CN1709412A - Liver-benefiting dropping pill prepared from total neterosides of swertia mileensis, and its preparing method - Google Patents
Liver-benefiting dropping pill prepared from total neterosides of swertia mileensis, and its preparing method Download PDFInfo
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- CN1709412A CN1709412A CN 200510075165 CN200510075165A CN1709412A CN 1709412 A CN1709412 A CN 1709412A CN 200510075165 CN200510075165 CN 200510075165 CN 200510075165 A CN200510075165 A CN 200510075165A CN 1709412 A CN1709412 A CN 1709412A
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Abstract
The present invention discloses a Chinese medicine composition with the actions of soothing liver and strengthening spleen for curing hepatitis. Said Chinese medicine composition can be made into oral preparation Ligankang dripping pills, and is made up by using Chinese medicine extract swertia mileensis total glucoside as raw material and medicinal carrier as matrix through a certain preparation process.
Description
Technical field
The present invention relates to a kind of the liver soothing and the spleen invigorating effect that has, be used for the treatment of the pharmaceutical composition of hepatitis, is a kind of drug composition oral preparation that feedstock production forms with the Chinese medicine extract Herba Swertiae Mileensis total glycosides particularly.
Background technology
The liver-benefiting sheet that is prepared from according to the preparation method that provides among the national drug standards WS-10997 (ZD-0997)-2002, it is a kind of the liver soothing and the spleen invigorating effect that has, the oral tablet that is used for the treatment of hepatitis, through clinical verification, determined curative effect is the common drug that clinical and family is used for the treatment of above-mentioned disease.
Below be prescription and technology and the brief description that provides among the drug standard WS-10997 (ZD-0997)-2002:
Prescription: Herba Swertiae Mileensis total glycosides 76g (coated tablet) or 152g (Film coated tablets), starch 118g (coated tablet) or 197g (Film coated tablets), magnesium stearate 6g (coated tablet) or 11g (Film coated tablets)
Method for making: get Herba Swertiae Mileensis total glycosides, add starch and magnesium stearate, mixing is made granule, drying, and tabletting, sugar coating or film-coat, promptly.
Function cures mainly: the liver soothing and the spleen invigorating.Be used for acute and chronic hepatitis and belong to syndrome of stagnation of liver qi and spleen deficiency.
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 is as tablet, capsule, granule (electuary) etc., in preparation process because the technology of granulation is arranged, therefore can produce bigger dust pollution, can staff's health be worked the mischief to a certain extent, also can cause certain pollution simultaneously to environment.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 is to replenish the existing deficiency that is used for the treatment of the oral drug preparation of hepatitis, and a kind of bioavailability height is provided, and has a quick release, produce effects fast, medicament contg height, taking convenience, cheap, and free of contamination aborning oral formulations liver-benefiting drop pill.Liver-benefiting drop pill involved in the present invention is a raw material with the Chinese medicine extract Herba Swertiae Mileensis total glycosides, is prepared from the pharmaceutically suitable carrier as substrate.
Be prepared by the following technical solutions, can obtain liver-benefiting drop pill involved in the present invention:
[preparation method]
1. medicine material: Herba Swertiae Mileensis total glycosides (drug extract that contains Chinese medicine Herba Swertiae Mileensis effective ingredient)
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 (Herba Swertiae Mileensis total glycosides): substrate=1: 1～1: 9;
4. according to the given ratio of prescription, accurately take by weighing drug extract (Herba Swertiae Mileensis total glycosides) and substrate, be placed in the heating container heating while stirring, standby until the fused solution that obtains containing drug extract (Herba Swertiae Mileensis total glycosides) 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 that the temperature of condensing agent in dropping-pill machine head and the condensation column is stable respectively and reaching desired state of temperature, to contain the fused solution of drug extract (Herba Swertiae Mileensis total glycosides) and substrate and/or emulsion and/or suspension places 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-benefiting sheet that is prepared from according to the preparation method that provides among the national drug standards WS-10997 (ZD-0997)-2002, it is a kind of the liver soothing and the spleen invigorating effect that has, the oral tablet that is used for the treatment of hepatitis, through clinical verification, determined curative effect is the common drug that clinical and family is used for the treatment of above-mentioned 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.In addition, conventional peroral dosage form is as tablet, capsule, granule (electuary) etc., in preparation process because the technology of granulation is arranged, therefore can produce bigger dust pollution, can staff's health be worked the mischief to a certain extent, also can cause certain pollution simultaneously to environment.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.
