WO2001076613A1 - Extract for abstaining from narcotics and its preparation - Google Patents

Extract for abstaining from narcotics and its preparation Download PDF

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WO2001076613A1
WO2001076613A1 PCT/CN2000/000086 CN0000086W WO0176613A1 WO 2001076613 A1 WO2001076613 A1 WO 2001076613A1 CN 0000086 W CN0000086 W CN 0000086W WO 0176613 A1 WO0176613 A1 WO 0176613A1
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component
extract
parts
detoxification
substances selected
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Zhizhong Zuo
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Zhizhong Zuo
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Priority to PCT/CN2000/000086 priority Critical patent/WO2001076613A1/en
Priority to AU2000236545A priority patent/AU2000236545A1/en
Publication of WO2001076613A1 publication Critical patent/WO2001076613A1/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K35/58Reptiles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/12Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/12Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
    • A61K35/48Reproductive organs
    • A61K35/50Placenta; Placental stem cells; Amniotic fluid; Amnion; Amniotic stem cells
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines

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  • the present invention relates to an extract for sedation, analgesia and / or detoxification and a method for preparing the same.
  • Another object of the present invention is to provide a pharmaceutical composition for use as a sedative, analgesic and / or detoxification drug.
  • component F 9-15 parts of component F, bezoar; (7) 12-15 parts of component G, which is one or more substances selected from hemp kernels and cypress seeds;
  • the composition optionally includes one or more of the following components to enhance the detoxification effect, enhance the patient's ability to resist disease in various organ systems, improve its physiological level, and reduce the drug's toxic side effect.
  • these optional components include:
  • the concentrated liquid is treated at about -50 ° C and a pressure of 0.1 OlKpa, and a dry powder containing about 3% water can be obtained. After 30 minutes of UV disinfection, the capsules were filled.
  • the filtrate can also be concentrated into a paste, diluted with an appropriate amount of water, refrigerated for 24 hours, filtered, and added with a single syrup, potassium citrate, volatile oil, and an appropriate amount of water to 1000 ml, refrigerated, filtered, and sealed in 10 ml It is obtained by sterilizing in an ampoule for 30 minutes at 100 ° C.
  • Inhibition of d 2 receptor activity in the brain can significantly alleviate and eliminate the symptoms of opiates (morphine, heroin, durodin) and drug addicts such as cocaine, marijuana and methamphetamine.
  • opiates morphine, heroin, durodin
  • drug addicts such as cocaine, marijuana and methamphetamine.
  • Patients can continue to take drugs at the same time (including the treatment group and the control group) using the detoxification drugs.
  • the drugs used can be used to reduce the amount of drug use. Medication will gradually reduce the amount of drug use until withdrawal, the course of treatment is about 2-3 months. Observation method
  • Efficacy standards refer to the Himme sbach withdrawal symptoms scoring system.
  • Treatment group (130 87 32 11 0 67. 2 100 patients)
  • Control group (42 16 11 12 38. 5 92. 1 cases)
  • the extracts of the present invention are prepared according to the amounts of various raw material ingredients listed in Table 5 (in the table in grams) according to the method described below, and the specific content of the preparation method is as follows:
  • the required amount of the raw materials was pulverized into a slurry-like fine powder by a liquefaction spiral method, and the average particle diameter of the fine powder was 50 nm.
  • the crushing equipment used is DRS-2 (produced by Jiangsu Superfine Powder Engineering Technology Research Center). Water was added to the fine powder and extracted at 100 ° C. The volume ratio of water to fine powder was 10: 1. The obtained extract was filtered to obtain a filtrate. The obtained residue was subjected to water extraction again, and then filtered. The first water extraction took 2 hours and the second water extraction took 1.5 hours. The volume ratio of water to fine powder during the second water extraction was 7: 1. The two filtrates were combined and concentrated. After cooling, 70% ethanol was added to the concentrated solution.
  • the method for preparing the extract of the present invention in this embodiment is the same as that in Examples 1 to 4, but the composition of the composition used for extraction is 45 g of purple river car, 25 g of ginseng, 9 g of cinnamon, 45 g of celandine, 15 g of Yanhusuo (yuanhu) , Qingfengteng 15g, bezoar 10g, hemp kernel 15g, Xiaoyao bamboo 15g, dried ginger 9g, salvia 20g, jujube kernel 20g, toad 9g, acacia peel 15g, astragalus 25g, ginkgo leaf 15g, stone calamus 12g, water flakes 2g, windproof 9g, and licorice 6g.

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Abstract

An extract is disclosed, the extract can be extracted from the following components: component A is Hominis Placenta. Flower of Datura metel L, toxin of Fugu ocellatus and/or toxin of Naja naja: component B is Root of Panax ginseng, Ginseng Radix Ferum, Ginseng Radix Coreensis and/or Panacis Quinquefolii Radix; component C is Root of Aconitum carmicharli Debx. and/or Skin of Cinnamomum cassia Presl; component D is Herb of Chelidonium majus L; component E is Stem of Corydalis turtschaninovii Bess. f. yuanhusuo Y.H. Chou et c.c. Hsu(yuan hu); component F is Gallstones of Bos taurus domesticus Gmelin and/or Trunk of Dryobalanops aromatica Gaertn. f.; component G is Fruit of Cannabis sativa L. and/or Fruit of Biota orientalis (L) Endl.; component H is Stem of Aipinia officinarum Hance and/or Stem of Zingiber officinale Rosc.; component I is Root of Salvia miltiorrhiza >Bge.; component J is Ziziphus jujuba Mill. and/or Fruit of Ziziphus jujuba Mill. var.inermis(Bge.) Rehd.; component K is Root of Glycyrrhiza uralensis Fish. and/or Honey-Fried Root of Glycyrrhiza uralensis Fish.. The inventive extract has effects including helping narcotic addicts to abstain physiological dependency and psychological dependency, and possesses very low retaking rate, moreover, it can be used to keep calm and ease pain. The invention also provides the preparation of the extract.

Description

说 明 书 戒毒提取物及其制备方法 背景技术  Description Detoxification extract and preparation method thereof
本发明涉及一种用于镇静、 镇痛和 /或戒毒的提取物及其制备方 法。  The present invention relates to an extract for sedation, analgesia and / or detoxification and a method for preparing the same.
