CN1634057A - Dripping pills for reducing swelling and easing pain and its preparing method - Google Patents
Dripping pills for reducing swelling and easing pain and its preparing method Download PDFInfo
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Abstract
The invention discloses a medicinal composition which has the actions of dispersing pathogenic wind and dehumidifying, promoting blood circulation, relieving pain, treating knuckle ache, rheumatism and chronic infectious arthritis. The composition has the advantages of high biological availability, quick-speed medicine release, quick-speed effect, and less toxic and side effects. The drop pill is prepared by employing the process for preparing traditional Chinese medicinal injections.
Description
Technical field
The present invention relates to a kind of expelling wind and removing dampness that has, promoting blood circulation to remove obstruction in the collateral, clear swollen analgesic effect, be used for the treatment of arthralgia due to wind-cold-dampness disease, disease sees that muscular soreness, arthroncus, pain, joint stuffiness, numb stiff and rheumatism and rheumatoid arthritis have the pharmaceutical composition of above-mentioned patient, be particularly related to prescription, change a social system a kind of oral formulations that forms through dosage form based on Chinese traditional patent formulation ZHENGQINGFENGTONGNING injection.
Background technology
The ZHENGQINGFENGTONGNING injection that is prepared from according to the prescription that provides among the drug standard WS3-B-3171-98 and preparation technology, it is a kind of arthralgia due to wind-cold-dampness disease that is used for the treatment of, disease sees that muscular soreness, arthroncus, pain, joint stuffiness, numb stiff and rheumatism and rheumatoid arthritis have the Chinese medicine of above-mentioned patient, 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 prescription and the preparation technology who provides among the drug standard WS3-B-3171-98:
Prescription: sinomenine hydrochloride 25g, Calcium Disodium Versenate 0.3g, sodium sulfite 1g;
Method for making: get sinomenine hydrochloride 25g, Calcium Disodium Versenate 0.3g, sodium sulfite 1g, with an amount of water dissolution, the solution filter adds the injection water to 1000ml to clear and bright on filter, packing, sterilization, promptly.
Be explained as follows for this product in the appended ZHENGQINGFENGTONGNING injection description:
Nomenclature of drug: ZHENGQINGFENGTONGNING injection;
Main component: sinomenine hydrochloride;
Character: this product is colourless or yellowish clear liquid;
Function cures mainly: expelling wind and removing dampness, promoting blood circulation to remove obstruction in the collateral, swollen clearly pain relieving.Be used for arthralgia due to wind-cold-dampness disease, disease sees that muscular soreness, arthroncus, pain, joint stuffiness, numb stiff and rheumatism and rheumatoid arthritis have above-mentioned patient;
Usage and dosage: intramuscular injection, a 1-2ml 2 times on the one, obtains and follows the doctor's advice;
Points for attention:
(1) medication under physician guidance;
(2) the careful usefulness of drug allergy history person, allergic asthma or hypotensive is previously arranged;
(3) the careful usefulness of anemia of pregnant woman or women breast-feeding their children;
(4) all usages, each consumption is no more than 4ml.
Writing out a prescription with this is that the oral formulations that make on the basis has tablet, its characteristics, the effect identical.
Owing to 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 Flos Carthami 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, be to replenish the existing arthralgia due to wind-cold-dampness disease that is used for the treatment of, disease sees that muscular soreness, arthroncus, pain, joint stuffiness, numb stiff and rheumatism and rheumatoid arthritis have the deficiency of the oral drug preparation of above-mentioned patient, provide a kind of bioavailability height, release fast, produce effects fast, toxic and side effects is little, manufacturing and medical treatment cost are low, low price, the dropping pill formulation that is suitable for family to use.
Dropping pill formulation involved in the present invention is determined through a large amount of experiment sievings, based on Chinese traditional patent formulation ZHENGQINGFENGTONGNING injection preparation technology, cooperates drop pill preparation technology to be prepared from.Be prepared by the following technical solutions, can obtain ZHENGQINGFENGTONGNING drop pill involved in the present invention;
[preparation method 1
1. medicine material---sinomenine hydrochloride;
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 sinomenine hydrochloride: 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, fused solution and/or the emulsion and/or the suspension that will contain medicine dry powder 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.
