WO2011127829A1 - 纳米碳颗粒作为治疗痔疮的外用药物的应用 - Google Patents

纳米碳颗粒作为治疗痔疮的外用药物的应用 Download PDF

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Publication number
WO2011127829A1
WO2011127829A1 PCT/CN2011/072792 CN2011072792W WO2011127829A1 WO 2011127829 A1 WO2011127829 A1 WO 2011127829A1 CN 2011072792 W CN2011072792 W CN 2011072792W WO 2011127829 A1 WO2011127829 A1 WO 2011127829A1
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Prior art keywords
treating acne
external preparation
acne
carbon particles
nano carbon
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PCT/CN2011/072792
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English (en)
French (fr)
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汪中
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Wang Zhong
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/44—Elemental carbon, e.g. charcoal, carbon black
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0031—Rectum, anus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers

Definitions

  • the present invention relates to a medicament for treating acne, and more particularly to a topical medicament comprising nanocarbon particles and a method of treating acne using the medicament.
  • Acne is caused by some living habits or daily posture problems, such as sitting, standing labor, constipation, and other causes of the disease, causing distortion and dilation of the distal vein of the lower rectum or anal canal, local veins from the blood backflow, in the anus
  • a chronic disease of one or more dilated venous masses formed by the varicose veins of the rectal base and the anal mucosa There are also views that hemorrhoids are pathological hypertrophy of the anal cushion, bleeding, prolapse and other symptoms associated with thrombosis, resulting in perianal inflammatory tissue hyperplasia and vascular congestion expansion of the mass formed, in the treatment of the preservation of anal cushion and protection of anal function .
  • acne Due to different anatomical locations, acne is divided into internal hemorrhoids, external hemorrhoids and mixed hemorrhoids.
  • the incidence of morbidity in the crowd is very high, and there are "ten people and nine baboons".
  • the surface of the medial malleolus is a columnar epithelium with almost no sensory nerve distribution and is located at the narrowest part of the anus.
  • the main symptom is defecation hemorrhage. Because of the sensory nerve distribution in the lateral malleolus, the symptoms are mainly pain and lumps; if mixed sputum occurs, both symptoms may occur.
  • the internal hemorrhoids can generally be divided into three phases.
  • the most common symptoms are painless hemorrhage during stool, bright red blood, drip-like or spray-like, which can appear before and after. Constipation, dry stools, increased bleeding when drinking alcohol and eating irritating foods. At this time, it is usually a period of sputum. If it is not treated in time, it may develop into two or three periods. In the second period, there is a hemorrhage in addition to hemorrhage, and the nucleus is removed from the anus, but the contraction of the anal nucleus can be naturally retracted after defecation. Into the anus. During the third period, the nucleus cannot retract itself, and must be returned to the anus by hand.
  • Nanomaterials are generally defined as materials that are less than 100 nanometers in size in a certain dimension. In recent years, nanoscience has developed rapidly, and people's understanding of nanomaterials has been deepening, and new discoveries and new applications have emerged. Scientific research has shown that when a substance is small to nanometer scale, it usually shows many different performance characteristics from macroscopic scale materials, which we call nanoeffects. Nano-effects include surface effects, small volume effects, and macroscopic quantum tunneling effects. The presence of these effects allows nanomaterials to have their own physicochemical properties that are different from macroscopic materials of the same material.
  • nanomaterials and macromaterials have different physicochemical properties, they are different from organisms. New functions and uses are continuously discovered and developed. The application of nanotechnology in medical treatment and diagnosis is developing rapidly.
  • Nanomaterials such as nanocarbon have the function and efficacy of promoting the absorption of organisms and promoting plant growth.
  • the development of nanosilver as a disinfectant and as a drug sterilization and anti-inflammatory has proved that nanomaterials interact with organisms.
  • the invention is a research on the new application of nano carbon materials in the medical field. Summary of the invention
  • the invention provides the application of nano carbon particles as a topical medicine for treating acne, which is used for solving the problem of treating acne with anti-inflammatory and analgesic drugs in the prior art, which can only relieve symptoms and can not cure, surgery A defect that is painful in the treatment of acne and is prone to recurrence after treatment.
  • the invention provides a topical medicine for treating acne, wherein the active ingredient has a particle size range of
  • the nano carbon particles are derived from a nanographite sol obtained by an electrolytic method. Specifically, it is a carbon nanoparticle in a nano-carbon sol obtained by electrolytically electropolating graphite.
  • the external pharmaceutical composition for treating acne further comprises: a dispersing agent and/or a liquid solvent.
  • the dispersing agent is one or more of lignosulfonate, oleic acid or fish oil, and the liquid solvent is water and/or glycerin.
