CN1682930A - Lemai dripping pill for treating cardiovascular diseases and its preparing method - Google Patents
Lemai dripping pill for treating cardiovascular diseases and its preparing method Download PDFInfo
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- CN1682930A CN1682930A CN 200510051535 CN200510051535A CN1682930A CN 1682930 A CN1682930 A CN 1682930A CN 200510051535 CN200510051535 CN 200510051535 CN 200510051535 A CN200510051535 A CN 200510051535A CN 1682930 A CN1682930 A CN 1682930A
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- polyethylene glycol
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- lemai
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- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 description 1
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- Medicinal Preparation (AREA)
Abstract
The present invention relates to a kind of medicine composition, Lemai dripping pill, with functions of activating vital energy, promoting blood circulation, alleviating mental depression, removing blood stasis, nourishing blood and dredging blood vessel and for treating coronary heart disease, atherosclerosis, pulmonary heart disease, infarct dementia, etc. The present invention has high bioavailability, fast medicine release, fast acting, high effective content, taking convenience and low cost, and the production process has no pollution. The Lemai dripping pill is prepared with seven kinds of Chinese medicinal materials, including red sage, Chuanxiong rhizome, red peony root, safflower, etc. and medicine carrier as matrix.
Description
Technical field
The present invention relates to a kind of promoting flow of QI and blood that has, the resolving depression blood stasis dispelling, the nourishing blood and promoting blood circulation effect, being used for the pharmaceutical composition of treatment for diseases such as headache that cardiovascular and cerebrovascular diseases such as coronary heart disease, arteriosclerosis, pulmonary heart disease, multiple infarction dementia belong to caused by energy stagnation and blood stasis, dizzy, chest pain, cardiopalmus, is a kind of drug composition oral dropping pill formulation that feedstock production forms with the extract that contains pharmaceutically active ingredient in 7 flavors such as Radix Salviae Miltiorrhizae, Rhizoma Chuanxiong, Radix Paeoniae Rubra, Flos Carthami, Rhizoma Cyperi, the Radix Aucklandiae, Fructus Crataegi particularly.
Background technology
According to drug standard WS promulgated by the ministries or commissions of the Central Government
3The LEMAI KELI that the preparation method that provides among-the B-2308-97 is prepared from, it is a kind of promoting flow of QI and blood that has, the resolving depression blood stasis dispelling, the nourishing blood and promoting blood circulation effect, the oral granular formulation that is used for treatment for diseases such as headache that cardiovascular and cerebrovascular diseases such as coronary heart disease, arteriosclerosis, pulmonary heart disease, multiple infarction dementia belong to caused by energy stagnation and blood stasis, dizzy, chest pain, cardiopalmus, 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-2308-97 and technology and brief description:
Prescription: Radix Salviae Miltiorrhizae 499g, Rhizoma Chuanxiong 249.5g, Radix Paeoniae Rubra 249.5g, Flos Carthami 249.5g, Rhizoma Cyperi 124.75g, Radix Aucklandiae 124.75g, Fructus Crataegi 62.4g.
Method for making: above seven flavors decoct with water each 0.5 hour three times, filter, filtrate is carried out low temperature (45～50) in centrifugal-film evaporator ℃ to be concentrated into relative density be 1.10-1.30 (50～60) ℃, in batch (-type) sulfuration bed and the lactose fluidisation, drying is made granule 1000g, promptly.
Function cures mainly: promoting flow of QI and blood, resolving depression blood stasis dispelling, nourishing blood and promoting blood circulation.Be used for headache that cardiovascular and cerebrovascular diseases such as coronary heart disease, arteriosclerosis, pulmonary heart disease, multiple infarction dementia belong to caused by energy stagnation and blood stasis, dizzy, chest pain, cardio palmus.
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.Granule also has medicament contg also lower, takes deficiencies such as inconvenience.