目前, 用于戒毒的药物有替代类、 解毒类两大系列。 替代类是用 毒瘾较小的毒品取代毒瘾较大的毒品, 以此来减轻毒品对吸毒者神经 系统的作用, 如使用最普遍的药物 "美沙酮", 其次有 "盐酸二氢埃 托菲"、 "丁丙诺菲"、 "杜冷丁"、 "福康片" 等。 缺点是如长期使用这 些药物容易形成新的药物依赖; 解毒类主要是利用药物的拮抗作用, 即用一种物质阻抑另一种物质对人体的作用。 来减轻毒品的戒断反 应。 此类药物治疗中, 常常使用的拮抗类药物有环唑星、 纳络酮、 可 乐宁和纳屈酮等, 帮助释放吸毒者因长期吸毒而在体内蓄积的毒素。 这类药物只能降低戒断反应, 不能完全消除戒断反应。 尽管不会形成 新的药物依赖, 但是, 这类药物在最初使用时, 会产生厌恶、 出汗、 不安和焦虑。 可乐宁这类的药, 效力短, 长期使用后突然停药, 会产 生轻微的非阿片样戒断症状。 另外, 拮抗类药物只对鸦片类毒品有拮 抗作用, 如果把它作用于可卡因成瘾者身上则会产生严重的身体机能 损害。  At present, there are two major series of drugs for detoxification: detoxification and detoxification. The alternative is to replace drugs with less addiction with drugs with less addiction in order to reduce the effects of drugs on the nervous system of drug users. For example, the most common drug is methadone, followed by "dihydroetofine hydrochloride "," Dubinofil "," Du Lunding "," Fukang tablets ", etc. The disadvantage is that if these drugs are used for a long time, it is easy to form new drug dependence. Detoxification mainly uses the antagonistic effect of drugs, that is, using one substance to inhibit the effect of another substance on the human body. To reduce drug withdrawal. In this kind of drug treatment, antagonisms often used are cyclazine, naloxone, clonine, and naldrone, which help release toxins accumulated in the body by drug users due to long-term drug use. These drugs can only reduce the withdrawal response and cannot completely eliminate it. Although they do not create new drug dependence, they can cause aversion, sweating, restlessness, and anxiety when initially used. Drugs such as clonidine are short-acting, and abrupt discontinuation after long-term use can produce mild non-opioid withdrawal symptoms. In addition, antagonists only have opioid antagonism, and if they are applied to cocaine addicts, they will cause severe physical impairment.
上述两大类药物仅限于降低戒断毒品引起的生理反应, 而不能解 决吸毒者的毒品饥饿感, 即上述两大类戒毒药物只限于解除吸毒者的 生理依赖, 不能解除吸毒者的心理依赖。 由于吸毒者对毒品的心理渴 求往往超过戒断毒品给他们生理上带来的痛苦, 因而吸毒者的复吸率 极高, 通常在 90 %以上。 发明目的 The above two types of drugs are limited to reducing the physiological response caused by drug withdrawal, but cannot solve the drug hunger of drug users, that is, the above two types of drug treatment are only limited to relieve the physical dependence of drug users and cannot relieve the psychological dependence of drug users. Because drug users' psychological thirst for drugs often exceeds the physical pain caused by quitting drugs, the relapse rate of drug users is extremely high, usually above 90%. Object of the invention
本发明是针对上述替代类、 解毒类等戒毒药物存在的缺点, 提供 一种用于镇静、 镇痛和 /或戒毒的提取物。 该提取物既能戒断吸毒者 的生理依赖, 又能戒断吸毒者的心理依赖, 是一种具有极低复吸率的 戒毒提取物, 同时该提取物还可用于镇静或镇痛。 本发明还提供了这 种提取物的制备方法。  The present invention aims at the shortcomings of the above-mentioned detoxification drugs such as alternatives and detoxification, and provides an extract for sedation, analgesia and / or detoxification. The extract can quit both the physical dependence and the psychological dependence of drug addicts. It is a detoxification extract with a very low relapse rate. At the same time, the extract can also be used for sedation or analgesia. The invention also provides a method for preparing such an extract.
本发明的另一个目的是提供一种药物组合物, 用作镇静剂、 镇痛 剂和 /或戒毒药物。  Another object of the present invention is to provide a pharmaceutical composition for use as a sedative, analgesic and / or detoxification drug.
本发明的又一个目的是提供一种治疗方法, 用于镇痛、 镇静和 / 或治疗吸毒患者对毒品的生理依赖和 ' 、理依赖。  Yet another object of the present invention is to provide a treatment method for analgesia, sedation and / or treatment of drug dependence on physical and psychological dependence of drug users.
本发明的其它目的 体现在对本发明的详细描述之中。 发明详述  Other objects of the present invention are embodied in the detailed description of the present invention. Detailed description of the invention
本发明人在长期的研究中, 发现了一种提取物。 该提取物不仅可 以镇痛、 镇静, 还可以有效地戒除吸毒者的毒瘾。  The inventors have found an extract in long-term research. The extract can not only relieve pain and sedation, but also effectively quit drug addiction.
根据本发明, 一种提取物, 从一种组合物中提取, 该组合物包括 下列组分, 以重量份计:  According to the present invention, an extract is extracted from a composition including the following components in parts by weight:
( 1 ) 45 - 60份的组分 A, 为一种或多种选自紫河车、 洋金花、 河豚毒和眼镜蛇毒的物质;  (1) 45 to 60 parts of component A, which is one or more substances selected from the group consisting of purple river car, daffodil, puffer venom and cobra venom;
(2) 15 - 30 份的组分 B, 为一种或多种选自人参、 野山参、 高丽参和西洋参的物质;  (2) 15-30 parts of component B, which is one or more substances selected from ginseng, wild ginseng, Korean ginseng and American ginseng;
( 3) 6 - 9份的组分 C, 为一种或多种选自附子和肉桂的物质; (4 ) 30 - 60份的组分 D, 为白屈菜;  (3) 6 to 9 parts of component C is one or more substances selected from aconite and cinnamon; (4) 30 to 60 parts of component D is celandine;
( 5 ) 9- 15的组分 E, 为延胡索 (元胡);  (5) Component E of 9-15 is Yanhusuo (Yuanhu);
( 6 ) 9- 15份的组分 F, 为牛黄; ( 7 ) 12 - 15 份的组分 G, 为一种或多种选自火麻仁和柏子仁 的物质; (6) 9-15 parts of component F, bezoar; (7) 12-15 parts of component G, which is one or more substances selected from hemp kernels and cypress seeds;
( 8 ) 6 - 12份的组分 H, 为一种或多种选自高良姜和干姜的物 质;  (8) 6 to 12 parts of component H, which is one or more substances selected from galangal and dried ginger;
( 9 ) 15 - 25份的组分 I, 为丹参;  (9) 15-25 parts of component I is salvia miltiorrhiza;
( 10) 15 - 30份的组分 J , 为一种或多种选自酸枣仁和大枣的 物质;  (10) 15 to 30 parts of component J, which is one or more substances selected from the group consisting of jujube kernel and jujube;
( 11 ) 6 - 10份的组分 K, 为一种或多种选自生甘草和炙甘草 的物质。  (11) 6-10 parts of component K, which is one or more substances selected from raw licorice and licorice root.
根据本发明, 用于制备提取物的组合物中, 组分 F 的牛黄可以用 冰片来替代或与冰片共用, 冰片的用量为 0.5 - 3.0份。  According to the present invention, in the composition for preparing an extract, bezoar of component F can be replaced with or shared with borneol, and the amount of borneol is 0.5-3.0 parts.
除了上述组分以外, 该组合物还任选包括下列组分中的一种或多 种, 以增强戒毒效果、 增强患者全身机体各器官系统对疾病的抵抗能 力、 改善其生理水平、 降低药物的毒副作用。 具体地说, 以重量份计, 这些任选组分包括:  In addition to the above components, the composition optionally includes one or more of the following components to enhance the detoxification effect, enhance the patient's ability to resist disease in various organ systems, improve its physiological level, and reduce the drug's toxic side effect. Specifically, in terms of parts by weight, these optional components include:
12 - 18份的青风藤;  12-18 copies of blue wind rattan;
12 - 18份的黄芩;  12-18 servings of Scutellaria baicalensis;
12 - 25份的徐长卿;  12-25 copies of Xu Changqing;
9 - 12份的防风;  9-12 windbreaks;
15 - 30份的黄芪;  15-30 servings of astragalus;
9 - 12份的鬼箭羽;  9-12 ghost arrow feathers;
12 - 15份的合欢皮;  12-15 acacia skins;
12 - 15份的银杏叶;  12-15 servings of ginkgo leaves;
9 - 12份的夜交藤;  9-12 night vines;
12 - 15份的石菖蒲;  12-15 iris
6-9份的蟾蜍: 12 - 25份的逍遥竹。 6-9 servings of toad: 12-25 servings of Happy Bamboo.
