CN1284530C - Compound tornado drop pills - Google Patents
Compound tornado drop pills Download PDFInfo
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- CN1284530C CN1284530C CNB2004100884206A CN200410088420A CN1284530C CN 1284530 C CN1284530 C CN 1284530C CN B2004100884206 A CNB2004100884206 A CN B2004100884206A CN 200410088420 A CN200410088420 A CN 200410088420A CN 1284530 C CN1284530 C CN 1284530C
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- polyethylene glycol
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- tornado
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- Medicinal Preparation (AREA)
Abstract
The present invention discloses compound tornado drop pills of a medicine composition, which have the functions of calming the liver and eliminating ache and are used for treating migraine, vascular headache, tension headache and neuralgia. The present invention has the goals of supplementing the insufficiency of an oral drug preparation for treating the migraine, the vascular headache, the tension headache and the neuralgia and providing the compound tornado drop pills of the medicine composition oral preparation, which have the advantages of high biological availability, rapid medicine release, rapid effect less toxic and side effects, low production cost and no contamination for production. The compound tornado drop pills of the present invention regard extract of belaying cleats, hemlock parsley, dahurian angelica root and radix which contain pharmaceutical active constituents as raw material and are prepared by particular technology.
Description
Technical field
The present invention relates to a kind of have suppressing the hyperactive liver, analgesic activity, be used for the treatment of migraine, vascular headache, tension headache, and neuralgic pharmaceutical composition, the particularly a kind of pure Chinese medicine composition composition oral preparation that is prepared from the Cheng Fangwei basis of pure Chinese medicinal preparation compound yangjiao granules.
Background technology
The compound yangjiao granules that is prepared from according to the prescription that provides among the drug standard WS3-B-2574-97 promulgated by the ministries or commissions of the Central Government and extraction process, be that extract with Cornu Caprae seu Ovis, Rhizoma Chuanxiong, the Radix Angelicae Dahuricae, Radix Aconiti Preparata is the pharmaceutical composition that feedstock production forms, it is the treatment migraine, vascular headache, tension headache, and the highly effective medicine of neuralgia, also be one of pure Chinese medicinal preparation commonly used clinically.Therefore be made into granule, capsule, tablet because it has the obvious treatment effect, do not come out but still there is drops extremely to the greatest extent.
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.
In addition, 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.
Various nanometer formulations about 'Compound Yangjiao ' are disclosed in Chinese patent 01102531.X number " nano medicine ' Compound Yangjiao ' and preparation method thereof ", in its claims, also list dropping pill formulation, but in its description, there is no the preparation technology of at all relevant compound tornado drop pills.As everyone knows, this new rise of drop pill, and be particularly suitable for the preparation of form of Chinese drug, because the dispersibility of its process conditions just makes many herbal species be difficult to make drop pill.According to the standards of pharmacopoeia that this patented technology provides, can't finish the preparation of compound tornado drop pills at all, therefore still there is not any technology data of compound tornado drop pills involved in the present invention with regard to the known technology field.And nanometer formulation industry manufacturing cost height, valuable product is unfavorable for the citizen stratum medication of non-socialized medicine.
Summary of the invention
Purpose of the present invention, be to replenish the existing migraine that is used for the treatment of, vascular headache, tension headache, and the deficiency of neuralgia oral drug preparation, a kind of bioavailability height is provided, release fast, quick produce effects, toxic and side effects is littler, and produce pollution-free, the drug composition oral preparation compound tornado drop pills that production cost is lower.
Compound tornado drop pills involved in the present invention, is prepared from through specific drop pill preparation technology obtain containing the extract of active constituents of medicine through extraction after with the Cheng Fangwei basis of pure Chinese medicinal preparation compound yangjiao granules again.Be prepared by the following technical solutions, can obtain compound tornado drop pills involved in the present invention:
[preparation of Cornu Caprae seu Ovis, Rhizoma Chuanxiong, the Radix Angelicae Dahuricae, Radix Aconiti Preparata extract]
With g or kg is unit, according to the weight portion meter, and 12 parts on Cornu Caprae seu Ovis, 4 parts of Rhizoma Chuanxiongs, 4 parts of the Radixs Angelicae Dahuricae, 3 parts of Radix Aconiti Preparatas, more than four flavors, Cornu Caprae seu Ovis pound sheet decocts with water secondary, each 3h, collecting decoction, filter, filtrate concentrates the back and adds 2.5 times of amounts of ethanol, stirs, and staticly settles 24h, and it is standby to get supernatant.Three flavors such as all the other Rhizoma Chuanxiongs, be ground into coarse powder, according to the percolation under fluid extract and the extractum item (appendix IO), make solvent with 70% ethanol, carry out percolation, filter liquid and Cornu Caprae seu Ovis supernatant merges, decompression recycling ethanol, and cryoconcentration to relative density is 1.2～1.5 thick paste, or be ground into dry powder promptly through cold drying again.
