CN101015541A - Diacetyl rhein dropping pills and its preparing process - Google Patents
Diacetyl rhein dropping pills and its preparing process Download PDFInfo
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- CN101015541A CN101015541A CN 200710037689 CN200710037689A CN101015541A CN 101015541 A CN101015541 A CN 101015541A CN 200710037689 CN200710037689 CN 200710037689 CN 200710037689 A CN200710037689 A CN 200710037689A CN 101015541 A CN101015541 A CN 101015541A
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- diacetyl rhein
- diacetyl
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Abstract
This invention relates to a dripping pill of diacetyl rhein. the pill is characterised in that it is prepared from diacetyl rhein and dripping pill substrate at a weight ratio of 1:1-5. the preparation method comprises pulverizing diacetyl rhein, adding substrate, heating, stirring to fusion, moving to a dripping pill engine with the temperature of materials and dripper at 75-85deg.C, stirring, dripping into coolant at 0-6deg.C and speed of 40+-10 pill/min, separating the dripping pill and coolant through a separating unit, and dripping to obtain the final product. The invention has the advantages of few air contact, uneasy oxidation, no hydrolysis, increase medicine stability, and improved shelf life.
Description
Technical field
The present invention relates to a kind of diacetyl rhein dropping pills and preparation method thereof, be used for the treatment of symptoms such as pain that degenerative osteoarthritis and relevant disease cause and joint function disturbance, belong to the spy technical field of pharmaceuticals.
Background technology
Diacetyl rhein, chemical name 4,5-diacetyl-9,10-dihydro-9,10 dioxies-2-anthracene carboxylic acid also claims diacerein (Diacerein), is osteoarthritis IL-1 inhibitor, can induce cartilage to generate, and has pain relieving, antiinflammatory and antipyretic effect.Be used for the treatment of symptoms such as pain that degenerative osteoarthritis and relevant disease cause and joint function disturbance clinically.
The diacetyl rhein preparation that uses clinically is mainly capsule at present.Diacetyl rhein itself is insoluble in water and alcohol, Chinese patent " be used for pharmaceutical composition for oral administration (the ZL patent No. 9719084.9) " and disclose with diacetyl rhein with pour into capsular technology after vegetable oil, animal oil or mineral oil and surfactant mix.But owing to used the vegetable oil and the animal wet goods liquid carrier oil of large percentage in the preparation, vegetable oil and animal oil itself have easy oxidation, easily corrupt and rotten, and the quality stability of medicine is affected adversely, and effect duration and shelf-life shorten.
Summary of the invention
It is molten diffusing fast to the purpose of this invention is to provide a kind of disintegrate, dissolution and bioavailability height, and release is quick, steady quality, effect duration and long shelf-life carry taking convenience, and production process is short, diacetyl rhein dropping pills that cost is low and preparation method thereof.
For realizing above purpose, technical scheme of the present invention provides a kind of diacetyl rhein dropping pills, it is characterized in that, formulated by diacetyl rhein and drop pill substrate, the weight proportion of each composition is:
Diacetyl rhein: drop pill substrate=1: 1-1: 5.
A kind of preparation method of diacetyl rhein dropping pills is characterized in that, behind diacetyl rhein and the drop pill substrate heating and melting, splashes in the immiscible liquid coolant and forms drop pill, and its technology is:
The first step. get diacetyl rhein, pulverize, be screened to 60-200 order/time;
Second step. 1 part of the diacetyl rhein of the pulverizing of learning from else's experience adds 1: the drop pill substrate of 1-5, heat while stirring to fusion, heating-up temperature is 75 ℃-85 ℃;
The 3rd step. the fused mass of step 2 is moved to the drop pill machine, spice insulation and water dropper temperature maintenance are at 75 ℃-85 ℃, splash into while stirring in the drop pill coolant, chilling temperature is 0 ℃-6 ℃, dripping speed is 40 ± 10/minute, segregation apparatus by the drop pill machine separates drop pill with coolant, the drying device by the drop pill machine promptly gets diacetyl rhein dropping pills with the drop pill drying.
Described drop pill substrate is a kind of or several compatibilities in polyethylene glycols, carboxymethyl starch sodium, poloxamer, sodium carboxymethyl cellulose, stearic acid, sodium stearate, the polyoxyethylene monostearate, and the content of each compatibility composition all is not equal to zero; Described polyethylene glycols is polyethylene glycol 6000 or Macrogol 4000; Described drop pill coolant is dimethicone or liquid paraffin.