根据本发明, 一种镇静、 镇痛和戒毒的方法, 包括对病人给用有 效量的本发明的提取物。  According to the invention, a method of sedation, analgesia and detoxification comprises administering to a patient an effective amount of an extract of the invention.
本发明提取物的给药方式可以是口服、 注射等等。 根据患者病情 的不同, 本发明提取物的服用剂量也是不同的。  The extract of the present invention may be administered orally, by injection, or the like. Depending on the condition of the patient, the dosage of the extract of the present invention is also different.
本发明提取物用于镇静时, 成人的口服剂量一般为每次 0. 3- 0.6g, 每日 2-3次; 注射剂量一般为每次 0.1-0.3g。 必要时可加大剂 量。  When the extract of the present invention is used for sedation, the oral dose for adults is generally 0.3-0.6g each time, 2-3 times a day; the injection dose is generally 0.1-0.3g each time. Increase the dose if necessary.
本发明提取物用于镇痛时, 成人的口服剂量一般为每次 0.6- 1.2g, 疼痛时服用; 注射剂量一般为每次 0.3-0.6g。 对于晚期癌症和 /或疼痛剧烈时患者可适当增加剂量。  When the extract of the present invention is used for analgesia, the oral dose for adults is generally 0.6-1.2g each time, and when the pain is taken, the injection dose is generally 0.3-0.6g each time. For patients with advanced cancer and / or severe pain, the dose may be appropriately increased.
本发明提取物用于戒毒时, 根据患者吸毒时间的长短、 吸毒方式、 吸毒种类等因素, 来决定服用的剂量。 一般来说, 口服给药时, 成人 为每次 1.5-9.0g, 每日二到四次; 注射给药时, 成人为每次 0.6-3.0g, 每日二到四次。 由于影响服用剂量的因素较多, 可以 居患者的病情, 在这些剂量范围的基础上, 适当增大服用剂量。 具体服用剂量举例如 下:  When the extract of the present invention is used for detoxification, the dosage to be taken is determined according to factors such as the length of the patient's drug use time, the method of drug use, the type of drug use and other factors. Generally speaking, when administered orally, adults take 1.5-9.0g each time, two to four times a day; when injected, adults take 0.6-3.0g each time, two to four times a day. Because there are many factors that affect the dosage, the patient's condition can be maintained. Based on these dosage ranges, the dosage should be appropriately increased. Specific dosages are as follows:
表 1  Table 1
吸毒时 吸毒方式 吸毒量 吸毒种类 口服药量 注射药量 间  At the time of drug use Mode of drug use Amount of drug A type of drug Oral dose Injectable dose
<3 个月 抽吸 <0.5g 单一海洛 1.5-2.4g 0.6-1.2g 因  <3 months suction <0.5g single heroin 1.5-2.4g 0.6-1.2g
<3 个月 用锡.箔抽吸 <0.5g 单一海洛 1.5-2.4g 0.6-1.2g 因 <3 个月 注射 <0. 5g 单一海洛 3. 6-4.8g 1.2-1. 8g 因 <3 months with tin. Foil suction <0.5g Single heroin 1.5-2.4g 0.6-1.2g <3 months injection <0.5g single heroin 3.6-4.8g 1.2-1. 8g
〉3 个月 非注射方式 <0. 5g 单一海洛 3.6—4.8g 1.2-1.8g 因  〉 3 months non-injection method <0.5g single heroin 3.6-4.8g 1.2-1.8g
>3 个月 注射 <0. 5g 单一海洛 3.6-4.8g 1.2- 1. 8g 因  > 3 months injection <0.5g single heroin 3.6-4.8g 1.2- 1.8g
>3 个月 非注射方式 >0. 5g 单一海洛 4. 5-6. Og 1.5-2.4g 因  > 3 months non-injection> 0.5g single heroin 4. 5-6. Og 1.5-2.4g
>3 个月 注射 >0. 5g 单一海洛 5. 0-9. Og 2. 0-3. Og 因 根据本发明的药物组合物, 包含有效量的本发明的提取物和可药 用的载体和 /或赋形剂。 所用的载体和 /或赋形剂, 为常用的载体和 / 或赋形剂, 如淀粉, 明胶等等。  > 3 months injection> 0.5g single heroin 5. 0-9. Og 2. 0-3. Og because the pharmaceutical composition according to the present invention contains an effective amount of the extract of the present invention and a pharmaceutically acceptable carrier And / or excipients. The carriers and / or excipients used are commonly used carriers and / or excipients, such as starch, gelatin and the like.
本发明的药物组合物可以做成各种剂型, 例如, 片剂、 胃溶、 肠 溶糖衣片剂, 可以制成粉剂, 制成颗粒或灌装成胶嚢如胃溶胶囊、 肠 溶胶嚢, 也可以将上述粉剂浸泡在 0.5-2%盐水中, 制成口服液, 也可 以制成针剂等等。  The pharmaceutical composition of the present invention can be made into various dosage forms, for example, tablets, stomach-soluble, enteric sugar-coated tablets, can be made into powder, granulated or filled into capsules such as stomach-soluble capsules, enteric-coated tablets, The powder can also be soaked in 0.5-2% saline to make an oral solution, and it can also be made into an injection.
本发明还提供了一种制备本发明提取物的方法, 该制备方法包括 下列步骤:  The present invention also provides a method for preparing the extract of the present invention, and the preparation method includes the following steps:
( 1 ) 粉碎原材料。 制备本发明提取物的原材料均可从市场上购 取。 原材料的粉碎可以采取多种常规方法, 例如研磨法、 液化螺旋法 等等, 优选采用液化螺旋法。 原材料粉碎后的颗粒为纳米级, 颗粒大 小通常在 10 - 300 纳米之间, 优选为 10 - 50 纳米。 4巴原材料 4分碎成 纳米级的细粉, 可以增大颗粒的表面能, 有利于提高提取率。 采用液 化螺旋法, 可以通过高频冲击使颗粒内部和表面出现大量晶格扭曲, 缺陷, 提高非晶化程度。 (2 )将粉碎后的原材料用适量的水进行提取。 水提取时, 加入的水量可以为原料量体积的 8 - 12倍以上, 优选为 10: 1。 温度控制在 90 - 100 °C之间, 水提取的时间一般为 90 - 10 (TC条件 下, 持续 1-2.5小时, 优选 1.5-2小时。 (1) Crush the raw materials. The raw materials for preparing the extract of the present invention can be purchased from the market. The pulverization of the raw materials may adopt various conventional methods, such as a grinding method, a liquefaction spiral method, and the like, and a liquefaction spiral method is preferably adopted. The crushed particles of the raw materials are nano-sized, and the particle size is usually between 10 and 300 nanometers, preferably between 10 and 50 nanometers. The 4 bar raw material is broken into 4 nanometer fine powders, which can increase the surface energy of the particles and help improve the extraction rate. Using the liquefaction spiral method, a large amount of lattice distortion can occur inside and on the surface of the particles through high-frequency impact. Defects, increasing the degree of amorphization. (2) The crushed raw materials are extracted with an appropriate amount of water. During water extraction, the amount of water added can be 8 to 12 times the volume of the raw material, preferably 10: 1. The temperature is controlled between 90-100 ° C, and the time for water extraction is generally 90-10 (under TC conditions, lasting 1-2.5 hours, preferably 1.5-2 hours.
