TWI277420B - Medicine using anemonin as active pharmaceutical ingredient for treating aseptic inflammation - Google Patents
Medicine using anemonin as active pharmaceutical ingredient for treating aseptic inflammation Download PDFInfo
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1277420 五、發明說明(1) 發明領域 本發明涉及 炎症的藥物,n ;藥領域,具體地是涉及—#、、Λ g k d *,特別是白s::及該藥物的製備方法和;; 啊素在治療無菌性炎症中的應用有效成 發明背景 醫學界才巴: 兩大類,細菌性、二,細菌性炎症J和「無菌# 起重視,大量的f症容易導致急性病症發作,、所21」 抗生辛作為右f細菌性感染藥物如青霉,::引 床,而無菌性炎症在=^ 被開發出來並陸續用於臨 能有效治療的藥物,也就异有4何特效甚至確實 物在國際醫藥界完全是办自s i K治療無菌性炎症的藥 公司生產抗無菌性炎::;效沒=何-家製藥 -般包括:頸椎病、腰椎病' 肩周炎、網球:n; 合症、風濕性關節炎、骨關節炎、肌寒骨冷、::= 腺炎、多發性神經炎、神經性皮炎、腱鞘[腰二生;列 骨頭壞死、支氣管哮喘偏:m生y義性股 菌性炎症的疫病。現代醫風研&二,疋 /、匕屬於無 入周圍軟組織,出現炎性渗出、水腫、及代謝物的 mrrr申經感受器產生祕,由椎』退 ^ \ 卜傷勞損本身及繼發的一系列病理改變引 起的無菌性炎症在肌肉、筋膜1帶、周圍神經叢、1277420 V. INSTRUCTION DESCRIPTION (1) FIELD OF THE INVENTION The present invention relates to inflammatory drugs, n; the field of medicine, in particular, -#, Λgkd*, especially white s:: and preparation methods of the drug; The application of sin in the treatment of aseptic inflammation is effective in the background of the invention. Two major categories, bacterial, two, bacterial inflammation J and "sterile # pay attention to, a large number of f can easily lead to the onset of acute illness, 21 Antibiotics as a right f bacterial infection drug such as Penicillium:: introduction bed, and aseptic inflammation in the = ^ was developed and used in the effective treatment of drugs, it is different 4 special effects or even In the international medical community, it is completely from the treatment of aseptic inflammation of si K to produce anti-sterile inflammation::; no effect = He-home pharmaceutical - including: cervical spondylosis, lumbar spondylosis 'periarthritis, tennis: n; Syndrome, rheumatoid arthritis, osteoarthritis, muscle cold bone cold:::= adenitis, polyneuritis, neurodermatitis, tendon sheath [waist two; bone necrosis, bronchial asthma partial: m y sense A disease of fecal inflammation. Modern medical research & Second, 疋 /, 匕 belongs to the surrounding soft tissue, inflammatory exudation, edema, and metabolite mrrr Shenjing sensory secret, from the vertebral vertebrate ^ \ 卜 injury itself and secondary a series of pathological changes caused by aseptic inflammation in the muscles, fascia 1 band, peripheral plexus,
第4頁 1277420 五 發明說明(2) 囊、血管壁形成的水腫和黏連壓迫脊 —^^ 根,導致頸腰椎病復雜症狀難以消除、椎動脈和神經 帶、,筋臈與肌肉牽拉是許多無菌性炎^ ?連和㉔化的知 周炎、網球肘、肌筋膜綜合症、骨=° .頸腰椎病、肩 現的原因,這些無菌性炎症所引發即尺等肌體能障礙出 但仍在摧殘著全世界數十億人的^康疾病雖多為慢性病, 發明概述 針對目前治療由於無菌性炎 固疼痛尚無有效的治療藥物的 弓丨起的各種疾病和頑 了-種可用於治療無菌性炎症的Jf明的-個目=是 括有化合物白頭於去 的樂物,其有效成分包 到,尤其可以來二化合物可以通過化學合成方法得 化合物為有效活性成八制:=原枓。臨床治療中證明以該 為病理的常見、多&刀、^的藥物對於許多無菌性炎症 障礙的疾病有顯^毛、、^7西醫报難治愈的頑固疼痛和肌體 除由無菌性炎症^的療效’能在消除無菌性炎症的同時消 腫、黏連引致的起的水腫和黏連,及由無菌性炎症、水 地治愈各種無菌^ ^疼痛和肌體障礙,從而高效快速安全 明進而提出了該白炎^疾病,並且無毒、無刺激性。本發 取物在治療無^性^翁素化合物或含有白頭翁素的天然提 化合物白頭翁素九方面的用途。本發明還提出了以該 劑型,尤其是外:有效成分的用於治療無菌性炎症的藥物 方式。 