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, be to replenish the existing deficiency that is used for the oral drug preparation of treatment for diseases such as headache that cardiovascular and cerebrovascular diseases such as coronary heart disease, arteriosclerosis, pulmonary heart disease, multiple infarction dementia belong to caused by energy stagnation and blood stasis, dizzy, chest pain, cardiopalmus, a kind of bioavailability height is provided, and has a quick release, quick produce effects, medicament contg height, taking convenience, cheap, and free of contamination aborning Lemai dripping pill.Lemai dripping pill involved in the present invention, with 7 flavor Chinese medicines such as Radix Salviae Miltiorrhizae, Rhizoma Chuanxiong, Radix Paeoniae Rubra, Flos Carthami, Rhizoma Cyperi, the Radix Aucklandiae, Fructus Crataegi is raw material, after extraction obtains containing the extract of pharmaceutically active ingredient in above 7 flavors, be prepared from pharmaceutically suitable carrier again as substrate.Be prepared by the following technical solutions, can obtain Lemai dripping pill involved in the present invention:
[preparation method]
1. the preparation of drug extract: with g or kg is unit, according to the weight portion meter, get 8 parts of Radix Salviae Miltiorrhizaes, 4 parts of Rhizoma Chuanxiongs, 4 parts of Radix Paeoniae Rubra, 4 parts on Flos Carthami, 2 parts of Rhizoma Cyperis, 2 parts of the Radix Aucklandiae, 1 part of Fructus Crataegi, more than seven the flavor, decoct with water three times, each 0.5 hour, filter, filtrate is 1.10～1.30 thick paste carry out cryoconcentration to relative density below 60 ℃ in centrifugal-film evaporator, promptly; Or under similarity condition, continue to make drying, be ground into dry powder, promptly;
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 LEMAI KELI that the preparation method that provides among-the B-2308-97 is prepared from, it is a kind of promoting flow of QI and blood that has, the resolving depression blood stasis dispelling, the nourishing blood and promoting blood circulation effect, the oral granular formulation that is used for treatment for diseases such as headache that cardiovascular and cerebrovascular diseases such as coronary heart disease, arteriosclerosis, pulmonary heart disease, multiple infarction dementia belong to caused by energy stagnation and blood stasis, dizzy, chest pain, cardiopalmus, 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 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.Granule also has medicament contg also lower, takes deficiencies such as inconvenience.
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.
Lemai dripping pill involved in the present invention is compared with LEMAI KELI has following beneficial effect:
1. Lemai dripping pill involved in the present invention; utilize surfactant to be substrate; the extract of pharmaceutically active ingredient is made solid dispersion in containing 7 flavors such as Radix Salviae Miltiorrhizae, Rhizoma Chuanxiong, Radix Paeoniae Rubra, Flos Carthami, Rhizoma Cyperi, the Radix Aucklandiae, Fructus Crataegi; making medicine be molecule, colloid or microcrystalline state is scattered in the substrate; the total surface area of medicine increases; and substrate is hydrophilic; medicine had wetting action; can make medicine molten microgranule or the solution of loosing into rapidly; thereby make the dissolving of medicine and absorb quickening; thereby improved bioavailability, brought into play efficient, quick-acting effects etc.
2. Lemai dripping 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. Lemai dripping pill involved in the present invention mixes the extract that contains active constituents of medicine mutually with molten matrix, splashes in the not miscible condensed fluid and makes.Therefore, the stability of drug height, not facile hydrolysis, oxidation, and the operation be under liquid state, to carry out, no dust pollution is not subject to the influence of crystal formation, thereby has guaranteed the quality of medicine, has increased stability.
4. production technology, the equipment of preparation drop pill are simple, easy to operate, the automaticity height, and labor intensity is low, the production efficiency height.Workshop does not have dust simultaneously, helps labor protection and environmental protection yet.
5. the production cost of preparation drop pill is usually with about 50% of other oral formulations of kind, and compares with oral liquid, and the dosage of drop pill is accurate, thereby makes the patient take metering control easily.
The specific embodiment
Now with several groups of specific embodiments, be described further with regard to the preparation method of Lemai dripping pill of the present invention:
First group: the test of single-matrix
1. the preparation of drug extract: it is standby to make drug extract dry powder earlier 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 Lemai dripping pill of different size.
[result of the test]
Test 1: for observe drug extract and different substrates when 1: 1 the proportioning prepared Lemai dripping pill 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 Lemai dripping pill 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 Lemai dripping pill 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. the preparation of drug extract: it is standby to make drug extract dry powder earlier 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 Lemai dripping pill of different size.
[result of the test]
Test 4: in order to observe the mass discrepancy of drug extract and mixed-matrix prepared Lemai dripping 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 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 Lemai dripping 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 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 Lemai dripping 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 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 Lemai dripping 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 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 Lemai dripping 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 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 Lemai dripping 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 are mixed again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 9.