( 3 ) 将水提取液过滤, 得到滤液, 并将滤液浓缩。 得到的滤渣 可以再次进行水提取。 再次进行水提取时的加水量为原料量体积的 5 - 8倍。 水提取步骤可以进行多次, 优选进行 2次。  (3) The water extract is filtered to obtain a filtrate, and the filtrate is concentrated. The obtained filter residue can be subjected to water extraction again. When water extraction is performed again, the amount of water added is 5-8 times the volume of the raw material. The water extraction step can be performed multiple times, preferably twice.
( 4 ) 向浓缩液中加入 70%的乙醇, 置 80 - 85°C的水浴中进行回 流。 乙醇的加入量与浓缩液的体积比例范围为 1.5-2.5: 1,优选 1.5: 1。 时间一般为 20 - 60分钟, 优选 30 - 45分钟。 回流后, 将浓缩液静置, 静置的时间一般为 2-3小时。  (4) Add 70% ethanol to the concentrate and place it in a water bath at 80-85 ° C for reflux. The ratio of the amount of ethanol added to the volume of the concentrate is 1.5-2.5: 1, preferably 1.5: 1. The time is generally 20-60 minutes, preferably 30-45 minutes. After refluxing, the concentrated solution is allowed to stand for a period of 2-3 hours.
( 5 ) 静置后的处理液进行过滤, 得到滤液, 然后将滤液浓缩。 可以根据需要, 对该浓缩液作进一步的处理。 例如对浓缩物进行 干燥, 得到粉末。 干燥采用常规的干燥方法, 例如, 喷雾干燥、 真空 冷冻干燥等等。 根据本发明的方法, 过滤可以采用常规的过滤方法, 例如离心过滤法等等。 浓缩可采用常规的真空膜蒸发器, 离心薄膜浓 缩。  (5) The treatment solution after standing is filtered to obtain a filtrate, and then the filtrate is concentrated. The concentrated solution can be further processed as required. For example, the concentrate is dried to obtain a powder. For drying, conventional drying methods are used, for example, spray drying, vacuum freeze drying, and the like. According to the method of the present invention, the filtration can adopt a conventional filtration method, such as a centrifugal filtration method and the like. Concentration can be condensed using a conventional vacuum film evaporator and centrifugal thin film.
用于制备本发明提取物的某些原材料如肉桂、 干姜中含有一些易 挥发性油如桂皮油、 姜酚。 当本发明提取物长期存放时, 这些挥发性 油会逐渐挥发, 影响本发明提取物的药效。 为了增加本发明提取物的 保存期, 可以在粉碎原材料步骤前, 对肉桂、 干姜等原材料进行预处 理, 用于稳定原材料中所含的易挥发性油。  Certain raw materials such as cinnamon and dried ginger used to prepare the extract of the present invention contain some volatile oils such as cinnamon oil and gingerol. When the extract of the present invention is stored for a long period of time, these volatile oils will gradually volatilize, affecting the medicinal effect of the extract of the present invention. In order to increase the shelf life of the extract of the present invention, the raw materials such as cinnamon and dried ginger may be pre-treated before the raw material pulverization step to stabilize the volatile oil contained in the raw materials.
在预处理步骤中, 用常规蒸馏蒸镏方法肉桂、 千姜等原材料, 温 度控制在 90- 120°C范围, 蒸馏时间在 10- 30分钟范围。 蒸馏后的原材 料送去粉碎步骤, 蒸馏出的挥发性油用 β -环糊精稳定后, 与粉碎后 的细粉一起进行水提取。 浓缩液一般浓缩到滤液体积的 20 - 50% , 然后再干燥。 采用喷雾 干燥时, 干燥过程中, 液滴干燥的实际温度仅 35 - 50°C, 在几秒或十 几秒钟完成。 通常, 浓缩液的进风温度为 110 — 130°C, 出风温度为 65 - 80°C都能喷出流动性好的粉末。 将这种粉末加入到 0.9%盐水中, 即可制成口 良液。 In the pretreatment step, the raw materials such as cinnamon and ginger are distilled by the conventional distillation and steaming method, the temperature is controlled in the range of 90-120 ° C, and the distillation time is in the range of 10-30 minutes. The distilled raw material is sent to a pulverization step, and the volatile oil that has been distilled off is stabilized with β-cyclodextrin, and then subjected to water extraction together with the pulverized fine powder. The concentrate is usually concentrated to 20-50% of the filtrate volume, and then dried. When spray drying is used, the actual temperature of droplet drying during the drying process is only 35-50 ° C, which is completed in a few seconds or ten seconds. Generally, the concentrated liquid's inlet air temperature is 110-130 ° C, and the outlet air temperature is 65-80 ° C. Add this powder to 0.9% saline to make a good mouth liquid.
在真空冷冻干燥法中, 将浓缩液在约 - 50°C和压力为 0. OlKpa 下 处理, 即可获得含水约 3%的干燥粉末。 紫外线消毒灭菌 30分钟后, 灌装入胶嚢。  In a vacuum freeze-drying method, the concentrated liquid is treated at about -50 ° C and a pressure of 0.1 OlKpa, and a dry powder containing about 3% water can be obtained. After 30 minutes of UV disinfection, the capsules were filled.
也可以把滤液浓缩成浸膏状, 用适量水稀释, 冷藏 24 小时, 滤 过, 加入单糖浆、 枸椽酸钾、 挥发油, 再加适量水至 1000 毫升, 冷 藏、 滤过, 封装于 10毫升安瓿中, 于 100°C下灭菌 30分钟即得。  The filtrate can also be concentrated into a paste, diluted with an appropriate amount of water, refrigerated for 24 hours, filtered, and added with a single syrup, potassium citrate, volatile oil, and an appropriate amount of water to 1000 ml, refrigerated, filtered, and sealed in 10 ml It is obtained by sterilizing in an ampoule for 30 minutes at 100 ° C.
本发明的提取物可以用于镇静、 镇痛以及戒毒。 本发明的提取物 用作戒毒药物时, 与现有技术中的戒毒药物相比具有十分突出的优 点, 具体表现在:  The extract of the present invention can be used for sedation, analgesia and detoxification. When the extract of the present invention is used as a detoxification drug, it has very prominent advantages compared with the detoxification drugs in the prior art.
( 1 ) 具有改善全身微循环, 尤其是大脑区域微循环, 有效促进 大脑内源性吗啡肽产生, 由此达到主观对抗毒品的诱惑。  (1) It can improve the microcirculation of the whole body, especially the microcirculation in the brain area, and effectively promote the production of endogenous morphinin in the brain, thereby achieving the subjective fight against the temptation of drugs.
( 2 ) 抑制脑内 d2受体活性, 能明显緩解和消除鸦片类 (吗啡、 海洛因、 杜冷丁) 及可卡因、 大麻和冰毒等毒品成瘾者的症状。 (2) Inhibition of d 2 receptor activity in the brain can significantly alleviate and eliminate the symptoms of opiates (morphine, heroin, durodin) and drug addicts such as cocaine, marijuana and methamphetamine.
