CN1634510A - Yam rhizoma drop-pill and its preparation method - Google Patents
Yam rhizoma drop-pill and its preparation method Download PDFInfo
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Abstract
The invention relates to a medicinal oral preparation, i.e., a Japanese yam drop pill having the functions of warming channel, relaxing vein, and dispersing pathogenic wind, which can be applied for treating joint pain caused by rheumatism. The medicine is prepared through the conventional drop pill preparing process with the advantages of high biological availability, quick-speed medicine release, quick-speed effect, less toxic and side effects, higher medicinal content, smaller amount of administration, accurate administration dosage, easy administration, low price, and facilitated carrying.
Description
Technical field
The present invention relates to a kind of Shujin Lip river network that has, the wind-expelling pain-stopping effect is used for the treatment of the pharmaceutical composition of the arthralgia due to the rheumatism resistance low, particularly based on the prescription of Chinese traditional patent formulation Rhizoma Dioscoreae Nipponicae injection, changes a social system a kind of oral formulations that forms through dosage form.
Background technology
According to the drug standard WS promulgated by the ministries or commissions of the Central Government of country
3The Rhizoma Dioscoreae Nipponicae injection that prescription that provides among-the B-3283-98 and extraction process are prepared from, be a kind of Chinese medicine that is used for the treatment of the arthralgia due to the rheumatism resistance low, 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-3283-98 and extraction process:
Prescription: Rhizoma Dioscoreae Nipponicae 1000g;
Method for making: get Rhizoma Dioscoreae Nipponicae 1000g, decoct with water secondary, each 1 hour, collecting decoction filters, and filtrate is concentrated into about 1000g, add ethanol and make and contain alcohol amount and reach 40%, cold preservation filters, filtrate recycling ethanol adds ethanol again and makes and contain alcohol amount and reach 60%, cold preservation, draw supernatant, reclaim ethanol, add ethanol again and make and contain the alcohol amount and reach 80%, supernatant is drawn in cold preservation; Reclaim ethanol to most; Add the injection water to nearly 1000ml, boil, add active carbon 3g, continued to boil 5 minutes, cold preservation filters, and filtrate is transferred pH value, adds benzyl alcohol 20ml, replenishes water for injection to 1000ml, filter to clear and bright, and embedding, sterilization, promptly.
Be explained as follows for this product in the appended Rhizoma Dioscoreae Nipponicae injection description:
Nomenclature of drug: Rhizoma Dioscoreae Nipponicae injection;
Main component: the dry rhizome of Dioscoreaceae plant Dioscorea nipponica Mak. Ningpo Yam Rhizome;
Character: this product is the clear liquid of yellowish-brown;
Function cures mainly: relaxing muscles and tendons and activating QI and blood in the collateral, wind-expelling pain-stopping.Be used for the arthralgia due to the rheumatism Zu Paralysis;
Usage and dosage: intramuscular injection, a 2ml, 1～2 time on the one.
Storage: sealing, lucifuge.
Because of reasons such as technologies of preparing, the oral formulations of most drug, 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.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.Therefore, be necessary to seek the peroral dosage form of better Rhizoma Dioscoreae Nipponicae medicine to satisfy the needs that clinical treatment and family use.
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 is to replenish the existing deficiency that is used for the treatment of the oral drug preparation of the arthralgia due to the rheumatism resistance low, and a kind of bioavailability height is provided, release fast, quick produce effects, toxic and side effects is little, manufacturing and medical treatment cost are low, low price, the Yam rhizoma drop-pill that is suitable for family to use.