  • the external medicine for treating acne is a dry powder, an aqueous solvent, an oily liquid, an ointment or a suppository.
  • the external medicine for treating acne further includes a pharmaceutics adjuvant and an auxiliary medicine.
  • the suppository is made by coating the nanocarbon particles with an outer layer of a pharmaceutical adjuvant or an auxiliary drug.
  • the above auxiliary drug may be a topical drug for treating acne which has been used clinically, and may be a topical ointment or a suppository.
  • the invention also provides an application of the nano carbon particles in preparing a topical medicine for treating acne, wherein the nano carbon particles have a particle size ranging from 1 to 100 nm.
  • the external pharmaceutical composition for treating acne further comprises: a dispersing agent and/or a liquid solvent.
  • the dispersing agent is one or more of lignosulfonate, oleic acid and fish oil, wherein the liquid solvent is water and /glycerol.
  • the nano carbon particles are derived from a nanographite sol obtained by an electrolytic method. Specifically, it is a carbon nanoparticle in a nano-carbon sol obtained by electrolytically electropolating graphite.
  • the external medicine for treating acne is a dry powder, an aqueous solvent, an oily liquid, an ointment or a suppository.
  • composition for external use of the acne treatment includes pharmaceutics auxiliary materials and auxiliary materials. Drugs.
  • the present invention also provides a method of treating acne comprising administering to a patient the topical medicament for treating acne. It has been experimentally proved that even if applied at a larger dose, the nano carbon particles are not harmful to the human body. Therefore, in theory, the dosage of the nano carbon particles for treating acne in the present invention can be used without limitation, and can usually be used in clinical treatment.
  • the dose for topical administration of the drug is controlled to be 6-200 mg of nanocarbon particles per day.
  • the invention utilizes the strong permeability of the nano carbon particles, can change the local dynamic state of the small blood vessels in the acne lesion site, and obviously improve the characteristics of the varicose blood vessels from the blood circulation state, and fundamentally solve the circulation problem of the anal local venous plexus plexus, which can not only alleviate The clinical symptoms of acne, and the physiological causes of acne can be eliminated, thereby curing acne.
  • the acne treatment medicine prepared by using the nano carbon particles of the invention has obvious curative effects on internal hemorrhoids, external hemorrhoids and mixed sputum.
  • the second and third stages of acne can be significantly improved after 2 to 3 days of treatment.
  • Two to three weeks of treatment can be cured, and the original acne blood vessels disappear from the varicose and inflammatory mass lesions, such as the original mass. Larger, can leave local skin relaxation.
  • the clinical data indicates that the drug prepared by the invention has an effective rate of more than 90% for the treatment of acne, and the recovery rate of the patient's self-conscious symptoms completely disappears by more than 72%. Under the condition of treatment, the treatment can be carried out under the guidance of a doctor.
  • the dosage and concentration can be adjusted according to the condition, so that the treatment effect can be optimized.
  • the patient can also treat himself according to the instructions.
  • the treatment process is simple, safe, quick and effective without any pain.
  • the practice of the present invention eliminates the need for surgery in patients with severe advanced acne, which saves the patient from the pain of surgery and is robust. If the acne relapses due to daily life, working condition problems, and own diseases or living habits after the healing, it is also convenient to perform the drug treatment again according to the method of the present invention.
  • FIG. 1 is a schematic view of a nano carbon particle acne plug according to a fifth embodiment of the present invention.
  • the present invention is based on the recognition of nano-effects of nanomaterials that differ from macroscale materials, and utilizes the special physicochemical properties of nanocarbon materials.
  • a research team at Peking University introduced a water-soluble carbon nanotube (about 1.4 nm in diameter and about 400 nm in length) into mice, and found that the carbon nanotubes can shuttle freely between different organs of mice. It is excreted in the urine, and 600,000 molecular weight conventional substances cannot be seen. It can be proved that the nano-carbon material has strong permeability, can enter the organism, and can promote the permeability of the organism medium, and strengthen its local circulation and absorption function.
  • nano-carbon particles have a small particle size, strong permeability, dredge blood vessels, promote blood circulation, and improve the effect of local blood circulation, thereby achieving the purpose of treating blood vessels and microcirculation diseases.
  • the specific mechanism of these effects is still in the process of further research, but its effects have been proved by a large number of experiments.
  • the nano-carbon particles are mainly composed of carbon elements. It has been proved by animal experiments that the nano-carbon particles are non-toxic and there is no abnormality in the mice eating a lot.
  • the inventor and the Institute of Molecular Medicine of Peking University conducted relevant toxicological and pathological experimental studies.
