CN1528309A - 复方青蒿素 - Google Patents

复方青蒿素 Download PDF

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Publication number
CN1528309A
CN1528309A CNA031469515A CN03146951A CN1528309A CN 1528309 A CN1528309 A CN 1528309A CN A031469515 A CNA031469515 A CN A031469515A CN 03146951 A CN03146951 A CN 03146951A CN 1528309 A CN1528309 A CN 1528309A
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China
Prior art keywords
primaquine
piperaquine
malaria
artemisinin
arteannuin
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CNA031469515A
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CN1255106C (zh
Inventor
李国桥
宋建平
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Guangdong New South Artesunate Pharmaceutical Co ltd
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Individual
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Priority to CNB031469515A priority Critical patent/CN1255106C/zh
Publication of CN1528309A publication Critical patent/CN1528309A/zh
Priority to PCT/CN2004/001064 priority patent/WO2005030197A1/zh
Priority to AP2006003588A priority patent/AP2485A/xx
Priority to EP04762197A priority patent/EP1702616A4/en
Priority to BRPI0414296-9A priority patent/BRPI0414296A/pt
Priority to ZA200602422A priority patent/ZA200602422B/xx
Priority to US10/587,277 priority patent/US7851512B2/en
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Publication of CN1255106C publication Critical patent/CN1255106C/zh
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    • 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
    • A61K31/336—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having three-membered rings, e.g. oxirane, fumagillin
    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

本发明提供一种治疗多重抗药性恶性疟、间日疟、三日疟等人类疟疾的新药复方青蒿素片及其相关儿童剂型(如颗粒剂、栓剂、混悬糖浆、干粉)。该复方由青蒿素、哌喹、伯氨喹组方制成。通过在东南亚疟疾流行国的临床试验证明，该药不仅具有当前国内外最优秀的青蒿素类复方抗疟药高效的、速效的疗效，而且具有疗程更短、副作用更小、原料成本更低、服用更方便的特点，其快速杀灭配子体，迅速切断传染源以阻断疟疾传播等，更是创新的特点。

Description

复方青蒿素
所属技术领域
本发明涉及治疗疟疾的药物，特别是具有高效速效疗效的复方青蒿素。
背景技术
现有技术中的治疟药物有的采用青蒿素衍生物(如双氢青蒿素、青蒿琥酯、蒿甲醚、蒿乙醚)与长半衰期的哌喹配伍，使得疗程长，容易使疟原虫产生抗药性；有的用哌喹和伯氨喹的磷酸盐，由于其磷酸盐对胃肠道有副作用，故疗效欠佳。现有技术的治疟药物还存在生产工艺长，成本高，药物稳定保质期短，服用量大等缺点。
发明内容
本发明的目的旨在克服现有技术的不足而提供一种具有疗程短，副作用更小，原料成本更低、服用更方便、有高效速效的复方青蒿素。
本发明的目的是这样实现的：
一种复方青蒿素，用该复方可制成片剂、儿童颗粒剂、栓剂、混悬糖浆或干粉，复方包括以下成份：青蒿素(Artemisinin)、哌喹(Piperaquine)、伯氨喹(Primaquine)，三药的配伍比例范围是：
青蒿素(Artemisinin)                       1份
哌喹(Piperaquine)                         3-9份
伯氨喹(Primaquine)                        0-0.2份
三药的最佳配比是1∶6∶0.6。
——所述的伯氨喹还可单独制成片剂与青蒿素+哌喹的混合片剂同时服用。
本发明通600多例临床试验，对多重抗药性恶性疟、间日疟和三日疟证明本药具有速效、高效、低毒、短疗程、快速清除传染源以阻断疟疾传播的特点，其疗效、功能明显优于目前国内外的同类药。
具体实施方式
按下述配方取量：
青蒿素(Artemisinin)                 120g
哌喹(Piperaquine)                   1200g
伯氨喹(Primaquine)                  6g
辅料(羟丙基纤维素等)                适量
制成                                1000片
制剂工艺：
将合格的原料分别粉碎，过100目筛，然后按处方量准确取原料及辅料，将各组分混合均匀压片或作成各种儿童剂型，包装即成为成品。
本发明复方青蒿素用于治疗各类疟疾(恶性疟、间日疟、三日疟等人类疟疾)，尤其是多重抗药性恶性疟，成人总剂量为2片，每天服1片。
本复方中的伯氨喹含量每片仅含6mg，即一天用量，仅用2天，此剂量是比常规用量3天67.5mg减少了82％，与青蒿素配合应用，经实验研究证明可使恶性疟原虫配子体在首剂服药后24小时即完全失去感染性，从而阻断其传播，又无任何副作用。这是该复方使用超低剂量伯氨喹的一大特点。
由于本复方比任何青蒿素类复方的主要原料的成本更低，体积更小，疗程更短，服用更方便(成人2天2片)，且具有明显杀灭配子体阻断疟疾传播的作用，因而有利于该复方以较低的价格进入发展中国家公立医院，更有利于全球抗疟措施的推广应用。

Claims (2)

1.一种复方青蒿素，其特征在于用该复方可制成片剂、儿童颗粒剂、栓剂、混悬糖浆或干粉，复方包括以下成份：青蒿素(Artemisinin)、哌喹(Piperaquine)、伯氨喹(Primaquine)，三药的配伍比例范围是：
青蒿素(Artemisinin)                1份
哌喹(Piperaquine)                  3-9份
伯氨喹(Primaquine)                 0-0.2份
三药的最佳配比是1∶6∶0.6。
2.根据权利要求1所述的复方青蒿素，其特征在于所述的伯氨喹还可单独制成片剂与青蒿素+哌喹的混合片剂同时服用。
CNB031469515A 2003-09-26 2003-09-26 复方青蒿素 Expired - Lifetime CN1255106C (zh)

