CN100486598C - Bupleurum root asarum herb dripping pill and its preparing method - Google Patents
Bupleurum root asarum herb dripping pill and its preparing method Download PDFInfo
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- CN100486598C CN100486598C CNB2005100086253A CN200510008625A CN100486598C CN 100486598 C CN100486598 C CN 100486598C CN B2005100086253 A CNB2005100086253 A CN B2005100086253A CN 200510008625 A CN200510008625 A CN 200510008625A CN 100486598 C CN100486598 C CN 100486598C
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Abstract
The bupleurum root-asarum herb dripping pill is a kind of oral medicine composition preparation with functions of expelling surficial evils and removing heat for treating cold causing nasal obstruction, sneezing cough, headache, fever and general malaise. It has high bioavailability, fast medicine release, fast acting, high effective component content, low cost and less toxic side effect, and the production process has no pollution. The bupleurum root-asarum herb dripping pill is prepared with the active components of bupleurum root-asarum herb and matrix carrier.
Description
Technical field
The present invention relates to a kind of antipyretic effect of inducing sweat that has, the nasal obstruction watery nasal discharge that is used to catch a cold and causes, sneeze, cough, headache, fever with aversion to cold, the pharmaceutical composition of treatment for diseases such as general malaise is a kind of drug composition oral preparation that feedstock production forms to contain 2 flavor Chinese medicine active pharmaceutical ingredient extracts such as Radix Bupleuri, Herba Asari particularly.
Background technology
According to the bupleurum root and asarum herb injection that the prescription that provides among the drug standard WS-11114 promulgated by the ministries or commissions of the Central Government (ZD-1114)-2002 and extraction process are prepared from, be a kind of have to induce sweat bring down a fever.The nasal obstruction watery nasal discharge that is used to catch a cold and causes, sneeze, cough, headache, fever with aversion to cold, the injection class preparation of symptom treatments such as general malaise, through clinical verification for many years, steady quality, determined curative effect is the common drug preparation that clinical and family is used for the treatment of above disease.Below be the prescription and the extraction process of the bupleurum root and asarum herb injection that provides among the drug standard WS-11114 promulgated by the ministries or commissions of the Central Government (ZD-1114)-2002:
Prescription: Radix Bupleuri 2500g, Herba Asari 250g, propylene glycol 30ml, sodium chloride 8g;
Method for making: above two flavor medical materials, add water and distill, collect the about 5500ml of distillate, the distillate redistillation is collected the about 950ml of re-distilled liquid, adds propylene glycol, jolting is dissolved oil fully, adds sodium chloride again, regulates pH value to 6.8 with 10% sodium hydroxide solution, add the injection water to ormal weight, continuing adds 0.5% active carbon, fully stirs, filter, embedding, sterilization, promptly.Be explained as follows for this injection in the appended bupleurum root and asarum herb injection description:
Nomenclature of drug: bupleurum root and asarum herb injection;
Main component: Radix Bupleuri, Herba Asari;
Character: this product is yellowish clear liquid;
Function cures mainly: induce sweat and bring down a fever.The nasal obstruction watery nasal discharge that is used to catch a cold and causes, sneeze, cough, headache, fever with aversion to cold, diseases such as general malaise;
Usage and dosage: intramuscular injection.2ml for the first time, 1～2 time on the one; Children please be followed the doctor's advice.