Test 10: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained Lemai dripping pill when 1: 1 proportioning, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 10 mixed evenly as mixed-matrix, according to 1: 1 ratio drug extract is mixed mutually with 4 kinds of different mixed-matrixes respectively again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 10.
Test 11: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained Lemai dripping pill when 1: 3 proportioning, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 10 mixed evenly as mixed-matrix, according to 1: 3 ratio drug extract is mixed mutually with 4 kinds of different mixed-matrixes respectively again and make evenly, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 4 pharmaceutical compositions that drug extract and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 11.
Test 12: in order to observe the mass discrepancy of drug extract and mixed-matrix obtained Lemai dripping pill when 1: 9 proportioning, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with 1: 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 | ??66 | ??＜30 | ＞10 | ??+ |
| Polyethylene Glycol 4000 | 50.0 | ??75 | ??＜30 | ＞10 | ??++ |
| Polyethylene Glycol 6000 | 50.0 | ??76 | ??＜30 | ＞10 | ??++ |
| Polyethylene Glycol 8000 | 50.0 | ??75 | ??＜30 | ＞10 | ??++ |
| Polyethylene Glycol 10000 | 50.0 | ??78 | ??＜30 | ＞10 | ??++ |
| Polyethylene Glycol 20000 | 50.0 | ??78 | ??＜30 | ＞10 | ??++ |
| Polyoxyethylene stearate 40 esters | 50.0 | ??73 | ??＜30 | ＞10 | ??++ |
| Betacyclodextrin | 50.0 | ??69 | ??＜30 | ＞10 | ??+ |
| Poloxamer | 50.0 | ??75 | ??＜30 | ＞10 | ??++ |
| Carboxymethyl starch sodium | 50.0 | ??74 | ??＜30 | ＞10 | ??+ |
| Sodium lauryl sulphate | 50.0 | ??68 | ??＞30 | ＞10 | ??++ |
| Stearic acid | 50.0 | ??55 | ??＞30 | ＞10 | ??++ |
| Sodium stearate | 50.0 | ??54 | ??＞30 | ＞10 | ??++ |
| Glycerin gelatine | 50.0 | ??57 | ??＞30 | ＞10 | ??+ |
| Lac | 50.0 | ??58 | ??＞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 | ??66 | ??＜30 | ??＞10 | ??+ |
| Polyethylene Glycol 2000 | ??25.0 | ??83 | ??＜30 | ??＞10 | ??++ |
| Polyethylene Glycol 4000 | ??25.0 | ??88 | ??＜30 | ??＜10 | ??+++ |
| Polyethylene Glycol 6000 | ??25.0 | ??91 | ??＜30 | ??＜10 | ??+++ |
| Polyethylene Glycol 8000 | ??25.0 | ??92 | ??＜30 | ??＜10 | ??+++ |
| Polyethylene Glycol 10000 | ??25.0 | ??91 | ??＜30 | ??＜10 | ??+++ |
| Polyethylene Glycol 20000 | ??25.0 | ??92 | ??＜30 | ??＜10 | ??+++ |
| Polyoxyethylene stearate 40 esters | ??25.0 | ??90 | ??＜30 | ??＜10 | ??++ |
| Betacyclodextrin | ??25.0 | ??82 | ??＜30 | ??＞10 | ??++ |
| Poloxamer | ??25.0 | ??92 | ??＜30 | ??＜10 | ??+++ |
| Carboxymethyl starch sodium | ??25.0 | ??87 | ??＜30 | ??＜10 | ??+++ |
| Sodium lauryl sulphate | ??25.0 | ??81 | ??＜30 | ??＞10 | ??++ |
| Stearic acid | ??25.0 | ??79 | ??＞30 | ??＞10 | ??+++ |
| Sodium stearate | ??25.0 | ??79 | ??＞30 | ??＞10 | ??+++ |
| Glycerin gelatine | ??25.0 | ??73 | ??＞30 | ??＞10 | ??+++ |
| Lac | ??25.0 | ??75 | ??＞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 | ??69 | ??＜30 | ??＞10 | ??+ |
| Polyethylene Glycol 2000 | ??10.0 | ??84 | ??＜30 | ??＞10 | ??++ |
| Polyethylene Glycol 4000 | ??10.0 | ??89 | ??＜30 | ??＜10 | ??+++ |
| Polyethylene Glycol 6000 | ??10.0 | ??92 | ??＜30 | ??＜10 | ??+++ |
| Polyethylene Glycol 8000 | ??10.0 | ??93 | ??＜30 | ??＜10 | ??+++ |
| Polyethylene Glycol 10000 | ??10.0 | ??92 | ??＜30 | ??＜10 | ??+++ |
| Polyethylene Glycol 20000 | ??10.0 | ??93 | ??＜30 | ??＜10 | ??+++ |
| Polyoxyethylene stearate 40 esters | ??10.0 | ??93 | ??＜30 | ??＜10 | ??++ |
| Betacyclodextrin | ??10.0 | ??88 | ??＜30 | ??＜10 | ??++ |
| Poloxamer | ??10.0 | ??92 | ??＜30 | ??＜10 | ??+++ |
| Carboxymethyl starch sodium | ??10.0 | ??89 | ??＜30 | ??＜10 | ??+++ |
| Sodium lauryl sulphate | ??10.0 | ??81 | ??＜30 | ??＞10 | ??+++ |
| Stearic acid | ??10.0 | ??82 | ??＞30 | ??＞10 | ??+++ |
| Sodium stearate | ??10.0 | ??82 | ??＞30 | ??＞10 | ??+++ |
| Glycerin gelatine | ??10.0 | ??78 | ??＞30 | ??＞10 | ??+++ |
