CN1315467C - liver-clearing dropping pill for treating hepatitis and its preparing method - Google Patents
liver-clearing dropping pill for treating hepatitis and its preparing method Download PDFInfo
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- CN1315467C CN1315467C CNB2005100751641A CN200510075164A CN1315467C CN 1315467 C CN1315467 C CN 1315467C CN B2005100751641 A CNB2005100751641 A CN B2005100751641A CN 200510075164 A CN200510075164 A CN 200510075164A CN 1315467 C CN1315467 C CN 1315467C
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Abstract
The present invention discloses a medicinal composition for curing acute hepatitis, which has the functions of clearing away heat and promoting diuresis. The purposes of the present invention comprise supplementing the defects of the existing oral medicine preparations for curing acute hepatitis and providing a liver-clearing dropping pill with the advantages of high bioavailability, quick medicine release, rapid effect, high medicine content, precise administration dose, low price, no acute anaphylactic reaction or adverse reaction, convenient transportation and portability. The liver-clearing dropping pill of the present invention is prepared from the raw materials of the extractives of the active ingredients of three traditional Chinese medicines, such as isatis root, Virgate Wormwood Herb and licorice root, and medicinal base material.
Description
Technical field
The present invention relates to a kind of clearing away heat-damp and promoting diuresis effect that has, be used for the pharmaceutical composition of acute hepatitis treatment, is a kind of oral formulations that feedstock production forms with the extract that contains 3 flavor active ingredient of Chinese herbs such as Radix Isatidis, Herba Artemisiae Scopariae, Radix Glycyrrhizae particularly.
Background technology
The liver heat removing injection that is prepared from according to the system each side method that provides among the national drug standards WS-11308 (ZD-1308)-2002 is a kind of clearing away heat-damp and promoting diuresis effect that has, the pure Chinese medicine injection that is used for the acute hepatitis treatment, through clinical verification, determined curative effect is the common drug that clinical and family is used for the treatment of this type of disease.
Below be prescription and technology and the brief description that provides among the drug standard WS-11308 (ZD-1308)-2002:
Prescription: Radix Isatidis 500g, Herba Artemisiae Scopariae 250g, Radix Glycyrrhizae 50g, polyoxyethylene sorbitan monoleate g/10ml, sodium sulfite 2g
Method for making: above three flavor medical materials, Herba Artemisiae Scopariae added water infiltration 30 minutes, with the steam distillation distillation, collected distillate 800ml, and redistillation is once collected re-distilled liquid 250ml, and is standby; Get Radix Isatidis, Radix Glycyrrhizae decocts with water secondary, and 2 hours for the first time, 1 hour for the second time, collecting decoction filters, and filtrate decompression is concentrated into the clear paste that relative density is 1.17～1.20 (50 ℃), put coldly, add ethanol and make and contain alcohol amount and reach 60%, stir evenly, left standstill 24 hours, and filtered filtrate recycling ethanol, cold preservation 48 hours filters, and filtrate adds active carbon 0.5g, boiled 30 minutes, cold preservation 24 hours filters, and filtrate adds above-mentioned re-distilled liquid, polyoxyethylene sorbitan monoleate, sodium sulfite, regulate pH value to 6.0～6.5 with sodium hydroxide test solution, add the injection water to ormal weight, filter embedding, sterilization, promptly.
Function cures mainly: clearing away heat-damp and promoting diuresis; Be used for jaundice and the non-icteric type acute hepatitis belongs to syndrome of dampness-heat of liver and gallbladder.
Owing to reasons such as technologies of preparing, the research of the compatibility of Chinese medicine injection can not show a candle to Western medicine, and causes allergy easily.Existing FUFANG BANBIANLIAN ZHUSHEYE does not still have similar other dosage form listings at present.This kind Chinese medicine is an effective component extracting from Chinese crude drug, the intravital concentrated solution of Gong the injection of making.Because the extensive use of modern biotechnology in the natural drug exploitation, the domestic herbal species that is used to inject is more and more, and application is more and more wider clinically, and adverse reaction rate also increases.According to data: the dosage form of Chinese patent medicine adverse reaction rate is that injection accounts for 31% successively, tablet accounts for 24%, pill accounts for 10%.Chinese medicine untoward reaction consequence is serious, and Chinese medicine and preparation thereof cause anaphylactic shock and rank first place, and the trend that increases is arranged year by year, this with use clinically more relevant.Chinese medicine composition more complicated is injected human body with this mixture from blood vessel, forces human body to go metabolism, and itself has just had potential danger, if again with the other medicines compatibility, contingent reaction often is difficult to prediction.The compatibility difficulty of Chinese medicine is bigger, and incompatibility is studied the compatibility of Chinese medicine without ready patterns to follow, and it is perfect also to can not show a candle to Western medicine.Chinese medicine injection causes allergy easily, and reason is to contain albumen, polysaccharide, polypeptide etc. in its composition; The purity of extracting is not enough; Plurality of Chinese is extracted, and each composition interacts; Contain cosolvent, solubilizing agent etc.
