CN101317839A - Preparation method for compound artemether dripping pill for treating malaria - Google Patents
Preparation method for compound artemether dripping pill for treating malaria Download PDFInfo
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- CN101317839A CN101317839A CNA2007100575371A CN200710057537A CN101317839A CN 101317839 A CN101317839 A CN 101317839A CN A2007100575371 A CNA2007100575371 A CN A2007100575371A CN 200710057537 A CN200710057537 A CN 200710057537A CN 101317839 A CN101317839 A CN 101317839A
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- artemether
- compound
- principal agent
- polyethylene glycol
- dripping pill
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The invention relates to the preparation of a chemical medicine preparation, which is a compound artemether methyl ether droping pill used for curing malaria. The present invention has the advantages that: 1. Serving as main ingredients, antimalarial lumefantrine and artemether are sufficiently dispersed by water-soluble auxiliary-ingredient polyethylene glycol or poloxamer, thus being favorable for absorbing the main ingredients. 2. The dropping pill preparation can be taken under tongue and also can be swallowed with very short disintegration (dissolve) time limit. And the invitro dissolve quantities are greatly improved and the peak value of the blood concentration can be reached rapidly, thus being beneficial to the improvement of the curative effect; 3. The main ingredients and the auxiliary ingredients are equably mixed at the temperature of 80 to 90 DEG C and insulated for some time, and then are dropped into methylsilicone oil or liquid paraffin at the temperature ranging from 5 to10 DEG C; 4. The method is simple in production process and short in production cycle. The cost can be decreased; 5. As the medicine is left in stomach for a short time or maybe the first-pass effect of the stomach can be avoided, so the generation of drug resistance and other side effects decreases.
Description
Technical field:
The invention belongs to a kind of chemical medicine preparation, particularly a kind of chemical medicine preparation for the treatment of malaria.
Background technology:
Malaria is a kind of very ancient disease, and rapid onset is propagated soon, is difficult to control for the moment.Past is all over the world, especially the torrid zone, the subtropical zone sickness rate is very high, eliminated malaria disease basically in a lot of countries now, but in South Asia, the Middle East, Africa and country in Southeast Asia be still serious epidemic infectious diseases, all will cause hundreds thousand of every year, even people up to a million dies from malaria.These countries and regions are treated malaria timely and effectively, effectively control spreading of malaria, are still the task of top priority, are the duty-bound tasks of government of these countries and regions, and the United Nations and World Health Organization (WHO) also very pay close attention to the treatment of these regional malaria.The President Hu Jintao promises to undertake in the non-high-rise forum meeting that in 2006 Chinese Government will provide the assistance of African country's anti-malaria medicaments, supports the malaria work of the high morbidity of African malaria countries and regions with practical action.
The determined curative effect of antimalarial benflumetol and Artemether, side effect is little, and drug resistance is little, is a line medicine of antimalarial.Played outstanding effect in the malaria work preventing and treating of malaria countries and regions occurred frequently.But be main dosage form with injection still in the past, using is not its major defect.Oral formulations has only tablet, and its major defect is that disintegration is long, because its non-water-soluble character is difficult for absorbing, onset is slow, is difficult to reach rapidly the peak value of blood drug level, has influenced oral administration biaavailability greatly, thereby has also influenced the performance of curative effect.The antimalarial of artemisine is competed very fierce in the international market, and competition focal point is transformed into finished medicines from crude drug at present, and the characteristics that drop pill had are occupied very strong advantage in the competition of finished medicines.
Shorten molten loosing (disintegrate) time limit, quicken the absorption of medicine, to improve oral administration biaavailability, its speed that reaches the blood drug level peak value is reached or, make it rapid-action, absorb fast near the speed of intravenously administrable, good effect, compound preparation is stronger than single preparations of ephedrine anti-drug resistance, and cost is low, the clinical value height.The present invention just is being based on this technical background, develops compound artemether dripping pill.
