CN1135974C - Antimalarial compound dihydroartemisinin - Google Patents
Antimalarial compound dihydroartemisinin Download PDFInfo
- Publication number
- CN1135974C CN1135974C CNB001131346A CN00113134A CN1135974C CN 1135974 C CN1135974 C CN 1135974C CN B001131346 A CNB001131346 A CN B001131346A CN 00113134 A CN00113134 A CN 00113134A CN 1135974 C CN1135974 C CN 1135974C
- Authority
- CN
- China
- Prior art keywords
- medicine
- dihydroartemisinin
- piperaquine
- present
- dihydroarteannuin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/357—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4706—4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
- A61P33/06—Antimalarials
-
- 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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- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The present invention provides a new medicine compound dihydroartemisinin for treating the pernicious malaria with multiple medicine resistance, which is prepared from components of dihydroartemisinin, piperaquine and trimethoprim. The medicine indicates that the medicine has the characteristics of immediate effect, high efficiency, low toxicity and short course of treatment by an animal experiment and clinical tryout; a therapeutic effect and a low-toxicity side effect are obviously superior to that of the current native and foreign medicine in the same class. Because of the match of two main components such as dihydroartemisinin and piperaquine of the present invention, the effect is good; the dihydroartemisinin and the piperaquine are important component parts of the patent of the present invention.
Description
The present invention relates to be used for the treatment of and prevent the compound dihydroartemisinin of pernicious malaria and other types malaria.
The multiple drug resistance pernicious malaria whole world spreads, and Southeast Asia is particularly serious.World Health Organization (WHO) has listed one of essential planning of 21 century to " containment malaria " in.Former mefloquine (Mefloquine) and compound recipe Fa Ximi (Fansimef) thereof are expressed very big hope, but because its drug-fast rapid appearance, at first in Thailand, then it is very poor to be in curative effect in Vietnam, and (Li Guoqiao etc. treat subtertian malaria in Vietnam Xuan Loc hospital with Fansimef in toxicity no small condition, cure rate 55%, unpublished data 1995).Arteannuin of having developed since China's the seventies and derivant artesunate thereof, Artemether, arteether, dihydroarteannuin etc. have efficient, quick-acting advantages, just can reach high curative rate in 7 days but must take medicine, otherwise the recrudescence rate height is unfavorable for the control of the malaria source of infection.
Switzerland NORVATIS drugmaker might be better than existing antimalarial from the technology Coartem (being made up of Artemether and benflumetol) that China buys, but still needs 3 days its course of treatment, and cost is higher.The Malarone that Britain Glaxo Wellcome company is developing, by how quinone (Naphthoquinone) and cyclochloroguanidum are formed, and do not have active remedy in its prescription, 3 days courses of treatment, take medicine every day 2 times.If with every day dose change into once and taking, then feel sick, the vomiting side effect is serious.
The object of the present invention is to provide the compound dihydroartemisinin of a kind of quick-acting, efficient, low toxicity, the pernicious Malaria of treatment multiple drug resistance of the short course of treatment.
Above-mentioned purpose of the present invention is to realize that by such technical scheme promptly a kind of antimalarial compound dihydroartemisinin is characterized in that: it is the medicament made from following weight (part) proportion raw material:
1 part of dihydroarteannuin (Dihydroartemisinin) or its similar medicine
3～7 parts of piperaquine (piperaquine)
0～5 part of trimethoprim (Trimethoprim)
The similar medicine of dihydroarteannuin is arteannuin and derivant thereof in the medicine of the present invention, as arteannuin, artesunate, Artemether, arteether.This type of medicine finally is converted into dihydroarteannuin and brings into play it and kill the protozoacide effect in body.
Above-mentioned solution of the present invention is based on pathogenetic understanding and the Therapeutic Principle of motherland's medical science to Malaria, draw with reference to the modern pharmacological research achievement, be that the principle that the present invention fills a prescription is: dihydroarteannuin has quick-acting, low toxicity, can kill the drug resistant falciparum malaria protozoon rapidly in a large number, but if discontinuous taking medicine 7 days, then relapse rate height; Piperaquine has long-acting characteristics, can make to shorten to 2 days the course of treatment; Can mend the deficiency of dihydroarteannuin; Trimethoprim is a kind of synergist, helps to improve cure rate and reduces recrudescence rate.Dihydroarteannuin can delay the drug-fast appearance of piperaquine and trimethoprim again.
The optimum weight of medicine of the present invention (part) proportioning is:
1 part of dihydroarteannuin
5 parts of piperaquine
2.5 parts of trimethoprims
Medicine of the present invention also can be the compatibility agent of dihydroarteannuin and piperaquine, and its optimum weight (part) proportioning is:
1 part of dihydroarteannuin
6 parts of piperaquine
Medicine of the present invention is through pharmacodynamics, toxicology, general pharmacology test and clinical research and researchs such as preparation technology, quality testing and study on the stability, and, the curative effect of subtertian malaria is tested in China Hainan Province and Vietnam, Thailand, the popular area of Cambodia's resistant malaria.Result of study proves that its curative effect to subtertian malaria is better than existing any antimalarial, can be used for treating subtertian malaria, ask day malaria and other types malaria, be in the world subtertian malaria to be had the cure rate height so far for this reason, parasite killing speed is fast and toxicity is low, and safety is big, and technology is simple, maturation, the new drug of good stability.Wherein one of main component piperaquine is without its phosphate, reduces dosage, alleviates side effect, reduced cost, and its maximum characteristics are to take simple and conveniently, only need take medicine and can cure for one day 2 times.Actual application value is very big.
