CN100528142C - Aidi drops for treating cancers and preparation thereof - Google Patents
Aidi drops for treating cancers and preparation thereof Download PDFInfo
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- CN100528142C CN100528142C CNB2005100028898A CN200510002889A CN100528142C CN 100528142 C CN100528142 C CN 100528142C CN B2005100028898 A CNB2005100028898 A CN B2005100028898A CN 200510002889 A CN200510002889 A CN 200510002889A CN 100528142 C CN100528142 C CN 100528142C
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Abstract
An Aidi dripping pill based on Aidi injection for treating primary liver cancer, lung cancer, rectum cancer, lymph cancer and gynopathic malignant tumor is disclosed. Its advantages are high release speed and quickly taking its high effect.
Description
Technical field
The present invention relates to a kind of heat-clearing and toxic substances removing that has, the effect of repercussive eliminating stagnation, be used for the treatment of primary hepatocarcinoma, pulmonary carcinoma, rectal cancer, malignant lymphoma, the pharmaceutical composition of diseases such as gynecologic malignant tumor, be particularly related to prescription, change a social system a kind of oral formulations that forms through dosage form based on the Chinese traditional patent formulation ad pro injection.
Background technology
(20-85 promulgated by the ministries or commissions of the Central Government)
According to the drug standard WS promulgated by the ministries or commissions of the Central Government of country
3The ad pro injection that prescription that provides among-the B-3809-98 and extraction process are prepared from, it is a kind of primary hepatocarcinoma that is used for the treatment of, pulmonary carcinoma, rectal cancer, malignant lymphoma, the pure Chinese medicine of diseases such as gynecologic malignant tumor, through clinical verification for many years, steady quality, determined curative effect is the common drug that is used for the treatment of above-mentioned disease clinically.
Below be drug standard WS
3Prescription that provides among-the B-3809-98 and extraction process:
Prescription: Mylabris 1.5g, Radix Ginseng 50g, Radix Astragali 100g, Radix Et Caulis Acanthopanacis Senticosi 150g;
Method for making: above four flavors, the Radix Ginseng section is extracted secondary with 50% alcohol heating reflux, and 3 hours for the first time, 1.5 hours for the second time, merge extractive liquid, filtered, and reclaims ethanol, and medicinal liquid is standby; Three flavors such as medicinal residues and all the other Mylabris decoct with water three times, and 3 hours for the first time, 1.5 hours for the second time, 1 hour for the third time, collecting decoction filters, and filtrate and Radix Ginseng extractive solution merge, with stone sulfur method precipitation process secondary, the gained supernatant adds ethanol to be made and contains alcohol amount and reach 80%, and standing over night is got the supernatant decompression recycling ethanol to there not being the alcohol flavor, add in injection water 100ml and embedding and the corresponding container, hot pressing (115 degree) sterilization secondary, each 30 minutes, after the cooling, the paper pulp sucking filtration, filtrate is diluted to 1000ml with water for injection, filters embedding by incipient fusion filtrate, 115 degree were sterilized 30 minutes again, promptly.
Be explained as follows for this product in the appended ad pro injection description:
Nomenclature of drug: ad pro injection;
Main component: Mylabris, Radix Ginseng, the Radix Astragali, Radix Et Caulis Acanthopanacis Senticosi;
Character: this product is the clear liquid of light brown;
Function cures mainly: heat-clearing and toxic substances removing, repercussive eliminating stagnation.Be used for primary hepatocarcinoma, pulmonary carcinoma, rectal cancer, malignant lymphoma, gynecologic malignant tumor etc.
Owing to be subjected to the influence of existing injection technology of preparing restriction and Chinese medicinal ingredients complexity, Chinese medicine injection often is easy to generate acute allergic reaction or untoward reaction, it is big also to exist operation easier simultaneously, the patient suffering is big, make and the medical treatment cost height, transportation stores inconvenience, and patient economy burden is heavy, shortcomings such as unsuitable family use.
In addition, owing to reasons such as technologies of preparing, the oral formulations of most drug exists 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.Simultaneously, 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.Therefore, be necessary to seek the peroral dosage form of better Flos Carthami medicine to satisfy the needs that clinical treatment and family use.
Summary of the invention
Purpose of the present invention is to replenish existing be used for the treatment of primary hepatocarcinoma, pulmonary carcinoma, rectal cancer, malignant lymphoma, the deficiency of the oral drug preparation of diseases such as gynecologic malignant tumor provides a kind of bioavailability height, release fast, quick produce effects, toxic and side effects is little, and manufacturing and medical treatment cost are low, low price, the oral Aidi drops that is suitable for family to use.