Here only enumerate the extracting method in the compound yangjiao granules that provides according to drug standard WS3-B-2574-97 promulgated by the ministries or commissions of the Central Government, but be not limited to this a kind of method.
[drop pill prescription]
1. raw material: through above method extract and thick paste that contains 4 flavor active ingredient of Chinese herbs such as Cornu Caprae seu Ovis, Rhizoma Chuanxiong, the Radix Angelicae Dahuricae, Radix Aconiti Preparata or dry powder (below be referred to as drug 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. (with g or kg is unit to proportioning, by weight): drug extract: substrate=1: 1～1: 9.
[preparation method]
1. according to the given ratio of prescription, accurately take by weighing drug extract and substrate, be placed on heating while stirring in the heating container, standby until the fused solution that obtains containing drug extract 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 drug extract and substrate places in the water dropper storage vat of drop pill machine, splashes 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
The compound yangjiao granules that is prepared from according to the prescription that provides among the drug standard WS3-B-2574-97 promulgated by the ministries or commissions of the Central Government and extraction process, be that extract with Cornu Caprae seu Ovis, Rhizoma Chuanxiong, the Radix Angelicae Dahuricae, Radix Aconiti Preparata is the pharmaceutical composition that feedstock production forms, it is the treatment migraine, vascular headache, tension headache, and the highly effective medicine of neuralgia, also be one of pure Chinese medicinal preparation commonly used clinically.Therefore be made into granule, capsule, tablet because it has the obvious treatment effect, do not come out but still there is drops extremely to the greatest extent.
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.
In addition, 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.
Various nanometer formulations about 'Compound Yangjiao ' are disclosed in Chinese patent 01102531.X number " nano medicine ' Compound Yangjiao ' and preparation method thereof ", but nanometer formulation industry manufacturing cost height, valuable product is unfavorable for the citizen stratum medication of non-socialized medicine.
Compound tornado drop pills involved in the present invention is compared with other oral formulations, has following beneficial effect:
1. compound tornado drop pills involved in the present invention; utilize surfactant to be substrate; make solid dispersion with extractum that contains active constituents of medicine or dry powder; 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. compound tornado drop pills 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. compound tornado drop pills involved in the present invention mixes the thick paste (perhaps dry powder) 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 compound tornado drop pills 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 compound tornado drop pills of the present invention.
First group: the test of single-matrix
[prescription]
1. raw material: according to the method that provides in [preparation of Cornu Caprae seu Ovis, Rhizoma Chuanxiong, the Radix Angelicae Dahuricae, Radix Aconiti Preparata extract] extract and the dry powder that contains 4 flavor active ingredient of Chinese herbs such as Cornu Caprae seu Ovis, Rhizoma Chuanxiong, the Radix Angelicae Dahuricae, Radix Aconiti Preparata (below be referred to as drug 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. (with g or kg is unit to proportioning, by weight): drug extract: substrate=1: 1～1: 9.
[result of the test]
Test 1: for observe the extract that contains active constituents of medicine and different substrates when 1: 1 the proportioning prepared compound tornado drop pills in qualitative difference, according to 1: 1 ratio, the 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 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 extract that contains active constituents of medicine and different substrates when 1: 3 the proportioning prepared compound tornado drop pills in qualitative difference, according to 1: 3 ratio, the 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 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 extract that contains active constituents of medicine and different substrates when 1: 9 the proportioning prepared compound tornado drop pills in qualitative difference, according to 1: 9 ratio, the 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 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. raw material: according to the method that provides in [preparation of Cornu Caprae seu Ovis, Rhizoma Chuanxiong, the Radix Angelicae Dahuricae, Radix Aconiti Preparata extract] extract and the dry powder that contains 4 flavor active ingredient of Chinese herbs such as Cornu Caprae seu Ovis, Rhizoma Chuanxiong, the Radix Angelicae Dahuricae, Radix Aconiti Preparata (below be referred to as drug 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,
The sodium salt of the starch carboxymethyl ester that 2.4 carboxymethyl starch sodium---English name Carboxymethylstach Sodium, starch generates with the monoxone effect under alkali condition,
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 drug extract: substrate=1: 1～1: 9.