Yam rhizoma drop-pill involved in the present invention determines that through a large amount of experiment sievings based on Chinese traditional patent formulation Rhizoma Dioscoreae Nipponicae injection extracting 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 Yam rhizoma drop-pill involved in the present invention:
[preparation method]
1. be unit with g or kg, calculate, get the Rhizoma Dioscoreae Nipponicae 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 the Rhizoma Dioscoreae Nipponicae of some according to weight, decocts with water secondary, each 1 hour, collecting decoction filtered, add ethanol after filtrate concentrates and make and contain the alcohol amount and reach 40%, cold preservation filters, filtrate recycling ethanol adds ethanol again and makes and contain alcohol amount and reach 60%, cold preservation, draw supernatant, reclaim ethanol, add ethanol again and make and contain the alcohol amount and reach 80%, supernatant is drawn in cold preservation; Reclaim ethanol to the greatest extent,, be condensed into relative density under 60 ℃ the condition and be 1.3～1.35 thick paste at 0.1Mpa, 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 Rhizoma Dioscoreae Nipponicae injection that is prepared from according to the prescription that provides among the drug standard WS3-B-3283-98 promulgated by the ministries or commissions of the Central Government of country and extraction process, it is a kind of Chinese medicine that is used for the treatment of the arthralgia due to the rheumatism resistance low, 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 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.Therefore, be necessary to seek the peroral dosage form of better Rhizoma Dioscoreae Nipponicae medicine to satisfy the needs that clinical treatment and family use; 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.
Yam rhizoma drop-pill involved in the present invention is compared with the Rhizoma Dioscoreae Nipponicae injection, and following beneficial effect is arranged:
1. Yam rhizoma drop-pill involved in the present invention; utilize surfactant to be substrate; make solid dispersion with extractum that contains the Rhizoma Dioscoreae Nipponicae 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.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. Yam rhizoma drop-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.
3. Yam rhizoma drop-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.
In sum, make Yam rhizoma drop-pill 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 Yam rhizoma drop-pill 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 Rhizoma Dioscoreae Nipponicae 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 Yam rhizoma drop-pill of various different sizes.
[result of the test]
Test 1: for observe drug extract and different substrates when 1: 1 the proportioning prepared Yam rhizoma drop-pill 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 Yam rhizoma drop-pill 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 Yam rhizoma drop-pill 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 Rhizoma Dioscoreae Nipponicae 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 Yam rhizoma drop-pill of various different sizes.
[result of the test]
Test 4: for observe drug extract and mixed-matrix when 1: 1 the proportioning prepared Yam rhizoma drop-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 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 Yam rhizoma drop-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 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 Yam rhizoma drop-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 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 Yam rhizoma drop-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 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 Yam rhizoma drop-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 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 Yam rhizoma drop-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 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 Yam rhizoma drop-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 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 Yam rhizoma drop-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 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 Yam rhizoma drop-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 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 | ??77 | ??＜30 | ??＞10 | ++ |
| Polyethylene Glycol 6000 | ??50.0 | ??80 | ??＜30 | ??＞10 | +++ |
| Polyethylene Glycol 8000 | ??50.0 | ??83 | ??＜30 | ??＞10 | +++ |
| Polyethylene Glycol 10000 | ??50.0 | ??87 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 20000 | ??50.0 | ??86 | ??＜30 | ??＜10 | +++ |
| Polyoxyethylene stearate 40 esters | ??50.0 | ??75 | ??＜30 | ??＞10 | ++ |
