CN1634507A - Tripterygium total terpenoids drop pill and its preparation method - Google Patents
Tripterygium total terpenoids drop pill and its preparation method Download PDFInfo
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Abstract
The invention relates to a medicinal oral preparation, i.e., Tripterygium wilfordii terpenes dripping pill for treating antirheumatic diseases. The advantages of the invention include 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. The medicine is prepared through the conventional drop pill preparing process.
Description
Technical field
The present invention relates to a kind of expelling wind and removing dampness that has, the Shujin Lip river of living, the reducing swelling and alleviating pain effect is used for the treatment of the cold-damp invasion and attack, the arthralgia that obstruction of collaterals by blood stasis causes, joint stuffiness, aversion to cold and cold limbs is met cold increasing the weight of, weakness of the waist and knees, or disease such as cold and heat are staggered; Rheumatoid arthritis is seen the pharmaceutical composition that above-mentioned symptom person is arranged, and particularly based on Chinese traditional patent formulation tripterygium total terpenoids sheet, changes a social system a kind of drug composition oral dropping pill formulation that forms through dosage form.
Background technology
The tripterygium total terpenoids sheet that is prepared from according to the prescription that provides among the national drug standards WS-10715 (ZD-0715)-2002 and preparation method, it is a kind of expelling wind and removing dampness that has, Shujin Lip river alive, the reducing swelling and alleviating pain effect is used for the treatment of the cold-damp invasion and attack, the arthralgia that obstruction of collaterals by blood stasis causes, joint stuffiness, aversion to cold and cold limbs is met cold increasing the weight of, weakness of the waist and knees, or disease such as cold and heat are staggered; Rheumatoid arthritis sees above-mentioned symptom person's oral Chinese medicine preparation, through clinical verification, steady quality, determined curative effect is clinical and family is used for the treatment of the common drug preparation of above disease.
Below be the contained partial content of this drug standard:
Prescription: Radix Tripterygii Wilfordii extract (in Radix Tripterygii Wilfordii lactone alcohol) 20mg, starch 75g, dextrin 75g, sucrose 4g, micropowder silica gel 0.75g;
Method for making: get Radix Tripterygii Wilfordii extract, behind dextrin, starch, the abundant mixing of micropowder silica gel, add 40% syrup, make granule, drying, tabletting, the bag film-coat, promptly.
Be explained as follows for this product in the appended description:
Nomenclature of drug: tripterygium total terpenoids sheet;
Main component: Radix Tripterygii Wilfordii extract;
Character: this product is a Film coated tablets, removes film-coat and shows brown;
Function cures mainly: expelling wind and removing dampness, Shujin Lip river alive, reducing swelling and alleviating pain.Be used for cold-damp invasion and attack, the arthralgia that obstruction of collaterals by blood stasis causes, joint stuffiness, aversion to cold and cold limbs is met cold increasing the weight of, weakness of the waist and knees, or disease such as cold and heat are staggered; Rheumatoid arthritis is seen above-mentioned symptom person;
Usage and dosage: oral, one time 2,3 times on the one.
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 is to replenish the existing cold-damp invasion and attack that are used for the treatment of, the arthralgia that obstruction of collaterals by blood stasis causes, and joint stuffiness, aversion to cold and cold limbs is met cold increasing the weight of, weakness of the waist and knees, or disease such as cold and heat are staggered; The deficiency of rheumatoid arthritis sees above-mentioned symptom person's oral drug preparation, a kind of bioavailability height is provided, release fast, quick produce effects, toxic and side effects is littler, and medicament contg height, taking dose is little, and taking dose is accurate, taking convenience, cheap, and be convenient to the drug composition oral preparation tripterygium total terpenoids drop pill of going out to carry.
