CN1679671A - Compound berberine dropping ball and preparation thereof - Google Patents
Compound berberine dropping ball and preparation thereof Download PDFInfo
- Publication number
- CN1679671A CN1679671A CNA2005100028811A CN200510002881A CN1679671A CN 1679671 A CN1679671 A CN 1679671A CN A2005100028811 A CNA2005100028811 A CN A2005100028811A CN 200510002881 A CN200510002881 A CN 200510002881A CN 1679671 A CN1679671 A CN 1679671A
- Authority
- CN
- China
- Prior art keywords
- polyethylene glycol
- substrate
- mixed
- berberine
- principal agent
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Classifications
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Medicinal Preparation (AREA)
Abstract
A dripping pill of the compound berberine hydrochloride for treating diarrhea, dysentery, etc is disclosed. Its advantages are high release speed and quickly taking its high curative effect.
Description
Technical field
The present invention relates to a kind of heat clearing and damp drying that has, circulation of qi promoting, pain relieving, the dysentery relieving anti-diarrhea effect is used for damp-heat in the large intestine, red white diarrhea, tenesmus or devastating diarrhea and watery stools, the pharmaceutical composition of treatment for diseases such as burning sensation of the anus particularly based on the Chinese traditional patent formulation FUFANG HUANGLIANSU PIAN, is changed a social system a kind of drug composition oral dropping pill formulation that forms through dosage form.
Background technology
According to national drug standards WS
3The FUFANG HUANGLIANSU PIAN that prescription that provides among-the B-2753-97 and extraction process are prepared from is a kind of heat clearing and damp drying, circulation of qi promoting, pain relieving, dysentery relieving antidiarrheal.Be used for damp-heat in the large intestine, red white diarrhea, tenesmus or devastating diarrhea and watery stools, symptom treatment tablet class preparations such as burning sensation of the anus, 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 drug standard WS
3The prescription of the FUFANG HUANGLIANSU PIAN that provides among-the B-2753-97 and extraction process:
Prescription: berberine hydrochloride 17g, Radix Aucklandiae 114g, Radix Paeoniae Alba 160g, Fructus Evodiae 40g;
Method for making: above four flavors, the Radix Aucklandiae, evodiae powder are broken into fine powder, sieve; The Radix Paeoniae Alba is ground into coarse powder, according to percolation (appendix IO) under fluid extract and the extractum item, makes solvent with 70% ethanol, floods and carries out percolation after 24 hours, almost colourless to the liquid of filtering, collect percolate, reclaim ethanol, be condensed into thick paste, add above-mentioned fine powder, mixing, drying is pulverized, and adds berberine hydrochloride and right amount of auxiliary materials, mixing is made granule, drying, be pressed into 1000, sugar coating, promptly.
Be explained as follows for this tablet in the appended FUFANG HUANGLIANSU PIAN description:
Nomenclature of drug: FUFANG HUANGLIANSU PIAN;
Main component: berberine hydrochloride, the Radix Aucklandiae, the Radix Paeoniae Alba, Fructus Evodiae;
Function cures mainly: a heat clearing and damp drying, circulation of qi promoting, pain relieving, dysentery relieving antidiarrheal.Be used for damp-heat in the large intestine, red white diarrhea, tenesmus or devastating diarrhea and watery stools, symptoms such as burning sensation of the anus;
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.
Summary of the invention
Purpose of the present invention, be to replenish existing be used for damp-heat in the large intestine, red white diarrhea, tenesmus or devastating diarrhea and watery stools, the deficiency of the oral drug preparation of symptom treatments such as burning sensation of the anus, provide a kind of bioavailability height, release fast, produce effects fast, toxic and side effects is littler, and the medicament contg height, cheap, and free of contamination drug composition oral preparation compound berberine dropping ball in producing.
