CN1686129A - Cepharanthine drip pill and its preparation method - Google Patents
Cepharanthine drip pill and its preparation method Download PDFInfo
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- CN1686129A CN1686129A CN 200510056857 CN200510056857A CN1686129A CN 1686129 A CN1686129 A CN 1686129A CN 200510056857 CN200510056857 CN 200510056857 CN 200510056857 A CN200510056857 A CN 200510056857A CN 1686129 A CN1686129 A CN 1686129A
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Abstract
A dripping pill of stephanine for treating the leukocytopenia caused by radiotherapy and chemicotherapy is prepared from stephanine and medical carrier.
Description
Technical field
The present invention relates to a kind of clearing away heat and cooling blood effect that has, the pharmaceutical composition that is used for the treatment of the leukopenia that tumour patient causes because of radiotherapy chemotherapy, being particularly related to the cepharanthine 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
The stephania sinica Diels tablets that is prepared from according to the preparation method that provides among the drug standard WS-11166 promulgated by the ministries or commissions of the Central Government (ZD-1166)-2002, be to be a kind of oral formulations that raw material of Chinese medicine is prepared from the cepharanthine, has the clearing away heat and cooling blood effect, the oral tablet that is used for the treatment of the leukopenia that tumour patient causes because of radiotherapy chemotherapy, 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 in WS-11166 (ZD-1166)-2002 drug standard:
Method for making: get cepharanthine, add dextrin, starch, mixing adds 5% starch slurry and granulates, and drying adds magnesium stearate, mixing, and tabletting, promptly.
Function cures mainly: clearing away heat and cooling blood.Be used for the leukopenia that tumour patient causes because of radiotherapy chemotherapy.
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 deficiency that is used for the treatment of the oral drug preparation of the diseases such as leukopenia that tumour patient causes because of radiotherapy chemotherapy, a kind of bioavailability height is provided, and has a quick release, quick produce effects, cheap, and free of contamination aborning drug composition oral preparation Cepharanthine drip pill.Cepharanthine drip pill involved in the present invention is a raw material with the Chinese medicine cepharanthine, is prepared from the pharmaceutically suitable carrier as substrate.Be prepared by the following technical solutions, can obtain Cepharanthine drip pill involved in the present invention:
[preparation method]
1. active constituents of medicine: cepharanthine;
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 cepharanthine: substrate=1: 1～1: 9;
4. according to the given ratio of prescription, accurately take by weighing cepharanthine and substrate, be placed on heating while stirring in the heating container, standby until the fused solution that obtains containing cepharanthine 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 cepharanthine 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 stephania sinica Diels tablets that is prepared from according to the preparation method that provides among the drug standard WS-11166 promulgated by the ministries or commissions of the Central Government (ZD-1166)-2002, be to be a kind of oral formulations that raw material of Chinese medicine is prepared from the cepharanthine, has the clearing away heat and cooling blood effect, the oral tablet that is used for the treatment of the leukopenia that tumour patient causes because of radiotherapy chemotherapy, 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.
Cepharanthine drip pill involved in the present invention is compared with stephania sinica Diels tablets has following beneficial effect:
1. Cepharanthine drip pill involved in the present invention; utilize surfactant to be substrate; make solid dispersion with cepharanthine, 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. Cepharanthine drip 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. Cepharanthine drip pill involved in the present invention mixes the dry powder that contains active constituents of medicine mutually with molten matrix, splashes in the not miscible condensed fluid and makes.Therefore, the stability of drug height, not facile hydrolysis, oxidation, and the operation be under liquid state, to carry out, no dust pollution is not subject to the influence of crystal formation, thereby has guaranteed the quality of medicine, has increased stability.
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 Cepharanthine drip pill of the present invention.
First group: the test of single-matrix
1. raw material: cepharanthine;
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 medicine dry powder: substrate=1: 1～1: 9;
4. the process that provides according to [preparation method] 4～7 is prepared, and can obtain the Cepharanthine drip pill of different size.
