethylene Glycol=1: 10 25 90 ＜30 ＜10 +++
The group practices of table 12 Rhododendron dahuricum extract and mixed-matrix
(Rhododendron dahuricum extract: mixed-matrix=1: 9)
The substrate title Effective ingredient (%) Rounding rate (%) Dissolve scattered time limit (minute) The ball method of double differences different (%) Hardness
Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 10 10 94 ＜30 ＜10 +++
Poloxamer: Polyethylene Glycol=1: 10 10 92 ＜30 ＜10 +++
Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 10 91 ＜30 ＜10 +++
Betacyclodextrin: Polyethylene Glycol=1: 10 10 91 ＜30 ＜10 +++
1. can be seen by the result in the table: when the ratio of the Rhododendron dahuricum extract that contains active constituents of medicine and substrate was 1: 1, its rounding rate, the ball method of double differences was different and index such as hardness is all undesirable, and dissolve scattered time limit influenced not obvious.
2. when the ratio of Rhododendron dahuricum extract that contains active constituents of medicine and substrate is 1: 3, the rounding rate, the ball method of double differences is different and index such as hardness slightly all begins to enter preferable state.
3. when the ratio of Rhododendron dahuricum extract that contains active constituents of medicine and substrate is 1: 9, though the rounding rate, the ball method of double differences is different and index such as hardness has raising, and is not obvious.
4. the general effect of composite interstitial substance is better than single-matrix.
5. the hardness method for expressing in the subordinate list adopts drop pill is placed on the glass plate, press...withes one's finger it, observes its metamorphosis."+" expression flicking promptly is out of shape, " ++ " expression distortion of firmly pressing, and " +++" expression is indeformable by it.
The partial reference data is as follows:
Mulberry honor, Li Wenlan, Wang Weiming, Ding Zhenduo. the research of triterpenes components in the Folium Rhododendri Daurici. secondary special product the 1st phase of February in 1998 of Chinese woods is P.13.

Claims (2)

1. an XIAOKECHUAN drop pill is a raw material with the Folium Rhododendri Daurici, makes with the pharmaceutically suitable carrier as substrate, it is characterized in that:
(1) it is some to get red autumnal leaves all over the mountain, add 40% ethanol, airtight, 30 ℃～40 ℃ flooded 7 down, stir every day 2～3 times, filter, the medicinal residues squeezing, press liquor and filtrate merge, filter, it is 1.2～1.5 thick paste that filtrate is concentrated into relative density, or with thick paste through decompression, dry, be ground into dry powder and promptly get the extract that contains the Folium Rhododendri Daurici effective ingredient, standby;
(2) described substrate is the mixture of Polyethylene Glycol and polyoxyethylene stearate 40 esters or carboxymethyl starch sodium; By weight, the mixed proportion of polyoxyethylene stearate 40 esters or carboxymethyl starch sodium and Polyethylene Glycol is 1: 1～1: 10, and the ratio of described Rhododendron dahuricum extract and substrate is 1: 3;
(3) according to aforementioned proportion, accurately take by weighing Rhododendron dahuricum extract and substrate, be placed in the heating container heating while stirring, standby until the fused solution that obtains containing Rhododendron dahuricum extract and substrate and/or emulsion and/or suspension;
(4) temperature control system of adjustment drop pill machine makes the water dropper temperature heating of drop pill machine and remains on 50 ℃～100 ℃, and the temperature cooling of condensing agent also remains on 40 ℃～-5 ℃;
When (5) temperature for the treatment of dropping-pill machine head and condensing agent was stablized described state of temperature respectively, the mixed liquor that will contain Rhododendron dahuricum extract and substrate placed in the water dropper storage vat of drop pill machine, splashes into to shrink in the condensing agent to be shaped, promptly.
2. XIAOKECHUAN drop pill as claimed in claim 1 is characterized in that: described condensing agent is any one in liquid paraffin, methyl-silicone oil, the vegetable oil.
CN 200410088415 2004-11-02 2004-11-02 Cough and asthma relieving drop pills prepared using dahurian rhododendron leaf Expired - Fee Related CN1294902C (en)

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