CN100358500C - Fleabane and earthworm dripping pill and its preparing method - Google Patents
Fleabane and earthworm dripping pill and its preparing method Download PDFInfo
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- CN100358500C CN100358500C CNB2005100086200A CN200510008620A CN100358500C CN 100358500 C CN100358500 C CN 100358500C CN B2005100086200 A CNB2005100086200 A CN B2005100086200A CN 200510008620 A CN200510008620 A CN 200510008620A CN 100358500 C CN100358500 C CN 100358500C
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Abstract
The present invention relates to a medicine composition which has the function of blood activation and channel dredging and is used for treating symptoms such as ischemic apoplexy, etc. caused by blood stasis and vessel blockage, and particularly relates to a medicine composition oral administration drop pill preparation which uses a Chinese medicine breviscapine earthworm capsule as a base and is formed by the reformation of a medicine form. The present invention has the purpose to solve the defects of the present oral administration medicine preparation for treating symptoms such as ischemic apoplexy, etc. caused by blood stasis and vessel blockage and to provide a medicine composition oral administration breviscapine earthworm drop pill without pollution during the preparation and with high biological availability, rapid medicine release, rapid effect, little toxic side effect, high medicine content, convenient taking and low price. The breviscapine earthworm drop pill of the present invention is prepared by that the extractive of active medicine components of two kinds of Chinese medicine with fresh earthworm and erigeron is used as a raw material, and is prepared with a carrier which can be medicinally used as a substrate.
Description
Technical field
The present invention relates to a kind of promoting blood circulation to remove obstruction in the collateral effect that has, the pharmaceutical composition that is used for the treatment of the diseases such as cerebral infarction that obstruction of collaterals by blood stasis causes, be particularly related to based on Chinese traditional patent formulation fleabane and earthworm capsule, change a social system a kind of drug composition oral dropping pill formulation that forms through dosage form.
Background technology
The fleabane and earthworm capsule that is prepared from according to the prescription that provides among the national drug standards WS-10424 (ZD-0424)-2002 and preparation technology, it is a kind of promoting blood circulation to remove obstruction in the collateral effect that has, the oral Chinese medicine preparation that is used for the treatment of the symptoms such as cerebral infarction that obstruction of collaterals by blood stasis causes, through clinical verification, steady quality, determined curative effect is the common drug preparation that clinical and family is used for the treatment of above disease.Below be prescription and the preparation technology who provides among the drug standard WS-10424 (ZD-0424)-2002;
Prescription: fresh Pheretima 1200g, Herba Erigerontis 1000g, starch 80g;
Method for making: above two flavor medical materials, get fresh Pheretima and add water logging and washed 1～2 hour, after cleaning, smash to pieces, homogenate 10～15 minutes, centrifugal with the sodium chloride solution extraction of 0.1mol/L 6 hours, get supernatant, cold drying, Pheretima extract is standby.Get Herba Erigerontis, use Diluted Alcohol heating and refluxing extraction 50 minutes, filter, filtrate decompression is concentrated into the thick paste that relative density is 1.25～1.35 (60 ℃), and hydro-oxidation sodium filters to alkalescence, filtrate adds hydrochloric acid and regulates pH value to 2.0, filters, and precipitate is extremely neutral with hot water wash, drain, after a small amount of Diluted Alcohol gradation washing, add an amount of thermosol of ethanol, adding medicinal activated carbon decolours in right amount, filter, filtrate concentrates, and places, separate out amorphous yellow powder, filter, drying is with Pheretima extract, starch, mixing, sieve, 1000 capsules of packing into, promptly.
In the appended fleabane and earthworm capsule description this kind is explained as follows:
Nomenclature of drug: fleabane and earthworm capsule;
Main component: fresh Pheretima, Herba Erigerontis;
Function cures mainly: promoting blood circulation to remove obstruction in the collateral.Be used for the cerebral infarction that obstruction of collaterals by blood stasis causes.
Owing to reasons such as technologies of preparing, the oral formulations of most drug, especially the oral formulations of Chinese medicine, 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.Moreover, the complex manufacturing of conventional oral formulations, production cost is higher, thereby patient's drug cost is also improved thereupon, is unfavorable for improving the ability of seeking medical advice of extensive patients, also is unfavorable for improving the general health level of society.
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 the symptoms such as cerebral infarction that obstruction of collaterals by blood stasis causes, a kind of bioavailability height is provided, release fast, quick produce effects, toxic and side effects is little, and medicament contg height, taking convenience, cheap, and in preparation process free of contamination drug composition oral preparation fleabane and earthworm dripping pill.