Tripterygium total terpenoids drop pill involved in the present invention determines that through a large amount of experiment sievings based on the preparation technology of Chinese traditional patent formulation tripterygium total terpenoids sheet, process is adjusted part technology, and cooperates drop pill preparation technology to be prepared from.Be prepared by the following technical solutions, can obtain tripterygium total terpenoids drop pill involved in the present invention:
[preparation method]
1. be unit with g or kg, calculate, get 1 part of Radix Tripterygii Wilfordii extract according to weight, standby;
2. substrate---one or more the mixture in pharmaceutically suitable carrier such as Polyethylene Glycol (2000,4000,6000,8000,10000,20000), polyoxyethylene stearate 40 esters, betacyclodextrin, poloxamer, carboxymethyl starch sodium, sodium lauryl sulphate, stearic acid, sodium stearate, glycerin gelatine, Lac;
3. proportioning---with g or kg is unit, Radix Tripterygii Wilfordii extract (in Radix Tripterygii Wilfordii lactone alcohol): substrate=1: 1～1: 9;
4. according to the given ratio of prescription, accurately take by weighing medicine dry powder and substrate, be placed on heating while stirring in the heating container, standby until the fused solution that obtains containing medicine dry powder 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, to contain in the fused solution and/or emulsion and/or suspension of medicine dry powder 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;
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 Radix Tripterygii Wilfordii extract]
Get the Radix Tripterygii Wilfordii root and rhizome, be cut into the thick decoction pieces of 3～5mm, with 85% ethanol (5,4,4 times of amounts) reflux, extract, 3 times, each 4 hours, the extracting solution decompression recycling ethanol is to thick paste shape (relative density 1.25～1.30,60 ℃), dry below 60 ℃, dry extract is pulverized, and takes off ester, removal of solvent under reduced pressure with No. 90 petroleum ether, dry below 60 ℃, promptly.
Given here is according to the preparation method of a kind of Chinese medicine dry powder 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 tripterygium total terpenoids sheet that is prepared from according to the prescription that provides among the national drug standards WS-10715 (ZD-0715)-2002 and preparation method, it is a kind of expelling wind and removing dampness that has, Shujin Lip river alive, the reducing swelling and alleviating pain effect is used for the treatment of the cold-damp invasion and attack, the arthralgia that obstruction of collaterals by blood stasis causes, joint stuffiness, aversion to cold and cold limbs is met cold increasing the weight of, weakness of the waist and knees, or disease such as cold and heat are staggered; Rheumatoid arthritis sees above-mentioned symptom person's oral Chinese medicine preparation, through clinical verification, steady quality, determined curative effect is clinical and family is used for the treatment of the common drug preparation 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.
Tripterygium total terpenoids drop pill involved in the present invention is compared with the tripterygium total terpenoids sheet has following beneficial effect:
1. tripterygium total terpenoids drop pill involved in the present invention; utilize surfactant to be substrate; make solid dispersion with the dry powder that contains the Radix Tripterygii Wilfordii extract active component, make medicine be molecule, colloid or microcrystalline state and be scattered in the substrate, the total surface area of medicine increases; and substrate is hydrophilic; 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 tripterygium total terpenoids sheet, exist essential distinction.Utilize the drop pill of solid dispersion technology preparation, can adopt oral and sublingual administration, effective ingredient is fully contacted with mucomembranous surface, absorb, directly enter blood circulation by mucomembranous epithelial cell.Because active constituents of medicine directly enters blood circulation without gastrointestinal tract and liver, avoided first pass effect effectively, also avoided gastrointestinal irritation, thereby thereby it is rapid to make that tripterygium total terpenoids drop pill involved in the present invention has an onset, the bioavailability height, characteristics such as side effect is little, and medication is convenient.
2. tripterygium total terpenoids 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. tripterygium total terpenoids drop pill involved in the present invention mixes the dry powder 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 tripterygium total terpenoids 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).
The specific embodiment
Now with several groups of specific embodiments, be described further with regard to the preparation method of tripterygium total terpenoids 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, and it is standby to make the dry powder that contains the Radix Tripterygii Wilfordii extract active component earlier according to [appendix: a kind of preparation method of Radix Tripterygii Wilfordii extract] joint 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, Radix Tripterygii Wilfordii extract (in Radix Tripterygii Wilfordii lactone alcohol): substrate=1: 1～1: 9;
4. be prepared according to the process of [preparation method] 4～7 again, promptly can make the tripterygium total terpenoids drop pill of various different sizes.
[result of the test]
Test 1: for observe the dry powder that contains active constituents of medicine and different substrates when 1: 1 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, according to 1: 1 ratio, the dry powder that will contain active constituents of medicine 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 that dry powder and different substrates constituted experiments that contain active constituents of medicine, and obtain 15 groups of different experimental results and see Table 1.
Test 2: for observe the dry powder that contains active constituents of medicine and different substrates when 1: 3 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, according to 1: 3 ratio, the dry powder that will contain active constituents of medicine 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 that dry powder and different substrates constituted experiments that contain active constituents of medicine, and obtain 15 groups of different experimental results and see Table 2.