  • the mice were orally administered with 5 ml of 0.3% sodium carbon granule water per kg body weight per day, and no adverse reactions were observed. Volunteers were given 15 ml of 0.3% carbon nanoparticle sol per day for adults and no abnormalities were observed for 60 consecutive days.
  • the culture medium was added to the mouse heart cells for one week by adding 0.3% by weight of carbon particles, and no abnormality was observed.
  • nano carbon particles are safe and non-toxic as drugs.
  • the particles of the nano carbon particles used in the invention have a particle diameter of 100 nm or less, 90% or more and 1 to 50 nm, and can be directly prepared into a nano carbon particle sol. It is recommended to use a dispersing agent to sufficiently disperse and not agglomerate.
  • the nano carbon particles used in the present invention preferably the dispersing agent is an anionic surfactant, such as lignosulfonate, the lignosulfonate is non-toxic, and the LD50 is > 5 g/kg.
  • the US Food and Drug Administration has approved the use of this product in the manufacture and processing of various food and food packaging. The use of such dispersants helps to ensure the safety of the drug.
  • This embodiment is an aqueous solvent.
  • the external drug for treating acne in this embodiment can make nano carbon particles 3% by weight. Prepare by adding directly to distilled water to 10%. The solvent can be dispersed by ultrasonication, so that the nano carbon particles are branched into nano carbon particle sols to achieve the best effect. The prepared sol agent can be directly sprayed on the affected area every time 0.5 to 1 ml twice a day to achieve the therapeutic effect.
  • Example 1 Using the preparation prepared in Example 1, a total of 18 clinical trials of different acne patients were performed in the volunteers, and the definition of the nucleus was significantly reduced and softened, and the related symptoms were alleviated. The nucleus of the nucleus disappeared, or only the skin was loose, and the patient had no symptoms associated with hemorrhoids. The patient was given medication under the guidance, and was reviewed 3 to 4 weeks after drug treatment, and the results were statistically analyzed. As shown in Table 1, it can be seen that the symptoms of acne were significantly improved by 94%, and the self-reported symptoms disappeared completely after four weeks. %.
  • This embodiment is an oily liquid, which is a mixture of nano carbon particles mixed with glycerin and water.
  • the typical weight ratio of nano carbon particles to glycerin and water is 1%: 52%: 47%. It is made into an oily liquid and filled in a small long-neck elastic medical plastic container.
  • the typical volume of each small container is 0.5ml ( The commonly used volume can also be 1 ml), and one or more small holes are opened at the top of the long neck.
  • the long neck can be inserted into the anus and then administered through one or more small holes near the tip.
  • One at a time twice a day.
  • One can be used in two times during the recovery period. This example is especially useful for patients with habitual constipation.
  • the present embodiment is a dry powder, which is a nano carbon particle dispersed by lignosulfonate (sodium salt), which is sterilized and sterilized, and is directly sprayed on the affected part in use, or directly sprayed on the affected part when used;
  • the container is directly applied to the affected area with a cotton swab.
  • Each time the amount of nanocarbon particles is 50 ⁇ 100mg, once or twice a day. After direct application of the affected area, the excess toner can be wiped off with a wet tissue for a few minutes. This method is generally used for patients with acne with more serious conditions, more local secretions, and odor.
  • Nano carbon particles have a strong adsorption function, in this case not only can treat acne, but also can adsorb And remove secretions and eliminate odors. After the patient has obviously improved, the liquid medicine of the first or second embodiment can be used for consolidation treatment, and most cases achieve the healing effect within 3-4 weeks.
  • Example 3 Using the preparation prepared in Example 3, a total of 10 clinical trials of sputum and internal and external acne patients in the late stage were performed in the volunteers. The definition of the nucleus was significantly smaller and softer, and the related symptoms were alleviated. The nucleus of the nucleus disappeared, or only the skin was slack, and the patient had no symptoms related to hemorrhoids. The patient is administered under the guidance, and the liquid solvent (for example, the liquid medicine of the first embodiment or the second embodiment) is once a day for the first three days, and the liquid medicine is obviously improved in about three days, and then the liquid medicine is used twice a day. Continued treatment for 3 to 4 weeks, and then review, and the results of statistics, as shown in Table 3, can be seen that the apparent improvement of 100%, after four weeks, the self-reported symptoms completely disappeared to 80%.
  • the liquid solvent for example, the liquid medicine of the first embodiment or the second embodiment
  • the aqueous solution is an electrolytic solution for producing a nano-graphite sol, which is diluted with purified water to a therapeutically suitable weight concentration of 1% to 10% (nano carbon particle concentration) after sterilization and sterilization, without adding a dispersing agent. And the drying process directly dilutes the nano-carbon sol application. Spray directly onto the affected area during treatment.