Liver-benefiting drop pill involved in the present invention is compared with the liver-benefiting sheet has following beneficial effect:
1. liver-benefiting drop pill involved in the present invention; utilize surfactant to be substrate; make solid dispersion with the Chinese medicine extract Herba Swertiae Mileensis total glycosides, make medicine be molecule, colloid or microcrystalline state and be scattered in the substrate, the total surface area of medicine increases; and substrate is hydrophilic; 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.
2. liver-benefiting drop 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-benefiting drop 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.
The specific embodiment
Now with several groups of specific embodiments, be described further with regard to the preparation method of liver-benefiting drop pill of the present invention.
[first group: the test of single-matrix]
1. raw material: Herba Swertiae Mileensis total glycosides (drug extract that contains Chinese medicine Herba Swertiae Mileensis effective ingredient);
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 (Herba Swertiae Mileensis total glycosides): substrate=1: 1～1: 9;
4. the process that provides according to [preparation method] 4～7 is prepared, and can obtain the liver-benefiting drop pill of different size.
[result of the test]
Test 1: for observe drug extract (Herba Swertiae Mileensis total glycosides) and different substrates when 1: 1 the proportioning prepared liver-benefiting drop pill in qualitative difference, according to 1: 1 ratio, with drug extract (Herba Swertiae Mileensis total glycosides) 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 (Herba Swertiae Mileensis total glycosides) and different substrates, and obtain 13 groups of different experimental results and see Table 1.
Test 2: for observe drug extract (Herba Swertiae Mileensis total glycosides) and different substrates when 1: 3 the proportioning prepared liver-benefiting drop pill in qualitative difference, according to 1: 3 ratio, with drug extract (Herba Swertiae Mileensis total glycosides) 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 (Herba Swertiae Mileensis total glycosides) and different substrates, and obtain 13 groups of different experimental results and see Table 2.
Test 3: for observe drug extract (Herba Swertiae Mileensis total glycosides) and different substrates when 1: 9 the proportioning prepared liver-benefiting drop pill in qualitative difference, according to 1: 9 ratio, with drug extract (Herba Swertiae Mileensis total glycosides) 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 (Herba Swertiae Mileensis total glycosides) and different substrates, and obtain 13 groups of different experimental results and see Table 3.
[second group: the test of mixed-matrix]
1. raw material: Herba Swertiae Mileensis total glycosides (drug extract that contains Chinese medicine Herba Swertiae Mileensis effective ingredient);
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 (Herba Swertiae Mileensis total glycosides): substrate=1: 1～1: 9;
4. the process that provides according to [preparation method] 4～7 is prepared, and can obtain the liver-benefiting drop pill of different size.
[result of the test]
Test 4: in order to observe the mass discrepancy of drug extract (Herba Swertiae Mileensis total glycosides) and mixed-matrix prepared liver-benefiting drop pill when 1: 1 the 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 (Herba Swertiae Mileensis total glycosides) are mixed again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the pharmaceutical composition experiment that 4 drug extracts (Herba Swertiae Mileensis total glycosides) and mixed-matrix are constituted, and obtain 4 groups of different experiments and the results are shown in Table 4.
Test 5: in order to observe the mass discrepancy of drug extract (Herba Swertiae Mileensis total glycosides) and mixed-matrix prepared liver-benefiting drop pill when 1: 3 the 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 (Herba Swertiae Mileensis total glycosides) are mixed again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the pharmaceutical composition experiment that 4 drug extracts (Herba Swertiae Mileensis total glycosides) and mixed-matrix are constituted, and obtain 4 groups of different experiments and the results are shown in Table 5.
Test 6: in order to observe the mass discrepancy of drug extract (Herba Swertiae Mileensis total glycosides) and mixed-matrix prepared liver-benefiting drop pill when 1: 9 the 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 (Herba Swertiae Mileensis total glycosides) are mixed again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the pharmaceutical composition experiment that 4 drug extracts (Herba Swertiae Mileensis total glycosides) and mixed-matrix are constituted, and obtain 4 groups of different experiments and the results are shown in Table 6.
Test 7: in order to observe the mass discrepancy of drug extract (Herba Swertiae Mileensis total glycosides) and mixed-matrix prepared liver-benefiting drop pill when 1: 1 the 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 (Herba Swertiae Mileensis total glycosides) are mixed again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the pharmaceutical composition experiment that 4 drug extracts (Herba Swertiae Mileensis total glycosides) and mixed-matrix are constituted, and obtain 4 groups of different experiments and the results are shown in Table 7.