( 3 ) 调节大脑细胞内介质的平衡分布, 有助于调整因毒品产生 的植物神经功能紊乱, 即 "想瘾" 和 "返瘾" 后遗症。  (3) Adjusting the balance of the mediators in the brain cells helps to adjust the autonomic dysfunction caused by drugs, that is, the sequelae of "think addiction" and "relapse".
( 4 ) 益气温阳、 理气化痰、 透窍逐秽、 解毒止痛、 醒脑安神、 清心除烦、 醒脾开窍、 健脾益肾、 滋补强壮、 调整人体机能平衡。  (4) Yiyangyang, qi-eliminating phlegm, clearing the phlegm, detoxifying and analgesic, refreshing the brain and soothe the nerves, clearing the mind and annoying, refreshing the spleen and resuscitating, strengthening the spleen and kidney, nourishing and strengthening, and adjusting the balance of human function.
由于上述突出的优点, 本发明提取物的戒毒效果是十分明显的: Due to the above-mentioned outstanding advantages, the detoxification effect of the extract of the present invention is very obvious:
1.戒毒功效显著, 无毒副作用及不良反应, 应用面广 (可适用于 吗啡、 海洛因、 杜冷丁、 可卡因、 大麻及冰毒成瘾者〉. 1. Significant detoxification effect, no toxic side effects and adverse reactions, and a wide range of applications (applicable to morphine, heroin, durodin, cocaine, marijuana and ice addicts>.
2.起效快, 疗程短, 3 - 7 天可解除身体依赖, 即毒瘾, 7 - 20 天 可^"抗心理依赖, 即心瘾。 2. Fast onset, short treatment period, 3-7 days can relieve physical dependence, namely drug addiction, 7-20 days But ^ "anti-psychological dependence, that is, heart addiction.
3.不产生欣快感, 无成瘾性。  3. No euphoria, no addiction.
4.戒断率高, 复吸率低。 喜理试验  4. High withdrawal rate and low relapse rate. Heineken test
用本发明提取物进行的急性毒性试验的结果是, 小鼠半数致死剂 量 LD5。为 4. 86+0. 58g/kg。 As a result of the acute toxicity test performed with the extract of the present invention, the mouse has a lethal dose of LD 5 . It is 4. 86 + 0. 58g / kg.
用本发明提取物进行的长期毒理试验表明, 本发明的提取物无致 畸、 致癌、 致突变及脏腑功能损害现象。 本发明提取物疗效的动物试-险  The long-term toxicological test performed with the extract of the present invention shows that the extract of the present invention is free of teratogenic, carcinogenic, mutagenic and visceral function damage. Animal test-risk of curative effect of extract of the present invention
将 Wi s ter 纯种大鼠造成毒瘾抑制相关微循环模型, 断头取脑, 作脑干, 下丘脑, 纹状体三个脑区曱 -脑啡肽( MEK )和亮脑啡呔( LEK ) 放射免疫测定。 结果显示毒瘾大鼠三个脑区的 MEK和 LEK含量均低于 正常大鼠, 除脑干 MEK 外均呈显著差异。 服用本发明的戒毒提取物组 三个脑区的 MEK, LEK , 除脑干 MEK外, 其余均向正常体质大鼠的脑啡 肽值回升。 前。 本发明提取物的临床试验  A pure microcirculation model related to drug addiction suppression was established in Wister purebred rats. The brain was decapitated for brainstem, hypothalamus, and striatum. LEK) radioimmunoassay. The results showed that the MEK and LEK contents of the three brain regions of drug-addicted rats were lower than those of normal rats, with significant differences except for the brainstem MEK. The MEK and LEK in the three brain regions of the group taking the detoxification extract of the present invention, except for the brainstem MEK, all returned to the enkephalin value of normal constitution rats. before. Clinical trial of the extract of the invention
用本发明的提取物治疗海洛因戒毒综合症患者 432 例, 经与其它 药物对照组比较, 疗效满意。  432 patients with heroin detoxification syndrome were treated with the extract of the present invention, and the effect was satisfactory by comparison with other drug control groups.
本试验全部病例均符合 《国际疾病分类》( ICD — 10 ) 中关于使 用精神活性药物引致心理与行为障碍的分类与诊断指导及美国精神病 学会 《精神疾病诊断系统性手册》 (第二次修订本) (DSMI I I - R ) 中 对药物滥用和药物依赖性有关障碍的诊断标准。 All cases in this trial conform to the classification and diagnosis guidance for the use of psychoactive drugs in mental and behavioral disorders in the International Classification of Diseases (ICD-10) and the American College of Psychiatry's Systematic Manual for the Diagnosis of Mental Illness (the second revised edition) ) (DSMI II-R) Diagnostic criteria for substance abuse and drug dependence-related disorders.
治疗组 432例: 男 270例, 女 162例. 年龄 12 - 67 岁, 平均年 龄 23岁, 病程 1 月一 10年, 平均 36. 8 月, 其中 3月以内 38例, 3 - 6月 42例, 6月一 1年 54例, 1 - 5年 236例, 5年以上 62例; 单 纯用海洛因的 372 例; 先后用海洛因及大麻的 26 例; 海洛因、 埃托 菲、 杜冷丁三者共用 25 例; 海洛因、 摇头丸 9 例; 吸食者 132 例; 注射者 264 例; 吸食及注射共用者 36 例; 吸毒量 0. 5 克以下者 180 例; 0. 5 _ 1克者 192例; 1 克以上者 60例; 除 6例系初次治疗外, 其余均进行过强制法、 冬眠法、 美沙酮、 杨氏 1 + 1、 丁丙诺菲等戒毒 法, 1次者 31例, 2次者 64例, 3次者 43例, 4次者 57例, 5次及 5次以上者 231例。  Treatment group 432 cases: 270 males and 162 females. Aged 12 to 67 years, with an average age of 23 years, with a course of January to 10 years, with an average of 36.8 months, of which 38 cases were within March and 42 were from March to June. In June, there were 54 cases in 1 year, 236 cases in 1 to 5 years, and 62 cases in more than 5 years; 372 cases of heroin alone; 26 cases of heroin and marijuana; 25 cases of heroin, etofi, and dulentin 9 cases of heroin and ecstasy; 132 cases of smokers; 264 cases of injectors; 36 cases of inhalers and injectors; 180 cases of 0.5 g or less; 192 cases of 0.5 -1 g or more; 1 g or more There were 60 cases; except for 6 cases which were treated for the first time, all others had undergone detoxification methods such as compulsory method, hibernation method, methadone, Young's +1, buprenorphine, one case for 31 cases, and two cases for 64 cases. There were 43 cases with 3 times, 57 cases with 4 times, and 231 cases with 5 times or more.