Beneficial effect
The ZHENGQINGFENGTONGNING injection that is prepared from according to the prescription that provides among the drug standard WS3-B-3171-98 and preparation technology, it is a kind of arthralgia due to wind-cold-dampness disease that is used for the treatment of, disease sees that muscular soreness, arthroncus, pain, joint stuffiness, numb stiff and rheumatism and rheumatoid arthritis have the Chinese medicine of above-mentioned patient, 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.This product oral formulations has tablet at present.
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.
ZHENGQINGFENGTONGNING drop pill involved in the present invention is compared with ZHENGQINGFENGTONGNING injection and tablet, and following beneficial effect is arranged:
1. ZHENGQINGFENGTONGNING drop pill involved in the present invention; utilize surfactant to be substrate; make solid dispersion with the dry powder that contains sinomenine hydrochloride; 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. ZHENGQINGFENGTONGNING 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. ZHENGQINGFENGTONGNING 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 ZHENGQINGFENGTONGNING 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 ZHENGQINGFENGTONGNING drop pill of the present invention.
First group: the test of single-matrix
1. medicine material: sinomenine hydrochloride;
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 sinomenine hydrochloride: substrate=1: 1～1: 9;
4. be prepared according to the process of [preparation method] 4～7 again, promptly can make the ZHENGQINGFENGTONGNING drop pill of various different sizes.
[result of the test]
Test 1: for observe medicine dry powder and different substrates when 1: 1 the proportioning prepared ZHENGQINGFENGTONGNING drop pill in qualitative difference, according to 1: 1 ratio, with medicine dry powder 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 medicine dry powder and different substrates, and obtain 15 groups of different experimental results and see Table 1.
Test 2: for observe medicine dry powder and different substrates when 1: 3 the proportioning prepared ZHENGQINGFENGTONGNING drop pill in qualitative difference, according to 1: 3 ratio, with medicine dry powder 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 pharmaceutical composition experiment that 15 medicines dry powder and different substrates are constituted, and obtain 15 groups of different experimental results and see Table 2.
Test 3: for observe medicine dry powder and different substrates when 1: 9 the proportioning prepared ZHENGQINGFENGTONGNING drop pill in qualitative difference, according to 1: 9 ratio, with medicine dry powder 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 pharmaceutical composition experiment that 15 medicines dry powder and different substrates are constituted, and obtain 15 groups of different experimental results and see Table 3.
Second group; The test of mixed-matrix
1. medicine material---sinomenine hydrochloride;
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 sinomenine hydrochloride: mixed-matrix weight and=1: 1～1: 9;
4. be prepared according to [preparation method] again, promptly can make the ZHENGQINGFENGTONGNING drop pill of various different sizes.
[result of the test]
Test 4: for observe sinomenine hydrochloride and mixed-matrix when 1: 1 the proportioning prepared ZHENGQINGFENGTONGNING 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 medicine dry powder 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 sinomenine hydrochloride and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 4.
Test 5: for observe sinomenine hydrochloride and mixed-matrix when 1: 3 the proportioning prepared ZHENGQINGFENGTONGNING 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 medicine dry powder 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 sinomenine hydrochloride and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 5.
Test 6: for observe sinomenine hydrochloride and mixed-matrix when 1: 9 the proportioning prepared ZHENGQINGFENGTONGNING 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 medicine dry powder 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 sinomenine hydrochloride and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 6.
Test 7: for observe sinomenine hydrochloride and mixed-matrix when 1: 1 the proportioning prepared ZHENGQINGFENGTONGNING 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 medicine dry powder 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 sinomenine hydrochloride and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 7.
Test 8: for observe sinomenine hydrochloride and mixed-matrix when 1: 3 the proportioning prepared ZHENGQINGFENGTONGNING 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 medicine dry powder 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 sinomenine hydrochloride and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 8.
Test 9: for observe sinomenine hydrochloride and mixed-matrix when 1: 9 the proportioning prepared ZHENGQINGFENGTONGNING 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 medicine dry powder 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 sinomenine hydrochloride and mixed-matrix constituted, and obtain 4 groups of different experimental results and see Table 9.
Test 10: for observe sinomenine hydrochloride and mixed-matrix when 1: 1 the proportioning prepared ZHENGQINGFENGTONGNING 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 medicine dry powder 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 sinomenine hydrochloride and mixed-matrix constituted, and obtain 4 groups of different experiments and the results are shown in Table 10.