Test 8: in order to observe the mass discrepancy of drug extract (Herba Swertiae Mileensis total glycosides) and mixed-matrix prepared liver-benefiting drop pill when 1: 3 the 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 (Herba Swertiae Mileensis total glycosides) are mixed again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the pharmaceutical composition experiment that 4 drug extracts (Herba Swertiae Mileensis total glycosides) and mixed-matrix are constituted, and obtain 4 groups of different experiments and the results are shown in Table 8.
Test 9: in order to observe the mass discrepancy of drug extract (Herba Swertiae Mileensis total glycosides) and mixed-matrix prepared liver-benefiting drop pill when 1: 9 the 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 (Herba Swertiae Mileensis total glycosides) are mixed again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the pharmaceutical composition experiment that 4 drug extracts (Herba Swertiae Mileensis total glycosides) and mixed-matrix are constituted, and obtain 4 groups of different experiments and the results are shown in Table 9.
Test 10: in order to observe the mass discrepancy of drug extract (Herba Swertiae Mileensis total glycosides) and mixed-matrix prepared liver-benefiting drop pill when 1: 1 the 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 (Herba Swertiae Mileensis total glycosides) 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 pharmaceutical composition experiment that 4 drug extracts (Herba Swertiae Mileensis total glycosides) and mixed-matrix are 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 (Herba Swertiae Mileensis total glycosides) and mixed-matrix prepared liver-benefiting drop pill when 1: 3 the 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 (Herba Swertiae Mileensis total glycosides) 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 pharmaceutical composition experiment that 4 drug extracts (Herba Swertiae Mileensis total glycosides) and mixed-matrix are 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 (Herba Swertiae Mileensis total glycosides) and mixed-matrix prepared liver-benefiting drop pill when 1: 9 the 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: 9 ratio drug extract (Herba Swertiae Mileensis total glycosides) 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 pharmaceutical composition experiment that 4 drug extracts (Herba Swertiae Mileensis total glycosides) and mixed-matrix are 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 | ????69 | ????＜30 | ????＞10 | + |
| Polyethylene Glycol 4000 | ????50.0 | ????85 | ????＜30 | ????＞10 | + |
| Polyethylene Glycol 6000 | ????50.0 | ????85 | ????＜30 | ????＞10 | + |
| Polyethylene Glycol 10000 | ????50.0 | ????85 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 20000 | ????50.0 | ????84 | ????＜30 | ????＞10 | ++ |
| Span 40 | ????50.0 | ????63 | ????＜30 | ????＞10 | ++ |
| Polyoxyethylene stearate 40 esters | ????50.0 | ????78 | ????＜30 | ????＞10 | ++ |
| Poloxamer | ????50.0 | ????78 | ????＜30 | ????＞10 | ++ |
| Sodium lauryl sulphate | ????50.0 | ????75 | ????＞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 | ????60 | ????＞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 | ????73 | ????＜30 | ????＞10 | + |
| Polyethylene Glycol 4000 | ????25.0 | ????88 | ????＜30 | ????＜10 | ++ |
| Polyethylene Glycol 6000 | ????25.0 | ????88 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 10000 | ????25.0 | ????88 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 20000 | ????25.0 | ????87 | ????＜30 | ????＜10 | +++ |
| Span 40 | ????25.0 | ????75 | ????＜30 | ????＞10 | +++ |
| Polyoxyethylene stearate 40 esters | ????25.0 | ????87 | ????＜30 | ????＜10 | ++ |
| Poloxamer | ????25.0 | ????87 | ????＜30 | ????＜10 | +++ |
| Sodium lauryl sulphate | ????25.0 | ????73 | ????＜30 | ????＞10 | ++ |
| Stearic acid | ????25.0 | ????75 | ????＞30 | ????＞10 | +++ |
| Sodium stearate | ????25.0 | ????74 | ????＞30 | ????＞10 | +++ |
| Glycerin gelatine | ????25.0 | ????73 | ????＞30 | ????＞10 | +++ |
| Lac | ????25.0 | ????73 | ????＞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 | ????90 | ????＜30 | ????＜10 | ++ |
| Polyethylene Glycol 6000 | ????10.0 | ????90 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 10000 | ????10.0 | ????90 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 20000 | ????10.0 | ????89 | ????＜30 | ????＜10 | +++ |
| Span 40 | ????10.0 | ????73 | ????＜30 | ????＜10 | +++ |
| Polyoxyethylene stearate 40 esters | ????10.0 | ????87 | ????＜30 | ????＜10 | ++ |
| Poloxamer | ????10.0 | ????89 | ????＜30 | ????＜10 | +++ |
| Sodium lauryl sulphate | ????10.0 | ????78 | ????＜30 | ????＞10 | +++ |
| Stearic acid | ????10.0 | ????77 | ????＞30 | ????＞10 | +++ |
| Sodium stearate | ????10.0 | ????75 | ????＞30 | ????＞10 | +++ |
| Glycerin gelatine | ????10.0 | ????73 | ????＞30 | ????＞10 | +++ |
