CN1092048C - Compound piperaquine tablet - Google Patents
Compound piperaquine tablet Download PDFInfo
- Publication number
- CN1092048C CN1092048C CN98113233A CN98113233A CN1092048C CN 1092048 C CN1092048 C CN 1092048C CN 98113233 A CN98113233 A CN 98113233A CN 98113233 A CN98113233 A CN 98113233A CN 1092048 C CN1092048 C CN 1092048C
- Authority
- CN
- China
- Prior art keywords
- piperaquine
- tablet
- compound
- phosphate
- trimethoprim
- 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.)
- Expired - Fee Related
Links
- UCRHFBCYFMIWHC-UHFFFAOYSA-N piperaquine Chemical compound ClC1=CC=C2C(N3CCN(CC3)CCCN3CCN(CC3)C=3C4=CC=C(C=C4N=CC=3)Cl)=CC=NC2=C1 UCRHFBCYFMIWHC-UHFFFAOYSA-N 0.000 title claims abstract description 19
- 229950006717 piperaquine Drugs 0.000 title claims abstract description 19
- 150000001875 compounds Chemical class 0.000 title claims abstract description 10
- 239000003814 drug Substances 0.000 claims abstract description 13
- GJOHLWZHWQUKAU-UHFFFAOYSA-N 5-azaniumylpentan-2-yl-(6-methoxyquinolin-8-yl)azanium;dihydrogen phosphate Chemical compound OP(O)(O)=O.OP(O)(O)=O.N1=CC=CC2=CC(OC)=CC(NC(C)CCCN)=C21 GJOHLWZHWQUKAU-UHFFFAOYSA-N 0.000 claims abstract description 8
- 229960005462 primaquine phosphate Drugs 0.000 claims abstract description 8
- IEDVJHCEMCRBQM-UHFFFAOYSA-N trimethoprim Chemical compound COC1=C(OC)C(OC)=CC(CC=2C(=NC(N)=NC=2)N)=C1 IEDVJHCEMCRBQM-UHFFFAOYSA-N 0.000 claims abstract description 8
- 229960001082 trimethoprim Drugs 0.000 claims abstract description 8
- 229930187998 Dihydroarteannuin Natural products 0.000 claims description 9
- 229930191701 arteannuin Natural products 0.000 claims description 5
- 229960004191 artemisinin Drugs 0.000 claims description 5
- BLUAFEHZUWYNDE-NNWCWBAJSA-N artemisinin Chemical compound C([C@](OO1)(C)O2)C[C@H]3[C@H](C)CC[C@@H]4[C@@]31[C@@H]2OC(=O)[C@@H]4C BLUAFEHZUWYNDE-NNWCWBAJSA-N 0.000 claims description 5
- 229960000981 artemether Drugs 0.000 claims description 2
- 229960004991 artesunate Drugs 0.000 claims description 2
- FIHJKUPKCHIPAT-AHIGJZGOSA-N artesunate Chemical compound C([C@](OO1)(C)O2)C[C@H]3[C@H](C)CC[C@@H]4[C@@]31[C@@H]2O[C@@H](OC(=O)CCC(O)=O)[C@@H]4C FIHJKUPKCHIPAT-AHIGJZGOSA-N 0.000 claims description 2
- SXYIRMFQILZOAM-HVNFFKDJSA-N dihydroartemisinin methyl ether Chemical compound C1C[C@H]2[C@H](C)CC[C@H]3[C@@H](C)[C@@H](OC)O[C@H]4[C@]32OO[C@@]1(C)O4 SXYIRMFQILZOAM-HVNFFKDJSA-N 0.000 claims description 2
- 201000004792 malaria Diseases 0.000 abstract description 8
- 230000000694 effects Effects 0.000 abstract description 6
- 206010048723 Multiple-drug resistance Diseases 0.000 abstract description 4
- 231100000053 low toxicity Toxicity 0.000 abstract description 4
- 230000000505 pernicious effect Effects 0.000 abstract description 4
- 229960002521 artenimol Drugs 0.000 abstract description 2
- BJDCWCLMFKKGEE-ISOSDAIHSA-N artenimol Chemical compound C([C@](OO1)(C)O2)C[C@H]3[C@H](C)CC[C@@H]4[C@@]31[C@@H]2O[C@H](O)[C@@H]4C BJDCWCLMFKKGEE-ISOSDAIHSA-N 0.000 abstract description 2
- 229930016266 dihydroartemisinin Natural products 0.000 abstract description 2