对照组 175例, 男 105例, 女 70例, 年龄 15 - 39岁, 平均年龄 26岁, 病程 3月 — 7年, 平均 33. 6月。 其中 3 - 6月 13例, 6月一 1 年 47例, 1 - 5年 90例, 5年以上 25例; 单纯用海洛因的 95例; 先 后用海洛因及大麻的 32例; 海洛因, 埃托菲, 杜冷丁三者共用 41例; 海洛因, 摇头丸 7例: 吸食者 85例; 注射者 73例; 吸食注射共用者 17例; 吸毒量 0. 5克以下者 17例, 0. 5 - 1克者 93例, 1克以上者 65 例, 除 17 例系初次治疗外, 其余已进行过强制法、 冬眠法、 美沙酮、 杨氏 1 + 1等戒毒法, 1次者 39例, 2次者 18例, 3次者 29例, 4次 者 63例, 5次及 5次以上者 26例。  The control group consisted of 175 patients, 105 males and 70 females, aged 15-39 years, with an average age of 26 years, with a course of March to 7 years, with an average of 33. June. There were 13 cases from March to June, 47 cases from June to 1 year, 90 cases from 1 to 5 years, and 25 cases from more than 5 years; 95 cases were treated with heroin alone; 32 cases were treated with heroin and marijuana; heroin, Etofi 41 cases were shared by Du Leng Ding; 7 cases were heroin and Ecstasy: 85 cases were ingested; 73 cases were injected; 17 cases were shared by inhalation and injection; 17 cases were ingested under 0.5 g, 0.5-1 g were ingested 93 cases, 65 cases with 1 gram or more, except for 17 cases which were treated for the first time, the rest have undergone detoxification methods such as compulsory method, hibernation method, methadone, Young's 1 + 1, etc., 39 cases in one case, and 18 cases in 2 cases There were 29 cases with 3 times, 63 cases with 4 times, and 26 cases with 5 times or more.
按随机对照试验分三大组, 各组均包括治疗组和对照组。 A组按 2: 1随机分配治疗组 1 30例, 对照组 65例; B组按 2. 5 : 1 随机分配 治疗组 170例, 对照组 68组; C组按 2: 1随机分配治疗组 85例, 对 照组 42例; 另 47例未设对照组。  Randomized controlled trials are divided into three major groups, each of which includes a treatment group and a control group. A group of 30 patients were randomly assigned to the treatment group according to 2: 1, and 65 patients in the control group; 170 patients in the treatment group were randomly assigned to 2.5: 1, and 68 patients in the control group; C group was randomly assigned to 85 in the 2: 1 treatment group. There were 42 cases in the control group and 47 cases without a control group.
治疗方法 treatment method
( 1 ) 直接戒断法 表 2 (1) Direct withdrawal Table 2
Figure imgf000011_0001
Figure imgf000011_0001
服用本发明的提取物后 7 天, 辅助少量镇静催眠药。 病人服用本 发明的提取物后不再使用毒品和吗啡类麻醉药, 症状特别严重的病人 用非麻醉药对症处理。  Seven days after taking the extract of the present invention, a small amount of sedative hypnotics is assisted. After taking the extract of the present invention, patients no longer use drugs and morphine anesthetics, and patients with particularly severe symptoms are treated symptomatically with non-narcotic drugs.
表 3  table 3
Figure imgf000011_0002
Figure imgf000011_0002
( 2 ) 减量脱瘾法 (2) Reduced withdrawal method
病人使用戒毒药品同时 (含治疗组和对照组) 可继续吸毒, 所服 用药品以能减少吸毒量为度 (一般用本发明的提取物后病人会因吸毒 感到不适而自然减少吸毒量), 继续用药使病人逐渐减少吸毒量直到 脱瘾, 疗程 2 - 3个月左右。 观察方法  Patients can continue to take drugs at the same time (including the treatment group and the control group) using the detoxification drugs. The drugs used can be used to reduce the amount of drug use. Medication will gradually reduce the amount of drug use until withdrawal, the course of treatment is about 2-3 months. Observation method
各治疗组和对照组的患者均记录症状体征变化  Patients in each treatment group and control group recorded changes in symptoms and signs
疗效标准参照 H imme i sbach戒断症状记分体系。  Efficacy standards refer to the Himme sbach withdrawal symptoms scoring system.
-治愈: 病人停用一切药物后 3 个月以上不再出现戒断症状或肌注纳 络酮 0. 4 - 0. 8mg后不出现戒断症状 (身体症状消失, 心理依赖消失 )。 -显著: 病人停用一切药物后可在 3 个月以内出现戒断症状或肌注纳 络酮 0. 4 - 0. 8mg后出现部分身体症状, 大部分心理依赖。 -Cure: Withdrawal symptoms no longer occur or the intramuscular injection of naloxone 0.4 to 0.8 mg does not occur after the patient stops using all drugs (physical symptoms disappear, psychological dependence disappears). -Significant: Patients withdraw all symptoms within 3 months after withdrawal of all drugs or intramuscular injection of naloxone 0.4-0.8 mg, some physical symptoms, most psychological dependence.
-好转: 病人停用一切药物后可在 1 个月以内仍出现部分戒断症状或 肌注纳络酮 0. 4 - 0. 8mg后出现大部分身体症状及心理依赖。  -Improvement: The patient may still experience partial withdrawal symptoms or intramuscular injection of naloxone 0.4 to 0.8 mg after the withdrawal of all medications, and most of the physical symptoms and psychological dependence may occur.
-无效: 身体症状无改变, 病人仍依赖毒品, 并且肌注纳络酮后即出 现戒断症状者。  -Ineffective: No change in physical symptoms, patients still dependent on drugs, and withdrawal symptoms after intramuscular injection of naloxone.
试验结果列于下表 4中:  The test results are listed in Table 4 below:
表 4  Table 4
治愈 显著 好转 无效 治愈率 总有效率 Healing markedly improved ineffective cure rate total effective
(例) (例) (例) (例) ( % ) ( % )(Example) (example) (example) (example) (%) (%)
A组: Group A:
治疗组( 130 87 32 11 0 67. 2 100 例) Treatment group (130 87 32 11 0 67. 2 100 patients)
对照组 ( 65 23 23 14 5 35. 3 92 例) Control group (65 23 23 14 5 35. 3 92 patients)
B组  Group B
治疗组( 170 106 47 15 2 62. 6 98. 7 例) Treatment group (170 106 47 15 2 62. 6 98. 7 cases)
对照组 ( 68 29 18 19 3 42. 3 95. 2 例) Control group (68 29 18 19 3 42. 3 95. 2 cases)
C组  Group C
治疗组 ( 85 51 19 12 3 60. 4 96. 8 例) Treatment group (85 51 19 12 3 60. 4 96. 8 cases)
对照组 ( 42 16 11 12 38. 5 92. 1 例) Control group (42 16 11 12 38. 5 92. 1 cases)
ί 使用直接戒断法 387 例, 全部脱瘾, 治愈率 100 % , 随访 3 - 24 个月, 复吸率 1. 3 % 。 ί Direct abstinence was used in 387 patients, all of whom were completely free of addiction, with a cure rate of 100%, and a follow-up of 3 to 24 months. The relapse rate was 1.3%.
使用减量脱瘾法的病人均主诉使用本发明的提取物后再吸食或注 射毒品既觉得索然无味, 又觉得头脑胀裂疼痛, 在服用本发明的提取 物期间, 吸毒量比平时减少 70 - 80 %, 精神状态明显改善, 倘若加大 吸毒量, 将再会出现头晕, 恶心甚至呕吐等症状。  Patients who use the reduced-dose withdrawal method complain that the use of the extract of the present invention before taking or injecting drugs is both boring and painful, and the brain is painful. During the taking of the extract of the present invention, the drug consumption is reduced by 70- 80%, the mental state is obviously improved. If you increase the amount of drug use, you will have dizziness, nausea and even vomiting.