Aidi drops involved in the present invention determines that through a large amount of experiment sievings based on Chinese traditional patent formulation ad pro injection extraction process, process is adjusted extracting section technology, and cooperates drop pill preparation technology to be prepared from.Be prepared by the following technical solutions, can obtain Aidi drops involved in the present invention:
[preparation method]
1. be unit with g or kg, calculate, get Mylabris, Radix Ginseng, the Radix Astragali, the Radix Et Caulis Acanthopanacis Senticosi of some according to weight, through the extracting method of routine make the drug extract thick paste or dry powder standby;
2. substrate---Polyethylene Glycol
(2000,4000,6000,8000,10000,20000), 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. treating that the temperature of condensing agent in dropping-pill machine head and the condensation column is stable respectively is in above the 2nd step during desired state of temperature, 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, under the state of insulation, place in the water dropper jar of drop pill machine, splash in the condensing agent by water dropper;
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.
[appendix: a kind of preparation method of Chinese medicine extract]
With g or kg is unit, takes by weighing Mylabris, Radix Ginseng, the Radix Astragali, the Radix Et Caulis Acanthopanacis Senticosi of some according to weight, and the Radix Ginseng section is extracted secondary with 50% alcohol heating reflux, and 3 hours for the first time, 1.5 hours for the second time, merge extractive liquid, filtered, recovery ethanol, and medicinal liquid is standby; Three flavors such as medicinal residues and all the other Mylabris decoct with water three times, and 3 hours for the first time, 1.5 hours for the second time, 1 hour for the third time, collecting decoction filtered, filtrate and Radix Ginseng extractive solution merge, and with stone sulfur method precipitation process secondary, the gained supernatant adds ethanol to be made and contain the alcohol amount and reach 80%, standing over night is got the supernatant decompression recycling ethanol to there not being the alcohol flavor, at 0.1Mpa, be condensed into relative density under 60 ℃ the condition and be 1.3～1.35 thick paste, or with thick paste through the low-temperature reduced-pressure drying, pulverize, promptly get dry powder;
Given here is according to a kind of preparation method of extract comparatively commonly used, its processing step adjustment is formed again.Similarly method is a lot, is not limited to this a kind of method during actual enforcement.
Beneficial effect
The ad pro injection that is prepared from according to the prescription that provides among the drug standard WS3-B-3809-98 promulgated by the ministries or commissions of the Central Government of country and extraction process, it is a kind of primary hepatocarcinoma that is used for the treatment of, pulmonary carcinoma, rectal cancer, malignant lymphoma, the pure Chinese medicine of diseases such as gynecologic malignant tumor, through clinical verification for many years, steady quality, determined curative effect is the common drug that is used for the treatment of above-mentioned disease clinically.
Owing to reasons such as technologies of preparing, the oral formulations of most drug, especially the oral formulations of Chinese medicine, exist all after taking that dissolve scattered time limit is long, dissolution is low, absorption is relatively poor, problem such as liver sausage first pass effect and bioavailability are lower, thereby influence the performance of drug effect, also directly affect therapeutic effect.
In addition, conventional peroral dosage form 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.
Aidi drops involved in the present invention is compared with ad pro injection, and following beneficial effect is arranged:
1. Aidi drops involved in the present invention; utilize surfactant to be substrate; make solid dispersion with the extractum or the dry powder that contain Mylabris, Radix Ginseng, the Radix Astragali, Radix Et Caulis Acanthopanacis Senticosi active constituents of medicine; making medicine be molecule, colloid or microcrystalline state is scattered in the substrate; the total surface area of medicine increases, and substrate is hydrophilic, and 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.
Compare with the administering mode of traditional oral formulations, exist essential distinction.Drop pill with the solid dispersion technology preparation can adopt oral and sublingual administration, and effective ingredient is fully contacted with mucomembranous surface, absorbs by mucomembranous epithelial cell, directly enters blood circulation.Owing to directly enter blood circulation without gastrointestinal tract and liver, avoided first pass effect effectively, also avoided gastrointestinal irritation, thereby it is rapid to have an onset, bioavailability height, characteristics such as side effect is little, and medication is convenient.