Owing to reasons such as technologies of preparing, the research of the compatibility of Chinese medicine injection can not show a candle to Western medicine, and causes allergy easily.Existing bupleurum root and asarum herb injection does not still have similar other dosage form listings at present.This kind Chinese medicine is an effective component extracting from Chinese crude drug, the intravital concentrated solution of Gong the injection of making.Because the extensive use of modern biotechnology in the natural drug exploitation, the domestic herbal species that is used to inject is more and more, and application is more and more wider clinically, and adverse reaction rate also increases.According to data: the dosage form of Chinese patent medicine adverse reaction rate is that injection accounts for 31% successively, tablet accounts for 24%, pill accounts for 10%.Chinese medicine untoward reaction consequence is serious, and Chinese medicine and preparation thereof cause anaphylactic shock and rank first place, and the trend that increases is arranged year by year, this with use clinically more relevant.Chinese medicine composition more complicated is injected human body with this mixture from blood vessel, forces human body to go metabolism, and itself has just had potential danger, if again with the other medicines compatibility, contingent reaction often is difficult to prediction.The compatibility difficulty of Chinese medicine is bigger, and incompatibility is studied the compatibility of Chinese medicine without ready patterns to follow, and it is perfect also to can not show a candle to Western medicine.Chinese medicine injection causes allergy easily, and reason is to contain albumen, polysaccharide, polypeptide etc. in its composition; The purity of extracting is not enough; Plurality of Chinese is extracted, and each composition interacts; Contain cosolvent, solubilizing agent etc.
In addition, the oral formulations of 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 the peroral dosage form of therapeutic effect routine, as tablet, capsule etc.In addition, in preparation process,, 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 because the technology of granulation is arranged.Moreover, the complex manufacturing of conventional oral formulations, production cost is higher, thereby patient's drug cost is also improved thereupon, is unfavorable for improving the ability of seeking medical advice of extensive patients, also is unfavorable for improving the general health level of society.
Summary of the invention
Purpose of the present invention is to replenish the existing nasal obstruction watery nasal discharge that is used to catch a cold and causes, sneeze, cough, headache, fever with aversion to cold, the deficiency of the oral drug preparation of symptom treatments such as general malaise provides a kind of bioavailability height, release fast, quick produce effects, toxic and side effects is little, and the medicament contg height, taking convenience, cheap, and be convenient to the drug composition oral preparation bupleurum root and asarum herb dripping pill of going out to carry.Bupleurum root and asarum herb dripping pill involved in the present invention is a raw material to contain 2 flavor Chinese medicine active pharmaceutical ingredient extracts such as Radix Bupleuri, Herba Asari, is prepared from the pharmaceutically suitable carrier as substrate.Be prepared by the following technical solutions, can obtain bupleurum root and asarum herb dripping pill involved in the present invention:
[preparation method]
1. active pharmaceutical ingredient---contain the extract of 2 flavor Chinese medicine active pharmaceutical ingredients such as Radix Bupleuri, Herba Asari;
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 in dropping-pill machine head and the condensation column that the temperature of condensing agent reaches desired state of temperature respectively, will contain the fused solution of drug extract and substrate and/or emulsion and/or suspension and place in the water dropper jar of drop pill machine, splash in the condensing agent;
Condensing agent can be any one of liquid paraffin, methyl-silicone oil, 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.
[appendix: a kind of preparation method of Chinese medicine extract] is unit with g, gets Radix Bupleuri 2500g, Herba Asari 250g, more than two flavor medical materials, add water and distill, collect the about 5500ml of distillate, distillate redistillation, the about 950ml of collection re-distilled liquid.The bottoms part is extracted three times with suitable quantity of water, and each 2 hours, merge extractive liquid, and distillate.Through low temperature, drying under reduced pressure below 80 ℃, pulverize again, promptly get dry powder.
What provide above is a kind of common Radix Bupleuri and Herba Asari active pharmaceutical ingredient preparation method of extract of containing, and under the same or analogous prerequisite of main active pharmaceutical ingredient of extract, is not limited to this a kind of method.