In addition, the oral formulations of the oral formulations of most drug, especially Chinese medicine exists 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.Simultaneously, conventional peroral dosage form, regular meeting produces 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.The production technology of conventional oral formulations is more complicated also, and 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 oral drug preparation of acute hepatitis treatment, a kind of bioavailability height is provided, and has a quick release, produce effects fast, medicament contg height, take accurate measurement, cheap, no acute allergic reaction or untoward reaction, and be convenient to the liver-clearing dropping pill that transports and carry.Liver-clearing dropping pill involved in the present invention is a raw material with the extract that contains 3 flavor active ingredient of Chinese herbs such as Radix Isatidis, Herba Artemisiae Scopariae, Radix Glycyrrhizae, is prepared from pharmaceutically acceptable substrate.
Be prepared by the following technical solutions, can obtain liver-clearing dropping pill involved in the present invention:
[preparation method]
1. the preparation of drug extract: get Radix Isatidis 500g, Herba Artemisiae Scopariae 250g, Radix Glycyrrhizae 50g, more than three flavor medical materials, Herba Artemisiae Scopariae added water infiltration 30 minutes, with steam distillation distillation, collected distillate 800ml, redistillation is once collected re-distilled liquid 250ml, and is standby; Get Radix Isatidis, Radix Glycyrrhizae decocts with water secondary, 2 hours for the first time, 1 hour for the second time, collecting decoction filters, and it is 1.17～1.20 clear paste that filtrate decompression is concentrated into relative density, put coldly, add ethanol and make and contain alcohol amount and reach 60%, stir evenly, left standstill 24 hours, and filtered filtrate recycling ethanol, add above-mentioned distillate, being decompressed to 0.1MPa, being condensed into relative density below 60 ℃ is 1.3～1.35 thick paste, or continues to make under the same conditions drying, be ground into dry powder, promptly;
2. substrate: the mixture of one or more in pharmaceutically suitable carrier such as polyethylene glycols, sorbitol anhydride class, polyoxyethylene sorbitol acid anhydride class, 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 drug extract: substrate=1: 1～1: 9;
4. 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;
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 (50～90) ℃, 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, fused solution and/or the emulsion and/or the suspension that will contain drug extract 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.
[beneficial effect]
The liver heat removing injection that is prepared from according to the preparation method that provides among the national drug standards WS-11308 (ZD-1308)-2002 is a kind of clearing away heat-damp and promoting diuresis effect that has, the pure Chinese medicine injection that is used for the acute hepatitis treatment, through clinical verification, determined curative effect is the common drug that clinical and family is used for the treatment of this type of disease.
Owing to reasons such as technologies of preparing, the research of the compatibility of Chinese medicine injection can not show a candle to Western medicine, and causes allergy easily.Existing FUFANG BANBIANLIAN ZHUSHEYE does not still have similar other dosage form listings at present.This kind Chinese medicine is an effective component extracting from Chinese crude drug, the intravital concentrated solution of Gong the injection of making.Because the extensive use of modern biotechnology in the natural drug exploitation, the domestic herbal species that is used to inject is more and more, and application is more and more wider clinically, and adverse reaction rate also increases.According to data: the dosage form of Chinese patent medicine adverse reaction rate is that injection accounts for 31% successively, tablet accounts for 24%, pill accounts for 10%.Chinese medicine untoward reaction consequence is serious, and Chinese medicine and preparation thereof cause anaphylactic shock and rank first place, and the trend that increases is arranged year by year, this with use clinically more relevant.Chinese medicine composition more complicated is injected human body with this mixture from blood vessel, forces human body to go metabolism, and itself has just had potential danger, if again with the other medicines compatibility, contingent reaction often is difficult to prediction.The compatibility difficulty of Chinese medicine is bigger, and incompatibility is studied the compatibility of Chinese medicine without ready patterns to follow, and it is perfect also to can not show a candle to Western medicine.Chinese medicine injection causes allergy easily, and reason is to contain albumen, polysaccharide, polypeptide etc. in its composition; The purity of extracting is not enough; Plurality of Chinese is extracted, and each composition interacts; Contain cosolvent, solubilizing agent etc.
