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CN1116036C一种治疗酒渣鼻及光敏性疾病的含双氢青蒿素的药物组合物---含有双氢青蒿素药物组合物是治疗红斑狼疮和光敏性疾病的有效药物|CN1116036C A pharmaceutical composition containing dihydroartemisinin for treating rosacea and photosensitive diseases---The pharmaceutical composition containing dihydroartemisinin is


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CN1116036C一种治疗酒渣鼻及光敏性疾病的含双氢青蒿素的药物组合物---含有双氢青蒿素药物组合物是治疗红斑狼疮和光敏性疾病的有效药物

CN1116036C A pharmaceutical composition containing dihydroartemisinin for treating rosacea and photosensitive diseases---The pharmaceutical composition containing dihydroartemisinin is an effective treatment for lupus erythematosus and photosensitive diseases.

 

治疗红斑狼疮和光敏性疾病的含双氢青蒿素的药物组合物

本发明涉及含有双氢青蒿素的药物组合物,经药效学、毒理学及临床研究,表明本发明的药物组合物是治疗红斑狼疮和光敏性疾病的有效药物,该药物组合物可以制成各种常用的剂型用于临床,具有高效、安全、无毒副作用的特点。
 
治疗红斑狼疮和光敏性疾病的含双氢青蒿素的药物组合物
本发明涉及一种用于治疗红斑狼疮和光敏性疾病的药物,特别是用于治疗红斑狼疮和光敏性疾病的含有双氢青蒿素的药物组合物。
红斑狼疮和多形性日光疹等均为光敏性疾病,而红斑狼疮又属免疫性疾病,严重危害人体健康,特别是系统性红斑狼疮往往侵犯结缔组织、血管、内脏、皮肤等多种器官并伴有免疫学异常的全身性疾病。现代医学认为自身免疫性疾病是由机体免疫功能紊乱,导致B细胞功能亢进而产生大量自体抗体,引起免疫复合物在组织,特别是肾小球内基底膜内沉着(狼疮性肾常是致死的原因)导致III型变态反应。
近年来红斑狼疮发病率有不断上升的趋势,据美国Siegel和Fessel对纽约和旧金山人群调查,患病率分别为13.4/10万和50.8/10万。国内上海纺织系统人群调查患病率为70.4/10万(女性则为113.3/10万)故有关本病的流行病学及治疗学研究已日益受到国内外重视。对于该病的治疗,西医多用大剂量皮质类固醇激素以及免疫抑制剂治疗,对部分患者可控制病情,但长期用药则引起严重的毒副作用和并发症,甚至成为本病致死的主要原因。中医采用辨证施治的方针,近年来开发了一些治疗系统性红斑狼疮的药物。例如中国专利申请91103109公开了一种治疗系统性红斑狼疮的药物组合物,其中含有34种中药;中国专利申请94103378公开了一种治疗系统性红斑狼疮的药物组合物,其中含有十多种中药。上述这些中药组合物一般都是处方药,使用时一般都需医生根据患者的实际情况对药物组合物的成分进行取舍。尽管也有中成药,但因为其成分多,制备复杂,因此在实际使用过程中还不是非常方便。双氢青蒿素是青蒿素的还原化合物,其结构式如下:...
 