Test 11: for observe sinomenine hydrochloride and mixed-matrix when 1: 3 the proportioning prepared ZHENGQINGFENGTONGNING 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 medicine dry powder 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 sinomenine hydrochloride and mixed-matrix constituted, and obtain 4 groups of different experiments and the results are shown in Table 11.
Test 12: for observe sinomenine hydrochloride and mixed-matrix when 1: 9 the proportioning prepared ZHENGQINGFENGTONGNING 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 medicine dry powder 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 sinomenine hydrochloride and mixed-matrix constituted, and obtain 4 groups of different experiments and the results are shown in 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 | ??68 | ??＜30 | ??＞10 | + |
| Polyethylene Glycol 4000 | ??50.0 | ??72 | ??＜30 | ??＞10 | ++ |
| Polyethylene Glycol 6000 | ??50.0 | ??80 | ??＜30 | ??＞10 | +++ |
| Polyethylene Glycol 8000 | ??50.0 | ??83 | ??＜30 | ??＞10 | +++ |
| Polyethylene Glycol 10000 | ??50.0 | ??84 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 20000 | ??50.0 | ??86 | ??＜30 | ??＜10 | +++ |
| Polyoxyethylene stearate 40 esters | ??50.0 | ??75 | ??＜30 | ??＞10 | ++ |
| Betacyclodextrin | ??50.0 | ??73 | ??＜30 | ??＞10 | ++ |
| Poloxamer | ??50.0 | ??71 | ??＜30 | ??＞10 | ++ |
| Carboxymethyl starch sodium | ??50.0 | ??74 | ??＜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 | ??55 | ??＜30 | ??＞10 | +++ |
| Lac | ??50.0 | ??56 | ??＞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 | ??81 | ??＜30 | ??＞10 | ++ |
| Polyethylene Glycol 4000 | ??25.0 | ??82 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 6000 | ??25.0 | ??91 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 8000 | ??25.0 | ??90 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 10000 | ??25.0 | ??91 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 20000 | ??25.0 | ??92 | ??＜30 | ??＜10 | +++ |
| Polyoxyethylene stearate 40 esters | ??25.0 | ??87 | ??＜30 | ??＜10 | ++ |
| Betacyclodextrin | ??25.0 | ??84 | ??＜30 | ??＜10 | ++ |
| Poloxamer | ??25.0 | ??85 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium | ??25.0 | ??82 | ??＜30 | ??＞10 | ++ |
| Sodium lauryl sulphate | ??25.0 | ??76 | ??＜30 | ??＞10 | ++ |
| Stearic acid | ??25.0 | ??72 | ??＞30 | ??＞10 | ++ |
| Sodium stearate | ??25.0 | ??74 | ??＞30 | ??＞10 | +++ |
| Glycerin gelatine | ??25.0 | ??68 | ??＞30 | ??＞10 | +++ |
| Lac | ??25.0 | ??70 | ??＞30 | ??＞10 | +++ |
The group practices of table 3 medicine dry powder and single-matrix
(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 | ??86 | ??＜30 | ??＞10 | ++ |
| Polyethylene Glycol 4000 | ??10.0 | ??84 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 6000 | ??10.0 | ??90- | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 8000 | ??10.0 | ??91 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 10000 | ??10.0 | ??93 | ??＜30 | ??＜10 | +++ |
| Polyethylene Glycol 20000 | ??10.0 | ??92 | ??＜30 | ??＜10 | +++ |
| Polyoxyethylene stearate 40 esters | ??10.0 | ??90 | ??＜30 | ??＜10 | ++ |
| Betacyclodextrin | ??10.0 | ??87 | ??＜30 | ??＜10 | ++ |
| Poloxamer | ??10.0 | ??92 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium | ??10.0 | ??82 | ??＜30 | ??＞10 | +++ |
| Sodium lauryl sulphate | ??10.0 | ??81 | ??＜30 | ??＞10 | +++ |
| Stearic acid | ??10.0 | ??79 | ??＞30 | ??＞10 | +++ |
| Sodium stearate | ??10.0 | ??80 | ??＞30 | ??＞10 | +++ |
| Glycerin gelatine | ??10.0 | ??76 | ??＞30 | ??＞10 | +++ |
| Lac | ??10.0 | ??78 | ??＞30 | ??＞10 | +++ |
The group practices of table 4 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 | ??83 | ??＜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 | ??75 | ??＜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 | ??85 | ??＜30 | ??＞10 | ++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | 25 | ??84 | ??＜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 | 88 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 1 | ??10 | 85 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 1 | ??10 | 84 | ??＜30 | ??＞10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 1 | ??10 | 86 | ??＜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 | 91 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | ??50 | 92 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ??50 | 87 | ??＜30 | ??＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ??50 | 86 | ??＜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 | 91 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | ??25 | 91 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ??25 | 90 | ??