| Lac | ??10.0 | ??81 | ??＞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 | 82 | ??＜30 | ??＞10 | ??++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 50 | 81 | ??＜30 | ??＞10 | ??++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 50 | 72 | ??＜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 | 89 | ??＜30 | ??＜10 | ??+++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ??25 | 86 | ??＜30 | ??＜10 | ??+++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ??25 | 85 | ??＜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 | ??89 | ??＜30 | ??＜10 | ??+++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 10 | ??86 | ??＜30 | ??＜10 | ??+++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 10 | ??83 | ??＜30 | ??＞10 | ??+++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 10 | ??82 | ??＜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 | ??93 | ??＜30 | ??＜10 | ??+++ |
| Poloxamer: Polyethylene Glycol=1: 5 | ??50 | ??90 | ??＜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 | ??93 | ??＜30 | ??＜10 | ??+++ |
| Poloxamer: Polyethylene Glycol=1: 5 | ??25 | ??93 | ??＜30 | ??＜10 | ??+++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ??25 | ??91 | ??＜30 | ??＜10 | ??+++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ??25 | ??87 | ??＜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 | ??92 | ??＜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 | ??89 | ??＜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 | ??91 | ??＜30 | ??＜10 | ??+++ |
| Poloxamer: Polyethylene Glycol=1: 10 | ??25 | ??92 | ??＜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 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 | ??90 | ??＜30 | ??＜10 | ??+++ |
| Poloxamer: Polyethylene Glycol=1: 10 | ??10 | ??92 | ??＜30 | ??＜10 | ??+++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | ??10 | ??92 | ??＜30 | ??＜10 | ??+++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | ??10 | ??90 | ??＜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. pharmaceutical composition Lemai dripping pill that is used for the treatment of cardiovascular and cerebrovascular disease, with the extract that contains pharmaceutically active ingredient in Radix Salviae Miltiorrhizae, Rhizoma Chuanxiong, Radix Paeoniae Rubra, Flos Carthami, Rhizoma Cyperi, the Radix Aucklandiae, Fructus Crataegi etc. 7 flavor is raw material, be prepared from pharmaceutically suitable carrier as substrate, wherein:
1.1 the preparation of drug extract: with g or kg is unit, according to the weight portion meter, get 8 parts of Radix Salviae Miltiorrhizaes, 4 parts of Rhizoma Chuanxiongs, 4 parts of Radix Paeoniae Rubra, 4 parts on Flos Carthami, 2 parts of Rhizoma Cyperis, 2 parts of the Radix Aucklandiae, 1 part of Fructus Crataegi, more than seven the flavor, decoct with water three times, each 0.5 hour, filter, filtrate is 1.10～1.30 thick paste carry out cryoconcentration to relative density below 60 ℃ in centrifugal-film evaporator, promptly; Or continue to make drying with this understanding, be ground into 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. Lemai dripping 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 Lemai dripping 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 Lemai dripping pill is characterized in that being made of following process:
4.1 the preparation of drug extract: with g or kg is unit, according to the weight portion meter, get 8 parts of Radix Salviae Miltiorrhizaes, 4 parts of Rhizoma Chuanxiongs, 4 parts of Radix Paeoniae Rubra, 4 parts on Flos Carthami, 2 parts of Rhizoma Cyperis, 2 parts of the Radix Aucklandiae, 1 part of Fructus Crataegi, more than seven the flavor, decoct with water three times, each 0.5 hour, filter, filtrate is 1.10～1.30 thick paste carry out cryoconcentration to relative density below 60 ℃ in centrifugal-film evaporator, promptly; Or continue to make drying with this understanding, be ground into 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, fused solution and/or the emulsion and/or the suspension that will contain drug extract and substrate, under the temperature conditions close, make evenly through fully stirring with the water dropper temperature, place in the water dropper jar of drop pill machine, splash in the condensing agent, shrink molding promptly.