Chinese patent medicine injection series products is because of producing and basic research seriously lags behind, and the standardization issue of medicine never is resolved.The Chinese crude drug raw material itself is exactly a miscellaneous complex of chemical constituent, also there is not a kind of effective quality control method can reflect the quality and the difference thereof of product comprehensively, comprehensively, truly so far, and can carry out the quality control of production overall process effectively, cause the drug quality instability.The untoward reaction of Chinese medicine at present happens occasionally, but can't fundamentally understand fully to be due to which kind of composition, therefore can not in time make and deal with the aftermath of remedial measure targetedly, stay hidden danger for the hospital clinical medication.Injection manufacturing in addition, cost of transportation height use inconvenience, and this had both increased the weight of patient economy burden, have increased the misery of using again.Compare with Flos Carthami injection, the oral administration dripping pill agent has avoided medicine directly into blood, can reduce acute toxic and side effects and anaphylactoid generation effectively, and is safe and convenient to use, and effect is lasting, applied range; Manufacturing and medical treatment cost reduce greatly simultaneously, have effectively alleviated patient's financial burden, and have stored, transport, carry and use all more convenient.
2. Aidi drops 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.
3. Aidi drops 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.
In sum, make Aidi drops involved in the present invention have the advantage of triple effect (quick-acting, efficient, long-acting), three little (taking dose is little, toxicity is little, side effect little), five convenience (convenient for production, store convenience, convenient transportation, easy to carry, easy to use), meet the basic demand of modernization of Chinese medicine theory.
The specific embodiment
Now with several groups of specific embodiments, be described further with regard to the preparation method of Aidi drops of the present invention.
First group: the test of single-matrix
1. the ratio that provides according to [preparation method] 1 takes by weighing the raw material of Chinese medicine of some, makes earlier according to [appendix: a kind of preparation method of Chinese medicine extract] one joint that to contain Chinese medicine Mylabris, Radix Ginseng, the Radix Astragali, Radix Et Caulis Acanthopanacis Senticosi extraction of active ingredients thing dry powder standby again;
2. substrate: Polyethylene Glycol
(2000,4000,6000,8000,10000,20000), 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 Aidi drops of various different sizes.
[result of the test]
Test 1: for observe drug extract and different substrates when 1: 1 the proportioning prepared Aidi drops in qualitative difference, according to 1: 1 ratio, with drug extract respectively with 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, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 15 pharmaceutical compositions experiments that contain drug extract and different substrates, and obtain 15 groups of different experimental results and see Table 1.
Test 2: for observe drug extract and different substrates when 1: 3 the proportioning prepared Aidi drops in qualitative difference, according to 1: 3 ratio, with drug extract respectively with 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, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 15 pharmaceutical compositions that drug extract and different substrates constituted, and obtain 15 groups of different experimental results and see Table 2.
Test 3: for observe drug extract and different substrates when 1: 9 the proportioning prepared Aidi drops in qualitative difference, according to 1: 9 ratio, with drug extract respectively with 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, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain the experiment of 15 pharmaceutical compositions that drug extract and different substrates constituted, and obtain 15 groups of different experimental results and see Table 3.
Second group: the test of mixed-matrix
1. the ratio that provides according to [preparation method] 1 takes by weighing the raw material of Chinese medicine of some, and it is standby to make the extract dry powder that contains Chinese medicine Mylabris, Radix Ginseng, the Radix Astragali, Radix Et Caulis Acanthopanacis Senticosi active constituents of medicine earlier according to [appendix: a kind of preparation method of Chinese medicine extract] joint again;
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 [preparation method] again, promptly can make the Aidi drops of various different sizes.