Advantage of the present invention is:
1. solid dispersion technology is used for the present invention,, solidifies, make medicine be molecule, colloid or crystallite shape and be scattered in the substrate by system of dripping and quenching with being insoluble in fusion behind the diacetyl rhein of water and the substrate mixing.Prepared drop pill disintegrate is molten loose fast, the dissolution height, the bioavailability height, rapid-action, both can swallow, but also sublingual administration.
2. behind diacetyl rhein and the substrate heating and melting, splash in the immiscible liquid coolant and form drop pill, medicine contacts few with air, be difficult for oxidation.Substrate is non-water thing, is difficult for causing drug hydrolysis, and medicine stability is increased, and effect duration and shelf-life are longer.
3. technology of the present invention is simple, with short production cycle, and cost is low, the efficient height.
The specific embodiment
The invention will be further described below in conjunction with embodiment.
Embodiment 1-9
The present invention is by the preparation of diacetyl rhein and different substrates, investigates indexs such as roundness, the ball method of double differences are different, hardness, molten diffusing time, to determine the weight ratio of diacetyl rhein and single or mixed-matrix.
Table 1 diacetyl rhein and different substrates proportioning test (diacetyl rhein is 1 part)
Its technology is:
The first step. get diacetyl rhein, pulverize, be screened to 60-200 order/time;
Second step. 1 part of the diacetyl rhein of the pulverizing of learning from else's experience, the drop pill substrate in the adding in the table heats while stirring to fusion, and heating-up temperature is 80 ℃;
The 3rd step. the fused mass of step 2 is moved to the drop pill machine, spice insulation and water dropper temperature maintenance are at 80 ℃, splash into while stirring in the drop pill coolant, chilling temperature is 4 ℃, dripping speed is 40 ± 10/minute, segregation apparatus by the drop pill machine separates drop pill with coolant, the drying device by the drop pill machine promptly gets diacetyl rhein dropping pills with the drop pill drying.
As seen from Table 1, it is all better to test every investigation index 2,6,7,8, No. 9, and promptly diacetyl rhein and substrate ratio are 1: 1-1: can drip system smoothly at 5 o'clock.But consider factors such as taking dose, optimum ratio is 2,7, No. 8 tests, and promptly diacetyl rhein and substrate ratio are 1: 1-1: 2.
Diacetyl rhein capsule (content is an oily) compares with drop pill stability
| Preparation | Capsule (content is an oily) | Drop pill | ||||
| Investigate index | Abnormal smells from the patient | Color | Acid number | Hardness | Color | The molten diffusing time |
| The result | Foreign odor, tapinoma-odour are arranged | Deepen | ＞0.56 | +++ | Do not become | ＜9 minutes |
Annotate: 40 ± 2 ℃ of test temperatures; Relative humidity 75% ± 5%; Time is 6 months.
The result shows: diacetyl rhein capsule (content is an oily) is under the accelerated stability test condition, foreign odor and tapinoma-odour were promptly arranged in six months, darken, acid number exceeds standard, and diacetyl rhein dropping pills is in same experimental condition and test period, and every investigation index does not change.It is buttery capsule that the stability that shows drop pill is better than content.
Claims (5)
1. a diacetyl rhein dropping pills is characterized in that, formulated by diacetyl rhein and drop pill substrate, the weight proportion of each composition is:
Diacetyl rhein: drop pill substrate=1: 1-1: 5.
2. the preparation method of diacetyl rhein dropping pills according to claim 1 is characterized in that, behind diacetyl rhein and the drop pill substrate heating and melting, splashes in the immiscible liquid coolant and forms drop pill, and its technology is:
The first step. get diacetyl rhein, pulverize, be screened to 60-200 order/time;
Second step. 1 part of the diacetyl rhein of the pulverizing of learning from else's experience adds 1: the drop pill substrate of 1-5, heat while stirring to fusion, heating-up temperature is 75 ℃-85 ℃;
The 3rd step. the fused mass of step 2 is moved to the drop pill machine, spice insulation and water dropper temperature maintenance are at 75 ℃-85 ℃, splash into while stirring in the drop pill coolant, chilling temperature is 0 ℃-6 ℃, dripping speed is 40 ± 10/minute, segregation apparatus by the drop pill machine separates drop pill with coolant, the drying device by the drop pill machine promptly gets diacetyl rhein dropping pills with the drop pill drying.
