CN1686362A - Hairy holly root drip pill and its preparation method - Google Patents
Hairy holly root drip pill and its preparation method Download PDFInfo
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- CN1686362A CN1686362A CN 200510056859 CN200510056859A CN1686362A CN 1686362 A CN1686362 A CN 1686362A CN 200510056859 CN200510056859 CN 200510056859 CN 200510056859 A CN200510056859 A CN 200510056859A CN 1686362 A CN1686362 A CN 1686362A
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Abstract
A Chinese medicine in the form of dripping pill for treating coronary arteriosclerotic heart disease, thromboangiitis obliterans, central retinitis, infantile pneumonia, etc is prepared from pubescent holly root and medicinal carrier. Its preparing process is also disclosed.
Description
Technical field
The present invention relates to a kind of have blood vessel dilating and antibacterial and anti-inflammation functions, be used for the treatment of coronary atherosclerotic heart disease, thromboangiitis obliterans, and be used for central serous chorioretinopathy, the pharmaceutical composition of diseases such as infantile pneumonia, being particularly related to the Radix Ilicis Pubescentis is raw material of Chinese medicine, a kind of drug composition oral preparation that is prepared from the pharmaceutically suitable carrier as substrate.
Background technology
According to drug standard WS promulgated by the ministries or commissions of the Central Government
3The Radix Ilicis Pubescentis capsule that the preparation method that provides among-the B-1290-93 is prepared from, be to be a kind of oral formulations that raw material of Chinese medicine is prepared from the Radix Ilicis Pubescentis, have blood vessel dilating and antibacterial and anti-inflammation functions, be used for the treatment of coronary atherosclerotic heart disease, thromboangiitis obliterans, and be used for central serous chorioretinopathy, the oral capsule of diseases such as infantile pneumonia, 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 drug standard WS
3Prescription that provides among-the B-1290-93 and technology and brief description:
Method for making: get Radix Ilicis Pubescentis and decoct with water twice, 4 hours for the first time, 2 hours for the second time, collecting decoction filters, and filtrate is concentrated into thick paste, put coldly, add ethanol precipitation, filter, filtrate recycling ethanol is concentrated into the thick paste shape, cold drying, be ground into fine powder, adding starch is an amount of, mixing, incapsulate, promptly.
Function cures mainly: Drugs for Cardiovascular Diseases, blood vessel dilating and antibacterial and anti-inflammation functions are arranged, and be used for coronary atherosclerotic heart disease, rhomboembolia type fat Guan Yan, and be used for central serous chorioretinopathy, infantile pneumonia.
Owing to reasons such as technologies of preparing, the oral formulations of most drug, especially oral preparation of Chinese traditional medicinal, 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 coronary atherosclerotic heart disease that is used for the treatment of, thromboangiitis obliterans, and being used for central serous chorioretinopathy, the deficiency of the oral drug preparation of diseases such as infantile pneumonia provides a kind of bioavailability height, and has a quick release, produce effects is cheap fast, and free of contamination aborning drug composition oral preparation hairy holly drop pills.Hairy holly drop pills involved in the present invention is a raw material with the Chinese medicine Radix Ilicis Pubescentis, is prepared from the pharmaceutically suitable carrier as substrate.Be prepared by the following technical solutions, can obtain hairy holly drop pills involved in the present invention:
[preparation method]
1. the preparation of drug extract: get Radix Ilicis Pubescentis and decoct with water twice, the 1 time 4 hours, the 2nd time 2 hours, collecting decoction filters, and filtrate is concentrated into thick paste, put coldly, add ethanol precipitation, filter, filtrate recycling ethanol, below 60 ℃, be decompressed under the 0.1Mpa condition, be concentrated into relative density and be 1.35～1.45 thick paste, or continue to make drying under the same conditions, be ground into dry powder, promptly get drug extract thick paste or dry powder;
2. substrate: Polyethylene Glycol
(1000～20000), 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 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 that the temperature of condensing agent in dropping-pill machine head and the condensation column is stable respectively and reaching desired state of temperature, 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
According to drug standard WS promulgated by the ministries or commissions of the Central Government
3The Radix Ilicis Pubescentis capsule that the preparation method that provides among-the B-1290-93 is prepared from, be to be a kind of oral formulations that raw material of Chinese medicine is prepared from the Radix Ilicis Pubescentis, have blood vessel dilating and antibacterial and anti-inflammation functions, be used for the treatment of coronary atherosclerotic heart disease, thromboangiitis obliterans, and be used for central serous chorioretinopathy, the oral capsule of diseases such as infantile pneumonia, 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 oral formulations of most drug, especially oral preparation of Chinese traditional medicinal, 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.