＜30 | ??＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ??25 | 88 | ??＜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 | ??91 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 5 | ??10 | ??93 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 5 | ??10 | ??91 | ??＜30 | ??＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 5 | ??10 | ??92 | ??＜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 | ??91 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | ??50 | ??88 | ??＜30 | ??＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | ??50 | ??86 | ??＜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 | ??91 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | ??25 | ??92 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | ??25 | ??89 | ??＜30 | ??＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | ??25 | ??87 | ??＜30 | ??＜10 | +++ |
The group practices of table 12 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 | 91 | ??＜30 | ??＜10 | +++ |
| Poloxamer: Polyethylene Glycol=1: 10 | 10 | 92 | ??＜30 | ??＜10 | +++ |
| Carboxymethyl starch sodium: Polyethylene Glycol=1: 10 | 10 | 91 | ??＜30 | ??＜10 | +++ |
| Betacyclodextrin: Polyethylene Glycol=1: 10 | 10 | 91 | ??＜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 (5)
1. one kind is used for the treatment of arthralgia due to wind-cold-dampness disease, disease sees that muscular soreness, arthroncus, pain, joint stuffiness, numb stiff and rheumatism and rheumatoid arthritis have the drug composition oral dropping pill formulation of above-mentioned patient, with the sinomenine hydrochloride is raw material, be prepared from a certain proportion of pharmaceutically suitable carrier, wherein:
1.1. medicine material---sinomenine hydrochloride;
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 sinomenine hydrochloride: substrate=1: 1～1: 9.
2. dropping pill formulation 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 dropping pill formulation 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. the preparation method of a dropping pill formulation is characterized in that being made of following process:
4.1. medicine material---sinomenine hydrochloride;
4.2. 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;
4.3. proportioning---with g or kg is unit, by weight, and medicine dry powder: substrate=1: 1～1: 9;
4.4., 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;
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, fused solution and/or the emulsion and/or the suspension that will contain 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.
5. as the preparation method of dropping pill formulation 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.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100971628A CN1332669C (en) | 2004-12-13 | 2004-12-13 | Dripping pills for reducing swelling and easing pain and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB2004100971628A CN1332669C (en) | 2004-12-13 | 2004-12-13 | Dripping pills for reducing swelling and easing pain and its preparing method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1634057A true CN1634057A (en) | 2005-07-06 |
| CN1332669C CN1332669C (en) | 2007-08-22 |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106176866A (en) * | 2016-08-31 | 2016-12-07 | 孟凡珍 | Local injection treats the medicine of chronic neck, shoulder, waist and leg arthralgia |
| CN106333950A (en) * | 2015-07-10 | 2017-01-18 | 中国中医科学院医学实验中心 | Medicine for treating mirror image pain due to cancerous invasion |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1186668A (en) * | 1996-12-31 | 1998-07-08 | 四川太极制药有限公司 | Sinomenine hydrocloride preparation and its preparing process |
| CN1076604C (en) * | 1998-12-24 | 2001-12-26 | 湖南正清制药集团股份有限公司 | Slow releasing agent of tuduvanine and its preparing method |
-
2004
- 2004-12-13 CN CNB2004100971628A patent/CN1332669C/en not_active Expired - Fee Related
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106333950A (en) * | 2015-07-10 | 2017-01-18 | 中国中医科学院医学实验中心 | Medicine for treating mirror image pain due to cancerous invasion |
| CN106333950B (en) * | 2015-07-10 | 2019-04-02 | 中国中医科学院医学实验中心 | A kind of drug for treating mirror-image pain caused by cancerous invasion |
| CN106176866A (en) * | 2016-08-31 | 2016-12-07 | 孟凡珍 | Local injection treats the medicine of chronic neck, shoulder, waist and leg arthralgia |
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| Publication number | Publication date |
|---|---|
| CN1332669C (en) | 2007-08-22 |
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