Test 3: for observe the dry powder that contains active constituents of medicine and different substrates when 1: 9 the proportioning prepared tripterygium total terpenoids drop pill in qualitative difference, according to 1: 9 ratio, the dry powder that will contain active constituents of medicine 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 that dry powder and different substrates constituted experiments that contain active constituents of medicine, 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 dry powder that contains the Radix Tripterygii Wilfordii extract active component earlier according to [appendix: a kind of preparation method of Chinese medicine dry powder] 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 Radix Tripterygii Wilfordii extract (in Radix Tripterygii Wilfordii lactone alcohol): mixed-matrix weight and=1: 1～1: 9;
4. be prepared according to [preparation method] again, promptly can make the tripterygium total terpenoids drop pill of various different sizes.
[result of the test]
Test 4: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared tripterygium total terpenoids 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, the dry powder that will contain active constituents of medicine according to 1: 1 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 4.
Test 5: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared tripterygium total terpenoids 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, the dry powder that will contain active constituents of medicine according to 1: 3 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 5.
Test 6: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared tripterygium total terpenoids 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, the dry powder that will contain active constituents of medicine according to 1: 9 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 6.
Test 7: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared tripterygium total terpenoids 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, the dry powder that will contain active constituents of medicine according to 1: 1 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 7.
Test 8: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared tripterygium total terpenoids 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, the dry powder that will contain active constituents of medicine according to 1: 3 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 8.
Test 9: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared tripterygium total terpenoids 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, the dry powder that will contain active constituents of medicine according to 1: 9 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 9.
Test 10: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 1 the proportioning prepared tripterygium total terpenoids 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, the dry powder that will contain active constituents of medicine according to 1: 1 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 10.
Test 11: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 3 the proportioning prepared tripterygium total terpenoids 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, the dry powder that will contain active constituents of medicine according to 1: 3 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 11.
Test 12: for observe the dry powder that contains active constituents of medicine and mixed-matrix when 1: 9 the proportioning prepared tripterygium total terpenoids 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, the dry powder that will contain active constituents of medicine according to 1: 9 ratio mixes mutually with 4 kinds of different mixed-matrixes and makes evenly again, adopt homemade drop pill machine, be prepared according to the step of stipulating in the preparation method, can obtain 4 pharmaceutical compositions that dry powder and mixed-matrix constituted experiments that contain active constituents of medicine, and obtain 4 groups of different experimental results and see Table 12.
The group practices of table 1 medicine dry powder and single-matrix
(medicine dry powder: 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 | ??67 | ??＜30 | ??＞10 | + |
| Polyethylene Glycol 4000 | ??50.0 | ??71 | ??＜30 | ??＞10 | ++ |
| Polyethylene Glycol 6000 | ??50.0 | ??81 | ??＜30 | ??＞10 | +++ |
| Polyethylene Glycol 8000 | ??50.0 | ??80 | ??＜30 | ??＞10 | +++ |
| Polyethylene Glycol 10000 | ??50.0 | ??85 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 20000 | ??50.0 | ??84 | ??＜30 | ??＜10 | +++ |
| Polyoxyethylene stearate 40 esters | ??50.0 | ??75 | ??＜30 | ??＞10 | ++ |
| Betacyclodextrin | ??50.0 | ??73 | ??＜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 | ??59 | ??＜30 | ??＞10 | ++ |
| Sodium stearate | ??50.0 | ??54 | ??＜30 | ??＞10 | +++ |
| Glycerin gelatine | ??50.0 | ??57 | ??＜30 | ??＞10 | +++ |
| Lac | ??50.0 | ??54 | ??＞30 | ??＞10 | +++ |
The group practices of table 2 medicine dry powder and single-matrix
(medicine dry powder: 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 | ??82 | ??＜30 | ??＞10 | ++ |
| Polyethylene Glycol 4000 | ??25.0 | ??82 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 6000 | ??25.0 | ??90 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 8000 | ??25.0 | ??91 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 10000 | ??25.0 | ??93 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 20000 | ??25.0 | ??92 | ??＜30 | ??＜10 | +++ |
| Polyoxyethylene stearate 40 esters | ??25.0 | ??85 | ??＜30 | ??＜10 | ++ |
| Betacyclodextrin | ??25.0 | ??82 | ??＜30 | ??＜10 | ++ |
| Poloxamer | ??25.0 | ??85 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium | ??25.0 | ??83 | ??＜30 | ??＞10 | ++ |
| Sodium lauryl sulphate | ??25.0 | ??77 | ??＜30 | ??＞10 | ++ |