| Betacyclodextrin | ??50.0 | ??70 | ??＜30 | ??＞10 | ++ |
| Poloxamer | ??50.0 | ??72 | ??＜30 | ??＞10 | ++ |
| Carboxymethyl starch sodium | ??50.0 | ??71 | ??＜30 | ??＞10 | ++ |
| Sodium lauryl sulphate | ??50.0 | ??69 | ??＜30 | ??＞10 | ++ |
| Stearic acid | ??50.0 | ??54 | ??＜30 | ??＞10 | ++ |
| Sodium stearate | ??50.0 | ??54 | ??＜30 | ??＞10 | +++ |
| Glycerin gelatine | ??50.0 | ??53 | ??＜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 2000 | ??25.0 | 79 | ??＜30 | ??＞10 | ++ |
| Polyethylene Glycol 4000 | ??25.0 | 83 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 6000 | ??25.0 | 91 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 8000 | ??25.0 | 90 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 10000 | ??25.0 | 93 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 20000 | ??25.0 | 92 | ??＜30 | ??＜10 | +++ |
| Polyoxyethylene stearate 40 esters | ??25.0 | 86 | ??＜30 | ??＜10 | ++ |
| Betacyclodextrin | ??25.0 | 84 | ??＜30 | ??＜10 | ++ |
| Poloxamer | ??25.0 | 85 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium | ??25.0 | 81 | ??＜30 | ??＞10 | ++ |
| Sodium lauryl sulphate | ??25.0 | 76 | ??＜30 | ??＞10 | ++ |
| Stearic acid | ??25.0 | 74 | ??＞30 | ??＞10 | ++ |
| Sodium stearate | ??25.0 | 73 | ??＞30 | ??＞10 | +++ |
| Glycerin gelatine | ??25.0 | 69 | ??＞30 | ??＞10 | +++ |
| Lac | ??25.0 | 69 | ??＞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 | ??85 | ??＜30 | ??＞10 | ++ |
| Polyethylene Glycol 4000 | ??10.0 | ??88 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 6000 | ??10.0 | ??91 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 8000 | ??10.0 | ??93 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 10000 | ??10.0 | ??91 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 20000 | ??10.0 | ??94 | ??＜30 | ??＜10 | +++ |
| Polyoxyethylene stearate 40 esters | ??10.0 | ??90 | ??＜30 | ??＜10 | ++ |
| Betacyclodextrin | ??10.0 | ??87 | ??＜30 | ??＜10 | ++ |
| Poloxamer | ??10.0 | ??92 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium | ??10.0 | ??86 | ??＜30 | ??＞10 | +++ |
| Sodium lauryl sulphate | ??10.0 | ??81 | ??＜30 | ??＞10 | +++ |
| Stearic acid | ??10.0 | ??79 | ??＞30 | ??＞10 | +++ |
| Sodium stearate | ??10.0 | ??81 | ??＞30 | ??＞10 | +++ |
| Glycerin gelatine | ??10.0 | ??76 | ??＞30 | ??＞10 | +++ |
| Lac | ??10.0 | ??75 | ??＞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 | ??83 | ??＜30 | ??＞10 | ++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ??50 | ??77 | ??＜30 | ??＞10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ??50 | ??74 | ??＜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 | ??88 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | 25 | ??85 | ??＜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 | ??90 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | ??50 | ??92 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ??50 | ??88 | ??＜30 | ??＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ??50 | ??85 | ??＜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 | ??91 | ??＜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 | ??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 | 93 | ??＜30 | ＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | ??10 | 93 | ??＜30 | ＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ??10 | 92 | ??＜30 | ＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ??10 | 89 | ??＜30 | ＜10 | +++ |
The group practices of table 10 drug extract and mixed-matrix
(drug extract: mixed-matrix=1: 1)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 10 | ??50 | ??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 | ??86 | ??＜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 | ??92 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | ??25 | ??91 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | ??25 | ??89 | ??＜30 | ??＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | ??25 | ??86 | ??＜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 | ??93 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | ??10 | ??92 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | ??10 | ??90 | ??＜30 | ??＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | ??10 | ??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 (7)
1. a pharmaceutical composition Yam rhizoma drop-pill that is used for the treatment of the arthralgia due to the rheumatism resistance low is a raw material with the Chinese medicine Rhizoma Dioscoreae Nipponicae, be prepared from a certain proportion of pharmaceutically suitable carrier, wherein:
1.1. with g or kg is unit, calculates according to weight, takes by weighing the Rhizoma Dioscoreae Nipponicae of some, makes drug extract thick paste or dry powder through the extracting method of routine;
1.2. 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;
1.3. proportioning---with g or kg is unit, by weight, and drug extract: substrate=1: 1～1: 9.