使用此法的 45 例病人, 在服用本发明的提取物 2 个月后都能无 痛苦脱瘾。  Forty-five patients who used this method had no painful withdrawal after taking the extract of the present invention for 2 months.
下面将结合本发明的提取物的具体实施例对本发明作更进一步的 描述, 应当明白这些例子不是要对本发明的保护范围进行限制。 在这 些例子中, 除非另有说明, 提取物中各种成分均是以重量份计。 实施例 1 - 4  The present invention will be further described below with reference to specific examples of the extract of the present invention. It should be understood that these examples are not intended to limit the protection scope of the present invention. In these examples, the various ingredients in the extract are in parts by weight unless otherwise stated. Examples 1-4
在这些实施例中, 按照表 5 中所列出的各种原料成分用量 (表中 以克为单位)、 按照下面所说的方法制备本发明的提取物, 该制备方 法具体内容如下:  In these examples, the extracts of the present invention are prepared according to the amounts of various raw material ingredients listed in Table 5 (in the table in grams) according to the method described below, and the specific content of the preparation method is as follows:
将所需量的原料用液化螺旋法粉碎成浆状细粉, 细粉的平均粒径 为 50 纳米。 所用粉碎设备为 DRS-2 型 (江苏省超细粉体工程技术研 究中心出品)。 把水加入细粉, 在 100 °C温度下提取, 水与细粉的体积 比为 10: 1。 所得提取液过滤后得到滤液。 得到的滤渣再次进行水提 取, 然后过滤。 第一次水提取的时间为 2 小时, 第二次水提取的时间 为 1. 5 小时。 第二次水提取时水与细粉的体积比为 7: 1。 将两次滤液 合并后浓缩, 冷却后向浓缩液中加入 70 %的乙醇, 置 80-85 °C水浴中 回流 30分钟后, 静置 24 小时, 然后过滤, 乙醇的加入量为浓缩液体 积的 1. 5倍。 过滤后的滤液浓缩至每毫升浓缩液中含有 30 总生物 碱。提取液的过滤, 用普通离心机分离, 除残渣, 再用高速离心机( 1. 4 万- 1.6 万转 /分) 离心分离。 浓縮液经喷雾干燥后得到粉末状的本发 明提取物。 The required amount of the raw materials was pulverized into a slurry-like fine powder by a liquefaction spiral method, and the average particle diameter of the fine powder was 50 nm. The crushing equipment used is DRS-2 (produced by Jiangsu Superfine Powder Engineering Technology Research Center). Water was added to the fine powder and extracted at 100 ° C. The volume ratio of water to fine powder was 10: 1. The obtained extract was filtered to obtain a filtrate. The obtained residue was subjected to water extraction again, and then filtered. The first water extraction took 2 hours and the second water extraction took 1.5 hours. The volume ratio of water to fine powder during the second water extraction was 7: 1. The two filtrates were combined and concentrated. After cooling, 70% ethanol was added to the concentrated solution. After refluxing in a water bath at 80-85 ° C for 30 minutes, it was left for 24 hours and then filtered. The amount of ethanol added was the volume of the concentrated solution. 1. 5 times. The filtered filtrate was concentrated to contain 30 total alkaloids per milliliter of the concentrate. The extraction solution was filtered, separated by a common centrifuge, the residue was removed, and then a high-speed centrifuge (1.4 (10,000-16,000 rpm) centrifugation. The concentrated liquid is spray-dried to obtain a powdery extract of the present invention.
表 5  table 5
编号 成分 实施例 1 实施例 2 实施例 3 实施例 4 Number Composition Example 1 Example 2 Example 3 Example 4
1 紫河车 60 30 50 60 1 Purple River Car 60 30 50 60
人参 15 15  Ginseng 15 15
2 野山参 18  2 Wild ginseng 18
高丽参  Korean Ginseng
西洋参 30  American Ginseng 30
3 肉桂 6 8 6  3 cinnamon 6 8 6
附子 9  Aconite 9
4 白屈菜 30 60 50 60  4 Celandine 30 60 50 60
5 延胡索 15 9 12 15  5 Yanhusuo 15 9 12 15
(元胡)  (Yuanhu)
6 牛黄 15 9 12 15  6 Bezoar 15 9 12 15
7 柏子仁 15  7 Boziren 15
火麻仁 15 12 15  Hemp seeds 15 12 15
8 高良姜 9  8 Galangal 9
干姜 6 9 6  Dried ginger 6 9 6
9 丹参 25 15 20 25  9 Salvia 25 15 20 25
10 大枣 30  10 jujubes 30
酸枣仁 15 20 15  Jujube kernel 15 20 15
11 炙甘草 6  11 Licorice 6
生甘草 10 9 10  Raw Licorice 10 9 10
12 青风藤 12 15 18 13 黄茶 12 15 18 12 Blue Wind Rattan 12 15 18 13 Yellow tea 12 15 18
14 徐长卿 12 20 15  14 Xu Changqing 12 20 15
15 防风 12 10 9  15 Windproof 12 10 9
16 黄芪 15 20 30  16 Astragalus 15 20 30
17 鬼箭羽 9 10 12  17 Ghost Arrow Feather 9 10 12
18 合欢皮 12 12 15  18 acacia leather 12 12 15
19 银杏叶 12 15 15  19 Ginkgo biloba 12 15 15
20 夜交藤 12 10 9  20 Yejiao 12 10 9
21 石菖蒲 12 15 15 实施例 5  21 Iris calamus 12 15 15 Example 5
本实施例中本发明提取物的制备方法同实施例 1 - 4, 但用于提取 的组合物的组成为紫河车 45g、 人参 25g、 肉桂 9g、 白屈菜 45g、 延 胡索 (元胡) 15g、 青风藤 15g、 牛黄 10g、 火麻仁 15g、 逍遥竹 15g、 干姜 9g、 丹参 20g、 酸枣仁 20g、 蟾蜍 9g、 合欢皮 15g、 黄芪 25g、 银杏叶 15g、 石菖蒲 12g、 ;水片 2g、 防风 9g、 炙甘草 6g。 实施例 6  The method for preparing the extract of the present invention in this embodiment is the same as that in Examples 1 to 4, but the composition of the composition used for extraction is 45 g of purple river car, 25 g of ginseng, 9 g of cinnamon, 45 g of celandine, 15 g of Yanhusuo (yuanhu) , Qingfengteng 15g, bezoar 10g, hemp kernel 15g, Xiaoyao bamboo 15g, dried ginger 9g, salvia 20g, jujube kernel 20g, toad 9g, acacia peel 15g, astragalus 25g, ginkgo leaf 15g, stone calamus 12g, water flakes 2g, windproof 9g, and licorice 6g. Example 6
本实施例中本发明提取物的制备方法同实施例 1 - 4, 但用于提取 的组合物的组成为洋金花 45g、 高丽参 15g、 肉桂 6g、 附子 6g、 白屈 菜 30g、 青风藤 16g、 火麻仁 15g、 牛黄 10g、 丹参 15g、 干姜 6g、 酸 枣仁 15g、 生甘草 6g、 延胡索 (元胡) 12g、 石菖蒲 12g、 黄芪 20g、 防风 9g、 徐长卿 20g。 的内容的基础上对本发明作出改变, 例如可以将本发明的戒毒提取物 制成不同的剂型以方便服用和携带, 或者在本发明戒毒提取物加入药 物领域内公知的一些辅助成分, 如香料、 色剂等, 这些内容均属于本 发明的精神, 它们应该被视为落在本发明所附的权利要求书所确定的 保护范围内。 The method for preparing the extract of the present invention in this embodiment is the same as that in Examples 1 to 4, but the composition of the composition for extraction is 45g of golden lily, 15g of Korean ginseng, 6g of cinnamon, 6g of aconite, 30g of celandine, blue wind Rattan 16g, hemp kernel 15g, bezoar 10g, salvia 15g, dried ginger 6g, jujube kernel 15g, raw licorice 6g, Yanhusuo (Yuanhu) 12g, stone calamus 12g, astragalus 20g, windproof 9g, Xu Changqing 20g. Based on the content of the invention, changes can be made to the present invention, for example, the detoxification extract of the present invention can be made into different dosage forms for convenient taking and carrying, or the detoxification extract of the present invention is added with a drug Some auxiliary components, such as perfumes, toners, and the like, which are well known in the physical field, belong to the spirit of the present invention, and they should be regarded as falling within the protection scope determined by the claims attached to the present invention.