Fleabane and earthworm dripping pill involved in the present invention is a raw material with the extract that contains 2 flavor Chinese medicine active pharmaceutical ingredients such as fresh Pheretima and Herba Erigerontis, is prepared from the pharmaceutically suitable carrier as substrate.Be prepared by the following technical solutions, can obtain fleabane and earthworm dripping pill involved in the present invention:
[preparation method]
1. be unit with g or kg, calculate, get 6 parts of fresh Pheretimas according to weight, 5 parts of Herba Erigerontiss, more than two flavors to make the extract that contains 2 flavor Chinese medicine active pharmaceutical ingredients such as fresh Pheretima and Herba Erigerontis in advance standby;
2. substrate---Polyethylene Glycol
(1000,2000,4000,6000,8000,10000,20000), 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 medicine dry powder: substrate=1: 1～1: 9.
4. according to the given ratio of prescription, accurately take by weighing medicine dry powder and substrate, be placed on heating while stirring in the heating container, standby until the fused solution that obtains containing medicine dry powder and substrate and/or emulsion and/or suspension;
5. 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) ℃;
6. when treating in dropping-pill machine head and the condensation column that the temperature of condensing agent reaches desired state of temperature respectively, will contain fused solution and/or the emulsion and/or the suspension of medicine dry powder and substrate, place in the water dropper jar of drop pill machine, splash in the condensing agent;
Condensing agent can be any one in liquid paraffin, methyl-silicone oil, the vegetable oil;
7. 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.
[appendix: contain 2 flavor Chinese medicine active pharmaceutical ingredient preparation method of extract such as fresh Pheretima and Herba Erigerontis] is unit with g or kg, according to the weight portion meter, gets 6 parts of fresh Pheretimas, 5 parts of Herba Erigerontiss, more than two the flavor medical materials, fresh Pheretima adds water logging and washed 1～2 hour, after cleaning, smash homogenate 10～15 minutes, the sodium chloride solution extraction of usefulness 0.1mol/L 6 hours to pieces, centrifugal, get supernatant, cold drying, it is standby to get Pheretima extract.Get Herba Erigerontis, use Diluted Alcohol heating and refluxing extraction 50 minutes, filter, filtrate decompression is concentrated into the thick paste that relative density is 1.25～1.35 (60 ℃), hydro-oxidation sodium filters to alkalescence, and filtrate adds hydrochloric acid and regulates pH value to 2.0, filter, precipitate, is drained to neutral with hot water wash, after a small amount of Diluted Alcohol gradation washing, add an amount of thermosol of ethanol, add medicinal activated carbon and decolour in right amount, filter, filtrate concentrates, place, separate out amorphous yellow powder, filter drying, with the Pheretima extract mixing, be dried and crushed into dry powder promptly through decompression (0.1Mpa) low temperature (60 ℃) again.
What provide above is a kind of preparation method of common drug extract, under the same or analogous prerequisite of main active pharmaceutical ingredient of extract, is not limited to this a kind of method.
Beneficial effect
The fleabane and earthworm capsule that is prepared from according to the prescription that provides among the national drug standards WS-10424 (ZD-0424)-2002 and preparation technology, it is a kind of promoting blood circulation to remove obstruction in the collateral effect that has, the oral Chinese medicine preparation that is used for the treatment of the symptoms such as cerebral infarction that obstruction of collaterals by blood stasis causes, through clinical verification, steady quality, determined curative effect is the common drug preparation that clinical and family is used for the treatment of above disease.Owing to reasons such as technologies of preparing, the oral formulations of most drug, especially the oral formulations of Chinese medicine, 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 the syrups preparation also exists medicament contg is low, and taking dose is big, and taking dose is inaccurate, takes inconvenient characteristics, also is not easy to go out to carry wait deficiency.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.Moreover, the complex manufacturing of conventional oral formulations, production cost is higher, thereby patient's drug cost is also improved thereupon, is unfavorable for improving the ability of seeking medical advice of extensive patients, also is unfavorable for improving the general health level of society.