劑’提供了治療無菌性炎症的最佳給藥Page 4 1277420 Five inventions description (2) The edema and adhesion of the sac and blood vessel wall compresses the ridge - ^^ root, which makes the complex symptoms of cervical and lumbar spondylosis difficult to eliminate, vertebral artery and nerve belt, tendons and muscle traction Many aseptic inflammations and 24 weeks of periarthritis, tennis elbow, myofascial syndrome, bone = °. cervical and lumbar spondylosis, the cause of shoulder, these aseptic inflammation caused by the physical fitness of the scale But the diseases that are still plaguing billions of people around the world are mostly chronic diseases. The invention outlines the various diseases and stubborns that are currently available for the treatment of aseptic effective inflammatory pain. For the treatment of aseptic inflammation, Jf Ming is a music that contains a compound whitehead, and its active ingredient is included. In particular, the compound can be obtained by chemical synthesis to obtain an effective activity into an eight system: Original. In the clinical treatment, it is proved that the common, multi-ample, and medicinal drugs for the pathology have many ailments of the inflammatory inflammatory disease, and the intractable pain of the physiology is difficult to cure and the body is removed by aseptic inflammation. The curative effect can eliminate edema and adhesion caused by aseptic inflammation and adhesion, as well as aseptic inflammation and water treatment to cure various aseptic and painful body disorders, so as to be efficient, rapid and safe. The white inflammation disease is non-toxic and non-irritating. The use of the present invention for the treatment of a non-toxic compound or a natural extracting compound, Pulsatilla chinensis, containing pulsatilla. The present invention also proposes a pharmaceutical form for treating aseptic inflammation in this dosage form, especially the external: active ingredient. Agent' provides optimal administration for the treatment of aseptic inflammation
1^77420 ·1^77420 ·
本發明還提供了—、 中的有效成分為來自^ f療無菌性炎症的天然藥物,其 本發明同時提草藥的白頭翁素提取液。 天然藥用植物中提取=藥物的—種製備方法,尤其是從 提供的方法可使原料=^備白頭翁素的方法,通過本發明 頭翁素轉化成為盔刺:w:含的具有強烈毒副作用的原白 化生產。巧.、、、則缴性的白頭翁素’實現該藥物的工業 發明詳述 本發明提供的可 有效治療量的化合物 構式: 用於治療無菌性炎症的藥物中包括了 白頭翁素,該化合物具有如下化學結 、違化合物可以來自任何含有毛茛苷和原白頭翁素的天 然中草藥的提取物,適合的天然中草藥原料可包括毛茛科 植物、禾本科植物專。其中’毛笑科植物(況⑶此扣似 plant)包括•毛良(Ranunculus japonicus Thunb. )、馬蹄 葉(Caltha palustris L·)、石龍芮(Ramin cuius ^ceieratus L.)、打破碗花花(hupehensis Lem·)、 白頭翁(Pzx/加chinensis (Bge.) Regel )、竹節香附The present invention also provides that the active ingredient in the formula is a natural medicine derived from aseptic inflammation, and the present invention simultaneously extracts the extract of the pulverizer. A method for preparing a natural medicinal plant for extracting a drug, in particular, a method for providing a raw material=a preparation of a pulverizer from the method provided, and converting into a thorn thorn by the present invention: w: containing a strong toxic side effect The original whitening