Beneficial effect
According to the bupleurum root and asarum herb injection that the prescription that provides among the drug standard WS-11114 promulgated by the ministries or commissions of the Central Government (ZD-1114)-2002 and extraction process are prepared from, be a kind of have to induce sweat bring down a fever.The nasal obstruction watery nasal discharge that is used to catch a cold and causes, sneeze, cough, headache, fever with aversion to cold, the injection class preparation of symptom treatments such as general malaise, through clinical verification for many years, steady quality, determined curative effect is the common drug preparation that clinical and family is used for the treatment of above disease.Below be the prescription and the extraction process of the bupleurum root and asarum herb injection that provides among the drug standard WS-11114 promulgated by the ministries or commissions of the Central Government (ZD-1114)-2002:
Owing to reasons such as technologies of preparing, the research of the compatibility of Chinese medicine injection can not show a candle to Western medicine, and causes allergy easily.Existing bupleurum root and asarum herb injection does not still have similar other dosage form listings at present.This kind Chinese medicine is an effective component extracting from Chinese crude drug, the intravital concentrated solution of Gong the injection of making.Because the extensive use of modern biotechnology in the natural drug exploitation, the domestic herbal species that is used to inject is more and more, and application is more and more wider clinically, and adverse reaction rate also increases.According to data: the dosage form of Chinese patent medicine adverse reaction rate is that injection accounts for 31% successively, tablet accounts for 24%, pill accounts for 10%.Chinese medicine untoward reaction consequence is serious, and Chinese medicine and preparation thereof cause anaphylactic shock and rank first place, and the trend that increases is arranged year by year, this with use clinically more relevant.Chinese medicine composition more complicated is injected human body with this mixture from blood vessel, forces human body to go metabolism, and itself has just had potential danger, if again with the other medicines compatibility, contingent reaction often is difficult to prediction.The compatibility difficulty of Chinese medicine is bigger, and incompatibility is studied the compatibility of Chinese medicine without ready patterns to follow, and it is perfect also to can not show a candle to Western medicine.Chinese medicine injection causes allergy easily, and reason is to contain albumen, polysaccharide, polypeptide etc. in its composition; The purity of extracting is not enough; Plurality of Chinese is extracted, and each composition interacts; Contain cosolvent, solubilizing agent etc.
In addition, the oral formulations of 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 the peroral dosage form of therapeutic effect routine, as tablet, capsule etc.In addition, in preparation process,, 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 because the technology of granulation is arranged.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.
Bupleurum root and asarum herb dripping pill involved in the present invention is compared with the bupleurum root and asarum herb injection, has following beneficial effect:
1. bupleurum root and asarum herb dripping pill involved in the present invention; utilize surfactant etc. to be substrate; with containing Radix Bupleuri and Herba Asari active pharmaceutical ingredient extract is made solid dispersion; making medicine be molecule, colloid or microcrystalline state is scattered in the substrate; the total surface area of medicine increases; and substrate is that medicine has wetting action, can make that medicine is rapidly molten to loose into microgranule or solution, thereby makes the dissolving of medicine and absorb and accelerate.Thereby improved bioavailability, brought into play efficient, quick-acting effects etc.
2. bupleurum root and asarum herb dripping pill involved in the present invention contacts promptly with saliva and to dissolve rapidly, and is absorbed by oral mucosa, and is not only rapid-action, and the influence of not taken food, and promptly all can containing take after meal ante cibum, and local application's onset is faster.Thereby make that patient's medication is safer, also have medication convenience, characteristic of accurate simultaneously.
3. bupleurum root and asarum herb 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. bupleurum root and asarum herb dripping pill involved in the present invention, stable in properties; Than injection, it is not prone to anaphylaxis, and side effect is little, and high bioavailability is arranged again.
5. production technology, the equipment of preparation drop pill are simple, easy to operate, the automaticity height, and labor intensity is low, the production efficiency height.Workshop does not have dust simultaneously, helps labor protection and environmental protection yet.
6. the production cost of preparation drop pill is usually with about 50% of other oral formulations of kind, and 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 bupleurum root and asarum herb dripping pill of the present invention.