[result of the test]
Test 1: for observe cepharanthine and different substrates when 1: 1 the proportioning prepared Cepharanthine drip pill in qualitative difference, according to 1: 1 ratio, with cepharanthine 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 cepharanthine and different substrates, and obtain 16 groups of different experimental results and see Table 1.
Test 2: for observe cepharanthine and different substrates when 1: 3 the proportioning prepared Cepharanthine drip pill in qualitative difference, according to 1: 3 ratio, with cepharanthine 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 cepharanthine and different substrates, and obtain 16 groups of different experimental results and see Table 2.
Test 3: for observe cepharanthine and different substrates when 1: 9 the proportioning prepared Cepharanthine drip pill in qualitative difference, according to 1: 9 ratio, with cepharanthine respectively with Polyethylene Glycol
1000, Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, Polyethylene Glycol
G000, 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 cepharanthine 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: cepharanthine;
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 medicine dry powder: substrate=1: 1～1: 9;
4. the process that provides according to [preparation method] 4～7 is prepared, and can obtain the Cepharanthine drip pill of different size.
[result of the test]
Test 4: in order to observe the mass discrepancy of cepharanthine and mixed-matrix prepared Cepharanthine drip 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 cepharanthine 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 cepharanthine 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 cepharanthine and mixed-matrix prepared Cepharanthine drip 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 cepharanthine 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 cepharanthine 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 cepharanthine and mixed-matrix prepared Cepharanthine drip 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 cepharanthine 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 cepharanthine 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 cepharanthine and mixed-matrix prepared Cepharanthine drip 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 cepharanthine 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 cepharanthine 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 cepharanthine and mixed-matrix prepared Cepharanthine drip 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 cepharanthine 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 cepharanthine 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 cepharanthine and mixed-matrix prepared Cepharanthine drip 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 cepharanthine 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 cepharanthine 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 cepharanthine and mixed-matrix prepared Cepharanthine drip 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 cepharanthine 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 cepharanthine 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 cepharanthine and mixed-matrix prepared Cepharanthine drip 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 cepharanthine 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 cepharanthine 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 cepharanthine and mixed-matrix prepared Cepharanthine drip 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 cepharanthine 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 cepharanthine and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 12.
The group practices of table 1 cepharanthine and single-matrix
(cepharanthine: 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 | ????63 | ????＜30 | ????＞10 | + |
| Polyethylene Glycol 4000 | ????50.0 | ????72 | ????＜30 | ????＞10 | + |
| Polyethylene Glycol 6000 | ????50.0 | ????73 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 8000 | ????50.0 | ????74 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 10000 | ????50.0 | ????76 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 20000 | ????50.0 | ????77 | ????＜30 | ????＞10 | ++ |
| Polyoxyethylene stearate 40 esters | ????50.0 | ????76 | ????＜30 | ????＞10 | ++ |
| Betacyclodextrin | ????50.0 | ????69 | ????＜30 | ????＞10 | + |
| Poloxamer | ????50.0 | ????78 | ????＜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 | ????64 | ????＞30 | ????＞10 | ++ |
| Glycerin gelatine | ????50.0 | ????61 | ????＞30 | ????＞10 | + |
| Lac | ????50.0 | ????62 | ????＞30 | ????＞10 | + |
The group practices of table 2 cepharanthine and single-matrix
(cepharanthine: 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 | ????65 | ????＜30 | ????＞10 | + |
| Polyethylene Glycol 2000 | ????25.0 | ????84 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 4000 | ????25.0 | ????86 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 6000 | ????25.0 | ????91 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 8000 | ????25.0 | ????90 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 10000 | ????25.0 | ????91 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 20000 | ????25.0 | ????90 | ????＜30 | ????＜10 | +++ |