production. DETAILED DESCRIPTION OF THE INVENTION The invention provides a therapeutically effective amount of a compound configuration: The medicament for treating aseptic inflammation includes pulsatilla, the compound having The following chemically and illegal compounds may be derived from any extract of natural Chinese herbal medicine containing edulis and protothecin. Suitable natural Chinese herbal medicine materials may include ranunculaceae and gramineous plants. Among them, 'Mulberry plants (conditions (3) this buckle-like plant) include • Ranunculus japonicus Thunb., Caltha palustris L., Ramin cuius ^ceieratus L., broken bowl flowers ( Hupehensis Lem·), Pulsatilla (Pzx/plus chinensis (Bge.) Regel), bamboo scent
5163-4131-Pf.ptd 第6頁 1277420 五、發明說明(4) (Anemone raddeana Regel Ranunculus5163-4131-Pf.ptd Page 6 1277420 V. INSTRUCTIONS (4) (Anemone raddeana Regel Ranunculus
Chinensis Regel )、九節舊蒲(Anemone altaica Fisch )等, 及選自威靈仙中含有白頭翁素的威靈仙( chinensis osbeck )、山木通Unetiana Ievi et )、棉團鐵線蓮(Clematis: hexapetala 抑H )、東北鐵線 蓮(Clematis Manshurica Rupr· )、錐花鐵線蓮( paniculata )、毛落鐵象遂(Clematis cktsiandra Μΰχ/m )、柱 果鐵線蓮( Clematis uncinata champ.e:c Benth )、毛柱鐵線 蓮(Clematis meyeniana Walp )等九種,和打破碗花花的變 種秋牡丹( Anemone hupehensis Lem. var. japonic (Thunb.)Chinensis Regel ), Anemone altaica Fisch, etc., and chinensis osbeck containing pulsatilla, Unetiana Ievi et, and clematis: hexapetala H), Clematis Manshurica Rupr·, paniculata, Clematis cktsiandra Μΰχ/m, Clematis uncinata champ.e:c Benth), Clematis meyeniana Walp, and other nine species, and a variety of autumn peony that breaks the flower of the bowl (Anemone hupehensis Lem. var. japonic (Thunb.)
Bowles et Steam )等;禾本科植物中的白茅根(root of Imperata cylindrical )、含有毛笑脊()的毛笑科 鐵筷子屬(Ranunculaceae Helleborus )植物、銀蓮花族的銀 蓮花屬(乂)植物、擇耳細辛屬(价<3 )植物、毛 1族中的毛%屬(Ranunculus )、水毛 1 屬(Bratrachium )植 物、翠雀花族中的聚葉花高烏頭(Aconitum scaposum var· vaginatum )。 \ 在本發明以前的公開報導中,上述天然原料藥中都含 有毛茛苷或原白頭翁素,經臨床實驗證實具有一定的抗癌 活性,對腫瘤有抑制作用,特別是新鮮毛茛外敷治療,歷 史十分久遠,用途十分廣泛,對許多常見病如肩周炎、風 濕性關節炎,坐骨神經痛有很好的療效。但原白頭翁素有 強烈的刺激性和毒性,如使這些植物長時間與皮膚接觸可Bowles et Steam), etc.; root of Imperata cylindrical in gramineous plants, Ranunculaceae Helleborus plant containing hairy ridge (), anemone (乂) plant of the anemone family Phytophthora (valence <3) plants, Ranunculus, Bratrachium, and the genus Aconitum scaposum var · vaginatum). In the previous public report of the present invention, the above-mentioned natural raw materials contained trichostatin or protothecin, which has been confirmed by clinical experiments to have a certain anti-cancer activity, and has an inhibitory effect on tumors, especially the treatment of fresh edulis externally, and the history is very It has a long-term use and is very effective. It has a good effect on many common diseases such as frozen shoulder, rheumatoid arthritis and sciatica. However, the original pulsatilla has strong irritancy and toxicity, such as making these plants contact with the skin for a long time.