First group: the test of single-matrix
1. it is standby to make the extract dry powder that contains 2 flavor Chinese medicine active pharmaceutical ingredients such as Radix Bupleuri, Herba Asari in advance according to [appendix: a kind of preparation method of Chinese medicine extract];
2. substrate: Polyethylene Glycol
(1000～20000), pharmaceutically suitable carrier such as polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac;
3. proportioning: with g or kg is unit, by weight, and drug extract: substrate=1:1～1:9;
4. be prepared according to the process of [preparation method] 4～7 again, promptly can make the bupleurum root and asarum herb dripping pill of various different sizes.
[result of the test]
Test 1: for observe drug extract and different substrates when the proportioning of 1:1 prepared bupleurum root and asarum herb dripping pill in qualitative difference, according to the ratio of 1:1, with drug extract respectively with Polyethylene Glycol
1000, Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, Polyethylene Glycol
8000, Polyethylene Glycol
9300, 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 17 pharmaceutical compositions experiments that contain drug extract and different substrates, and obtain 17 groups of different experimental results and see Table 1.
Test 2: for observe drug extract and different substrates when the proportioning of 1:3 prepared bupleurum root and asarum herb dripping pill in qualitative difference, according to the ratio of 1:3, with drug extract respectively with Polyethylene Glycol
1000, Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, Polyethylene Glycol
8000, Polyethylene Glycol
9300, 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 17 pharmaceutical compositions experiments that contain drug extract and different substrates, and obtain 17 groups of different experimental results and see Table 2.
Test 3: for observe drug extract and different substrates when the proportioning of 1:9 prepared bupleurum root and asarum herb dripping pill in qualitative difference, according to the ratio of 1:9, with drug extract respectively with Polyethylene Glycol
1000, Polyethylene Glycol
2000, Polyethylene Glycol
4000, Polyethylene Glycol
6000, Polyethylene Glycol
8000, Polyethylene Glycol
9300, 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 17 pharmaceutical compositions experiments that contain drug extract and different substrates, and obtain 17 groups of different experimental results and see Table 3.
Second group: the test of mixed-matrix
1. it is standby to make the extract dry powder that contains 2 flavor Chinese medicine active pharmaceutical ingredients such as Radix Bupleuri, Herba Asari in advance according to [appendix: a kind of preparation method of Chinese medicine extract];
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. (with g or kg is unit to proportioning, by weight)
3.1 the ratio of composite interstitial substance---polyoxyethylene stearate 40 esters: Polyethylene Glycol or poloxamer: Polyethylene Glycol or carboxymethyl starch sodium: Polyethylene Glycol or betacyclodextrin: Polyethylene Glycol=1:1～1:10,
3.2 hybrid medicine extract: mixed-matrix weight and=1:1～1:9;
4. be prepared according to the process of [preparation method] 4～7 again, promptly can make the bupleurum root and asarum herb dripping pill of various different sizes.
[result of the test]
Test 4: for observe drug extract and mixed-matrix when the proportioning of 1:1 prepared bupleurum root and asarum herb dripping pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with the mixed of 1:1 evenly as mixed-matrix, according to the ratio of 1:1 drug extract is mixed mutually with 4 kinds of different mixed-matrixes 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: for observe drug extract and mixed-matrix when the proportioning of 1:3 prepared bupleurum root and asarum herb dripping pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with the mixed of 1:1 evenly as mixed-matrix, according to the ratio of 1:3 drug extract is mixed mutually with 4 kinds of different mixed-matrixes 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: for observe drug extract and mixed-matrix when the proportioning of 1:9 prepared bupleurum