| Stearic acid | ??25.0 | ??72 | ??＞30 | ??＞10 | ++ |
| Sodium stearate | ??25.0 | ??73 | ??＞30 | ??＞10 | +++ |
| Glycerin gelatine | ??25.0 | ??68 | ??＞30 | ??＞10 | +++ |
| Lac | ??25.0 | ??70 | ??＞30 | ??＞10 | +++ |
The group practices of table 3 medicine dry powder and different substrates
(medicine dry powder: substrate=1: 9)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyethylene Glycol 2000 | ??10.0 | ??84 | ??＜30 | ??＞10 | ++ |
| Polyethylene Glycol 4000 | ??10.0 | ??87 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 6000 | ??10.0 | ??92 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 8000 | ??10.0 | ??90 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 10000 | ??10.0 | ??92 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 20000 | ??10.0 | ??94 | ??＜30 | ??＜10 | +++ |
| Polyoxyethylene stearate 40 esters | ??10.0 | ??88 | ??＜30 | ??＜10 | ++ |
| Betacyclodextrin | ??10.0 | ??89 | ??＜30 | ??＜10 | ++ |
| Poloxamer | ??10.0 | ??92 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium | ??10.0 | ??82 | ??＜30 | ??＞10 | +++ |
| Sodium lauryl sulphate | ??10.0 | ??84 | ??＜30 | ??＞10 | +++ |
| Stearic acid | ??10.0 | ??81 | ??＞30 | ??＞10 | +++ |
| Sodium stearate | ??10.0 | ??82 | ??＞30 | ??＞10 | +++ |
| Glycerin gelatine | ??10.0 | ??76 | ??＞30 | ??＞10 | +++ |
| Lac | ??10.0 | ??76 | ??＞30 | ??＞10 | +++ |
The group practices of table 4 medicine dry powder and mixed-matrix
(medicine dry powder: 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 | ??81 | ??＜30 | ??＞10 | ++ |
| Poloxamer: Polyethylene Glycol=1: 1 | ??50 | ??82 | ??＜30 | ??＞10 | ++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ??50 | ??79 | ??＜30 | ??＜10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ??50 | ??71 | ??＜30 | ??＞10 | + |
The group practices of table 5 medicine dry powder and mixed-matrix
(medicine dry powder: mixed-matrix=1: 3)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 1 | ??25 | ??87 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | ??25 | ??88 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ??25 | ??86 | ??＜30 | ??＜10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ??25 | ??85 | ??＜30 | ??＞10 | ++ |
The group practices of table 6 medicine dry powder and mixed-matrix
(medicine dry powder: 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 | ??91 | ??＜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 | ??88 | ??＜30 | ??＜10 | +++ |
The group practices of table 7 medicine dry powder and mixed-matrix
(medicine dry powder: 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 | ??86 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | ??50 | ??85 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ??50 | ??84 | ??＜30 | ??＜10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ??50 | ??85 | ??＜30 | ??＞10 | ++ |
The group practices of table 8 medicine dry powder and mixed-matrix
(medicine dry powder: mixed-matrix=1: 3)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 5 | ??25 | ??92 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | ??25 | ??92 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ??25 | ??90 | ??＜30 | ??＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ??25 | ??87 | ??＜30 | ??＜10 | ++ |
The group practices of table 9 medicine dry powder and mixed-matrix
(medicine dry powder: 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 | 92 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | ??10 | 91 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ??10 | 90 | ??＜30 | ??＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ??10 | 91 | ??＜30 | ??＜10 | +++ |
The group practices of table 10 medicine dry powder and mixed-matrix
(medicine dry powder: mixed-matrix=1: 1)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 10 | ??50 | ??92 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | ??50 | ??89 | ??＜30 | ??＜10 | ++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | ??50 | ??88 | ??＜30 | ??＜10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | ??50 | ??87 | ??＜30 | ??＞10 | ++ |
The group practices of table 11 medicine dry powder and mixed-matrix
(medicine dry powder: 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 | ??92 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | ??25 | ??90 | ??＜30 | ??＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | ??25 | ??93 | ??＜30 | ??＜10 | +++ |
The group practices of table 12 medicine dry powder and mixed-matrix
(medicine dry powder: mixed-matrix=1: 9)
| The substrate title | Effective ingredient (%) | Rounding rate (%) | Dissolve scattered time limit (minute) | The ball method of double differences different (%) | Hardness |
| Polyoxyethylene stearate 40 esters: Polyethylene Glycol=1: 10 | ??10 | ??92 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | ??10 | ??93 | ??＜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 medicine dry powder 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 medicine dry powder 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 medicine dry powder 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 tripterygium total terpenoids drop pill that is used for the treatment of rheumatism is a raw material of Chinese medicine with the Radix Tripterygii Wilfordii extract, be prepared from a certain proportion of pharmaceutically suitable carrier, wherein:
1.1. medicine material---Radix Tripterygii Wilfordii extract;
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, in Radix Tripterygii Wilfordii lactone alcohol, and Radix Tripterygii Wilfordii extract: substrate=1: 1～1: 9;
2. tripterygium total terpenoids 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 tripterygium total terpenoids drop pill as claimed in claim 1 or 2 is characterized in that: the mixed proportion of described medicine dry powder and substrate is 1: 1～1: 5.