Hairy holly drop pills involved in the present invention is compared with the Radix Ilicis Pubescentis capsule has following beneficial effect:
1. hairy holly drop pills involved in the present invention; utilize surfactant to be substrate; make solid dispersion with the extract that contains Chinese medicine Radix Ilicis Pubescentis effective ingredient, 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. hairy holly drop pills 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. hairy holly drop pills 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 hairy holly drop pills of the present invention.
First group: the test of single-matrix
1. raw material: it is standby to make the dry powder that contains Chinese medicine Radix Ilicis Pubescentis active pharmaceutical ingredient in advance according to preparation method 1;
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 etc.;
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 hairy holly drop pills of different size.
[result of the test]
Test 1: for observe drug extract and different substrates when 1: 1 the proportioning prepared hairy holly drop pills in qualitative difference, according to 1: 1 ratio, with drug extract 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, be prepared according to the step of stipulating in the preparation method, can obtain 16 pharmaceutical compositions experiments that contain drug extract and different substrates, and obtain 16 groups of different experimental results and see Table 1.
Test 2: for observe drug extract and different substrates when 1: 3 the proportioning prepared hairy holly drop pills in qualitative difference, according to 1: 3 ratio, with drug extract 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, be prepared according to the step of stipulating in the preparation method, can obtain 16 pharmaceutical compositions experiments that contain drug extract and different substrates, and obtain 16 groups of different experimental results and see Table 2.
Test 3: for observe drug extract and different substrates when 1: 9 the proportioning prepared hairy holly drop pills in qualitative difference, according to 1: 9 ratio, with drug extract 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, be prepared according to the step of stipulating in the preparation method, can obtain 16 pharmaceutical compositions experiments that contain drug extract and different substrates, and obtain 16 groups of different experimental results and see Table 3.
Second group: the test of mixed-matrix
1. raw material: it is standby to make the dry powder that contains Chinese medicine Radix Ilicis Pubescentis active pharmaceutical ingredient 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 hairy holly drop pills of different size.
[result of the test]
Test 4: in order to observe the mass discrepancy of drug extract and mixed-matrix prepared hairy holly drop pills 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 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 prepared hairy holly drop pills 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 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 prepared hairy holly drop pills 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 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 prepared hairy holly drop pills 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 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 prepared hairy holly drop pills 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 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 prepared hairy holly drop pills 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 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 prepared hairy holly drop pills 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 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 experimental results and see Table 10.
Test 11: in order to observe the mass discrepancy of drug extract and mixed-matrix prepared hairy holly drop pills 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 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 experimental results and see Table 11.
Test 12: in order to observe the mass discrepancy of drug extract and mixed-matrix prepared hairy holly drop pills 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 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 experimental results and see Table 12.