Fleabane and earthworm dripping pill involved in the present invention is compared with the fleabane and earthworm capsule has following beneficial effect:
1. fleabane and earthworm dripping pill involved in the present invention; utilize surfactant to be substrate; make solid dispersion with the extract that contains two flavor Chinese medicine active pharmaceutical ingredients such as fresh Pheretima, Herba Erigerontis; making medicine be molecule, colloid or microcrystalline state is scattered in the substrate; the total surface area of medicine increases; and substrate is hydrophilic; medicine had wetting action; can make medicine molten microgranule or the solution of loosing into rapidly; thereby make the dissolving of medicine and absorb quickening; thereby improved bioavailability, brought into play efficient, quick-acting effects etc.Compare with the capsular administering mode of fleabane and earthworm, exist essential distinction.Utilize the drop pill of solid dispersion technology preparation, can adopt oral and sublingual administration, effective ingredient is fully contacted with mucomembranous surface, absorb, directly enter blood circulation by mucomembranous epithelial cell.Because active constituents of medicine directly enters blood circulation without gastrointestinal tract and liver, avoided first pass effect effectively, also avoided gastrointestinal irritation, thereby thereby it is rapid to make that fleabane and earthworm dripping pill involved in the present invention has an onset, the bioavailability height, characteristics such as side effect is little, and medication is convenient.
2. fleabane and earthworm dripping 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. fleabane and earthworm dripping pill involved in the present invention mixes the 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.
4. 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.
5. the production cost of preparation drop pill is usually with about 50% of other oral formulations of kind, and compares with oral liquid, and the dosage of drop pill is accurate, thereby makes the patient take metering control easily.
In sum, make fleabane and earthworm dripping 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 several groups of specific embodiments, be described further with regard to the preparation method of fleabane and earthworm dripping pill of the present invention.
First group: the test of single-matrix
1. it is standby that the preparation method that provides according to [appendix] makes the extract dry powder that contains fresh Pheretima, two kinds of Chinese medicine active pharmaceutical ingredients of Herba Erigerontis earlier;
2. substrate: Polyethylene Glycol
(1000,2000,4000,6000,8000,10000,20000), 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 medicine dry powder: substrate=1: 1～1: 9;
4. be prepared according to the process of [preparation method] 4～7 again, promptly can make the fleabane and earthworm dripping pill of all size.
[result of the test]
Test 1: for observe the dry powder that contains active constituents of medicine and different substrates when 1: 1 proportioning prepared fleabane and earthworm dripping pill in qualitative difference, according to 1: 1 ratio, the dry powder that will contain active constituents of medicine respectively with Polyethylene Glycol
1000, 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 16 pharmaceutical compositions that dry powder and different substrates constituted experiments that contain active constituents of medicine, and obtain 16 groups of different experimental results and see Table 1.
Test 2: for observe the dry powder that contains active constituents of medicine and different substrates when 1: 3 proportioning prepared fleabane and earthworm dripping pill in qualitative difference, according to 1: 3 ratio, the dry powder that will contain active constituents of medicine respectively with Polyethylene Glycol
1000, 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 16 pharmaceutical compositions that dry powder and different substrates constituted experiments that contain active constituents of medicine, and obtain 16 groups of different experimental results and see Table 2.
Test 3: for observe the dry powder that contains active constituents of medicine and different substrates when 1: 9 proportioning prepared fleabane and earthworm dripping pill in qualitative difference, according to 1: 9 ratio, the dry powder that will contain active constituents of medicine respectively with Polyethylene Glycol
1000, 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 16 pharmaceutical compositions that dry powder and different substrates constituted experiments that contain active constituents of medicine, and obtain 16 groups of different experimental results and see Table 3.
Second group: the test of mixed-matrix
1. it is standby that the preparation method that provides according to [appendix] makes the extract dry powder that contains fresh Pheretima, two kinds of Chinese medicine active pharmaceutical ingredients of Herba Erigerontis earlier;
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 hybrid medicine dry powder: mixed-matrix weight and=1: 1～1: 9,
4. be prepared according to [preparation method] again, promptly can make the fleabane and earthworm dripping pill of various different sizes.