5. as the preparation method of Lemai dripping 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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| Application Number | Priority Date | Filing Date | Title |
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| CNB2005100515352A CN1307980C (en) | 2005-03-04 | 2005-03-04 | Lemai dripping pill for treating cardiovascular diseases and its preparing method |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100515352A CN1307980C (en) | 2005-03-04 | 2005-03-04 | Lemai dripping pill for treating cardiovascular diseases and its preparing method |
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| CN1682930A true CN1682930A (en) | 2005-10-19 |
| CN1307980C CN1307980C (en) | 2007-04-04 |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1925302A1 (en) * | 2006-11-24 | 2008-05-28 | DSMIP Assets B.V. | Dietary or pharmaceutical compositions containing tricyclic diterpenes and derivatives thereof for the treatment of depression |
| CN102698030A (en) * | 2012-06-21 | 2012-10-03 | 陈慧婷 | Traditional Chinese medicine preparation of spatula spatula for treating headache and its preparation method |
| CN105343365A (en) * | 2015-12-10 | 2016-02-24 | 韩雪海 | Traditional Chinese medicine fumigating and soaking combined liquid medicine for treating hyperlipidemia cerebral arteriosclerosis |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1202816C (en) * | 2002-02-07 | 2005-05-25 | 王志刚 | Glimepiride dripping pills |
| CN1546027A (en) * | 2003-12-02 | 2004-11-17 | 北京正大绿洲医药科技有限公司 | Dripping pills for treating allergic disease and its preparation process |
| CN1256954C (en) * | 2003-12-12 | 2006-05-24 | 北京科信必成医药科技发展有限公司 | Blumea oil dripping pills and its preparation process |
-
2005
- 2005-03-04 CN CNB2005100515352A patent/CN1307980C/en not_active Expired - Fee Related
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1925302A1 (en) * | 2006-11-24 | 2008-05-28 | DSMIP Assets B.V. | Dietary or pharmaceutical compositions containing tricyclic diterpenes and derivatives thereof for the treatment of depression |
| WO2008061754A1 (en) * | 2006-11-24 | 2008-05-29 | Dsm Ip Assets B.V. | Dietary or pharmaceutical compositions containing tricyclic diterpenes and derivatives thereof for the treatment of depression |
| US8552055B2 (en) | 2006-11-24 | 2013-10-08 | Dsm Ip Assets B.V. | Dietary and pharmaceutical compositions containing tricyclic diterpenes and their derivates and their uses |
| US8748491B2 (en) | 2006-11-24 | 2014-06-10 | Dsm Ip Assets B.V. | Dietary and pharmaceutical compositions containing tricyclic diterpenes and their derivatives and their uses |
| CN102698030A (en) * | 2012-06-21 | 2012-10-03 | 陈慧婷 | Traditional Chinese medicine preparation of spatula spatula for treating headache and its preparation method |
| CN105343365A (en) * | 2015-12-10 | 2016-02-24 | 韩雪海 | Traditional Chinese medicine fumigating and soaking combined liquid medicine for treating hyperlipidemia cerebral arteriosclerosis |
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| CN1307980C (en) | 2007-04-04 |
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