| Polyoxyethylene stearate 40 esters | ????25.0 | ????92 | ????＜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 | ????72 | ????＞30 | ????＞10 | +++ |
| Glycerin gelatine | ????25.0 | ????71 | ????＞30 | ????＞10 | +++ |
| Lac | ????25.0 | ????74 | ????＞30 | ????＞10 | +++ |
The group practices of table 3 cepharanthine and single-matrix
(cepharanthine: 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 | ????70 | ????＜30 | ????＞10 | + |
| Polyethylene Glycol 2000 | ????10.0 | ????81 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 4000 | ????10.0 | ????86 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 6000 | ????10.0 | ????91 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 8000 | ????10.0 | ????90 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 10000 | ????10.0 | ????91 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 20000 | ????10.0 | ????92 | ????＜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 | ????77 | ????＞30 | ????＞10 | +++ |
| Sodium stearate | ????10.0 | ????73 | ????＞30 | ????＞10 | +++ |
| Glycerin gelatine | ????10.0 | ????75 | ????＞30 | ????＞10 | +++ |
| Lac | ????10.0 | ????74 | ????＞30 | ????＞10 | +++ |
The group practices of table 4 cepharanthine and mixed-matrix
(cepharanthine: 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 | ????80 | ????＜30 | ????＞10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ????50 | ????77 | ????＜30 | ????＞10 | + |
The group practices of table 5 cepharanthine and mixed-matrix
(cepharanthine: 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 | ????87 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ????25 | ????86 | ????＜30 | ????＞10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ????25 | ????83 | ????＜30 | ????＞10 | ++ |
The group practices of table 6 cepharanthine and mixed-matrix
(cepharanthine: 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 | ????91 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ????10 | ????88 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ????10 | ????87 | ????＜30 | ????＞10 | +++ |
The group practices of table 7 cepharanthine and mixed-matrix
(cepharanthine: 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 | ????89 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ????50 | ????88 | ????＜30 | ????＜10 | ++ |
The group practices of table 8 cepharanthine and mixed-matrix
(cepharanthine: 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 | ????91 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ????25 | ????90 | ????＜30 | ????＜10 | +++ |
The group practices of table 9 cepharanthine and mixed-matrix
(cepharanthine: 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 cepharanthine and mixed-matrix
(cepharanthine: 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 cepharanthine and mixed-matrix
(cepharanthine: 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 | ????91 | ????＜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 | ????88 | ????＜30 | ????＜10 | +++ |
The group practices of table 12 cepharanthine and mixed-matrix
(cepharanthine: 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 | ????90 | ????＜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 medicine dry powder 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 medicine dry powder and substrate is 1: 3, the rounding rate, the ball method of double differences is different and index such as hardness slightly all begins to enter preferable state.
3. when the ratio of medicine dry powder and substrate is 1: 9, 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 Cepharanthine drip pill that is used for the treatment of the leukopenia that tumour patient causes because of radiotherapy chemotherapy is a raw material with the cepharanthine, be prepared from pharmaceutically suitable carrier as substrate, wherein:
1.1 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;
1.2 proportioning: with g or kg is unit, by weight, and medicine dry powder: substrate=1: 1～1: 9.
2. Cepharanthine drip 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 Cepharanthine drip pill as claimed in claim 1 or 2 is characterized in that: the mixed proportion of described medicine dry powder and substrate is 1: 1～1: 5.
4. the preparation method of a Cepharanthine drip pill is characterized in that being made of following process:
4.1 active constituents of medicine: cepharanthine;
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 cepharanthine: substrate=1: 1～1: 9;
4.4, accurately take by weighing cepharanthine 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 cepharanthine 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 cepharanthine 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 Cepharanthine drip 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.
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| CN110151691A (en) * | 2019-06-19 | 2019-08-23 | 宁夏医科大学 | A kind of paternogenin nano-suspension and preparation method thereof |
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| CN1615865A (en) * | 2003-11-10 | 2005-05-18 | 彭红 | Cepharanthine dripping pill and preparing process |
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