CN101310720A - Preparation method of artemether drop pills for treating malaria - Google Patents
Preparation method of artemether drop pills for treating malaria Download PDFInfo
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- CN101310720A CN101310720A CNA2007100574059A CN200710057405A CN101310720A CN 101310720 A CN101310720 A CN 101310720A CN A2007100574059 A CNA2007100574059 A CN A2007100574059A CN 200710057405 A CN200710057405 A CN 200710057405A CN 101310720 A CN101310720 A CN 101310720A
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- artemether
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- polyethylene glycol
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- drug
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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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Abstract
The invention relates to a preparation method of a chemical drug preparation for treating malaria which is artemether dropping pills. The preparation method has the advantages that: 1. compared with tablets, capsules and soft capsules of the normal-release preparations, the disintegration time limit is greatly shortened, and the onset of action is rapid; 2. water-soluble excipients are used for the full dispersing non-water-soluble main drug, thus being conductive to the absorption of the main drug and improving the oral bioavailability; 3. the dropping pills of the invention can be swallowed, carried out the sublingual administration and directly absorbed by sublingual mucosal veins, thus avoiding the first-pass effect of the stomach, rapidly achieving the peak value of the plasma-drug concentration, having rapid onset of action and improving the efficacy; 4. as the dropping pills of the invention have rapid absorption, the stagnation time in the stomach is short, and the dropping pills can further reduce the generation of drug resistance and other side effects; 5. the production process is simple, the production period is short, and the cost can be lowered; 6. the dropping pills can not only overcome the inconvenient usage of the intravenous drug delivery, but also can overcome the shortcoming of low bioavailability of other oral normal-release preparations.
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 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 Artemether sheet, Artemether capsule, Artemether soft capsule (soft gelatin capsule), its major defect is that disintegration is long, because its non-water-soluble character is difficult for absorbing, onset is slow, be difficult to reach rapidly the peak value of blood drug level, influenced oral administration biaavailability greatly, thereby also influenced the competition of the performance of curative effect, the antimalarial of artemisine is competed very fierce in the international market, competition focal point is transformed into finished medicines from crude drug at present, the characteristics that drop pill had are occupied very strong advantage in the competition of finished medicines.
Shorten molten (disintegrate) time limit of loosing, quicken the absorption of medicine,, its speed that reaches the blood drug level peak value is reached or, make it rapid-action near the speed of intravenously administrable to improve oral administration biaavailability, absorb fast, good effect.The present invention just is being based on this technical background, develops 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 normal release formulation (tablet, capsule, soft capsule), and have actual application value.
Technical scheme of the present invention is: a kind of chemical medicine drop pill for the treatment of malaria, and it is to be principal agent with the antimalarial Artemether, adopts 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), normal release formulation tablet of its time limit, capsule, soft capsule (soft gelatin capsule) foreshorten to 1/10th, and its external stripping quantity also improves greatly, can in 45 minutes, reach more than 70%, therefore improve oral administration biaavailability greatly.
This drop pill has adopted adjuvant as dispersant, and original non-water-soluble Artemether is fully disperseed by water miscible adjuvant, is beneficial to the absorption of principal agent 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 medicine degree and absorb; 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 10-60mg, calculates the content of principal agent, determines oral consumption.
Embodiment 1.
100 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 Artemether 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 0.8-1.1mm bore, splash in 5-10 ℃ the methyl-silicone oil coolant, the elimination methyl-silicone oil gets rid of clean, airing, promptly.The heavy 35-60mg of every ball.
Embodiment 2.
100 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 Artemether 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 0.8-1.1mm bore, get rid of clean, airing, promptly, every ball weight 35-60mg.
Embodiment 3.
100 parts of principal agent Artemether
250 parts of poloxamers
Operation: with poloxamer fusion in 70-80 ℃ of water-bath of recipe quantity, the Artemether that adds recipe quantity, stir, be incubated 20 minutes, go in the 5-10 ℃ of methyl-silicone oil coolant elimination methyl-silicone oil with the dropping-pill machine of 0.8-1.1mm bore, get rid of clean, airing, that is, and the heavy 35-60mg of every ball.
Claims (8)
1. chemical medicine drop pill for the treatment of malaria, it is characterized in that: with the antimalarial Artemether is the drop pill that principal agent is made.
2. a kind of artemether dripping pill according to claim 1 is characterized in that: Artemether is a principal agent,, as dispersant principal agent is fully disperseed with water miscible adjuvant.
3. a kind of 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 Artemether 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.
4. a kind of artemether dripping pill according to claim 1 is characterized in that: its preparation method is with low-molecular-weight Polyethylene Glycol fusion or heating in water-bath, adds the principal agent Artemether, abundant mixing, fully disperse, add high-molecular weight Polyethylene Glycol, fully stirring and evenly mixing.
5. a kind of artemether dripping pill according to claim 1, it is characterized in that: its preparation method is with in high-molecular weight Polyethylene Glycol or the poloxamer one or both, fusion mixing in water-bath, bath temperature is 80-90 ℃, add the principal agent Artemether, stir, be incubated 15-30 minute, splash in the coolant.
6. a kind of 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 ℃.
7. a kind of artemether dripping pill according to claim 1 is characterized in that: the bore of the dropper of drop pill machine is 0.8-1.1mm.
8. a kind of artemether dripping pill according to claim 1 is characterized in that: prepared drop pill, the heavy 10-60mg of every ball.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007100574059A CN101310720A (en) | 2007-05-22 | 2007-05-22 | Preparation method of artemether drop pills for treating malaria |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2007100574059A CN101310720A (en) | 2007-05-22 | 2007-05-22 | Preparation method of artemether drop pills for treating malaria |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101310720A true CN101310720A (en) | 2008-11-26 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2007100574059A Pending CN101310720A (en) | 2007-05-22 | 2007-05-22 | Preparation method of artemether drop pills for treating malaria |
Country Status (1)
| Country | Link |
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| CN (1) | CN101310720A (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 |
| CN103235072A (en) * | 2013-05-14 | 2013-08-07 | 张家港威胜生物医药有限公司 | Method for determining content of artemether in artemether injection with high performance liquid chromatography |
-
2007
- 2007-05-22 CN CNA2007100574059A patent/CN101310720A/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 |
| CN103235072A (en) * | 2013-05-14 | 2013-08-07 | 张家港威胜生物医药有限公司 | Method for determining content of artemether in artemether injection with high performance liquid chromatography |
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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: 20081126 |