  • FIG. 1 is a schematic view of a nano carbon particle acne plug provided in Example 5 of the present invention.
  • This embodiment is a suppository which is used in combination with a hemorrhoid suppository.
  • the hemorrhoids plug can be a medicine for clinical treatment of acne, and can be directly purchased or prepared according to the formulated ingredients, and a layer of nano carbon particles 2 is coated on the acne suppository 1 by smearing to form nano carbon.
  • a granule hemorrhoid plug with a length of 25 mm and a diameter of 7 mm. It is administered from the anus twice a day, each time the amount of nano-carbon particles is 50 ⁇ 100mg.
  • This embodiment is a suppository made of glycerin gelatin and added with starch, flour or dextrin as a base material and an appropriate proportion of nanocarbon particles.
  • the specific weight ratio is 50% glycerin, 20% gelatin, starch, dextrin, flour or a mixture thereof 20%, and nano carbon particles 10%. Molded by a mold, each suppository contains 100 to 150 mg of nanocarbon particles.
  • the nanocarbon used in each of the above examples has a daily dose of 6 to 200 mg, which is a clinically administered amount according to an effective use dose. From the above toxicological studies, it can be seen that the nano-carbon powder has no toxic side effects when used externally, so there is no upper dose limit, any dosage modification, addition of auxiliary drugs, and addition of an existing acne medicine as an active ingredient are included in the scope of the present invention. Inside.

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Description

纳米碳颗粒作为治疗痔疮的外用药物的应用
技术领域
本发明涉及一种治疗痔疮的药物， 尤其涉及一种包含纳米碳颗粒的外 用药物和利用该药物治疗痔疮的方法。 背景技术
痔疮是由于某些生活习惯或日常体态问题，如常坐、站立劳动、便秘， 以及疾病等其他一些原因引起直肠下端或肛管的末梢静脉发生迂曲、 扩 张， 局部静脉从血液回流不畅， 在肛门、 直肠底部及肛门粘膜的静脉丛发 生曲张而形成的一个或多个扩张静脉团的一种慢性疾病。 亦有观点认为痔 疮是肛垫的病变性肥大、 发生出血、 脱垂等症状伴发血栓， 造成肛周炎性 组织增生和血管淤血扩张形成的肿块， 在治疗上主张保存肛垫及保护肛门 功能。 因解剖位置不同， 痔疮分成内痔、 外痔与混合痔。 人群中发病几率 很高， 有"十人九痔"之说。 内痔表面是柱状上皮， 几乎没有感觉神经分布， 又位于肛门最狭窄处， 其症状主要为排便出血。 外痔处由于有感觉神经分 布， 其症状主要为疼痛、 肿块； 若发生混合痔， 则两种症状皆可能发生。