- 229940079593 drug Drugs 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 229960001962 mefloquine Drugs 0.000 description 3
- XEEQGYMUWCZPDN-DOMZBBRYSA-N (-)-(11S,2'R)-erythro-mefloquine Chemical compound C([C@@H]1[C@@H](O)C=2C3=CC=CC(=C3N=C(C=2)C(F)(F)F)C(F)(F)F)CCCN1 XEEQGYMUWCZPDN-DOMZBBRYSA-N 0.000 description 2
- 239000002671 adjuvant Substances 0.000 description 2
- 239000003430 antimalarial agent Substances 0.000 description 2
- 230000007812 deficiency Effects 0.000 description 2
- -1 mefloquine compound Chemical class 0.000 description 2
- 239000002547 new drug Substances 0.000 description 2
- 239000002994 raw material Substances 0.000 description 2
- HQWQVBJUIIJTRE-LKRNKTNVSA-N 4-amino-n-(5,6-dimethoxypyrimidin-4-yl)benzenesulfonamide;(s)-[2,8-bis(trifluoromethyl)quinolin-4-yl]-[(2r)-piperidin-2-yl]methanol;5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine;hydron;chloride Chemical compound Cl.CCC1=NC(N)=NC(N)=C1C1=CC=C(Cl)C=C1.COC1=NC=NC(NS(=O)(=O)C=2C=CC(N)=CC=2)=C1OC.C([C@@H]1[C@@H](O)C=2C3=CC=CC(=C3N=C(C=2)C(F)(F)F)C(F)(F)F)CCCN1 HQWQVBJUIIJTRE-LKRNKTNVSA-N 0.000 description 1
- 241000223960 Plasmodium falciparum Species 0.000 description 1
- 208000035999 Recurrence Diseases 0.000 description 1
- 230000000078 anti-malarial effect Effects 0.000 description 1
- 229940033495 antimalarials Drugs 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 210000000038 chest Anatomy 0.000 description 1
- 210000000973 gametocyte Anatomy 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 239000002423 protozoacide Substances 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Classifications
-
- 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
Landscapes
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
The present invention provides a new compound piperaquine tablet used for treating multiple drug resistance pernicious malaria. The compound piperaquine tablet is prepared from piperaquine phosphate, dihydroartemisinin, trimethoprim and primaquine phosphate. Clinical experiments show that the tablet has the characteristics of immediate effect, high efficiency, low toxicity and short course of treatment. The therapeutic effect is obviously better than that of the existing homogeneous drug at home and abroad.
Description
The present invention relates to a kind of new drug for the treatment of malaria, particularly compound piperaquine tablet new drug.
At present, the multiple drug resistance pernicious malaria whole world spreads, and Southeast Asia is particularly serious.It is commonly used that antimalarial such as mefloquine (Mefloquine) and mefloquine compound recipe---Fa Ximi (Fansimef) curative effect gradually descends at thorax; Though the arteannuin medicine curative effect is pretty good, the course of treatment is long partially, and promoting in the malaria district has certain difficulty.
Purpose of the present invention is intended to overcome the deficiency of existing various antimalarials and new drug---the compound piperaquine tablet of a kind of quick-acting, efficient, low toxicity, the treatment multiple drug resistance pernicious malaria of the short course of treatment is provided.