 
我国自七十年代开始,对青蒿素进行了广泛深入的研究,开发出了青蒿素及其衍生物是一类有效的抗疟药物组合物。近年来,随着对青蒿素及其衍生物研究的深入,不断发现了其在新领域中的应用。
本发明的目的是提供一种高效、安全且无毒副作用的治疗红斑狼疮和光敏性疾病的药物组合物。
本发明是基于这样的事实而完成的:本发明人以其发明的双氢青蒿素致力于抗疟研究,结果证明双氢青蒿素在高效、低毒、制备方便等方面均优于其它青蒿素类衍生物,同时又在免疫研究领域取得新发现,即在发现双氢青蒿素具有显著免疫抑制并对细胞免疫及体液免疫具有双向调节作用的基础上,经药效学和临床研究证明双氢青蒿素对红斑狼疮和光敏性疾病具有肯定的疗效,且无明显的毒副作用。
本发明提供了一种用于治疗红斑狼疮和光敏性疾病的含有双氢青蒿素的药物组合物,该组合物含有治疗有效剂量的双氢青蒿素。
本发明的目的是提供一种用于治疗红斑狼疮和光敏性疾病的含有双氢青蒿素的药物组合物,该组合物含有双氢青蒿素1-10重量%。
本发明的药物组合物适用于所有红斑狼疮(系统性红斑狼疮和盘状红斑狼疮)和光敏性疾病(多形性日光疹等)。
本发明的药物组合物可以是任何常用的药剂形式,可以为固体制剂,例如片剂、胶囊、栓剂、粉剂、颗粒剂、透皮软膏、霜剂等,也可以为液体制剂,例如口服液、喷雾剂、注射液等。本发明的药物组合物的制备方式是本领域的普通技术人员所公知的。
按照本发明的药物组合物,优选是将其制成片剂或胶囊,每一片片剂或每一粒胶囊含有20-80mg的双氢青蒿素。
本发明的药物组合物一般为口服给药,也可以经其他途径给药,例如治疗光敏性皮肤病可以使用外用制剂。用量一般为1-5mg/kg体重/天。
本发明的药物组合物可以单独使用。在治疗症状较重的系统性红斑狼疮时,也可以与现有的治疗红斑狼疮和光敏性疾病的其他药物,例如常用的激素类药物组合使用。
本发明使用的双氢青蒿素的制备方法是已知的。有关其制备方法已经见诸于文献报道。
以下通过实验例对本发明进行更进一步的说明。但应该理解的是,本发明的实验例只是用于说明而不是限制本发明。药效学实验...
 
 
 

Medicinal composition containing dihydroartemisine for treating rosacea and photosensitive diseases

The present invention relates to a medical composition containing dihydroartemisinin. Pharmacodynamical, toxicological and clinical research indicates that the medical composition of the present invention is effective medicine for treating lupus erythematosus and photosensitive diseases. The medical composition can be made into various common preparations for clinical application, and has the characteristics of high efficiency, safety and no toxic effect and side effect.
 
The pharmaceutical composition that contains dihydroarteannuin of treatment lupus erythematosus and photosensitive diseases
The present invention relates to a kind of medicine that is used for the treatment of lupus erythematosus and photosensitive diseases, especially for the pharmaceutical composition that contains dihydroarteannuin of treatment lupus erythematosus and photosensitive diseases.
Lupus erythematosus and polymorphous light eruption etc. are photosensitive diseases, and lupus erythematosus belongs to immune disease, serious harm health, particularly systemic lupus erythematosus (sle) are often invaded multiple organs such as connective tissue, blood vessel, internal organs, skin and with the systemic disease of crucial immunological abnormality.Modern medicine thinks that autoimmune disease is by the body's immunity disorder, cause the B cell function hyperfunction and produce a large amount of autoantibody, cause that immune complex calm (the lupus kidney often is lethal reason) in basement membrane in the tissue, particularly glomerule causes the III allergic reaction type.
The lupus erythematosus sickness rate has the trend of continuous rising in recent years, and to New York and San Francisco census of population, prevalence is respectively 13.4/10 ten thousand and 50.8/10 ten thousand according to U.S. Siegel and Fessel.Domestic Shanghai textile department census of population prevalence is that 70.4/10 ten thousand (women then is 113.3/10 ten thousand) are so the epidemiology of relevant primary disease and therapeutics research are subjected to domestic and international attention day by day.For the treatment of this disease, doctor trained in Western medicine is used heavy dose of corticosteroid hormone and immunosuppressant treatment more, and to the part patient may command state of an illness, but long-term prescription then causes serious toxic and side effects and complication, even becomes the lethal main cause of primary disease.The traditional Chinese medical science adopts the policy of determination of treatment based on pathogenesis obtained through differentiation of symptoms and signs, has developed the medicine of some therapy system lupus erythematosus in recent years.For example Chinese patent application 91103109 discloses a kind of pharmaceutical composition of therapy system lupus erythematosus, wherein contains 34 kinds of Chinese medicines; Chinese patent application 94103378 discloses a kind of pharmaceutical composition of therapy system lupus erythematosus, wherein contains ten plurality of Chinese.Above-mentioned these Chinese medicine compositions all are prescription drugss generally, generally all need the doctor according to patient's practical situation the composition of pharmaceutical composition to be accepted or rejected during use.Although Chinese patent medicine is also arranged, because its composition is many, preparation is complicated, also is not very convenient in actual use therefore.Dihydroarteannuin is the reducing compound of arteannuin, and its structural formula is as follows:...
 