In addition, the oral formulations of the oral formulations of most drug, especially Chinese medicine exists 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.Simultaneously, conventional peroral dosage form, regular meeting produces 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.The production technology of conventional oral formulations is more complicated also, and 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.
Liver-clearing dropping pill involved in the present invention is compared the following beneficial effect of tool with the liver heat removing injection:
1. liver-clearing dropping pill involved in the present invention; utilize surfactant to be substrate; make solid dispersion with the extract that contains 3 flavor active ingredient of Chinese herbs such as Radix Isatidis, Herba Artemisiae Scopariae, Radix Glycyrrhizae; 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.
2. liver-clearing dropping pill involved in the present invention, contact promptly with saliva and to dissolve rapidly, and absorb by oral mucosa, not only rapid-action, and the influence of not taken food, promptly all can containing take after meal ante cibum, can not produce any residual harmful substance at gastric yet, thereby make that patient's medication is safer, also have medication convenience, characteristic of accurate simultaneously.
3. liver-clearing dropping 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. liver-clearing dropping pill involved in the present invention, stable in properties than injection, has the anaphylaxis of not being prone to, and side effect is little, also has advantages such as high bioavailability simultaneously.
5. 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.
6. 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.
The specific embodiment
Now with several groups of specific embodiments, be described further with regard to the preparation method of liver-clearing dropping pill of the present invention.
[first group: the test of single-matrix]
1. the preparation of drug extract: it is standby to make the extract dry powder that contains 3 flavor active ingredient of Chinese herbs such as Radix Isatidis, Herba Artemisiae Scopariae, Radix Glycyrrhizae in advance according to [preparation method 1];
2. substrate: Polyethylene Glycol
1000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, Polyethylene Glycol
10000, Polyethylene Glycol
20000, span 40, polyoxyethylene stearate 40 esters, poloxamer, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac;
3. proportioning: with g or kg is unit, by weight, and drug extract: substrate=1: 1～1: 9;
4. the process that provides according to [preparation method] 4～7 is prepared, and can obtain the liver-clearing dropping pill of different size.
[result of the test]
Test 1: for observe drug extract and different substrates when 1: 1 the proportioning prepared liver-clearing dropping pill in qualitative difference, according to 1: 1 ratio, with drug extract respectively with Polyethylene Glycol
1000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, Polyethylene Glycol
10000, Polyethylene Glycol
20000, pharmaceutically suitable carrier such as span 40, polyoxyethylene stearate 40 esters, poloxamer, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac matches, be prepared according to the step of stipulating in the preparation method, can obtain 13 pharmaceutical compositions experiments that contain drug extract and different substrates, and obtain 13 groups of different experimental results and see Table 1.
Test 2: for observe drug extract and different substrates when 1: 3 the proportioning prepared liver-clearing dropping pill in qualitative difference, according to 1: 3 ratio, with drug extract respectively with Polyethylene Glycol
1000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, Polyethylene Glycol
10000, Polyethylene Glycol
20000, pharmaceutically suitable carrier such as span 40, polyoxyethylene stearate 40 esters, poloxamer, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac matches, be prepared according to the step of stipulating in the preparation method, can obtain 13 pharmaceutical compositions experiments that contain drug extract and different substrates, and obtain 13 groups of different experimental results and see Table 2.
Test 3: for observe drug extract and different substrates when 1: 9 the proportioning prepared liver-clearing dropping pill in qualitative difference, according to 1: 9 ratio, with drug extract respectively with Polyethylene Glycol
1000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, Polyethylene Glycol
10000, Polyethylene Glycol
20000, pharmaceutically suitable carrier such as span 40, polyoxyethylene stearate 40 esters, poloxamer, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac matches, be prepared according to the step of stipulating in the preparation method, can obtain 13 pharmaceutical compositions experiments that contain drug extract and different substrates, and obtain 13 groups of different experimental results and see Table 3.