Claims

权 利 要 求 书 Claim
1.一种用于镇静、 镇痛和 /或戒毒的提取物, 从一种含有下列组 分的组合物中提取, 按重量份计, 这些组分为: An extract for sedation, analgesia and / or detoxification, which is extracted from a composition containing the following components, and by weight parts, these components are:
( 1 ) 45 - 60份的组分 A, 为一种或多种选自紫河车、 洋金花、 河豚毒和眼镜蛇毒的物质;  (1) 45 to 60 parts of component A, which is one or more substances selected from the group consisting of purple river car, daffodil, puffer venom and cobra venom;
( 2 ) 15 - 30 份的组分 B, 为一种或多种选自人参、 野山参、 高丽参和西洋参的物质;  (2) 15 to 30 parts of component B, which is one or more substances selected from ginseng, wild mountain ginseng, Korean ginseng and American ginseng;
( 3 ) 6 - 9 份的组分 (:, 为一种或多种选自附子和去挥发性的 油的肉桂的物质;  (3) 6-9 parts of component (:, is one or more substances selected from aconite and cinnamon of devolatile oil;
( 4 ) 30 - 60份的组分 D, 为白屈菜;  (4) 30-60 parts of component D is celandine;
( 5 ) 9 - 15的组分 E, 为延胡索 (元胡);  (5) Component E of 9-15 is Yanhusuo (Yuanhu);
( 6 ) 组分 F, 为 9 - 15份的牛黄和 /或 0.5-3.0份的水片; (6) component F, which is 9-15 parts of bezoar and / or 0.5-3.0 parts of water flakes;
( 7 ) 12 - 15 份的组分 G, 为一种或多种选自火麻仁和柏子仁 的物质; (7) 12 to 15 parts of component G, which is one or more substances selected from hemp kernels and cypress seeds;
( 8 ) 6 - 12份的组分 H, 为一种或多种选自高良姜和去挥发性 的干姜的物质;  (8) 6-12 parts of component H, which is one or more substances selected from the group consisting of galangal and devolatile dried ginger;
( 9 ) 15 - 25份的组分 I, 为丹参;  (9) 15-25 parts of component I is salvia miltiorrhiza;
(10) 15 - 30份的组分 J, 为一种或多种选自酸枣仁和大枣的 物质;  (10) 15 to 30 parts of component J, which is one or more substances selected from the group consisting of jujube kernel and jujube;
(11) 6 - 10 份的组分 K, 为一种或多种选自生甘草和炙甘草 的物质。  (11) 6 to 10 parts of component K, which is one or more substances selected from raw licorice and licorice root.
2.权利要求 1 的提取物, 其中该组合物还含有一种或多种选自下 列的物质: 2. The extract of claim 1, wherein the composition further contains one or more substances selected from the group consisting of:
12 - 18份的青风藤: 12 - 18份的黄芩; 12-18 Blue Wind Vine: 12-18 servings of Scutellaria baicalensis;
12 - 25份的徐长卿;  12-25 copies of Xu Changqing;
9 - 12份的防风;  9-12 windbreaks;
15 - 30份的黄芪;  15-30 servings of astragalus;
9 - 12份的鬼箭羽;  9-12 ghost arrow feathers;
12 - 15份的合欢皮;  12-15 acacia skins;
12 - 15份的银杏叶;  12-15 servings of ginkgo leaves;
9 - 12份的夜交藤;  9-12 night vines;
12 - 15份的石菖蒲;  12-15 iris
6 - 9份的蟾餘;  6-9 toads;
12 - 25份的逍遥竹。  12-25 servings of Happy Bamboo.
3.—种药物组合物, 含有有效量的权利要求 1或 2的提取物和可 药用的赋形剂或载体。  3. A pharmaceutical composition comprising an effective amount of the extract of claim 1 or 2 and a pharmaceutically acceptable excipient or carrier.
4.权利要求 3的药物组合物, 用于戒毒、 镇静和 Z或镇痛。  4. A pharmaceutical composition according to claim 3 for detoxification, sedation and Z or analgesia.
5.—种戒毒、 镇静和 /或镇痛的方法, 包括给病人服用有效量的 权利要求 1或 1的提取物。  5. A method of detoxification, sedation and / or analgesia, comprising administering to a patient an effective amount of the extract of claim 1 or 1.
6.权利要求 5的方法, 其中用于戒毒的成人口服剂量为 1.5-9. Og/ 次, 每曰 2 - 4次。  6. The method of claim 5, wherein the oral dose for an adult for detoxification is 1.5-9. Og / times, 2 to 4 times per day.
7.权利要求 5的方法,其中用于戒毒的成人注射剂量为 0.6-3. Og/ 次, 每日 2 - 4次。  7. The method of claim 5, wherein the injection dose for adults for detoxification is 0.6-3. Og / times, 2 to 4 times a day.
8.一种制备权利要求 1或 2的提取物的方法, 其步骤包括:  8. A method for preparing the extract of claim 1 or 2, comprising the steps of:
( 1 ) 粉碎原材料至颗粒大小为约 10 - 300纳米,  (1) crush the raw materials to a particle size of about 10-300 nm,
( 2 ) 将粉碎后的原材料用适量水提取, 提取温度为约 90 - 100°C,  (2) extract the crushed raw materials with an appropriate amount of water, and the extraction temperature is about 90-100 ° C,
( 3 ) 将水提取液过滤后的滤液进行第一次浓缩,  (3) the filtrate after the water extract is concentrated for the first time,
(4 ) 将浓缩液用 70%的乙醇进行回流处理后, 再静置处理, 一 (4) after the concentrated solution is subjected to reflux treatment with 70% ethanol, and then allowed to stand, One
( 5 ) 静置后的处理液过滤后, 将滤液进行第二次浓缩。 (5) After filtering the treatment solution after standing, the filtrate is concentrated for the second time.
9.权利要求 8 的方法, 其中步骤 ( 3) 中得到的滤渣进行第二次 水提取。  The method according to claim 8, wherein the filter residue obtained in step (3) is subjected to a second water extraction.
10. 权利要求 8或 9的方法, 其中粉碎采用液化螺旋法。  10. The method according to claim 8 or 9, wherein the pulverization uses a liquefaction spiral method.
PCT/CN2000/000086 2000-04-11 2000-04-11 Extract for abstaining from narcotics and its preparation WO2001076613A1 (en)

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