root and asarum herb dripping pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with the mixed of 1:1 evenly as mixed-matrix, according to the ratio of 1:9 drug extract is mixed mutually with 4 kinds of different mixed-matrixes 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: for observe drug extract and mixed-matrix when the proportioning of 1:1 prepared bupleurum root and asarum herb dripping pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with the mixed of 1:5 evenly as mixed-matrix, according to the ratio of 1:1 drug extract is mixed mutually with 4 kinds of different mixed-matrixes 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: for observe drug extract and mixed-matrix when the proportioning of 1:3 prepared bupleurum root and asarum herb dripping pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with the mixed of 1:5 evenly as mixed-matrix, according to the ratio of 1:3 drug extract is mixed mutually with 4 kinds of different mixed-matrixes 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: for observe drug extract and mixed-matrix when the proportioning of 1:9 prepared bupleurum root and asarum herb dripping pill in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with the mixed of 1:5 evenly as mixed-matrix, according to the ratio of 1:9 drug extract is mixed mutually with 4 kinds of different mixed-matrixes 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 bupleurum root and asarum herb dripping pill that drug extract and mixed-matrix make when the proportioning of 1:1 in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with the mixed of 1:10 evenly as mixed-matrix, according to the ratio of 1:1 drug extract is mixed mutually with 4 kinds of different mixed-matrixes 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 bupleurum root and asarum herb dripping pill that drug extract and mixed-matrix make when the proportioning of 1:3 in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with the mixed of 1:10 evenly as mixed-matrix, according to the ratio of 1:3 drug extract is mixed mutually with 4 kinds of different mixed-matrixes 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 bupleurum root and asarum herb dripping pill that drug extract and mixed-matrix make when the proportioning of 1:9 in qualitative difference, with polyoxyethylene stearate 40 esters, poloxamer, carboxymethyl starch sodium, 4 kinds of carriers such as betacyclodextrin respectively with Polyethylene Glycol with the mixed of 1:10 evenly as mixed-matrix, according to the ratio of 1:9 drug extract is mixed mutually with 4 kinds of different mixed-matrixes 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 | 75 | <30 | >10 | + |
| Polyethylene Glycol 2000 | 50.0 | 82 | <30 | >10 | + |
| Polyethylene Glycol 4000 | 50.0 | 80 | <30 | >10 | ++ |
| Polyethylene Glycol 6000 | 50.0 | 85 | <30 | >10 | ++ |
| Polyethylene Glycol 8000 | 50.0 | 79 | <30 | >10 | ++ |
| Polyethylene Glycol 9300 | 50.0 | 88 | <30 | >10 | ++ |
| Polyethylene Glycol 10000 | 50.0 | 82 | <30 | >10 | ++ |
| Polyethylene Glycol 20000 | 50.0 | 80 | <30 | >10 | ++ |
| Polyoxyethylene stearate 40 esters | 50.0 | 78 | <30 | >10 | ++ |
| Betacyclodextrin | 50.0 | 74 | <30 | >10 | + |
| Poloxamer | 50.0 | 80 | <30 | >10 | ++ |
| Carboxymethyl starch sodium | 50.0 | 73 | <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 | 55 | >30 | >10 | +++ |
| Lac | 50.0 | 52 | >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 | 77 | <30 | >10 | + |
| Polyethylene Glycol 2000 | 25.0 | 79 | <30 | >10 | ++ |
| Polyethylene Glycol 4000 | 25.0 | 86 | <30 | <10 | ++ |
| Polyethylene Glycol 6000 | 25.0 | 93 | <30 | <10 | +++ |
| Polyethylene Glycol 8000 | 25.0 | 93 | <30 | <10 | +++ |
| Polyethylene Glycol 9300 | 25.0 | 94 | <30 | >10 | ++ |
| Polyethylene Glycol 10000 | 25.0 | 94 | <30 | <10 | +++ |
| Polyethylene Glycol 20000 | 25.0 | 91 | <30 | <10 | ++ |
| Polyoxyethylene stearate 40 esters | 25.0 | 93 | <30 | <10 | ++ |
| Betacyclodextrin | 25.0 | 83 | <30 | >10 | ++ |
| Poloxamer | 25.0 | 89 | <30 | <10 | +++ |
| Carboxymethyl starch sodium | 25.0 | 79 | <30 | >10 | ++ |
| Sodium lauryl sulphate | 25.0 | 77 | <30 | >10 | ++ |
| Stearic acid | 25.0 | 73 | >30 | >10 | +++ |
| Sodium stearate | 25.0 | 72 | >30 | >10 | +++ |