[second group: the test of mixed-matrix]
1. the preparation of drug extract: it is standby to make the extract dry powder that contains 3 flavor active ingredient of Chinese herbs such as Radix Isatidis, Herba Artemisiae Scopariae, Radix Glycyrrhizae in advance according to [preparation method 1];
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. proportioning: with g or kg is unit, by weight, and drug extract: substrate=1: 1～1: 9;
4. the process that provides according to [preparation method] 4～7 is prepared, and can obtain the liver-clearing dropping pill of different size.
[result of the test]
Test 4: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained liver-clearing dropping pill when 1: 1 proportioning, 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, according to 1: 1 ratio different with the 4 kinds respectively mixing matrix phases of drug extract are mixed again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 4.
Test 5: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained liver-clearing dropping pill when 1: 3 proportioning, 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, according to 1: 3 ratio different with the 4 kinds respectively mixing matrix phases of drug extract are mixed again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 5.
Test 6: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained liver-clearing dropping pill when 1: 9 proportioning, 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, according to 1: 9 ratio different with the 4 kinds respectively mixing matrix phases of drug extract are mixed again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 6.
Test 7: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained liver-clearing dropping pill when 1: 1 proportioning, 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, according to 1: 1 ratio different with the 4 kinds respectively mixing matrix phases of drug extract are mixed again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 7.
Test 8: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained liver-clearing dropping pill when 1: 3 proportioning, 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, according to 1: 3 ratio different with the 4 kinds respectively mixing matrix phases of drug extract are mixed again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 8.
Test 9: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained liver-clearing dropping pill when 1: 9 proportioning, 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, according to 1: 9 ratio different with the 4 kinds respectively mixing matrix phases of drug extract are mixed again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 9.
Test 10: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained liver-clearing dropping pill when 1: 1 proportioning, 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, according to 1: 1 ratio drug extract is mixed mutually with 4 kinds of different mixed-matrixes respectively again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experiments and the results are shown in Table 10.
Test 11: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained liver-clearing dropping pill when 1: 3 proportioning, 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, according to 1: 3 ratio drug extract is mixed mutually with 4 kinds of different mixed-matrixes respectively again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experiments and the results are shown in Table 11.
Test 12: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained liver-clearing dropping pill when 1: 9 proportioning, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, doubly 4 kinds of carriers such as his bad dextrin respectively with Polyethylene Glycol with 1: 10 mixed evenly as mixed-matrix, according to 1: 9 ratio drug extract is mixed mutually with 4 kinds of different mixed-matrixes respectively again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experiments and the results are shown in 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 1000 | 50.0 | 65 | ＜30 | ＞10 | + |
| Polyethylene Glycol 4000 | 50.0 | 81 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 6000 | 50.0 | 82 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 10000 | 50.0 | 83 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 20000 | 50.0 | 83 | ＜30 | ＞10 | ++ |
| Span 40 | 50.0 | 60 | ＜30 | ＞10 | ++ |
| Polyoxyethylene stearate 40 esters | 50.0 | 81 | ＜30 | ＞10 | + |
| Poloxamer | 50.0 | 82 | ＜30 | ＞10 | + |
| Sodium lauryl sulphate | 50.0 | 62 | ＞30 | ＞10 | ++ |
| Stearic acid | 50.0 | 61 | ＞30 | ＞10 | ++ |
| Sodium stearate | 50.0 | 61 | ＞30 | ＞10 | + |
| Glycerin gelatine | 50.0 | 60 | ＞30 | ＞10 | + |
| Lac | 50.0 | 59 | ＞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 1000 | 25.0 | 78 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 4000 | 25.0 | 87 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 6000 | 25.0 | 88 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 10000 | 25.0 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 20000 | 25.0 | 90 | ＜30 | ＜10 | +++ |
| Span 40 | 25.0 | 63 | ＜30 | ＜10 | +++ |
| Polyoxyethylene stearate 40 esters | 25.0 | 81 | ＜30 | ＞10 | ++ |
| Poloxamer | 25.0 | 86 | ＜30 | ＜10 | +++ |
| Sodium lauryl sulphate | 25.0 | 74 | ＞30 | ＞10 | +++ |
| Stearic acid | 25.0 | 73 | ＞30 | ＞10 | +++ |
| Sodium stearate | 25.0 | 72 | ＞30 | ＞10 | +++ |
| Glycerin gelatine | 25.0 | 71 | ＞30 | ＞10 | +++ |
| Lac | 25.0 | 71 | ＞30 | ＞10 | ++ |
The group practices of table 3 drug extract and single-matrix
(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 1000 | 10.0 | 83 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 4000 | 10.0 | 88 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 6000 | 10.0 | 89 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 10000 | 10.0 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 20000 | 10.0 | 91 | ＜30 | ＜10 | +++ |