The object of the present invention is achieved like this:
A kind of compound piperaquine tablet, it is characterized in that this tablet comprises piperaquine phosphate (Piperaquinephosphate), dihydroarteannuin (Dihydroartemisinin) or its similar medicine, trimethoprim (Trimethoprim) and primaquine phosphate (Primaquine Phosphate), the weight proportion scope of four medicine parts is:
Piperaquine phosphate 25-35 part
Dihydroarteannuin or its similar medicine 2-5 part
Trimethoprim 6-12 part
1 part of primaquine phosphate
---the similar medicine of described dihydroarteannuin is meant other derivants of arteannuin, artesunate, Artemether or arteannuin.This type of medicine finally is converted into dihydroarteannuin and brings into play it and kill the protozoacide effect in body.
The principle of the present invention's prescription is: piperaquine phosphate has long-acting characteristics, can make to shorten to 2 days the course of treatment; Dihydroarteannuin has quick-acting low toxicities, can kill the resistance Plasmodium falciparum rapidly in a large number to mend the deficiency of piperaquine; Trimethoprim is a kind of synergist, helps to improve cure rate and reduces recrudescence rate; Primaquine phosphate is mainly used in kills gametocyte, removes the source of infection and blocking propagation.
The invention will be further described below by embodiment:
By the following prescription amount of getting:
Piperaquine phosphate 160g
Dihydroarteannuin or its similar medicine 16g
Trimethoprim 45g
Primaquine phosphate 5g
Adjuvant (its cellulose of hydroxypropyl) is an amount of
Make 1000
Preparation process:
Earlier raw and auxiliary 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.
Compound piperaquine tablet of the present invention can be used for treating all kinds of malaria and is particularly useful for treating subtertian malaria and multiple drug resistance pernicious malaria, and adult's consumption is 2 days, 8 of total dose of curative course: promptly 0 hour, 8 hours, 24 hours and 32 hours, at every turn obey 2.By 500 these medical instruments of many cases clinical trial certificate have immediate effect, efficiently, low toxicity, the characteristics of the short course of treatment, its curative effect obviously is better than similar medicine both domestic and external at present.
Claims (2)
1, a kind of compound piperaquine tablet is characterized in that this tablet comprises that the weight proportion scope of piperaquine phosphate, dihydroarteannuin or its similar medicine, trimethoprim and primaquine phosphate four medicine parts is:
Piperaquine phosphate 25-35 part
Dihydroarteannuin or its similar medicine 2-5 part
Trimethoprim 6-12 part
1 part of primaquine phosphate
2, compound piperaquine tablet according to claim 1, the similar medicine that it is characterized in that dihydroarteannuin is meant other derivants of arteannuin, artesunate, Artemether formula arteannuin.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN98113233A CN1092048C (en) | 1998-06-02 | 1998-06-02 | Compound piperaquine tablet |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN98113233A CN1092048C (en) | 1998-06-02 | 1998-06-02 | Compound piperaquine tablet |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1237416A CN1237416A (en) | 1999-12-08 |
| CN1092048C true CN1092048C (en) | 2002-10-09 |
Family
ID=5222990
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN98113233A Expired - Fee Related CN1092048C (en) | 1998-06-02 | 1998-06-02 | Compound piperaquine tablet |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1092048C (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1135974C (en) * | 2000-08-23 | 2004-01-28 | 重庆健桥医药开发有限公司 | Antimalarial compound dihydroartemisinin |
| CN1255106C (en) | 2003-09-26 | 2006-05-10 | 李国桥 | Complex artemisia apiacea extract |
-
1998
- 1998-06-02 CN CN98113233A patent/CN1092048C/en not_active Expired - Fee Related
Non-Patent Citations (1)
| Title |
|---|