[result of the test]
Test 4: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared fleabane and earthworm dripping 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 dry powder 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 dry powder 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 dry powder that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared fleabane and earthworm dripping 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 dry powder 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 dry powder 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 dry powder that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared fleabane and earthworm dripping 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 dry powder 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 dry powder 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 dry powder that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared fleabane and earthworm dripping 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 dry powder 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 dry powder 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 dry powder that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared fleabane and earthworm dripping 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 dry powder 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 dry powder 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 dry powder that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared fleabane and earthworm dripping 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 dry powder 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 dry powder 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 dry powder that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared fleabane and earthworm dripping 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 dry powder 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 dry powder 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 dry powder that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared fleabane and earthworm dripping 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 dry powder 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 dry powder 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 dry powder that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared fleabane and earthworm dripping 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 dry powder 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 dry powder 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 medicine dry powder and single-matrix
(medicine dry powder: 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 | 64 | ＜30 | ＞10 | + |
| Polyethylene Glycol 4000 | 50.0 | 74 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 6000 | 50.0 | 81 | ＜30 | ＞10 | +++ |
| Polyethylene Glycol 8000 | 50.0 | 82 | ＜30 | ＞10 | +++ |
| Polyethylene Glycol 10000 | 50.0 | 84 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 20000 | 50.0 | 85 | ＜30 | ＜10 | +++ |
| Polyoxyethylene stearate 40 esters | 50.0 | 75 | ＜30 | ＞10 | ++ |
| Betacyclodextrin | 50.0 | 72 | ＜30 | ＞10 | ++ |
| Poloxamer | 50.0 | 73 | ＜30 | ＞10 | ++ |
| Carboxymethyl starch sodium | 50.0 | 71 | ＜30 | ＞10 | ++ |
| Sodium lauryl sulphate | 50.0 | 69 | ＜30 | ＞10 | ++ |
| Stearic acid | 50.0 | 57 | ＜30 | ＞10 | ++ |
| Sodium stearate | 50.0 | 56 | ＜30 | ＞10 | +++ |
| Glycerin gelatine | 50.0 | 55 | ＜30 | ＞10 | +++ |
| Lac | 50.0 | 54 | ＞30 | ＞10 | +++ |
The group practices of table 2 medicine dry powder and single-matrix
(medicine dry powder: 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 | 78 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 4000 | 25.0 | 86 | ＜30 | ＜10 | ++ |
| Polyethylene Glycol 6000 | 25.0 | 93 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 8000 | 25.0 | 91 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 10000 | 25.0 | 92 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 20000 | 25.0 | 91 | ＜30 | ＜10 | ++ |
| Polyoxyethylene stearate 40 esters | 25.0 | 92 | ＜30 | ＜10 | ++ |
| Betacyclodextrin | 25.0 | 85 | ＜30 | ＞10 | ++ |
| Poloxamer | 25.0 | 89 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium | 25.0 | 80 | ＜30 | ＞10 | ++ |
| Sodium lauryl sulphate | 25.0 | 77 | ＜30 | ＞10 | ++ |
| Stearic acid | 25.0 | 76 | ＞30 | ＞10 | +++ |
| Sodium stearate | 25.0 | 72 | ＞30 | ＞10 | +++ |
| Glycerin gelatine | 25.0 | 74 | ＞30 | ＞10 | +++ |
| Lac | 25.0 | 72 | ＞30 | ＞10 | +++ |
The group practices of table 3 medicine dry powder and single-matrix
(medicine dry powder: 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 | 85 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 4000 | 10.0 | 93 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 6000 | 10.0 | 94 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 8000 | 10.0 | 92 | ＜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 | 88 | ＜30 | ＜10 | ++ |
| Poloxamer | 10.0 | 92 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium | 10.0 | 86 | ＜30 | ＜10 | +++ |
| Sodium lauryl sulphate | 10.0 | 83 | ＜30 | ＞10 | +++ |
| Stearic acid | 10.0 | 76 | ＞30 | ＞10 | +++ |
| Sodium stearate | 10.0 | 77 | ＞30 | ＞10 | +++ |
| Glycerin gelatine | 10.0 | 74 | ＞30 | ＞10 | +++ |
| Lac | 10.0 | 76 | ＞30 | ＞10 | +++ |
The group practices of table 4 medicine dry powder and mixed-matrix
(medicine dry powder: 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 | 85 | ＜30 | ＜10 | ++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 50 | 86 | ＜30 | ＜10 | ++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 50 | 81 | ＜30 | ＞10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 50 | 79 | ＜30 | ＞10 | + |
The group practices of table 5 medicine dry powder and mixed-matrix
(medicine dry powder: 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 | 92 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 25 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 25 | 89 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 25 | 87 | ＜30 | ＞10 | ++ |
The group practices of table 6 medicine dry powder and mixed-matrix
(medicine dry powder: 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 | 86 | ＜30 | ＞10 | +++ |
The group practices of table 7 medicine dry powder and mixed-matrix
(medicine dry powder: 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 | 93 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 50 | 94 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 50 | 89 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 50 | 87 | ＜30 | ＞10 | ++ |
The group practices of table 8 medicine dry powder and mixed-matrix
(medicine dry powder: 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: poly-second triol=1: 5 | 25 | 95 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 25 | 95 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 25 | 92 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 25 | 89 | ＜30 | ＜10 | ++ |
The group practices of table 9 medicine dry powder and mixed-matrix
(medicine dry powder: 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 | 94 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 10 | 91 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 10 | 88 | ＜30 | ＜10 | +++ |
The group practices of table 10 medicine dry powder and mixed-matrix
(medicine dry powder: 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 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 50 | 89 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 50 | 82 | ＜30 | ＞10 | +++ |
The group practices of table 11 medicine dry powder and mixed-matrix
(medicine dry powder: 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 | 92 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 25 | 90 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 25 | 89 | ＜30 | ＜10 | +++ |
The group practices of table 12 medicine dry powder and mixed-matrix
(medicine dry powder: 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 | 93 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 10 | 91 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 10 | 92 | ＜30 | ＜10 | +++ |
1. can be seen by the result in the table: when being 1: 1 when medicine dry powder with the ratio of substrate, its rounding rate, the ball method of double differences is different and index such as hardness is all undesirable, and dissolve scattered time limit institute is influenced not obvious.