Compound berberine dropping ball involved in the present invention determines that through a large amount of experiment sievings based on the extraction process of Chinese traditional patent formulation FUFANG HUANGLIANSU PIAN, 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 compound berberine dropping ball involved in the present invention:
[preparation method]
1. be unit with g or kg, according to the weight portion meter, get 17 parts of berberine hydrochloride, 114 parts of the Radix Aucklandiae, 160 parts of the Radix Paeoniae Albas, 40 parts of Fructus Evodiaes, the Radix Aucklandiae, evodiae powder are broken into fine powder, sieve; The Radix Paeoniae Alba is ground into coarse powder, according to percolation (appendix IO) under fluid extract and the extractum item, makes solvent with 70% ethanol, flood and carry out percolation after 24 hours, almost colourless to the liquid of filtering, collect percolate, reclaim ethanol, be condensed into thick paste, add above-mentioned fine powder, mixing, dry, pulverize, add berberine hydrochloride, it is standby promptly to get medicine dry powder;
2. substrate: the mixture of one or more in pharmaceutically suitable carrier such as Polyethylene Glycol (1000～20000), 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 principal agent: substrate=1: 1～1: 9;
4. according to the given ratio of prescription, accurately take by weighing principal agent and substrate, be placed on heating while stirring in the heating container, standby until the fused solution that obtains containing principal agent 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, 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 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.
Beneficial effect
According to national drug standards WS
3The FUFANG HUANGLIANSU PIAN that prescription that provides among-the B-2753-97 and extraction process are prepared from is a heat clearing and damp drying, circulation of qi promoting, pain relieving, dysentery relieving antidiarrheal.Be used for damp-heat in the large intestine, red white diarrhea, tenesmus or devastating diarrhea and watery stools, the tablet class preparation of symptom treatments such as burning sensation of the anus, 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.
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.
Compound berberine dropping ball involved in the present invention is compared with FUFANG HUANGLIANSU PIAN, has following beneficial effect:
1. compound berberine dropping ball involved in the present invention; utilize surfactant etc. to be substrate; make solid dispersion with extractum that contains active constituents of medicine or dry powder; 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.With the drop pill of solid dispersion technology preparation, can adopt oral, can also sublingual administration, effective ingredient is fully contacted with mucomembranous surface, by the mucomembranous epithelial cell absorption, directly enter 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.
2. compound berberine dropping ball 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.
3. compound berberine dropping ball 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.
In sum, make compound berberine dropping ball 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).
The specific embodiment
Now with several groups of specific embodiments, be described further with regard to the preparation method of compound berberine dropping ball of the present invention.
First group: the test of single-matrix
1. be unit with g or kg, according to the weight portion meter, get 17 parts of berberine hydrochloride, 114 parts of the Radix Aucklandiae, 160 parts of the Radix Paeoniae Albas, 40 parts of Fructus Evodiaes, the Radix Aucklandiae, evodiae powder are broken into fine powder, sieve; The Radix Paeoniae Alba is ground into coarse powder, according to percolation (appendix IO) under fluid extract and the extractum item, makes solvent with 70% ethanol, flood and carry out percolation after 24 hours, almost colourless to the liquid of filtering, collect percolate, reclaim ethanol, be condensed into thick paste, add above-mentioned fine powder, mixing, dry, pulverize, add berberine hydrochloride, it is standby promptly to get medicine dry powder;
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 principal agent: substrate=1: 1～1: 9;
4. be prepared according to the process of [preparation method] 4～7 again, promptly can make the compound berberine dropping ball of various different sizes.
[result of the test]
Test 1: for observe principal agent and different substrates when 1: 1 the proportioning prepared compound berberine dropping ball in qualitative difference, according to 1: 1 ratio, with principal agent 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, 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 principal agent and different substrates, and obtain 15 groups of different experimental results and see Table 1.
Test 2: for observe principal agent and different substrates when 1: 3 the proportioning prepared compound berberine dropping ball in qualitative difference, according to 1: 3 ratio, with principal agent 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, 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 principal agent and different substrates, and obtain 15 groups of different experimental results and see Table 2.