| 《医学研究通讯》，14(11) 1985.1.1 许德余等"疟疾和肺治疗新药羟基哌喹" * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1237416A (en) | 1999-12-08 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1085527C (en) | Preparation method of synergistic antimalarial compound benzfluorenol | |
| JP2010047609A (en) | Pharmaceutical composition active in reducing production of mcp-1 protein | |
| CN1041694A (en) | The anti-malaria composition of quinidine, arteannuin and derivant thereof and Therapeutic Method | |
| CN1092048C (en) | Compound piperaquine tablet | |
| CN1255106C (en) | Complex artemisia apiacea extract | |
| CN1135974C (en) | Antimalarial compound dihydroartemisinin | |
| CN105213321B (en) | A kind of medicinal-bathing particle agent and application thereof of qinghaosu or derivatives thereof | |
| CN1081035C (en) | Antimalarial compound naphtholquine | |
| CN101342185A (en) | Application of forsythiaside in the preparation of anti-tumor chemotherapy sensitization and attenuation drugs or anti-AIDS sensitization and attenuation drugs | |
| JPH02184632A (en) | Drug composition | |
| CN1067245C (en) | Application of N-aceto-D-aminoglucose in medicinal preparation for curing respiratory tract diseases | |
| CN1235595C (en) | Chitin soft capsule and preparing method thereof | |
| CN1177603C (en) | Gingko leaf slow-releasing table and preparation process thereof | |
| CN1111033C (en) | Psoriasis treating medicine | |
| CN1132593C (en) | Mixture of white pepper and borneol and its application | |
| CN1352988A (en) | Exterior-applied Chinese medicine for treating cold in stomach | |
| CN1115663A (en) | Medicine for curing hypertension | |
| CN1187358A (en) | Compound powder for curing ulcer erosion | |
| CN1111419C (en) | A kind of medicine for the treatment of cardiovascular and cerebrovascular vessel apoplexy and premonitory apoplexy symptom and preparation method thereof | |
| CN1084627C (en) | Traditional Chinese medicinal plaster for treating psoriasis | |
| CN1183288A (en) | Yiai pill (powder) and method for manufacturing same | |
| CN1253171C (en) | Chinese medicine preparation for treating blood viscosity symdrome and its preparing method | |
| CN1915253A (en) | Exterior coating medication for treating tinea of feet, and preparation method | |
| CN1399957A (en) | Application of shikonin and its derivative in pharmaceutical industry | |
| CN1110145A (en) | Scorpion venom oil for treating skin diseases |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C06 | Publication | ||
| PB01 | Publication | ||
| ASS | Succession or assignment of patent right |
Owner name: JIANQIAO MEDICINE SCIENCE DEVELOPMENT CO., LTD., Free format text: FORMER OWNER: JIANQIAO MEDICAL TECHNOLOGY IMPORT + EXPORT CO., LTD., GUANGZHOU CITY Effective date: 20010804 |
|
| C41 | Transfer of patent application or patent right or utility model | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20010804 Address after: 510400 Guangzhou Guanghua Road No. 11-21 Xiangkang trade building room 804 Applicant after: Jianqiao Sci & Tech. Dev. Co., Ltd., Guangzhou City Address before: Yun Lu, Baiyun District of Guangzhou City, Guangdong province 510405 Ling Jing No. 100 East ladder 302 or 402 Applicant before: Jianqiao Medicine Science & Technology Import & Export Co. Ltd. |
|
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| ASS | Succession or assignment of patent right |
Owner name: CHONGQING JIANQIAO MEDICINAL DEVELOPMENT CO., LTD Free format text: FORMER OWNER: JIANQIAO MEDICINE SCIENCE DEVELOPMENT CO., LTD., GUANGZHOU CITY Effective date: 20050520 |
|
| C41 | Transfer of patent application or patent right or utility model | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20050520 Address after: 408200, Baisha County, Mingshan County, Fengdu, Chongqing Patentee after: Jianqiao Medicine Development Co., Ltd., Chongqing City Address before: 510400 Guangzhou Guanghua Road No. 11-21 Xiangkang trade building room 804 Patentee before: Jianqiao Sci & Tech. Dev. Co., Ltd., Guangzhou City |
|
| C17 | Cessation of patent right | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20021009 Termination date: 20140602 |