4. tripterygium total terpenoids drop pill as claimed in claim 1 is characterized in that described Radix Tripterygii Wilfordii extract obtains by the following method: get the Radix Tripterygii Wilfordii root and rhizome, be cut into the thick decoction pieces of 3～5mm, use 85% ethanol, be respectively 5,4,4 times of amounts, reflux, extract, 3 times, each 4 hours, 60 ℃ of decompression recycling ethanols of extracting solution are to the thick paste shape of relative density 1.25～1.30, and dry below 60 ℃, dry extract is pulverized, and take off ester with No. 90 petroleum ether, removal of solvent under reduced pressure, dry below 60 ℃, promptly.
5. the preparation method of a tripterygium total terpenoids drop pill is characterized in that being made of following process:
5.1. with g or kg is unit, in Radix Tripterygii Wilfordii lactone alcohol, it is standby to get 1 part of Radix Tripterygii Wilfordii extract;
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 medicine dry powder: substrate=1: 1～1: 9;
5.4., accurately take by weighing medicine dry powder 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 medicine dry powder 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 ℃;
Be in above the 2nd step during desired state of temperature 5.6. the temperature for the treatment of dropping-pill machine head and condensing agent is stable respectively, to contain in the fused solution and/or emulsion and/or suspension of medicine dry powder 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 Xinnao Shutong drop pill as described in the claim 5, it is characterized in that method 5.1 described medicine dry powder obtain by the following method: get the Radix Tripterygii Wilfordii root and rhizome, be cut into the thick decoction pieces of 3～5mm, use 85% ethanol, be respectively 5,4,4 times of amounts, reflux, extract, 3 times, each 4 hours, 60 ℃ of decompression recycling ethanols of extracting solution are to the thick paste shape of relative density 1.25～1.30, and dry below 60 ℃, dry extract is pulverized, and take off ester with No. 90 petroleum ether, removal of solvent under reduced pressure, dry below 60 ℃, promptly.
7. as the preparation method of tripterygium total terpenoids 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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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100971577A CN1322851C (en) | 2004-12-13 | 2004-12-13 | Tripterygium total terpenoids drop pill and its preparation method |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100971577A CN1322851C (en) | 2004-12-13 | 2004-12-13 | Tripterygium total terpenoids drop pill and its preparation method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1634507A true CN1634507A (en) | 2005-07-06 |
| CN1322851C CN1322851C (en) | 2007-06-27 |
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|---|---|---|---|
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105147766A (en) * | 2015-10-26 | 2015-12-16 | 苏州麦迪仙医药科技有限公司 | Pharmaceutical composition for treating rheumatoid arthritis and preparation method and application thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1471945A (en) * | 2002-07-30 | 2004-02-04 | 中国人民解放军海军医学研究所 | Tripterygium wilfordii dropping pills for treating autoimmune diseases |
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2004
- 2004-12-13 CN CNB2004100971577A patent/CN1322851C/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105147766A (en) * | 2015-10-26 | 2015-12-16 | 苏州麦迪仙医药科技有限公司 | Pharmaceutical composition for treating rheumatoid arthritis and preparation method and application thereof |
| CN105147766B (en) * | 2015-10-26 | 2019-08-06 | 苏州麦迪仙医药科技有限公司 | A kind of pharmaceutical composition and its preparation method and application for treating rheumatoid arthritis |
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| Publication number | Publication date |
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| CN1322851C (en) | 2007-06-27 |
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