The group practices of table 1 drug extract and single-matrix
(drug extract: substrate=1: 1)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 1000 | ????50.0 | ????59 | ????＜30 | ????＞10 | + |
| Polyethylene Glycol 2000 | ????50.0 | ????64 | ????＜30 | ????＞10 | + |
| Polyethylene Glycol 4000 | ????50.0 | ????72 | ????＜30 | ????＞10 | + |
| Polyethylene Glycol 6000 | ????50.0 | ????74 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 8000 | ????50.0 | ????74 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 10000 | ????50.0 | ????76 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 20000 | ????50.0 | ????79 | ????＜30 | ????＞10 | ++ |
| Polyoxyethylene stearate 40 esters | ????50.0 | ????76 | ????＜30 | ????＞10 | ++ |
| Betacyclodextrin | ????50.0 | ????69 | ????＜30 | ????＞10 | + |
| Poloxamer | ????50.0 | ????76 | ????＜30 | ????＞10 | ++ |
| Carboxymethyl starch sodium | ????50.0 | ????70 | ????＜30 | ????＞10 | + |
| Sodium lauryl sulphate | ????50.0 | ????73 | ????＞30 | ????＞10 | + |
| Stearic acid | ????50.0 | ????62 | ????＞30 | ????＞10 | ++ |
| Sodium stearate | ????50.0 | ????60 | ????＞30 | ????＞10 | ++ |
| Glycerin gelatine | ????50.0 | ????61 | ????＞30 | ????＞10 | + |
| Lac | ????50.0 | ????65 | ????＞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 | ????67 | ????＜30 | ????＞10 | + |
| Polyethylene Glycol 2000 | ????25.0 | ????84 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 4000 | ????25.0 | ????87 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 6000 | ????25.0 | ????91 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 8000 | ????25.0 | ????90 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 10000 | ????25.0 | ????92 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 20000 | ????25.0 | ????91 | ????＜30 | ????＜10 | +++ |
| Polyoxyethylene stearate 40 esters | ????25.0 | ????90 | ????＜30 | ????＜10 | ++ |
| Betacyclodextrin | ????25.0 | ????82 | ????＜30 | ????＞10 | ++ |
| Poloxamer | ????25.0 | ????88 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium | ????25.0 | ????83 | ????＜30 | ????＞10 | +++ |
| Sodium lauryl sulphate | ????25.0 | ????76 | ????＜30 | ????＞10 | ++ |
| Stearic acid | ????25.0 | ????74 | ????＞30 | ????＞10 | +++ |
| Sodium stearate | ????25.0 | ????71 | ????＞30 | ????＞10 | +++ |
| Glycerin gelatine | ????25.0 | ????71 | ????＞30 | ????＞10 | +++ |
| Lac | ????25.0 | ????74 | ????＞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 | ????66 | ????＜30 | ????＞10 | + |
| Polyethylene Glycol 2000 | ????10.0 | ????81 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 4000 | ????10.0 | ????88 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 6000 | ????10.0 | ????87 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 8000 | ????10.0 | ????91 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 10000 | ????10.0 | ????92 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 20000 | ????10.0 | ????89 | ????＜30 | ????＜10 | +++ |
| Polyoxyethylene stearate 40 esters | ????10.0 | ????91 | ????＜30 | ????＜10 | ++ |
| Betacyclodextrin | ????10.0 | ????84 | ????＜30 | ????＞10 | ++ |
| Poloxamer | ????10.0 | ????87 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium | ????10.0 | ????84 | ????＜30 | ????＞10 | +++ |
| Sodium lauryl sulphate | ????10.0 | ????78 | ????＜30 | ????＞10 | +++ |
| Stearic acid | ????10.0 | ????75 | ????＞30 | ????＞10 | +++ |
| Sodium stearate | ????10.0 | ????76 | ????＞30 | ????＞10 | +++ |
| Glycerin gelatine | ????10.0 | ????73 | ????＞30 | ????＞10 | +++ |
| Lac | ????10.0 | ????75 | ????＞30 | ????＞10 | +++ |
The group practices of table 4 drug extract and mixed-matrix
(drug extract: mixed-matrix=1: 1)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 1 | ????50 | ????85 | ????＜30 | ????＞10 | ++ |
| Poloxamer: Polyethylene Glycol=1: 1 | ????50 | ????83 | ????＜30 | ????＞10 | ++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ????50 | ????81 | ????＜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 | ????87 | ????＜30 | ????＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | ????25 | ????87 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ????25 | ????84 | ????＜30 | ????＞10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ????25 | ????83 | ????＜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 | ????92 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ????10 | ????88 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ????10 | ????86 | ????＜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 | ????90 | ????＜30 | ????＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | ????50 | ????91 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ????50 | ????87 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ????50 | ????89 | ????＜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 | ????90 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ????25 | ????91 | ????＜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 | ????92 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ????10 | ????91 | ????＜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 | ????92 | ????＜30 | ????＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | ????50 | ????91 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | ????50 | ????87 | ????＜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 | ????91 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | ????25 | ????87 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | ????25 | ????89 | ????＜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 | ????92 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | ????10 | ????93 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | ????10 | ????91 | ????＜30 | ????＜10 | +++ |
1. can be seen by the result in the table: when the ratio of 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. one kind is used for the treatment of coronary atherosclerotic heart disease, thromboangiitis obliterans, and be used for central serous chorioretinopathy, the pharmaceutical composition hairy holly drop pills of diseases such as infantile pneumonia, with the Chinese medicine Radix Ilicis Pubescentis is raw material, be prepared from pharmaceutically suitable carrier as substrate, wherein:
1.1 the preparation of drug extract: get Radix Ilicis Pubescentis and decoct with water twice, the 1 time 4 hours, the 2nd time 2 hours, collecting decoction filters, and filtrate is concentrated into thick paste, put cold, add ethanol precipitation, filter filtrate recycling ethanol, below 60 ℃, be decompressed to that to be concentrated into relative density under the 0.1Mpa condition be 1.35～1.45 thick paste, or continue to make drying under the same conditions, and be ground into dry powder, promptly get drug extract thick paste or dry powder;
1.2 substrate: Polyethylene Glycol
(1000～20000), polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac, above-mentioned pharmaceutically suitable carrier one or more mixture wherein;
1.3 proportioning: with g or kg is unit, by weight, and drug extract: substrate=1: 1～1: 9.