Test 3: for observe principal agent and different substrates when 1: 9 the proportioning prepared compound berberine dropping ball in qualitative difference, according to 1: 9 ratio, with principal agent 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, 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 principal agent and different substrates, and obtain 15 groups of different experimental results and see Table 3.
Second group: the test of mixed-matrix
1. be unit with g or kg, according to the weight portion meter, get 17 parts of berberine hydrochloride, 114 parts of the Radix Aucklandiae, 160 parts of the Radix Paeoniae Albas, 40 parts of Fructus Evodiaes, the Radix Aucklandiae, evodiae powder are broken into fine powder, sieve; The Radix Paeoniae Alba is ground into coarse powder, according to percolation (appendix IO) under fluid extract and the extractum item, makes solvent with 70% ethanol, flood and carry out percolation after 24 hours, almost colourless to the liquid of filtering, collect percolate, reclaim ethanol, be condensed into thick paste, add above-mentioned fine powder, mixing, dry, pulverize, add berberine hydrochloride, it is standby promptly to get medicine dry powder;
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 mixing principal agent: 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 compound berberine dropping ball of various different sizes.
[result of the test]
Test 4: for observe principal agent and mixed-matrix when 1: 1 the proportioning prepared compound berberine dropping ball 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 principal agent 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 principal agent and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 4.
Test 5: for observe principal agent and mixed-matrix when 1: 3 the proportioning prepared compound berberine dropping ball 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 principal agent 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 principal agent and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 5.
Test 6: for observe principal agent and mixed-matrix when 1: 9 the proportioning prepared compound berberine dropping ball 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 principal agent 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 principal agent and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 6.
Test 7: for observe principal agent and mixed-matrix when 1: 1 the proportioning prepared compound berberine dropping ball 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 principal agent 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 principal agent and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 7.
Test 8: for observe principal agent and mixed-matrix when 1: 3 the proportioning prepared compound berberine dropping ball 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 principal agent 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 principal agent and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 8.
Test 9: for observe principal agent and mixed-matrix when 1: 9 the proportioning prepared compound berberine dropping ball 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 principal agent 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 principal agent and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 9.
Test 10: in order to observe compound berberine dropping ball that principal agent and mixed-matrix make when 1: 1 the proportioning 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 principal agent 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 principal agent and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 10.
Test 11: in order to observe compound berberine dropping ball that principal agent and mixed-matrix make when 1: 3 the proportioning 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 principal agent 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 principal agent and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 11.
Test 12: in order to observe compound berberine dropping ball that principal agent and mixed-matrix make when 1: 9 the proportioning 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 principal agent 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 principal agent and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 12.
The group practices of table 1 principal agent and single-matrix
(principal agent: 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 | ????85 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 2000 | ????50.0 | ????85 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 4000 | ????50.0 | ????84 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 6000 | ????50.0 | ????82 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 8000 | ????50.0 | ????79 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 9300 | ????50.0 | ????88 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 10000 | ????50.0 | ????80 | ????＜30 | ????＞10 | ++ |
| Polyethylene Glycol 20000 | ????50.0 | ????80 | ????＜30 | ????＞10 | ++ |
| Polyoxyethylene stearate 40 esters | ????50.0 | ????78 | ????＜30 | ????＞10 | ++ |
| Betacyclodextrin | ????50.0 | ????72 | ????＜30 | ????＞10 | + |
| Poloxamer | ????50.0 | ????79 | ????＜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 principal agent and single-matrix
(principal agent: 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 | ????85 | ????＜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 | ????92 | ????＜30 | ????＜10 | +++ |
| Polyethylene Glycol 20000 | ????25.0 | ????91 | ????＜30 | ????＜10 | ++ |
| Polyoxyethylene stearate 40 esters | ????25.0 | ????92 | ????＜30 | ????＜10 | ++ |
| Betacyclodextrin | ????25.0 | ????82 | ????＜30 | ????＞10 | ++ |
| Poloxamer | ????25.0 | ????89 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium | ????25.0 | ????80 | ????＜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 principal agent and single-matrix