内痔一般可分为三期，最常见的症状是大便时无痛性出血，血色鲜红， 呈点滴状或喷射状， 便前便后均可出现。 便秘、 粪便干硬， 饮酒及食用刺 激性食物时出血加重。 此时一般多为一期内痔， 没有得到及时治疗就可能 发展成二期内痔或三期内痔， 二期内痔除有出血外还有痔核从肛门口脱 出， 但排便后收缩肛门痔核可以自然回缩到肛内。 三期内痔核不能自行回 缩， 须用手托回肛内。 晚期内痔反复脱出， 可引起肛门括约肌松弛和分泌 物增多， 致使肛缘常感潮湿不洁， 出现瘙痒和肛门湿疹， 严重时还可引起 摩擦痛和痒痛。 现阶段， 药物和外科手术治疗的效果都很有限。 药物一般以消炎止痛 为主， 一般只能在痔疮发作时緩解症状， 不能根治， 尤其是二期和三期痔 疮用药物治疗效果都不好， 通常最后的解决办法只能是手术治疗。 外科手 术治疗在一定时期效果比较明显， 但治疗过程较痛苦， 手术后需要休息数 天， 且治疗后复发率很高。
从上世纪末开始纳米科技已经成为世界材料、 物理、 化学、 生物等多 学科研究的焦点和前沿。
纳米材料通常定义为在某一维度上尺寸小于 100纳米的物质。 近年来 纳米科学发展迅速， 人们对纳米材料的认识也在不断深入， 由此而产生的 新发现、 新应用层出不穷。 科学研究证明， 当一种物质尺寸小到纳米尺度 时， 通常都显示出许多与宏观尺度物质不同的性能特点， 我们称之为纳米 效应。 纳米效应包括表面效应、 小体积效应和宏观量子隧道效应等。 这些 效应的存在使得纳米材料具有其特殊的、 与相同材料的宏观尺度物质不同 的物理化学性质。
由于纳米材料与宏观材料有着不同的物理化学性质， 其与生物体的作 用也不同， 新的作用和用途被不断发现和开发出来， 纳米科技在医学治疗 和诊断方面的应用发展迅速。
纳米材料， 如纳米碳具有促进生物体循环吸收， 促进植物生长方面的 作用和功效； 纳米银在作为消毒剂， 以及作为药物杀菌消炎等方面的应用 开发，证明了纳米材料在与生物体相互作用中，具有很多我们尚未认识的， 有待发现的潜在应用功能。 本发明就是纳米碳材料在医疗领域一个新应用 的研究。 发明内容
本发明提供了纳米碳颗粒作为治疗痔疮的外用药物的应用， 用以解决 现有技术中的用消炎止痛药物治疗痔疮只能緩解症状不能根治， 外科手术 治疗痔疮过程痛苦且治疗后容易复发的缺陷。
本发明提供一种治疗痔疮的外用药物， 其有效成分为粒径大小范围为
1 ~ 100纳米的纳米碳颗粒。
进一步地， 所述纳米碳颗粒来自电解法得到的纳米石墨溶胶。 具体的 为通过电解法电解石墨得到的纳米碳溶胶中的碳纳米颗粒。
进一步地， 所述治疗痔疮的外用药物组成还包括： 分散剂和 /或液体溶 剂。 所述分散剂为木质素磺酸盐、 油酸或鱼油中的一种或多种， 所述液体 溶剂为水和 /或甘油。
进一步地， 所述治疗痔疮的外用药物为干粉剂、 水溶剂、 油性药液、 软膏或栓剂。
进一步地， 所述治疗痔疮的外用药物还包括药剂学辅料及辅助药物。 进一步地， 所述栓剂为在药剂学辅料或辅助药物外层包覆所述纳米碳 颗粒制成的。
上述辅助药物可以是目前已经在临床使用的治疗痔疮的外用药， 可以 是外用软膏或栓剂。
本发明还提供一种纳米碳颗粒在制备治疗痔疮的外用药物中的应用， 其中所述纳米碳颗粒的粒径大小范围为 1 ~ 100纳米。
进一步地， 所述治疗痔疮的外用药物组成中还包含： 分散剂和 /或液体 溶剂。
进一步地，所述分散剂为木质素磺酸盐、油酸和鱼油中的一种或多种， 其中所述液体溶剂为水和 /甘油。
进一步地， 所述纳米碳颗粒来自电解法得到的纳米石墨溶胶。 具体的 为通过电解法电解石墨得到的纳米碳溶胶中的碳纳米颗粒。
进一步地， 所述治疗痔疮的外用药物为干粉剂、 水溶剂、 油性药液、 软膏或栓剂。
进一步地， 所述治疗痔疮的外用药物组成中还包括药剂学辅料及辅助 药物。
本发明还提供了一种治疗痔疮的方法， 所述方法包括给患者施用所述 治疗痔疮的外用药物。 已经有实验证明即使以较大剂量施用， 纳米碳颗粒 对人体也不会有危害， 所以， 理论上讲， 本发明采用纳米碳颗粒治疗痔疮 的给药剂量可以没有限制， 在临床治疗中通常可以控制局部施用所述药物 的剂量为每日 6-200毫克纳米碳颗粒。