Summary of the invention:
The object of the present invention is to provide a kind of chemical medicine drop pill for the treatment of malaria, it is short that this drop pill has molten (disintegrate) time limit of loosing, the stripping quantity height, the characteristics that oral administration biaavailability is high, rapid-action in clinical practice, be easy to absorb, improve curative effect, have tangible advantage than other oral formulations tablet, and have actual application value.
Technical scheme of the present invention is: a kind of chemical medicine drop pill for the treatment of malaria, it is to be principal agent with antimalarial benflumetol and Artemether, adopt different adjuvants to do dispersant, these adjuvants comprise one or more mixture in different molecular weight polyethylene glycol and the poloxamer.Its principal agent is 1: 2 to 1: 5 with the ratio of adjuvant.The drop pill of making, very easily molten loosing (disintegrate), its time limit, normal release formulation tablet foreshortened to 1/10th, and its external stripping quantity also improves greatly, can reach more than 70% in 45 minutes, has therefore improved oral administration biaavailability greatly.
This drop pill has adopted adjuvant as dispersant, and original non-water-soluble benflumetol and Artemether are fully disperseed by water miscible adjuvant, is beneficial to the absorption of principal agent benflumetol and Artemether, gives full play to the drug action of principal agent.
This drop pill both can be swallowed, but also sublingual administration.Swallow and shorten molten loosing (disintegrate) time limit, be beneficial to the absorption of medicine; Sublingual administration can be rapidly in the Sublingual molten loosing, absorbed by hypoglossis mucous membrane, directly enter sublingual vein, avoided the first pass effect of stomach, can reach the blood drug level peak value rapidly, near or reach the speed of intravenously administrable, but overcome the shortcoming of intravenously administrable inconvenience.Since principal agent absorbs without stomach or under one's belt disintegrate absorb very fast, under one's belt the time of being detained short, thereby reduced the generation of side effect such as drug resistance.
The preparation of this drop pill is earlier low-molecular-weight adjuvant fully to be disperseed principal agent, adds high-molecular weight adjuvant fusion, mixing then, is incubated after 10-30 minute, adopts the drop pill machine of different bores to splash in the coolant under keeping warm mode.Holding temperature is looked the molecular weight size of adjuvant and different, usually between 80-95 ℃.Coolant comprises methyl-silicone oil or liquid paraffin, and the temperature of coolant is between 0-10 ℃.Dripping the drop pill of making is every 5-15mg, calculates the content of principal agent, determines oral consumption.
Embodiment 1.
120 parts of principal agent benflumetol
20 parts of principal agent Artemether
50 parts of Macrogol 4000s
200 parts of polyethylene glycol 6000s
Operation: with Macrogol 4000 fusion in 60-65 ℃ of water-bath of recipe quantity, add the benflumetol of recipe quantity, stir, the polyethylene glycol 6000 that adds recipe quantity, bath temperature is increased to 85-90 ℃, stirs, and is incubated 20 minutes, drop pill machine with the 0.4-0.6mm bore, splash in 5-10 ℃ the methyl-silicone oil coolant, the elimination methyl-silicone oil gets rid of clean, airing, promptly.The heavy 5-15mg of every ball.Obey once every day, once obeys 2.5g.
Embodiment 2.
120 parts of principal agent benflumetol
20 parts of principal agent Artemether
50 parts of PEG400s
250 parts of polyethylene glycol 6000s
Operation: with the PEG400 of recipe quantity and the abundant mix homogeneously of benflumetol of recipe quantity, place in the 85-90 ℃ of water-bath, the polyethylene glycol 6000 that adds recipe quantity, stir, be incubated 15 minutes, go in 5-10 ℃ the liquid paraffin coolant elimination liquid paraffin with the dropping-pill machine of 0.4-0.6mm bore, get rid of clean, airing, promptly, every ball weight 5-15mg.Inferior clothes 2.5g, day clothes once.
Embodiment 3.