| Glycerin gelatine | 25.0 | 71 | >30 | >10 | +++ |
| Lac | 25.0 | 72 | >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 | 77 | <30 | >10 | + |
| Polyethylene Glycol 2000 | 10.0 | 83 | <30 | >10 | ++ |
| Polyethylene Glycol 4000 | 10.0 | 93 | <30 | <10 | +++ |
| Polyethylene Glycol 6000 | 10.0 | 94 | <30 | <10 | +++ |
| Polyethylene Glycol 8000 | 10.0 | 92 | <30 | <10 | +++ |
| Polyethylene Glycol 9300 | 10.0 | 89 | <30 | >10 | +++ |
| Polyethylene Glycol 10000 | 10.0 | 93 | <30 | <10 | +++ |
| Polyethylene Glycol 20000 | 10.0 | 92 | <30 | <10 | +++ |
| Polyoxyethylene stearate 40 esters | 10.0 | 90 | <30 | <10 | ++ |
| Betacyclodextrin | 10.0 | 88 | <30 | <10 | ++ |
| Poloxamer | 10.0 | 92 | <30 | <10 | +++ |
| Carboxymethyl starch sodium | 10.0 | 86 | <30 | <10 | +++ |
| Sodium lauryl sulphate | 10.0 | 83 | <30 | >10 | +++ |
| Stearic acid | 10.0 | 76 | >30 | >10 | +++ |
| Sodium stearate | 10.0 | 77 | >30 | >10 | +++ |
| Glycerin gelatine | 10.0 | 74 | >30 | >10 | +++ |
| Lac | 10.0 | 73 | >30 | >10 | +++ |
The group practices of table 4 drug extract and mixed-matrix
(drug extract: mixed-matrix=1:1)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1:1 | 50 | 85 | <30 | <10 | ++ |
| Poloxamer: Polyethylene Glycol=1:1 | 50 | 87 | <30 | <10 | ++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1:1 | 50 | 82 | <30 | >10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1:1 | 50 | 79 | <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 | <30 | <10 | +++ | |
| Poloxamer: Polyethylene Glycol=1:1 | 25 | 94 | <30 | <10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1:1 | 25 | 88 | <30 | <10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1:1 | 25 | 86 | <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 | 92 | <30 | <10 | +++ |
| Poloxamer: Polyethylene Glycol=1:1 | 10 | 93 | <30 | <10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1:1 | 10 | 91 | <30 | <10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1:1 | 10 | 85 | <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 | 95 | <30 | <10 | +++ |
| Poloxamer: Polyethylene Glycol=1:5 | 50 | 94 | <30 | <10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1:5 | 50 | 90 | <30 | <10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1:5 | 50 | 83 | <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 | 94 | <30 | <10 | +++ |
| Poloxamer: Polyethylene Glycol=1:5 | 25 | 96 | <30 | <10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1:5 | 25 | 92 | <30 | <10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1:5 | 25 | 88 | <30 | <10 | ++ |
The group practices of table 9 drug extract and mixed-matrix
(drug extract: mixed-matrix=1:9)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1:5 | 10 | 95 | <30 | <10 | +++ |
| Poloxamer: Polyethylene Glycol=1:5 | 10 | 94 | <30 | <10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1:5 | 10 | 91 | <30 | <10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1:5 | 10 | 88 | <30 | <10 | +++ |
The group practices of table 10 drug extract and mixed-matrix
(drug extract: mixed-matrix=1:1)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1:10 | 50 | 91 | <30 | <10 | +++ |
| Poloxamer: Polyethylene Glycol=1:10 | 50 | 93 | <30 | <10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1:10 | 50 | 89 | <30 | <10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1:10 | 50 | 82 | <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 | 94 | <30 | <10 | +++ |
| Poloxamer: Polyethylene Glycol=1:10 | 25 | 92 | <30 | <10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1:10 | 25 | 88 | <30 | <10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1:10 | 25 | 87 | <30 | <10 | +++ |
The group practices of table 12 drug extract and mixed-matrix
(drug extract: mixed-matrix=1:9)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1:10 | 10 | 96 | <30 | <10 | +++ |
| Poloxamer: Polyethylene Glycol=1:10 | 10 | 94 | <30 | <10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1:10 | 10 | 91 | <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 comparatively 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, though the rounding rate, the ball method of double differences is different and index such as hardness has raising, and is not obvious.