[result of the test]
Test 4: for observe the extract that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared compound tornado drop pills 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 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 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 extract that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared compound tornado drop pills 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 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 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 extract that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared compound tornado drop pills 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 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 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 extract that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared compound tornado drop pills 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 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 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 extract that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared compound tornado drop pills 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 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 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 extract that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared compound tornado drop pills 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 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 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 extract that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared compound tornado drop pills 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 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 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 extract that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared compound tornado drop pills 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 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 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 extract that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared compound tornado drop pills 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 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 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 drug extract and single-matrix
(drug 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 | 77 | ＜30 | ＞10 | + |
| Polyethylene Glycol 6000 | 50.0 | 82 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 8000 | 50.0 | 83 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 10000 | 50.0 | 86 | ＜30 | ＜10 | ++ |
| Polyethylene Glycol 20000 | 50.0 | 87 | ＜30 | ＜10 | ++ |
| Stearic acid | 50.0 | 53 | ＜30 | ＞10 | + |
| Sodium stearate | 50.0 | 54 | ＜30 | ＞10 | |
| Glycerin gelatine | 50.0 | 52 | ＜30 | ＞10 | |
| Polyoxyethylene stearate 40 esters | 50.0 | 76 | ＜30 | ＞10 | ++ |
| Lac | 50.0 | 49 | ＜30 | ＞10 | |
| The polyoxyethylene monostearate | 50.0 | 70 | ＜30 | ＞10 | + |
| Polyethers | 50.0 | 72 | ＜30 | ＞10 | ++ |
| Carboxymethyl starch sodium | 50.0 | 71 | ＜30 | ＞10 | + |
| Sodium lauryl sulphate | 50.0 | 69 | ＜30 | ＞10 | + |
The group practices of table 2 drug extract and single-matrix
(drug 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 | 76 | ＜30 | ＞10 | + |
| Polyethylene Glycol 4000 | 25.0 | 89 | ＜30 | ＜10 | ++ |
| Polyethylene Glycol 6000 | 25.0 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 8000 | 25.0 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 10000 | 25.0 | 91 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 20000 | 25.0 | 93 | ＜30 | ＜10 | ++ |
| Stearic acid | 25.0 | 72 | ＜30 | ＞10 | + |
| Sodium stearate | 25.0 | 73 | ＜30 | ＞10 | + |
| Glycerin gelatine | 25.0 | 63 | ＜30 | ＞10 | + |
| Polyoxyethylene stearate 40 esters | 25.0 | 89 | ＜30 | ＜10 | +++ |
| Lac | 25.0 | 68 | ＜30 | ＞10 | + |
| The polyoxyethylene monostearate | 25.0 | 78 | ＜30 | ＞10 | + |
| Polyethers | 25.0 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium | 25.0 | 83 | ＜30 | ＞10 | ++ |
| Sodium lauryl sulphate | 25.0 | 75 | ＜30 | ＞10 | + |
The group practices of table 3 drug extract and different substrates
(drug 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 | 87 | ＜30 | ＜10 | ++ |
| Polyethylene Glycol 4000 | 10.0 | 92 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 6000 | 10.0 | 94 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 8000 | 10.0 | 92 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 10000 | 10.0 | 92 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 20000 | 10.0 | 92 | ＜30 | ＜10 | +++ |
| Stearic acid | 10.0 | 83 | ＜30 | ＞10 | +++ |
| Sodium stearate | 10.0 | 79 | ＜30 | ＞10 | +++ |
| Glycerin gelatine | 10.0 | 77 | ＜30 | ＞10 | ++ |
| Polyoxyethylene stearate 40 esters | 10.0 | 91 | ＜30 | ＜10 | +++ |
| Lac | 10.0 | 70 | ＜30 | ＞10 | ++ |
| The polyoxyethylene monostearate | 10.0 | 82 | ＜30 | ＞10 | +++ |
| Polyethers | 10.0 | 89 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium | 10.0 | 81 | ＜30 | ＞10 | +++ |
| Sodium lauryl sulphate | 10.0 | 75 | ＜30 | ＞10 | +++ |
The group practices of table 4 drug extract and mixed-matrix
(drug 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 | 82 | ＜30 | ＞10 | ++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 50 | 81 | ＜30 | ＞10 | ++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 50 | 78 | ＜30 | ＜10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 50 | 65 | ＜30 | ＞10 | + |
The group practices of table 5 drug extract and mixed-matrix