| Span 40 | 10.0 | 68 | ＜30 | ＜10 | +++ |
| Polyoxyethylene stearate 40 esters | 10.0 | 84 | ＜30 | ＜10 | ++ |
| Poloxamer | 10.0 | 89 | ＜30 | ＜10 | +++ |
| Sodium lauryl sulphate | 10.0 | 75 | ＞30 | ＞10 | +++ |
| Stearic acid | 10.0 | 74 | ＞30 | ＞10 | +++ |
| Sodium stearate | 10.0 | 73 | ＞30 | ＞10 | +++ |
| Glycerin gelatine | 10.0 | 73 | ＞30 | ＞10 | +++ |
| Lac | 10.0 | 72 | ＞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 | 85 | ＜30 | ＞10 | ++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 50 | 84 | ＜30 | ＞10 | ++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 50 | 83 | ＜30 | ＞10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 50 | 76 | ＜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 | 90 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 25 | 89 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 25 | 87 | ＜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 | 90 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 10 | 90 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 10 | 84 | ＜30 | ＞10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 10 | 83 | ＜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 | 91 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 50 | 90 | ＜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 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=l: 5 | 25 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 25 | 89 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 25 | 89 | ＜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 | 91 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 10 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 10 | 90 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 10 | 89 | ＜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 | 91 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | 50 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 50 | 90 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 50 | 88 | ＜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 | 90 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | 25 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 25 | 89 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 25 | 87 | ＜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 | 91 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | 10 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 10 | 90 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 10 | 89 | ＜30 | ＜10 | +++ |
1. can be seen by the result in the table: when the ratio of drug extract 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 drug extract 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 drug extract and substrate is 1: 9, the rounding rate, the ball method of double differences is different and index such as hardness improves 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 liver-clearing dropping pill that is used for the acute hepatitis treatment is a raw material with Radix Isatidis, Herba Artemisiae Scopariae, Radix Glycyrrhizae, is prepared from the pharmaceutically suitable carrier as substrate, it is characterized in that:
(1) get Radix Isatidis 500g, Herba Artemisiae Scopariae 250g, Radix Glycyrrhizae 50g, more than three flavors, Herba Artemisiae Scopariae added water infiltration 30 minutes, use vapor distillation, collected distillate 800ml, redistillation once, collection re-distilled liquid 250ml, standby; Get Radix Isatidis, Radix Glycyrrhizae decocts with water secondary, 2 hours for the first time, 1 hour for the second time, collecting decoction filters, and it is 1.17～1.20 clear paste that filtrate decompression is concentrated into relative density, put cold, add ethanol and make and contain alcohol amount and reach 60%, stir evenly, left standstill 24 hours, filter, filtrate recycling ethanol adds above-mentioned distillate, and being decompressed to 0.1MPa, being condensed into relative density below 60 ℃ is 1.3～1.35 thick paste, or continuation makes drying under the same conditions, be ground into dry powder, promptly get the extract that contains pharmaceutically active ingredient in above-mentioned three 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 the ratio of described extract and substrate is 1: 3;
(3) 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;
(4) 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 40 ℃～-5 ℃;
When (5) treating that dropping-pill machine head and condensing agent reach described state of temperature respectively, will contain the fused solution of described extract and substrate and/or emulsion and/or suspension and place in the water dropper jar of drop pill machine, splash in the condensing agent, shrink molding promptly.
2. liver-clearing dropping 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.
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| Application Number | Priority Date | Filing Date | Title |
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| CNB2005100751641A CN1315467C (en) | 2005-06-10 | 2005-06-10 | liver-clearing dropping pill for treating hepatitis and its preparing method |
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|---|---|---|---|
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| CN1315467C true CN1315467C (en) | 2007-05-16 |
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Non-Patent Citations (3)
| Title |
|---|
| 上海科技出版社 范碧亭等，中药药剂学，第1卷 1997 * |
| 国家药品监督管理局国家中成药标准汇编中成药地方标准上升国家标准部分内科肝胆分册清 2002 * |
| 国家药品监督管理局国家中成药标准汇编中成药地方标准上升国家标准部分内科肝胆分册清 2002;上海科技出版社 范碧亭等，中药药剂学，第1卷 1997 * |
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