2. hairy holly drop pills 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 hairy holly drop pills 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 hairy holly drop pills is characterized in that being made of following process:
4.1 the preparation of drug extract: get Radix Ilicis Pubescentis and decoct with water twice, the 1 time 4 hours, the 2nd time 2 hours, collecting decoction filters, and filtrate is concentrated into thick paste, put cold, add ethanol precipitation, filter filtrate recycling ethanol, below 60 ℃, be decompressed to that to be concentrated into relative density under the 0.1Mpa condition be 1.35～1.45 thick paste, or continue to make drying under the same conditions, and be ground into dry powder, promptly get drug extract thick paste or dry powder;
4.2 substrate: Polyethylene Glycol
(1000～20000), polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac, above-mentioned pharmaceutically suitable carrier one or more mixture wherein;
4.3 proportioning: with g or kg is unit, by weight, and drug extract: substrate=1: 1～1: 9;
4.4, accurately take by weighing drug extract 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 drug extract 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, to contain the fused solution of drug extract and substrate and/or emulsion and/or suspension places in the water dropper jar of drop pill machine, splash in the condensing agent, shrink molding promptly.
5. as the preparation method of hairy holly drop pills 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.
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| CN 200510056859 CN1301098C (en) | 2005-03-28 | 2005-03-28 | Hairy holly root drip pill and its preparation method |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200510056859 CN1301098C (en) | 2005-03-28 | 2005-03-28 | Hairy holly root drip pill and its preparation method |
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| CN1686362A true CN1686362A (en) | 2005-10-26 |
| CN1301098C CN1301098C (en) | 2007-02-21 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101926836A (en) * | 2009-06-27 | 2010-12-29 | 何国增 | Pubescent holly root preparation for treating heart cerebrovascular diseases |
| CN108836986A (en) * | 2018-07-25 | 2018-11-20 | 瑞阳制药有限公司 | Debubbling method is concentrated in ilex pubescens extracting solution |
| CN109846833A (en) * | 2018-12-17 | 2019-06-07 | 江西赣隆药业有限公司 | It is a kind of for treating the ilex pubescens broken wall medicine materical crude slice and preparation method thereof of anemopyretic cold and dyspnea and cough due to lung-heat |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101716200B (en) * | 2009-12-22 | 2012-04-11 | 江西泽众制药股份有限公司 | Pharmaceutical composition for promoting blood circulation, dredging collaterals and clearing away heat and toxic materials, and preparation method and application thereof |
-
2005
- 2005-03-28 CN CN 200510056859 patent/CN1301098C/en not_active Expired - Fee Related
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101926836A (en) * | 2009-06-27 | 2010-12-29 | 何国增 | Pubescent holly root preparation for treating heart cerebrovascular diseases |
| CN108836986A (en) * | 2018-07-25 | 2018-11-20 | 瑞阳制药有限公司 | Debubbling method is concentrated in ilex pubescens extracting solution |
| CN109846833A (en) * | 2018-12-17 | 2019-06-07 | 江西赣隆药业有限公司 | It is a kind of for treating the ilex pubescens broken wall medicine materical crude slice and preparation method thereof of anemopyretic cold and dyspnea and cough due to lung-heat |
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| Publication number | Publication date |
|---|---|
| CN1301098C (en) | 2007-02-21 |
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