本发明利用纳米碳颗粒渗透性强， 能够深入痔疮病灶部位改变小血管 局部动力学状态， 明显改善曲张血管从血液流通状态的特性， 从根本上解 决肛门局部静脉血管丛循环流通问题， 不仅可以緩解痔疮的临床症状， 而 且可以从生理上消除产生痔疮的病因， 从而根治痔疮。
本发明使用纳米碳颗粒制备的痔疮治疗药物， 对内痔、 外痔和混合痔 都有明显疗效。 经过志愿者临床试用证明， 二期和三期痔疮经过 2 ~ 3 天 治疗就可明显好转， 两到三周治疗即可痊愈， 使原痔疮血管从曲张和炎性 肿块病灶消失， 如原有肿块较大， 可留有局部皮肤松弛现象。 临床数据说 明本发明制备的药物， 对痔疮的治疗有效率达到 90%以上， 病人自觉症状 完全消失的痊愈率可达到 72%以上。有条件情况下治疗可在医生指导下进 行， 按阶段视病情调节药量和浓度， 可以使治疗效果达到最佳。 患者亦可 按说明自行治疗， 治疗过程简单、 安全， 见效快， 无任何痛苦。 本发明的 实施使严重晚期痔疮患者不必再动手术， 使病人免除了手术的痛苦， 而且 疗效稳固。 治愈后如果由于日常生活、 工作条件问题， 以及自身疾病或生 活习惯等导致痔疮复发， 再次按照本发明方法进行药物治疗也很方便。 附图说明
图 1为本发明实施例五提供的纳米碳颗粒痔疮栓的示意图。
结合附图， 本发明实施例中附图标记如下：
1 -已有的痔疮栓剂； 2-纳米碳颗粒； 具体实施方式
为使本发明的目的、 技术方案和优点更加清楚， 下面将结合具体实施 例对本发明的技术方案进行清楚、 完整地描述， 显然， 所描述的实施例是 本发明一部分实施例， 而不是全部的实施例。 基于本发明中的实施例教导 或启示， 本领域普通技术人员在没有做出创造性劳动前提下所获得的所有 其他实施例， 都属于本发明保护的范围。
本发明的提出是基于对纳米材料所表现出的不同于宏观尺度物质的 纳米效应的认识， 利用了纳米碳材料的特殊物理化学性质。 例如， 北京大 学一个研究组将一种水溶性的纳米碳管（直径约 1.4nm,长约 400nm)导入小 鼠体内， 结果发现这种纳米碳管可以在小鼠的不同器官之间自由穿梭， 通 过尿液排泄， 而 60 万分子量的常规物质不能出现如此现象。 由此可以证 明纳米碳材料具有很强的渗透性， 能够进入生物体， 并能够促进生物体介 质的通透性， 使其局部循环和吸收功能加强。 相关实验证明纳米碳颗粒粒 径微小， 有很强的渗透性， 具有疏通血管， 促进血液流通， 改进局部血液 循环的功效， 从而达到治疗血管和微循环类疾病的目的。 这些作用发生的 具体机制尚在进一步研究过程中， 但其作用效果已经被大量实验所证明。
以下说明本发明治疗痔疮的外用药物的毒理研究。
纳米碳颗粒主要由碳元素组成， 经动物实验证明， 纳米碳颗粒是无毒 的， 小鼠大量进食不会出现异常。 发明人与北京大学分子医学研究所， 进 行了相关毒理和病理实验研究。对小鼠给予每公斤体重每日 5ml 0.3%的纳 米碳颗粒水溶剂口服， 未发现不良反应。 志愿者成人每天口服 15ml 0.3% 纳米碳颗粒溶胶， 连续服用 60天未见异常。 培养液加入重量比 0.3%纳米 碳颗粒进行小鼠心脏细胞培养一周， 未见异常。 志愿者治疗过程中， 用 8% 纳米碳颗粒水溶剂， 肛门给药， 每日 2次， 每次 1毫升， 连续 4周以上未 见任何不良反应。 实验证明纳米碳颗粒作为药物是安全无毒的。
以下说明本发明治疗痔疮的外用药物的制备实施例。 本发明使用的纳米碳颗粒的颗粒为粒径 100纳米以下， 90%以上在 1 ~ 50纳米之间， 可以直接制成纳米碳颗粒溶胶， 推荐采用分散剂使其充分分 散， 不团聚。 本发明使用的纳米碳颗粒， 其优选分散剂为阴离子表面活性 剂， 例如木质素磺酸盐， 木质素磺酸盐无毒， LD50 > 5g/kg。 美国食品及 药物管理局业已批准允许在各种食品和食品包装的制造和加工过程中使 用此产品。 使用这类分散剂， 利于保证药物的安全性。
实施例一
本实施例为水溶剂， 本实施例治疗痔疮的外用药物可以将纳米碳颗粒 按重量比例 3%。至 10%直接放入蒸馏水中制备。 溶剂可以经过超声分散， 使纳米碳颗粒均勾分布成为纳米碳颗粒溶胶， 以达到最佳效果。 将制备的 溶胶药剂直接喷涂于患处每次 0.5至 1ml每日两次即可达到治疗效果。