2. Yam rhizoma drop-pill as claimed in claim 1 is characterized in that: described substrate is the mixture of Polyethylene Glycol and polyoxyethylene stearate 40 esters or Polyethylene Glycol and poloxamer or Polyethylene Glycol and carboxymethyl starch sodium or Polyethylene Glycol and betacyclodextrin; With g or kg is unit, and by weight, its mixed proportion is polyoxyethylene stearate 40 esters: Polyethylene Glycol or poloxamer: Polyethylene Glycol or carboxymethyl starch sodium: Polyethylene Glycol or betacyclodextrin: Polyethylene Glycol=1: 1～1: 10.
3. any Yam rhizoma drop-pill as claimed in claim 1 or 2 is characterized in that: the mixed proportion of described drug extract and substrate is 1: 1～1: 5.
4. Yam rhizoma drop-pill as claimed in claim 1, it is characterized in that described drug extract thick paste or dry powder obtain by the following method: with g or kg is unit, take by weighing the Rhizoma Dioscoreae Nipponicae of some according to weight, decoct with water secondary, each 1 hour, collecting decoction, filter, add ethanol after filtrate concentrates and make and contain the alcohol amount and reach 40%, cold preservation filters, filtrate recycling ethanol, add ethanol again and make and contain alcohol amount and reach 60%, supernatant is drawn in cold preservation, reclaim ethanol, add ethanol again and make and contain alcohol amount and reach 80%, supernatant is drawn in cold preservation; Reclaim ethanol to the greatest extent,, be condensed into relative density under 60 ℃ the condition and be 1.3～1.35 thick paste at 0.1Mpa, or with thick paste through the low-temperature reduced-pressure drying, pulverize, promptly get dry powder.
5. the preparation method of a Yam rhizoma drop-pill is characterized in that being made of following process:
5.1. with g or kg is unit, calculates according to weight, takes by weighing the Rhizoma Dioscoreae Nipponicae of some, through the extracting method of routine make the drug extract thick paste or dry powder standby;
5.2. 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;
5.3. proportioning---with g or kg is unit, by weight, and drug extract: substrate=1: 1～1: 9;
5.4., 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;
5.5. 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 ℃;
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, insulation, place in the water dropper jar of drop pill machine, splash in the condensing agent by water dropper and shrink shaping promptly.
6. as the preparation method of Yam rhizoma drop-pill as described in the claim 5, it is characterized in that method 5.1 described drug extract thick pastes or dry powder obtain by the following method: with g or kg is unit, take by weighing the Rhizoma Dioscoreae Nipponicae of some according to weight, decoct with water secondary, each 1 hour, collecting decoction, filter, add ethanol after filtrate concentrates and make and contain the alcohol amount and reach 40%, cold preservation filters, filtrate recycling ethanol, add ethanol again and make and contain alcohol amount and reach 60%, supernatant is drawn in cold preservation, reclaim ethanol, add ethanol again and make and contain alcohol amount and reach 80%, supernatant is drawn in cold preservation; Reclaim ethanol to the greatest extent,, be condensed into relative density under 60 ℃ the condition and be 1.3～1.35 thick paste at 0.1Mpa, or with thick paste through the low-temperature reduced-pressure drying, pulverize, promptly get dry powder.
7. as the preparation method of Yam rhizoma drop-pill as described in the claim 5, it is characterized in that: method 5.6 described condensing agents are methyl-silicone oils or/and liquid paraffin or/and vegetable oil.
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|---|---|---|---|
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104721469A (en) * | 2015-03-16 | 2015-06-24 | 天津大学 | Method for extracting dioscorea nipponica |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104721469A (en) * | 2015-03-16 | 2015-06-24 | 天津大学 | Method for extracting dioscorea nipponica |
| CN104721469B (en) * | 2015-03-16 | 2018-06-26 | 天津大学 | A kind of extracting method of rhizoma dioscoreae nipponicae |
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