120 parts of principal agent benflumetol
20 parts of principal agent Artemether
250 parts of poloxamers
Operation: with poloxamer fusion in 70-80 ℃ of water-bath of recipe quantity, add the benflumetol of recipe quantity, stir, be incubated 20 minutes, go in the 5-10 ℃ of methyl-silicone oil coolant with the dropping-pill machine of 0.4-0.6mm bore, the elimination methyl-silicone oil gets rid of clean, airing, that is, and the heavy 5-15mg of every ball.Inferior clothes 2.5g, day clothes once.
Claims (9)
1. chemical medicine drop pill for the treatment of malaria, it is characterized in that: with antimalarial benflumetol and Artemether is the drop pill that principal agent is made.
2. a kind of compound artemether dripping pill according to claim 1 is characterized in that: benflumetol and Artemether are principal agent,, as dispersant principal agent are fully disperseed with water miscible adjuvant.
3. compound artemether dripping pill according to claim 1 is characterized in that: the ratio of principal agent benflumetol and Artemether is 6: 1.
4. a kind of compound artemether dripping pill according to claim 1 is characterized in that: water miscible adjuvant comprises different molecular weight polyethylene glycol and poloxamer, and its principal agent Coartem is 1: 2 to 1: 5 with the ratio of adjuvant.Different molecular weight polyethylene glycol comprises polyethylene glycol 6000, Macrogol 4000, cetomacrogol 1000, PEG400, in one or more mixture.
5. a kind of compound artemether dripping pill according to claim 1, it is characterized in that: its preparation method is with low-molecular-weight Polyethylene Glycol fusion or heating in water-bath, add principal agent benflumetol and Artemether, abundant mixing, fully disperse, add high-molecular weight Polyethylene Glycol, fully stirring and evenly mixing.
6. a kind of compound artemether dripping pill according to claim 1, it is characterized in that: its preparation method is with a kind of in high-molecular weight Polyethylene Glycol or the poloxamer or several, fusion mixing in water-bath, bath temperature is 80-90 ℃, add principal agent benflumetol and Artemether, stir, be incubated 15-30 minute, splash in the coolant.
7. a kind of compound artemether dripping pill according to claim 1 is characterized in that: coolant comprises methyl-silicone oil or liquid paraffin.The temperature of coolant is 5-10 ℃.
8. a kind of compound artemether dripping pill according to claim 1 is characterized in that: the bore of the dropper of drop pill machine is 0.4-0.6mm.
9. a kind of compound artemether dripping pill according to claim 1 is characterized in that: prepared drop pill, the heavy 5-15mg of every ball.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007100575371A CN101317839A (en) | 2007-06-05 | 2007-06-05 | Preparation method for compound artemether dripping pill for treating malaria |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007100575371A CN101317839A (en) | 2007-06-05 | 2007-06-05 | Preparation method for compound artemether dripping pill for treating malaria |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101317839A true CN101317839A (en) | 2008-12-10 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2007100575371A Pending CN101317839A (en) | 2007-06-05 | 2007-06-05 | Preparation method for compound artemether dripping pill for treating malaria |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101317839A (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101835464B (en) * | 2007-10-25 | 2013-05-15 | 原始制药有限公司 | Anti-malarial pharmaceutical composition |
| CN107569482A (en) * | 2017-08-29 | 2018-01-12 | 昆药集团股份有限公司 | Artemisine compounds are preparing the application in treating embryonal-cell lipoma medicine |
-
2007
- 2007-06-05 CN CNA2007100575371A patent/CN101317839A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101835464B (en) * | 2007-10-25 | 2013-05-15 | 原始制药有限公司 | Anti-malarial pharmaceutical composition |
| CN107569482A (en) * | 2017-08-29 | 2018-01-12 | 昆药集团股份有限公司 | Artemisine compounds are preparing the application in treating embryonal-cell lipoma medicine |
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| Date | Code | Title | Description |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Open date: 20081210 |