[result of the test]
Test 4: for observe drug extract and mixed-matrix when 1: 1 the proportioning prepared Aidi drops in qualitative difference, 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 drug extract is mixed mutually with 4 kinds of different mixed-matrixes again and make evenly, adopt homemade drop pill machine, 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 1: 3 the proportioning prepared Aidi drops in qualitative difference, 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 drug extract is mixed mutually with 4 kinds of different mixed-matrixes again and make evenly, adopt homemade drop pill machine, 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 1: 9 the proportioning prepared Aidi drops in qualitative difference, 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 drug extract is mixed mutually with 4 kinds of different mixed-matrixes again and make evenly, adopt homemade drop pill machine, 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 1: 1 the proportioning prepared Aidi drops in qualitative difference, 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 drug extract is mixed mutually with 4 kinds of different mixed-matrixes again and make evenly, adopt homemade drop pill machine, 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 1: 3 the proportioning prepared Aidi drops in qualitative difference, 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 drug extract is mixed mutually with 4 kinds of different mixed-matrixes again and make evenly, adopt homemade drop pill machine, 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 1: 9 the proportioning prepared Aidi drops in qualitative difference, 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 drug extract is mixed mutually with 4 kinds of different mixed-matrixes again and make evenly, adopt homemade drop pill machine, 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: for observe drug extract and mixed-matrix when 1: 1 the proportioning prepared Aidi drops in qualitative difference, 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 again and make evenly, adopt homemade drop pill machine, 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: for observe drug extract and mixed-matrix when 1: 3 the proportioning prepared Aidi drops in qualitative difference, 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 again and make evenly, adopt homemade drop pill machine, 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: for observe drug extract and mixed-matrix when 1: 9 the proportioning prepared Aidi drops in qualitative difference, 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 again and make evenly, adopt homemade drop pill machine, 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 2000 | 50.0 | 64 | ＜30 | ＞10 | + |
| Polyethylene Glycol 4000 | 50.0 | 76 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 6000 | 50.0 | 80 | ＜30 | ＞10 | +++ |
| Polyethylene Glycol 8000 | 50.0 | 83 | ＜30 | ＞10 | +++ |
| Polyethylene Glycol 10000 | 50.0 | 85 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 20000 | 50.0 | 86 | ＜30 | ＜10 | +++ |
| Polyoxyethylene stearate 40 esters | 50.0 | 74 | ＜30 | ＞10 | ++ |
| Betacyclodextrin | 50.0 | 72 | ＜30 | ＞10 | ++ |
| Poloxamer | 50.0 | 73 | ＜30 | ＞10 | ++ |
| Carboxymethyl starch sodium | 50.0 | 71 | ＜30 | ＞10 | ++ |
| Sodium lauryl sulphate | 50.0 | 69 | ＜30 | ＞10 | ++ |
| Stearic acid | 50.0 | 58 | ＜30 | ＞10 | ++ |
| Sodium stearate | 50.0 | 54 | ＜30 | ＞10 | +++ |
| Glycerin gelatine | 50.0 | 56 | ＜30 | ＞10 | +++ |
| Lac | 50.0 | 53 | ＞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 2000 | 25.0 | 79 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 4000 | 25.0 | 84 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 6000 | 25.0 | 90 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 8000 | 25.0 | 91 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 10000 | 25.0 | 93 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 20000 | 25.0 | 92 | ＜30 | ＜10 | +++ |
| Polyoxyethylene stearate 40 esters | 25.0 | 84 | ＜30 | ＜10 | ++ |
| Betacyclodextrin | 25.0 | 82 | ＜30 | ＜10 | ++ |
| Poloxamer | 25.0 | 85 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium | 25.0 | 81 | ＜30 | ＞10 | ++ |
| Sodium lauryl sulphate | 25.0 | 77 | ＜30 | ＞10 | ++ |
| Stearic acid | 25.0 | 72 | ＞30 | ＞10 | ++ |
| Sodium stearate | 25.0 | 74 | ＞30 | ＞10 | +++ |
| Glycerin gelatine | 25.0 | 68 | ＞30 | ＞10 | +++ |
| Lac | 25.0 | 70 | ＞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 2000 | 10.0 | 84 | ＜30 | ＞10 | ++ |
| Polyethylene Glycol 4000 | 10.0 | 88 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 6000 | 10.0 | 93 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 8000 | 10.0 | 93 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 10000 | 10.0 | 92 | ＜30 | ＜10 | +++ |
| Polyethylene Glycol 20000 | 10.0 | 94 | ＜30 | ＜10 | +++ |
| Polyoxyethylene stearate 40 esters | 10.0 | 89 | ＜30 | ＜10 | ++ |
| Betacyclodextrin | 10.0 | 87 | ＜30 | ＜10 | ++ |
| Poloxamer | 10.0 | 92 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium | 10.0 | 82 | ＜30 | ＞10 | +++ |
| Sodium lauryl sulphate | 10.0 | 81 | ＜30 | ＞10 | +++ |
| Stearic acid | 10.0 | 79 | ＞30 | ＞10 | +++ |
| Sodium stearate | 10.0 | 80 | ＞30 | ＞10 | +++ |
| Glycerin gelatine | 10.0 | 76 | ＞30 | ＞10 | +++ |