5163-4131-Pf.ptd 第7頁 1277420 五、發明說明(5) — 引起炎症,如出現紅腫和水泊笙 毛茛苷酶解脫去糖成為原白頭 > 為白頭,素的前體, 成為二聚體白頭翁素,部分原:蘂:f白頓翁素經聚合可 (多為原料藥在放置過程中產生\、、亦含有白碩翁素 葡萄球菌、鏈球菌、白喉桿菌、:? η 2羽素對於 腫瘤和抗菌消炎的臨床治;㈡用於抗 仙在臨床常用於祛風濕、活血止痛梁對乂類植物如威靈 本發明人在長期的研究您; 内的一些含有原白頭翁素的鈇起包括上述原料在 用,均對人體有刺激作用卓樂無論是内服還是外 和中毒症狀,引起噪心:在内服可引發劇烈骨腸炎 血尿、蛋白尿;與皮膚接^下瀉甚至刺激腎臟產生 該成分有很強的抗=觸起炎症如紅腫和水泡,但 溶劑,並長期放置(或加熱m科=中加入水或有機 硫酸使原白頭翁素兩分子聶人,或加乙醚、丙酮、 對於無菌性炎症各種頑固二二,上述毋副作用則消失,但 卻具有快速治愈的特效,尤:二rc功能障礙的治療 Φ 乾向透皮給藥劑型時療效極為和疼痛區採用 翁素的化學結構在此過程祜杩:μ疋原料中原白碩 即使原白頭翁素兩分子疊時發生了改變, 素。在此研究結果的基礎刺激性的白頭翁 主要活性成分用於治療& 了以白頭翁素為 脣無函性炎症的藥物,其中’所用的5163-4131-Pf.ptd Page 7 1277420 V. Description of invention (5) — Causes inflammation, such as redness and irrigating 笙 茛 解 解 解 成为 成为 成为 成为 成为 & 为 为 为 为 为 为 为 为 为 为 为 为 为 为 为 为 为 为 为Polymeric Pulsatilla, part of the original: Rui: f white sinensis can be polymerized (mostly the raw material medicine produced during the process of placing, also contains Staphylococcus aureus, Streptococcus, diphtheria, :? η 2 For the clinical treatment of tumors and anti-bacterial anti-inflammatory; (2) for the anti-celery in the clinical use of rheumatism, activating blood and relieving pain in the long-term research of the inventors of the insults such as Welling; some of the original contains the original Pulsatilla Including the above-mentioned raw materials in use, all have a stimulating effect on the human body. No matter whether it is internal or external and poisoning symptoms, it causes noise: internal medicine can cause severe eosinophilic hematuria, proteinuria; diarrhea with the skin and even stimulate the kidney to produce this ingredient There is a strong anti-inflammation that triggers inflammation such as redness and blisters, but the solvent, and long-term placement (or heating m department = adding water or organic sulfuric acid to make the original pulsatilla two molecules Nie, or adding ether, acetone, for no Bacterial inflammation is intractable, and the above-mentioned side effects disappear, but it has the special effect of rapid healing, especially: the treatment of bic dysfunction Φ. The effect of dry transdermal administration is extremely effective and the chemical structure of the pain zone is used. In this process, 疋: μ疋 raw material in the original white stalks even if the original pulverizers have changed in two molecules, the prime. The results of this study are based on the irritating Pulsatilla main active ingredient for the treatment & a drug for non-functional inflammation, in which
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1277420 五、發明說明(6) 白頭翁素可以 提取產物,gp 按照醫學 炎症包括·· § 員 合症、風濕性 腺炎、多發性 由於無菌性炎 頭痛、頑固骨 提取液做外敷 明風濕性關節 之一,其中必 在本發明 常規的鎮痛藥 果也是暫時性 相比,本發明 的藥物對各種 藥,不打針, 引,不住院, 濕敷三次即可 通過在患病部 痛 '抗炎、消 皮吸收能力, 鍵,筋膜,關 症,快速消除 療多為 推拿, 術治療 或使用 效果極 灸,不 白頭翁 療機理 白頭翁 用、及 年沉積 管壁之 筋束和 =化學合成產物,或從 =白頭翁素提取液的形 拖對各類炎症的分類, 病、腰椎病、肩周炎 郎炎、骨關節炎、肌 子經炎、神經性皮炎、 症引起的坐骨神經痛、 2、癌症疼痛、支氣管 f療三次,有的僅治療 ^丨艾性骨炎、偏頭痛 疋有無痛性炎症。 以前’對這些病症的治 ’或物理療法如按摩, 的’嚴重者需要通過手 提供的白頭翁素提取液 無菌性炎症疾病的治療 不輸液,不手術,不針 僅通過外敷治療,如用 治愈;本發明藥物的治 位靶向透皮給藥,利用 腫、解痙、分解黏連作 在極短的時間内去除多 節,滑囊,神經叢,血 水腫,破除黏連,鬆地 天然原料藥中分離的 式提供。 