实验例： 使用实施例一中制备的制剂， 在志愿者中共进行了 18例不 同痔疮病人的临床治疗实验， 定义痔核明显变小变软， 相关症状减轻为有 效。 痔核基本消失， 或仅留有皮肤松弛， 病人已无痔疮相关症状为痊愈。 病人在指导下用药， 经药物治疗后 3 ~ 4周复查， 并进行结果统计， 如表 1 所示， 可以看出痔疮症状明显好转的达到 94%, 四周后自述原有症状完全 消失的达到 72%。
实施例一治疗结果统计
Figure imgf000007_0001
实施例二
本实施例为油性药液， 是将纳米碳颗粒与甘油和水混合， 制成的混合 物中纳米碳颗粒与甘油、 水的典型重量比为 1%: 52%: 47%, 制成油性液 并灌装于小型长颈弹性医用塑料容器中， 每个小型容器典型容积为 0.5ml (常用的容积还可以为 lml ) , 长颈顶端开有一个或多个小孔。 治疗时可 以将长颈一段插入肛门挤压后通过顶端附近一个或多个小孔给药。 一般每 次使用一只， 每日两次。 复原巩固期一只可以分 2次使用。 本例尤其适用 于伴有习惯性便秘的患者。
实验例： 使用实施例二中制备的制剂， 在志愿者中共进行了 21 例不 同痔疮病人的临床治疗实验， 定义痔核明显变小变软， 相关症状减轻为有 效。 痔核基本消失， 或仅留有皮肤松弛， 病人已无痔疮相关症状为痊愈。 病人在指导下用药， 经药物治疗后 3 ~ 4周复查， 并进行结果统计， 如表 2 所示， 可以看出明显好转的达到 95%, 四周后自述原有症状完全消失的达 到 76%。
实施例二治疗结果统计
Figure imgf000008_0001
实施例三
本实施例为干粉剂， 是将由木质素磺酸盐 （钠盐）分散的纳米碳颗粒， 经过灭菌消毒， 装于有喷涂功能的容器中， 使用时直接喷涂于患处； 或装于 适当的容器， 直接用棉签涂于患处。 每次纳米碳颗粒用量为 50〜100mg, 每 日一至两次。 直接喷涂患处给药后， 过数分钟可用湿纸巾将多余碳粉擦除。 这种方法一般用于病情较严重， 局部分泌物多， 有异味的痔疮病人。 纳米碳 颗粒具有艮强的吸附功能， 在这种情况下不仅可以治疗痔疮， 而且可以吸附 和去除分泌物， 并消除异味。 在病人明显好转后， 一般可改用实施例一或二 的液体药剂进行巩固治疗， 大多数病例在 3-4周内达到痊愈的效果。
实验例： 使用实施例三中制备的制剂， 在志愿者中共进行了 10例晚 期内痔和内外混合痔疮病人的临床治疗实验， 定义痔核明显变小变软， 相 关症状减轻为有效。 痔核基本消失， 或仅留有皮肤松弛， 病人已无痔疮相 关症状为痊愈。病人在指导下用药，前三天每日一次粉剂一次液体溶剂（例 如实施例一或实施例二的药液） ， 三天左右均明显好转， 然后每天两次全 部用液体药剂。 持续治疗 3 ~ 4周， 而后复查， 并进行结果统计， 如表 3 所示， 可以看出明显好转的达到 100%, 四周后自述原有症状完全消失的 达到 80%。
实施例三治疗结果统计
Figure imgf000009_0001
实施例四
本实施例为水溶液药剂， 是采用电解法生产纳米石墨溶胶， 经消毒灭 菌处理后用纯化水稀释到适于治疗的重量浓度 1% ~ 10% (纳米碳颗粒浓 度） ， 没有经过加入分散剂和干燥过程， 直接将纳米碳溶胶稀释应用。 治 疗时直接喷涂于患处。
实验例： 使用实施例四中制备的制剂， 在志愿者中共进行了 16例不 同痔疮病人的临床治疗实验， 定义痔核明显变小变软， 相关症状减轻为有 效。 痔核基本消失， 或仅留有皮肤松弛， 病人已无痔疮相关症状为痊愈。 病人在指导下用药， 经药物治疗后 3 ~ 4周复查， 并进行结果统计， 如表 4 所示， 可以看出明显好转的达到 100%, 四周后自述原有症状完全消失的 达到 75%。 实施例四治疗结果统计
Figure imgf000010_0001
实施例五
图 1 为本发明实施例五提供的纳米碳颗粒痔疮栓的示意图。 本实施例 为栓剂， 是将纳米碳与痔疮栓配合使用。 所述痔疮栓可以是目前临床用于 痔疮治疗的药物， 可以直接购买或按照记载的配方成分自行制作， 通过涂 抹的方式在所述痔疮栓剂 1外包覆一层纳米碳颗粒 2, 形成纳米碳颗粒痔 疮栓， 其长为 25mm, φ为 7mm。 从肛门给药， 每日两次， 每次纳米碳颗 粒用量为 50 ~ 100mg。
实验例： 应用实施例五制备的栓剂， 在志愿者中进行了 7例中、 重度 痔疮病例的治疗， 定义痔核明显变小变软， 相关症状减轻为有效。 痔核基 本消失， 或仅留有皮肤松弛， 病人已无痔疮相关症状为痊愈。 病人在指导 下用药， 此前病人都长期使用过同种痔疮栓剂， 没有明显疗效。 经痔疮栓 加纳米碳颗粒混合药物治疗后 3 ~ 4周复查， 并进行结果统计， 如表 5所 示。 有效率达到 100%, 痊愈率 85%, 本实验说明纳米碳颗粒与常规临床 痔疮药物配合使用， 疗效有显著提高。