2. when the ratio of medicine dry powder 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 medicine dry powder 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.
Claims (2)
1. a fleabane and earthworm dripping pill is a raw material with fresh Pheretima, Herba Erigerontis, is prepared from the pharmaceutically suitable carrier as substrate, it is characterized in that:
(1) according to the weight portion meter, get 6 parts of fresh Pheretimas, 5 parts of Herba Erigerontiss, more than two the flavor medical materials, fresh Pheretima adds water logging and washed 1～2 hour, after cleaning, smash homogenate 10～15 minutes, the sodium chloride solution extraction of usefulness 0.1mol/L 6 hours to pieces, centrifugal, get supernatant, cold drying, it is standby to get Pheretima extract;
(2) get Herba Erigerontis, use Diluted Alcohol heating and refluxing extraction 50 minutes, filter, to be concentrated into relative density be 1.25～1.35 thick paste to filtrate decompression under 60 ℃ of conditions, and hydro-oxidation sodium filters to alkalescence, filtrate adds hydrochloric acid and regulates pH value to 2.0, filters, and precipitate is extremely neutral with hot water wash, drain, after a small amount of Diluted Alcohol gradation washing, add an amount of thermosol of ethanol, adding medicinal activated carbon decolours in right amount, filter, filtrate concentrates, and places, separate out amorphous yellow powder, filter, drying is with above-mentioned Pheretima extract mixing, again through 0.1Mpa, under 60 ℃ of conditions, drying is ground into dry powder, and it is standby promptly to get the extract that contains pharmaceutically active ingredient in above-mentioned 2 flavors;
(3) 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 extract and substrate is 1: 3;
(4) according to aforementioned proportion, accurately take by weighing described extract and substrate, be placed in the heating container heating while stirring, standby until the fused solution that obtains containing described extract and substrate and/or emulsion and/or suspension;
(5) temperature control system of adjustment drop pill machine makes the water dropper heating of drop pill machine and maintains the temperature at 50 ℃～90 ℃, and the condensing agent cooling also maintains the temperature at-5 ℃～40 ℃;
When (6) treating that dropping-pill machine head and condensing agent reach described state of temperature respectively, will contain in the fused solution and/or emulsion and/or suspension of described extract and substrate, place in the water dropper jar of drop pill machine, and splash into to shrink in the condensing agent and be shaped promptly.
2. fleabane and earthworm dripping pill as claimed in claim 1 is characterized in that: described condensing agent be methyl-silicone oil or/and liquid paraffin or/and vegetable oil.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100086200A CN100358500C (en) | 2005-02-28 | 2005-02-28 | Fleabane and earthworm dripping pill and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100086200A CN100358500C (en) | 2005-02-28 | 2005-02-28 | Fleabane and earthworm dripping pill and its preparing method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1682818A CN1682818A (en) | 2005-10-19 |
| CN100358500C true CN100358500C (en) | 2008-01-02 |
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| US9585919B2 (en) * | 2013-03-10 | 2017-03-07 | Charles W Moro | Preparation for the treatment of itching and inflammation associated with psoriasis and other topical skin maladies |
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Non-Patent Citations (1)
| Title |
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| 国家中成药标准汇编（中成药地方标准上升国家标准部分）经络肢体 脑系分册. 第267页至268页. 2002 * |
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