(principal agent: 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 | ????50.0 | ????85 | ????＜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 | ????93 | ????＜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 principal agent and mixed-matrix
(principal agent: 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 | ????86 | ????＜30 | ????＜10 | ++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ????50 | ????81 | ????＜30 | ????＞10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ????50 | ????78 | ????＜30 | ????＞10 | + |
The group practices of table 5 principal agent and mixed-matrix
(principal agent: 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 | ????92 | ????＜30 | ????＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | ????25 | ????93 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ????25 | ????89 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ????25 | ????86 | ????＜30 | ????＞10 | ++ |
The group practices of table 6 principal agent and mixed-matrix
(principal agent: 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 | ????92 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ????10 | ????90 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ????10 | ????84 | ????＜30 | ????＞10 | +++ |
The group practices of table 7 principal agent and mixed-matrix
(principal agent: 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 | ????94 | ????＜30 | ????＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | ????50 | ????94 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ????50 | ????89 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ????50 | ????83 | ????＜30 | ????＞10 | ++ |
The group practices of table 8 principal agent and mixed-matrix
(principal agent: 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 | ????95 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ????25 | ????92 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ????25 | ????89 | ????＜30 | ????＜10 | ++ |
The group practices of table 9 principal agent and mixed-matrix
(principal agent: 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 principal agent and mixed-matrix
(principal agent: 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 | ????91 | ????＜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 principal agent and mixed-matrix
(principal agent: 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 | ????93 | ????＜30 | ????＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | ????25 | ????90 | ????＜30 | ????＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | ????25 | ????87 | ????＜30 | ????＜10 | +++ |
The group practices of table 12 principal agent and mixed-matrix
(principal agent: 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 | ????94 | ????＜30 | ????＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | ????10 | ????93 | ????＜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 principal agent 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 principal agent 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 principal agent 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 (5)
1. one kind is used for damp-heat in the large intestine, red white diarrhea, tenesmus or devastating diarrhea and watery stools, the pharmaceutical composition compound berberine dropping ball of treatment for diseases such as burning sensation of the anus, with berberine hydrochloride, the Radix Aucklandiae, the Radix Paeoniae Alba, Fructus Evodiae is raw material, be prepared from a certain proportion of pharmaceutically suitable carrier, wherein:
1.1 with g or kg is unit, according to the weight portion meter, gets 17 parts of berberine hydrochloride, 114 parts of the Radix Aucklandiae, 160 parts of the Radix Paeoniae Albas, 40 parts of Fructus Evodiaes, the Radix Aucklandiae, evodiae powder are broken into fine powder, sieve; The Radix Paeoniae Alba is ground into coarse powder, according to percolation (appendix IO) under fluid extract and the extractum item, makes solvent with 70% ethanol, flood and carry out percolation after 24 hours, almost colourless to the liquid of filtering, collect percolate, reclaim ethanol, be condensed into thick paste, add above-mentioned fine powder, mixing, dry, pulverize, add berberine hydrochloride, it is standby promptly to get medicine dry powder;
1.2 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;
1.3 proportioning: with g or kg is unit, by weight, and drug extract: substrate=1: 1～1: 9.
2. compound berberine dropping ball 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 compound berberine dropping ball 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 compound berberine dropping ball is characterized in that being made of following process:
4.1 with g or kg is unit, according to the weight portion meter, gets 17 parts of berberine hydrochloride, 114 parts of the Radix Aucklandiae, 160 parts of the Radix Paeoniae Albas, 40 parts of Fructus Evodiaes, the Radix Aucklandiae, evodiae powder are broken into fine powder, sieve; The Radix Paeoniae Alba is ground into coarse powder, according to percolation (appendix IO) under fluid extract and the extractum item, makes solvent with 70% ethanol, flood and carry out percolation after 24 hours, almost colourless to the liquid of filtering, collect percolate, reclaim ethanol, be condensed into thick paste, add above-mentioned fine powder, mixing, dry, pulverize, add berberine hydrochloride, it is standby promptly to get medicine dry powder;
4.2 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;
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 adopt homemade or general drop pill machine, and 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-5 ℃～40 ℃;
4.6 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, under the temperature conditions close, be incubated with the water dropper temperature, place in the water dropper jar of drop pill machine, splash in the condensing agent by water dropper and shrink shaping promptly.