实施例五治疗结果统计
Figure imgf000010_0002
实施例六
本实施例为栓剂， 是用甘油明胶并加入淀粉、 面粉或糊精等作为基料 与适当比例纳米碳颗粒制成的。 具体重量比例为甘油 50%、 明胶 20%、 淀 粉、 糊精、 面粉或其混合物 20%, 纳米碳颗粒 10%。 用模具成型， 每枚栓 剂含纳米碳颗粒 100至 150mg。
实验例： 应用实施例六制备的栓剂， 在志愿者中进行了 9例中、 重度 痔疮病例的治疗， 定义痔核明显变小变软， 相关症状减轻为有效。 痔核基 本消失， 或仅留有皮肤松弛， 病人已无痔疮相关症状为痊愈。 病人在指导 下用药，经纳米碳颗粒痔疮栓剂药物治疗后，一般 3 日左右出现显著疗效， 3 ~ 4周复查， 并进行结果统计， 如表 6所示， 有效率达到 100%, 痊愈率 77%。
实施例六治疗结果统计
Figure imgf000011_0001
以上各实施例中纳米碳每日使用的剂量为 6至 200mg, 是根据有效使 用剂量制定的临床给药量。 由上述毒理研究可知纳米碳粉外用时没有毒副 作用， 所以并无剂量上限， 任何剂量的修改， 辅助药物的加入， 以及作为 有效成分添加入已有的痔疮药物， 均应包含在本发明范围内。
最后应说明的是： 以上实施例仅用以说明本发明的技术方案， 而非对 其限制； 尽管参照前述实施例对本发明进行了详细的说明， 本领域的普通 技术人员应当理解： 其依然可以对前述各实施例所记载的技术方案进行修 改， 或者对其中部分技术特征进行等同替换； 而这些修改或者替换， 并不 使相应技术方案的本质脱离本发明各实施例技术方案的精神和范围。

Claims

权 利 要 求
1、 一种治疗痔疮的外用药物， 其有效成分为粒径大小范围为 1 ~ 100 纳米的纳米碳颗粒。
2、 根据权利要求 1 所述治疗痔疮的外用药物， 所述纳米碳颗粒来自 电解法得到的纳米石墨溶胶。
3、 根据权利要求 1 所述治疗痔疮的外用药物， 该外用药物组成还包 括： 分散剂和 /或液体溶剂。
4、 根据权利要求 3所述治疗痔疮的外用药物， 所述分散剂为木质素 磺酸盐、 油酸和鱼油中的一种或多种。
5、 根据权利要求 3所述治疗痔疮的外用药物， 所述液体溶剂为水和 / 或甘油。
6、根据权利要求 1-5任一项所述治疗痔疮的外用药物，该外用药物为 干粉剂、 水溶剂、 油性药液、 软膏或栓剂。
7、 根据权利要求 6所述治疗痔疮的外用药物， 还包括药剂学辅料及 辅助药物。
8、 根据权利要求 6所述治疗痔疮的外用药物， 其中， 所述栓剂为在 药剂学辅料或辅助药物外层包覆所述纳米碳颗粒制成的。
9、 纳米碳颗粒在制备治疗痔疮的外用药物中的应用， 所述纳米碳颗 粒的粒径大小范围为 1 ~ 100纳米。
10、 根据权利要求 9所述应用， 所述治疗痔疮的外用药物组成中还包 括： 分散剂和 /或液体溶剂。
11、 根据权利要求 10所述应用， 所述分散剂为木质素磺酸盐、 油酸 和鱼油中的一种或多种， 所述液体溶剂为水和 /或甘油。
12、 根据权利要求 9所述应用， 所述纳米碳颗粒来自电解法得到的纳 米石墨溶胶。
13、 根据权利要求 9所述应用， 所述外用药物为干粉剂、 水溶剂、 油 性药液、 软膏或栓剂。
14、根据权利要求 9-13任一项所述应用， 所述外用药物组成中还包括 药剂学辅料及辅助药物。
15、 一种治疗痔疮的方法， 包括给患者局部施用权利要求 1-8任意一 项所述治疗痔疮的外用药物。
16、 根据权利要求 15 所述的方法， 其中， 局部施用所述药物的剂量 为每日 6-200毫克纳米碳颗粒。
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CN104224837A (zh) * 2014-09-23 2014-12-24 贵州特力达纳米碳素科技有限公司 一种治疗外伤感染制剂及其制备方法
CN110151786B (zh) * 2019-05-06 2021-11-30 天津百纳生物技术有限公司 纳米碳颗粒在制备治疗口腔溃疡的药物中的应用及该药物

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