3. diacetyl rhein dropping pills according to claim 1, it is characterized in that, described drop pill substrate is a kind of or several compatibilities in polyethylene glycols, carboxymethyl starch sodium, poloxamer, sodium carboxymethyl cellulose, stearic acid, sodium stearate, the polyoxyethylene monostearate, and the content of each compatibility composition all is not equal to zero.
4. diacetyl rhein dropping pills according to claim 3 is characterized in that, described polyethylene glycols is polyethylene glycol 6000 or Macrogol 4000.
5. diacetyl rhein dropping pills according to claim 2 is characterized in that, described drop pill coolant is dimethicone or liquid paraffin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200710037689 CN101015541A (en) | 2007-02-25 | 2007-02-25 | Diacetyl rhein dropping pills and its preparing process |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200710037689 CN101015541A (en) | 2007-02-25 | 2007-02-25 | Diacetyl rhein dropping pills and its preparing process |
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| CN101015541A true CN101015541A (en) | 2007-08-15 |
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| CN 200710037689 Pending CN101015541A (en) | 2007-02-25 | 2007-02-25 | Diacetyl rhein dropping pills and its preparing process |
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Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2920991A1 (en) * | 2007-09-14 | 2009-03-20 | Wockhardt Ltd | Composition, useful to treat inflammation, preferably osteoarthritis, comprises diacerhein, polyols comprising mannitol, sorbitol, maltitol, maltol, lactitol or xylitol, and optionally excipients comprising e.g. fillers and lubricants |
| WO2009040702A2 (en) * | 2007-09-27 | 2009-04-02 | Wockhardt Research Centre | Pharmaceutical compositions of rhein or diacerein |
| CN102743370A (en) * | 2011-06-27 | 2012-10-24 | 王子厚 | Novel use of diacerein |
| CN104188951A (en) * | 2014-09-18 | 2014-12-10 | 上海慈瑞医药科技有限公司 | Diacerein composition and preparing method thereof |
| CN104274322A (en) * | 2013-07-11 | 2015-01-14 | 天士力制药集团股份有限公司 | Method for preparing drop pill by high-speed vibration in dropping way |
| CN108245557A (en) * | 2018-02-12 | 2018-07-06 | 浙江中医药大学 | A kind of preparation method of rhubarb total anthraquinone rapid-released droppills |
-
2007
- 2007-02-25 CN CN 200710037689 patent/CN101015541A/en active Pending
Cited By (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2920991A1 (en) * | 2007-09-14 | 2009-03-20 | Wockhardt Ltd | Composition, useful to treat inflammation, preferably osteoarthritis, comprises diacerhein, polyols comprising mannitol, sorbitol, maltitol, maltol, lactitol or xylitol, and optionally excipients comprising e.g. fillers and lubricants |
| WO2009040702A2 (en) * | 2007-09-27 | 2009-04-02 | Wockhardt Research Centre | Pharmaceutical compositions of rhein or diacerein |
| WO2009040702A3 (en) * | 2007-09-27 | 2009-08-06 | Wockhardt Research Center | Pharmaceutical compositions of rhein or diacerein |
| AU2008303277B2 (en) * | 2007-09-27 | 2013-04-04 | Wockhardt Limited | Pharmaceutical compositions of rhein or diacerein |
| RU2484816C2 (en) * | 2007-09-27 | 2013-06-20 | Вокхардт Рисерч Сентер | Pharmaceutical compositions of rhein or diacerein |
| CN102743370A (en) * | 2011-06-27 | 2012-10-24 | 王子厚 | Novel use of diacerein |
| CN102743370B (en) * | 2011-06-27 | 2013-05-15 | 王子厚 | Novel use of diacerein |
| CN104274322A (en) * | 2013-07-11 | 2015-01-14 | 天士力制药集团股份有限公司 | Method for preparing drop pill by high-speed vibration in dropping way |
| CN104188951A (en) * | 2014-09-18 | 2014-12-10 | 上海慈瑞医药科技有限公司 | Diacerein composition and preparing method thereof |
| CN104188951B (en) * | 2014-09-18 | 2016-09-28 | 上海慈瑞医药科技有限公司 | A kind of diacetyl rhein compositions and preparation method thereof |
| CN108245557A (en) * | 2018-02-12 | 2018-07-06 | 浙江中医药大学 | A kind of preparation method of rhubarb total anthraquinone rapid-released droppills |
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