4. the general effect of composite interstitial substance is better than single-matrix.
5. the hardness method for expressing in the subordinate list adopts drop pill is placed on the glass plate, press...withes one's finger it, observes its metamorphosis."+" expression flicking promptly is out of shape, " ++ " expression distortion of firmly pressing, and " +++" expression is indeformable by it.
Claims (2)
1. the hot drop pill of bavin is a raw material with Radix Bupleuri, Herba Asari, is prepared from the pharmaceutically suitable carrier as substrate, it is characterized in that:
(1) get Radix Bupleuri 2500g, Herba Asari 250g, more than two flavor medical materials, add water and distill, collect the about 5500ml of distillate, distillate redistillation, the about 950ml of collection re-distilled liquid.The bottoms part is extracted three times with suitable quantity of water, and each 2 hours, merge extractive liquid, and distillate again through low temperature, drying under reduced pressure below 80 ℃, are pulverized, and promptly get the extract that contains pharmaceutically active ingredient in above-mentioned two, and be standby;
(2) described substrate is the mixture of Polyethylene Glycol and polyoxyethylene stearate 40 esters or carboxymethyl starch sodium, by weight, the mixed proportion of polyoxyethylene stearate 40 esters or carboxymethyl starch sodium and Polyethylene Glycol is 1:1～1:10, and the mixing ratio of described extract and substrate is 1:3;
(3) according to aforementioned proportion, accurately take by weighing described extract and substrate, be placed in the heating container heating while stirring, standby until the fused solution that obtains containing described extract and substrate and/or emulsion and/or suspension;
(4) temperature control system of adjustment drop pill machine makes the water dropper heating of drop pill machine and maintains the temperature at 50 ℃～90 ℃, and the condensing agent cooling also maintains the temperature at-5 ℃～40 ℃;
When (5) temperature for the treatment of dropping-pill machine head and condensing agent reaches described state respectively, will contain the fused solution of described extract and substrate and/or emulsion and/or suspension and place in the water dropper jar of drop pill machine, and splash into to shrink in the condensing agent and be shaped, promptly.
2. the hot drop pill of bavin as claimed in claim 1 is characterized in that: described condensing agent be methyl-silicone oil or/and liquid paraffin or/and vegetable oil.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100086253A CN100486598C (en) | 2005-02-28 | 2005-02-28 | Bupleurum root asarum herb dripping pill and its preparing method |
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|---|---|---|---|
| CNB2005100086253A CN100486598C (en) | 2005-02-28 | 2005-02-28 | Bupleurum root asarum herb dripping pill and its preparing method |
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| Publication Number | Publication Date |
|---|---|
| CN1682822A CN1682822A (en) | 2005-10-19 |
| CN100486598C true CN100486598C (en) | 2009-05-13 |
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| CN103520268B (en) * | 2013-10-31 | 2015-11-11 | 青岛施维雅生物制药有限公司 | For the Traditional Chinese medicine extract injection fluid and preparation method thereof of domestic animal |
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Non-Patent Citations (2)
| Title |
|---|
| 中药滴丸剂的研究进展. 郑鑫等.中国中药杂志2003，第28卷第4期. 2003 * |
| 国家中成药标准汇编. 国家药品监督管理局，119-120. 2002 * |
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