(drug 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 | 89 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 25 | 89 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 25 | 85 | ＜30 | ＜10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 25 | 82 | ＜30 | ＞10 | ++ |
The group practices of table 6 drug extract and mixed-matrix
(drug 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 | 93 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 10 | 92 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 10 | 90 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 10 | 87 | ＜30 | ＜10 | +++ |
The group practices of table 7 drug extract and mixed-matrix
(drug 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 | 85 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 50 | 87 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 50 | 86 | ＜30 | ＜10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 50 | 84 | ＜30 | ＞10 | ++ |
The group practices of table 8 drug extract and mixed-matrix
(drug 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 | 91 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 25 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 25 | 89 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 25 | 87 | ＜30 | ＜10 | ++ |
The group practices of table 9 drug extract and mixed-matrix
(drug 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 drug extract and mixed-matrix
(drug 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 | 92 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | 50 | 89 | ＜30 | ＜10 | ++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 50 | 88 | ＜30 | ＜10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 50 | 85 | ＜30 | ＞10 | ++ |
The group practices of table 11 drug extract and mixed-matrix
(drug 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 | 94 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | 25 | 93 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 25 | 90 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 25 | 92 | ＜30 | ＜10 | +++ |
The group practices of table 12 drug extract and mixed-matrix
(drug 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 | 93 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | 10 | 92 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 10 | 92 | ＜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 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 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 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:
1. high cloud peak. compound cavel capsule treatment headache 300 routine clinical observations. 1994 03 phases of Inner Mongol Chinese medicine;
2. sieve is few quick, Wang Xi. inquire into the antalgic and sedative effect of compound yangjiao granules. and 2003 03 phases of Guangdong pharmacy;
3. normal Yu of king, Zhang Dingding. compound cavel tablet quality Study on standards. Harbin University of Commerce's journal (natural science edition) 02 phase of calendar year 2001;
4. fourth YULAN. compound yangjiao granules process modification observation of curative effect. the Gansu science journal S1 phase in 2002.
Claims (2)
1. the compound tornado drop pills with suppressing the hyperactive liver, analgesic activity is a raw material with four flavor Chinese medicines such as Cornu Caprae seu Ovis, Rhizoma Chuanxiong, the Radix Angelicae Dahuricae, Radix Aconiti Preparata, is prepared from the pharmaceutically suitable carrier as substrate, it is characterized in that:
(1), gets 12 parts on Cornu Caprae seu Ovis, 4 parts of Rhizoma Chuanxiongs, 4 parts of the Radixs Angelicae Dahuricae, 3 parts of Radix Aconiti Preparatas according to the weight portion meter, more than four the flavor, Cornu Caprae seu Ovis pound sheet decocts with water secondary, each 3 hours, collecting decoction, filter, filtrate concentrates the back and adds 2.5 times of amounts of ethanol, stirs, and staticly settles 24 hours, and it is standby to get supernatant; Three flavors such as all the other Rhizoma Chuanxiongs, be ground into coarse powder, according to the percolation under Chinese Pharmacopoeia 2000 editions appendix IO fluid extract and the extractum item, make solvent with 70% ethanol, carry out percolation, filter liquid and Cornu Caprae seu Ovis supernatant merge, decompression recycling ethanol, and cryoconcentration to relative density is 1.2～1.5 thick paste, or again through cold drying, pulverizing, promptly get the extract that contains pharmaceutically active ingredient in above-mentioned four flavors, 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 containing the thick paste of described 4 flavor active ingredient of Chinese herbs or the ratio of dry powder and substrate is 1: 3;
(3) according to aforementioned proportion, accurately take by weighing described Chinese medicine extract and substrate, be placed in the heating container heating while stirring, standby until the fused solution that obtains containing described Chinese medicine 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 reached the said temperature state respectively, the medicinal liquid that will contain described Chinese medicine extract and substrate placed in the water dropper storage vat of drop pill machine, splashed in the condensing agent, shrank molding, promptly.
2. compound gastrodia elata drop pills as claimed in claim 1 is characterized in that: described condensing agent is any one in liquid paraffin, methyl-silicone oil, the vegetable oil.
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| CNB2004100884206A CN1284530C (en) | 2004-11-02 | 2004-11-02 | Compound tornado drop pills |
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| CNB2004100884206A CN1284530C (en) | 2004-11-02 | 2004-11-02 | Compound tornado drop pills |
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