| Lac | ????10.0 | ????73 | ????＞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 | ????83 | ????＜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 | ????77 | ????＜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 | ????90 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ????25 | ????89 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ????25 | ????84 | ????＜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 | ????91 | ????＜30 | ????＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | ????10 | ????90 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ????10 | ????90 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ????10 | ????84 | ????＜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 | ????91 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ????50 | ????90 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ????50 | ????86 | ????＜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 | ????92 | ????＜30 | ????＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | ????25 | ????91 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ????25 | ????90 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ????25 | ????88 | ????＜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 | ????1?0 | ????92 | ????＜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 | ????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 | ????90 | ????＜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 | ????87 | ????＜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 | ????92 | ????＜30 | ????＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | ????25 | ????90 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | ????25 | ????89 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | ????25 | ????86 | ????＜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 | ????92 | ????＜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 | ????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 (5)
1. a pharmaceutical composition liver-benefiting drop pill that is used for the treatment of hepatitis is a raw material with the Chinese medicine extract Herba Swertiae Mileensis total glycosides, be prepared from pharmaceutically suitable carrier as substrate, wherein:
1.1 substrate: 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, above-mentioned carrier one or more mixture wherein;
1.2 proportioning: with g or kg is unit, by weight, and drug extract: substrate=1: 1～1: 9.
2. liver-benefiting drop pill as claimed in claim 1 is characterized in that: described substrate is the mixture of Polyethylene Glycol and polyoxyethylene stearate 40 esters or Polyethylene Glycol and poloxamer or Polyethylene Glycol and carboxymethyl starch sodium or Polyethylene Glycol and betacyclodextrin; With g or kg is unit, and by weight, its mixed proportion is 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. any liver-benefiting drop pill as claimed in claim 1 or 2 is characterized in that: the mixed proportion of described drug extract and substrate is 1: 1～1: 5.
4. the preparation method of a liver-benefiting drop pill is characterized in that being made of following process:
4.1 medicine material: Herba Swertiae Mileensis total glycosides
4.2 substrate: 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, above-mentioned carrier one or more mixture wherein;
4.3 proportioning: with g or kg is unit, by weight, and Herba Swertiae Mileensis total glycosides: substrate=1: 1～1: 9;
4.4, accurately take by weighing Herba Swertiae Mileensis total glycosides and substrate according to the given ratio of prescription, be placed on heating while stirring in the heating container, standby until the fused solution that obtains containing Herba Swertiae Mileensis total glycosides and substrate and/or emulsion and/or suspension;
4.5 adjust the temperature control system of 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 ℃;
4.6 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 Herba Swertiae Mileensis total glycosides and substrate, place in the water dropper jar of drop pill machine, splash in the condensing agent and shrink molding promptly.
5. as the preparation method of liver-benefiting drop pill as described in the claim 4, it 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 |
|---|---|---|---|
| CNB2005100751656A CN1315468C (en) | 2005-06-10 | 2005-06-10 | Liver-benefiting dropping pill prepared from total neterosides of swertia mileensis, and its preparing method |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100751656A CN1315468C (en) | 2005-06-10 | 2005-06-10 | Liver-benefiting dropping pill prepared from total neterosides of swertia mileensis, and its preparing method |
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| CN1709412A true CN1709412A (en) | 2005-12-21 |
| CN1315468C CN1315468C (en) | 2007-05-16 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102293794A (en) * | 2010-06-22 | 2011-12-28 | 上海雷允上科技发展有限公司 | Subing pill preparation and preparation thereof |
| CN102532156A (en) * | 2010-12-15 | 2012-07-04 | 中国科学院昆明植物研究所 | Swerilactones H-K, 1-4 and medicinal composition and application thereof |
-
2005
- 2005-06-10 CN CNB2005100751656A patent/CN1315468C/en not_active Expired - Fee Related
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102293794A (en) * | 2010-06-22 | 2011-12-28 | 上海雷允上科技发展有限公司 | Subing pill preparation and preparation thereof |
| CN102532156A (en) * | 2010-12-15 | 2012-07-04 | 中国科学院昆明植物研究所 | Swerilactones H-K, 1-4 and medicinal composition and application thereof |
| CN102532156B (en) * | 2010-12-15 | 2013-11-06 | 中国科学院昆明植物研究所 | Swerilactones H-K, 1-4 and medicinal composition and application thereof |
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|---|---|
| CN1315468C (en) | 2007-05-16 |
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