China begins from the seventies, and arteannuin has been carried out research extensively and profoundly, and having developed arteannuin and derivant thereof is the effective antimalarial agent compositions of a class.In recent years, along with to the going deep into of arteannuin and derivant research thereof, constantly found its application in frontier.
The purpose of this invention is to provide a kind of efficient, safety and the treatment lupus erythematosus that has no side effect and the pharmaceutical composition of photosensitive diseases.
The present invention is based on such fact and finishes: the inventor is devoted to malaria research with the dihydroarteannuin of its invention, the result proves that dihydroarteannuin is efficiently, low toxicity, aspect such as easy to prepare all is better than other artemisinin derivatives, simultaneously obtain new discovery in the immune Research field again, promptly finding that dihydroarteannuin has remarkable immunosuppressant and pair cell immunity and humoral immunization and has on the basis of dual regulation, through pharmacodynamics and clinical research proof dihydroarteannuin lupus erythematosus and photosensitive diseases are had sure curative effect, and do not have obvious toxic and side effects.
The invention provides a kind of pharmaceutical composition that contains dihydroarteannuin that is used for the treatment of lupus erythematosus and photosensitive diseases, said composition contains the dihydroarteannuin for the treatment of effective dose.
The purpose of this invention is to provide a kind of pharmaceutical composition that contains dihydroarteannuin that is used for the treatment of lupus erythematosus and photosensitive diseases, said composition contains dihydroarteannuin 1-10 weight %.
Pharmaceutical composition of the present invention is applicable to all lupus erythematosus (systemic lupus erythematosus (sle) and discoid lupus erythematosus) and photosensitive diseases (polymorphous light eruption etc.).
Pharmaceutical composition of the present invention can be any medicine type commonly used, can be solid preparation, and for example tablet, capsule, suppository, powder, granule, transdermal ointment, cream etc. also can be liquid preparation, for example oral liquid, spray, injection etc.Preparation of drug combination mode of the present invention is that those of ordinary skill in the art is known.
According to pharmaceutical composition of the present invention, preferably be made into tablet or capsule, each sheet tablet or each capsules contain the dihydroarteannuin of 20-80mg.
Pharmaceutical composition of the present invention is generally oral administration, also can for example treat light sensitive dermatoses and can use external preparation through other administrations.Consumption is generally the 1-5mg/kg body weight/day.
Pharmaceutical composition of the present invention can use separately.When the heavier systemic lupus erythematosus (sle) of treatment symptom, also can with the other drug of existing treatment lupus erythematosus and photosensitive diseases, for example Chang Yong hormone medicine is used in combination.
The preparation method of the dihydroarteannuin that the present invention uses is known.Relevant its preparation method is seen in bibliographical information.
Below example further illustrates the present invention by experiment.But it should be understood that experimental example of the present invention just is used for explanation rather than restriction the present invention.Pharmacodynamic experiment...
 
 

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