5. as the preparation method of compound berberine dropping ball as described in the claim 4, it is characterized in that: method 4.6 described condensing agents are methyl-silicone oils or/and liquid paraffin or/and vegetable oil.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2005100028811A CN1679671A (en) | 2005-01-28 | 2005-01-28 | Compound berberine dropping ball and preparation thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2005100028811A CN1679671A (en) | 2005-01-28 | 2005-01-28 | Compound berberine dropping ball and preparation thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1679671A true CN1679671A (en) | 2005-10-12 |
Family
ID=35066677
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2005100028811A Pending CN1679671A (en) | 2005-01-28 | 2005-01-28 | Compound berberine dropping ball and preparation thereof |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1679671A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102228530A (en) * | 2011-06-25 | 2011-11-02 | 南方医科大学 | Capsule for treating ulcerative colitis |
-
2005
- 2005-01-28 CN CNA2005100028811A patent/CN1679671A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102228530A (en) * | 2011-06-25 | 2011-11-02 | 南方医科大学 | Capsule for treating ulcerative colitis |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1686362A (en) | Hairy holly root drip pill and its preparation method | |
| CN1660364A (en) | 'Lianzhi' anti inflammation drop pill in use for clearing away heat and toxic material and preparation method | |
| CN1297254C (en) | Drop pills containing bear gall and tendril-leaved fritillary bulb and preparation method thereof | |
| CN1297255C (en) | Dripping pills for treating high blood fat and its preparing method | |
| CN1634509A (en) | Yitongshu drop pill for treating pain and its preparation method | |
| CN1679675A (en) | Chuanhuang anti-inflammation drops for clearing away heat and detoxicating, and preparation thereof | |
| CN1679671A (en) | Compound berberine dropping ball and preparation thereof | |
| CN1287771C (en) | Almond cough-relieving drop pills and preparation method thereof | |
| CN1679669A (en) | Polygala dropping balls and preparation thereof | |
| CN1634478A (en) | Tendril-leaved fritillary bulb loquat drop pills and preparation method thereof | |
| CN1686381A (en) | Jaundice capillaris drip pill and its preparation method | |
| CN1284529C (en) | Compound gastrodia elata drop pills | |
| CN1634452A (en) | Yin-nourishing lung-heat clearing drop pills | |
| CN1679673A (en) | Isatis root drops and preparation thereof | |
| CN1660316A (en) | Drop pills preparation in use for treating bronchitis and preparation method | |
| CN1709413A (en) | Golden gallbladder-normalizing dropping pill for relaxing-liver and normalizing gallbladder, and its preparing method | |
| CN1686382A (en) | Throat clearing drip pill and its preparation method | |
| CN1682833A (en) | Ginseng and schisandra fruit dripping pill and its preparing method | |
| CN1682817A (en) | Throat dripping pill for clearing away heat and toxic material and its preparing method | |
| CN1301095C (en) | 'Yinchai' drop pills for treating cold, fever and cough and preparation method | |
| CN1307978C (en) | Drop pill for diminishing inflammation in four seasons and its preparation method | |
| CN1301094C (en) | Throat pain relieving anti-inflammation drop pills for treating oral disease and preparation method thereof | |
| CN1284530C (en) | Compound tornado drop pills | |
| CN1682818A (en) | Fleabane and earthworm dripping pill and its preparing method | |
| CN1679672A (en) | Rabdosia rubescens drops and preparation thereof |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C12 | Rejection of a patent application after its publication | ||
| RJ01 | Rejection of invention patent application after publication |