| Lac | 10.0 | 78 | ＞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 | 82 | ＜30 | ＞10 | ++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 50 | 82 | ＜30 | ＞10 | ++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 50 | 77 | ＜30 | ＞10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 50 | 73 | ＜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 | 88 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 25 | 87 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 25 | 83 | ＜30 | ＞10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 25 | 82 | ＜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 | 87 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | 10 | 86 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 10 | 85 | ＜30 | ＞10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 10 | 83 | ＜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 | 92 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 50 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 50 | 87 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 50 | 84 | ＜30 | ＞10 | ++ |
The group practices of table 8 drug extract and mixed-matrix
(drug extract: mixed-matrix=1: 3)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 5 | 25 | 92 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 25 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 25 | 89 | ＜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 | 93 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | 10 | 93 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | 10 | 91 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | 10 | 90 | ＜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 | 86 | ＜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 | 93 | ＜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 | 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 | 92 | ＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | 10 | 91 | ＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 10 | 91 | ＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 10 | 92 | ＜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, 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. one kind is used for the treatment of primary hepatocarcinoma, pulmonary carcinoma, and rectal cancer, malignant lymphoma, the Aidi drops of gynecologic malignant tumor is a raw material with Chinese medicine Mylabris, Radix Ginseng, the Radix Astragali, Radix Et Caulis Acanthopanacis Senticosi, is prepared from the pharmaceutically suitable carrier as substrate, it is characterized in that:
(1), accurately takes by weighing Mylabris 15g, Radix Ginseng 500g, Radix Astragali 1000g, Radix Et Caulis Acanthopanacis Senticosi 1500g, above-mentioned four flavors, Radix Ginseng section according to the weight portion meter, extract secondary with 50% alcohol heating reflux, 3 hours for the first time, 1.5 hours for the second time, merge extractive liquid,, filter, reclaim ethanol, medicinal liquid is standby; Three flavors such as medicinal residues and all the other Mylabris decoct with water three times, 3 hours for the first time, 1.5 hours for the second time, 1 hour for the third time, collecting decoction filters, and filtrate and Radix Ginseng extractive solution merge, with stone sulfur method precipitation process secondary, the gained supernatant adds ethanol to be made and contains alcohol amount and reach 80%, and standing over night is got the supernatant decompression recycling ethanol to there not being the alcohol flavor, at 0.1Mpa, be condensed into relative density under 60 ℃ the condition and be 1.3～1.35 thick paste, or with thick paste through the low-temperature reduced-pressure drying, pulverize, promptly get the extract that contains pharmaceutically active ingredient in above-mentioned 4 flavors, standby;
(2) described substrate is the mixture of Polyethylene Glycol and polyoxyethylene stearate 40 esters or carboxymethyl starch sodium, by weight, its mixed proportion is that the ratio of polyoxyethylene stearate 40 esters or carboxymethyl starch sodium and Polyethylene Glycol is 1: 1～1: 10, and the ratio of described extract and substrate is 1: 3;
(3) according to aforementioned proportion, accurately take by weighing described extract and substrate, be placed on heating while stirring in the heating container, until the fused solution that obtains containing described extract and substrate, or emulsion, or suspension, standby;
(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) treating that dropping-pill machine head and condensing agent are stable respectively and reach described state of temperature, fused solution or the emulsion or the suspension that will contain described extract and substrate, under the temperature conditions close with water dropper, make evenly through fully stirring, insulation, place in the water dropper jar of drop pill machine, splash in the condensing agent and shrink shaping promptly.
2. Aidi drops according to claim 1, it is characterized in that the condensing agent described in (4) be methyl-silicone oil or/and liquid paraffin or/and vegetable oil.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100028898A CN100528142C (en) | 2005-01-28 | 2005-01-28 | Aidi drops for treating cancers and preparation thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2005100028898A CN100528142C (en) | 2005-01-28 | 2005-01-28 | Aidi drops for treating cancers and preparation thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1679678A CN1679678A (en) | 2005-10-12 |
| CN100528142C true CN100528142C (en) | 2009-08-19 |
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|---|---|---|---|
| CNB2005100028898A Expired - Fee Related CN100528142C (en) | 2005-01-28 | 2005-01-28 | Aidi drops for treating cancers and preparation thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN100528142C (en) |
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2005
- 2005-01-28 CN CNB2005100028898A patent/CN100528142C/en not_active Expired - Fee Related
Non-Patent Citations (4)
| Title |
|---|
| . 卫生部颁药品标准中药成方制剂第20册. 1998 |
| 中国中药杂志. 郑鑫等，292-295，中药滴丸剂的研究进展. 2003 |
| 中国中药杂志. 郑鑫等，292-295，中药滴丸剂的研究进展. 2003 * |
| 卫生部颁药品标准中药成方制剂第20册. 1998 * |
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| Publication number | Publication date |
|---|---|
| CN1679678A (en) | 2005-10-12 |
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