Preparation of the present invention is that said medicine is combined with multiple pharmaceutically acceptable excipient or carrier; adopt mixing, dissolving, granulation, in flakes, known methods such as sweet tablet or film coating are prepared into the preparation of solid-state or liquid form, as tablet, capsule, suppository, granule and injection etc.
Above-mentioned each component is made medicine production method of the present invention is:
Earlier supplementary material is detected,, cross 100 mesh sieves, accurately take by weighing raw material and adjuvant by recipe quantity then qualified raw material pulverize separately.With each component mix homogeneously tabletting, packing is finished product.
For example: 1000 of production medicines of the present invention are by the following prescription amount of getting:
Dihydroarteannuin or its similar medicine 75g
Piperaquine 375g
Trimethoprim 1875g
Adjuvant (its cellulose of hydroxypropyl) is an amount of.
The taking dose of medicine of the present invention: adult consumption be 2 days, 4 of total dose of curative course, promptly 0 hour, 8 hours, 24 constantly with 32 hours, obey 1 at every turn.By 500 these medical instruments of many cases clinical trial certificate have immediate effect, efficiently, low toxicity, characteristics, its curative effect of the short course of treatment obviously be better than similar medicine both domestic and external at present.
Claims (3)
1, a kind of compound recipe new antimalarial agent that contains dihydroarteannuin is characterized in that the active component of this medicine is:
1 part of dihydroarteannuin
Piperaquine or its phosphate 3-7 part
Trimethoprim 0-5 part.
2, compound recipe new antimalarial agent as claimed in claim 1 is characterized in that dihydroarteannuin can use arteannuin, artesunate, Artemether, arteether to substitute.
3, compound recipe new antimalarial agent as claimed in claim 1 is characterized in that pharmaceutical dosage form is tablet, capsule, suppository, granule and injection.
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB001131346A CN1135974C (en) | 2000-08-23 | 2000-08-23 | Antimalarial compound dihydroartemisinin |
| AU2001289506A AU2001289506A1 (en) | 2000-08-23 | 2001-05-31 | Pharmaceutical composition of dihydroartemisinin for treating malaria |
| PCT/CN2001/000884 WO2002026226A1 (en) | 2000-08-23 | 2001-05-31 | Pharmaceutical composition of dihydroartemisinin for treating malaria |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB001131346A CN1135974C (en) | 2000-08-23 | 2000-08-23 | Antimalarial compound dihydroartemisinin |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1305810A CN1305810A (en) | 2001-08-01 |
| CN1135974C true CN1135974C (en) | 2004-01-28 |
Family
ID=4582950
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB001131346A Ceased CN1135974C (en) | 2000-08-23 | 2000-08-23 | Antimalarial compound dihydroartemisinin |
Country Status (3)
| Country | Link |
|---|---|
| CN (1) | CN1135974C (en) |
| AU (1) | AU2001289506A1 (en) |
| WO (1) | WO2002026226A1 (en) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7842719B2 (en) | 2002-10-31 | 2010-11-30 | Kemin Foods, L.C. | Use of endoperoxides for the treatment of infections caused by flaviviridae, including hepatitis C, bovine viral diarrhea and classical swine fever virus |
| CN1255106C (en) * | 2003-09-26 | 2006-05-10 | 李国桥 | Complex artemisia apiacea extract |
| CN1833644B (en) * | 2005-03-18 | 2010-07-21 | 中国人民解放军第三军医大学 | Abrotine, its derivative dihydro-abrotine, artemether, arteether and arte sunate in use of pharmacy |
| WO2007132438A2 (en) * | 2006-05-17 | 2007-11-22 | Ranbaxy Laboratories Limited | Antimalarial therapy using a combination of synthetic artemisinin derivative and bisquinoline derivative |
| CN107929240A (en) * | 2017-12-13 | 2018-04-20 | 桂林南药股份有限公司 | Piperaquine phosphate oral liquid and preparation method thereof |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5219865A (en) * | 1987-05-08 | 1993-06-15 | Hoechst Aktiengesellschaft | Pharmaceutical combination for the prophylaxis and therapy of malaria |
| CN1081035C (en) * | 1997-11-18 | 2002-03-20 | 广州市健桥医药科技发展有限公司 | Antimalarial compound naphtholquine |
| CN1092048C (en) * | 1998-06-02 | 2002-10-09 | 广州市健桥医药科技发展有限公司 | Compound piperaquine tablet |
-
2000
- 2000-08-23 CN CNB001131346A patent/CN1135974C/en not_active Ceased
-
2001
- 2001-05-31 AU AU2001289506A patent/AU2001289506A1/en not_active Abandoned
- 2001-05-31 WO PCT/CN2001/000884 patent/WO2002026226A1/en active Application Filing
Also Published As
| Publication number | Publication date |
|---|---|
| CN1305810A (en) | 2001-08-01 |
| WO2002026226A1 (en) | 2002-04-04 |
| AU2001289506A1 (en) | 2002-04-08 |
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| C17 | Cessation of patent right | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20040128 Termination date: 20100823 |
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| C35 | Partial or whole invalidation of patent or utility model | ||
| IW01 | Full invalidation of patent right |
Decision date of declaring invalidation: 20081001 Decision number of declaring invalidation: 12148 Granted publication date: 20040128 |