Priority Applications (7)

Application Number Priority Date Filing Date Title
CNB031469515A CN1255106C (zh) 2003-09-26 2003-09-26 复方青蒿素
PCT/CN2004/001064 WO2005030197A1 (fr) 2003-09-26 2004-09-20 Compose a base d'artemisinine
AP2006003588A AP2485A (en) 2003-09-26 2004-09-20 Compound artemisinin
EP04762197A EP1702616A4 (en) 2003-09-26 2004-09-20 CONNECTION ARTEMISININE
BRPI0414296-9A BRPI0414296A (pt) 2003-09-26 2004-09-20 combinação compreendendo artemisinina
ZA200602422A ZA200602422B (en) 2003-09-26 2004-09-20 Compound artemisinin
US10/587,277 US7851512B2 (en) 2003-09-26 2004-09-20 Composition containing artemisinin for treatment of malaria

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CNB031469515A CN1255106C (zh) 2003-09-26 2003-09-26 复方青蒿素

Publications (2)

Publication Number Publication Date
CN1528309A true CN1528309A (zh) 2004-09-15
CN1255106C CN1255106C (zh) 2006-05-10

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Family Applications (1)

Application Number Title Priority Date Filing Date
CNB031469515A Expired - Lifetime CN1255106C (zh) 2003-09-26 2003-09-26 复方青蒿素

Country Status (7)

Country Link
US (1) US7851512B2 (zh)
EP (1) EP1702616A4 (zh)
CN (1) CN1255106C (zh)
AP (1) AP2485A (zh)
BR (1) BRPI0414296A (zh)
WO (1) WO2005030197A1 (zh)
ZA (1) ZA200602422B (zh)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102485226A (zh) * 2010-12-03 2012-06-06 昆明制药集团股份有限公司 一种复方青蒿素类哌喹微丸及其制备方法
CN111249275A (zh) * 2020-03-03 2020-06-09 云南省寄生虫病防治所 一种治疗间日疟的药物的配伍方案及其使用方法
CN111514299A (zh) * 2020-04-29 2020-08-11 广州中医药大学科技产业园有限公司 一种用于防治肺炎的组合物及其在制备用于防治肺炎的药物中的应用

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101472582A (zh) * 2006-05-17 2009-07-01 兰贝克赛实验室有限公司 联用合成青蒿素衍生物和双喹啉衍生物的抗疟疗法
WO2008098586A1 (en) * 2007-02-13 2008-08-21 Dafra Pharma N.V. Pharmaceutical carrier composition and pharmaceutical composition
CH700941B1 (de) * 2007-12-04 2010-11-15 Mepha Ag Pharmazeutische Zusammensetzung zur Behandlung von Malaria.
WO2010004573A1 (en) * 2008-07-07 2010-01-14 Ipca Laboratories Limited Synergistic antimalarial pharmaceutical composition
MX2016005959A (es) 2013-11-08 2016-10-14 Exthera Medical Corp Métodos para diagnosticar enfermedades infecciosas usando medio de adsorción.

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN166154B (zh) 1987-05-08 1990-03-24 Hoechst India
US5219865A (en) * 1987-05-08 1993-06-15 Hoechst Aktiengesellschaft Pharmaceutical combination for the prophylaxis and therapy of malaria
US5270037A (en) * 1990-07-12 1993-12-14 Boehringer Ingelheim Gmbh Use of interferon and a substance with an antimalarial activity for the treatment of malaria infections
CA2224115A1 (en) 1995-06-07 1996-12-19 Washington University Multidentate metal complexes and methods of making and using thereof
CN1092048C (zh) 1998-06-02 2002-10-09 广州市健桥医药科技发展有限公司 复方哌喹片
CN1135974C (zh) 2000-08-23 2004-01-28 重庆健桥医药开发有限公司 抗疟药新药复方双氢青蒿素
CN1668293A (zh) * 2002-06-06 2005-09-14 华盛顿大学 使用青蒿素样化合物预防或延缓癌症显现的方法
US7670631B2 (en) * 2003-03-12 2010-03-02 ALFAMA—Investigação e Desenvolvimento de Produtos Farmacêuticos, Lda. Method for the prevention of malaria infection of humans by hepatocyte growth factor antagonists

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102485226A (zh) * 2010-12-03 2012-06-06 昆明制药集团股份有限公司 一种复方青蒿素类哌喹微丸及其制备方法
CN102485226B (zh) * 2010-12-03 2013-06-05 昆明制药集团股份有限公司 一种复方青蒿素类哌喹微丸及其制备方法
CN111249275A (zh) * 2020-03-03 2020-06-09 云南省寄生虫病防治所 一种治疗间日疟的药物的配伍方案及其使用方法
CN111514299A (zh) * 2020-04-29 2020-08-11 广州中医药大学科技产业园有限公司 一种用于防治肺炎的组合物及其在制备用于防治肺炎的药物中的应用

Also Published As

Publication number Publication date
EP1702616A1 (en) 2006-09-20
CN1255106C (zh) 2006-05-10
WO2005030197A1 (fr) 2005-04-07
BRPI0414296A (pt) 2006-11-07
US20060281785A1 (en) 2006-12-14
AP2006003588A0 (en) 2006-04-30
AP2485A (en) 2012-10-03
EP1702616A4 (en) 2008-04-30
US7851512B2 (en) 2010-12-14
ZA200602422B (en) 2007-11-28

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