本發明所述的無菌性 、網球肘、肌筋膜綜 寒骨冷、無菌性前列 腱鞘炎、腰肌勞損; 足根痛、偏頭痛、偏 哮喘,使用白頭翁素 一次即快速康復,證 、技氣管哮喘的病因 在發病時服用 牵引專,而效 。與現有技術 白頭翁素製成 為顯者,不吃 推拿,不牽 素提取液透皮 在於白頭翁素 素顯著的鎮 十分強大的透 在肌肉,肌 間的無菌性炎 已有#5化的拿刃1277420 V. Description of invention (6) Pulsatilla can extract products, gp is one of the external rheumatoid joints according to medical inflammation including ·· § complication, rheumatic adenitis, multiple due to aseptic inflammation headache, stubborn bone extract In the case where the conventional analgesic drug of the present invention is also temporary, the drug of the present invention can be used for various drugs, without injection, introduction, no hospitalization, and wet application for three times to pass the pain in the affected part. Absorptive capacity, key, fascia, dysentery, rapid elimination of treatment for massage, treatment or use of extreme moxibustion, no Pulsatilla treatment mechanism for Pulsatilla, and annual deposition of wall bundles and = chemical synthesis products, or from = The classification of various types of inflammation of the extract of Pulsatillae, disease, lumbar spondylosis, scapulohumeral inflammation, osteoarthritis, myocarditis, neurodermatitis, sciatica caused by disease, 2, cancer pain, bronchial fever Three times, some only treated ^ 丨 性 osteitis, migraine 疋 have painless inflammation. In the past 'treatment of these diseases' or physical therapy such as massage, the 'serious person needs to provide the treatment of aseptic inflammatory diseases of the pulsatilla extract by hand. No infusion, no surgery, no needle only by external application, such as healing; The treatment of the drug of the present invention is targeted to transdermal administration, and the use of swelling, dispelling, and decomposing adhesions to remove multiple segments, bursae, nerve plexus, blood edema, and adhesion removal, loose natural drug substance in a very short time. The separation is provided. The sterility, tennis elbow, myofascial collateral cold, aseptic front tenosynovitis, lumbar muscle strain according to the present invention; foot root pain, migraine, partial asthma, rapid recovery using pulsatilla once, syndrome, technical air tube The cause of asthma is to take traction at the time of onset. Compared with the prior art, Pulsatilla is made, not to be massaged, and the extract is not transdermal. It is a very strong town of Pulsatilla. It is very strong in the muscle, the aseptic inflammation between the muscles has been #5化的刃
1277420 五、發明說明(7) 帶,肌肉鬆弛 成黏連的血管 到增加,從而 和血管的壓力 周炎、肱骨上 痛、偏頭痛、 勞損、骨關節 痛、腱鞘炎、 起的疼痛的目 綜合症輕壓力 勃帶黏連和約 及運動障礙也 根據本發 白頭翁素,同 使用與否或選 製藥方法,本 中,外用劑型 劑、擦劑、塗 使用合成的或 以上述天然藥 例如科學出版 頁中記載的方 劑、口服劑、 到的白頭翁素 後大量血液 擴張滲出液 使受無菌性 減輕和消除 踝炎、肌筋 頑固胃痛、 炎、無菌性 多發性神經 的,這與手 ’消除刺激 化後運動發 因無菌性炎 明提供的藥 時還可包括 擇的種類取 發明可製成 包括可被透 佈劑等多種 從天然原料 為原料按照 社出版的「 法’使Λ提 外用劑,或 提取液製成 進入肌肉而使有宝 得f y σ的代謝物如形 Γ 广:,循環改善後肌張力得 龙症刺激和壓迫的袖 刀件 達到治愈頸椎病、 知 膣Ρ人Α 腾椎病、肩 W合症、坐骨神月 關節炎、肌寒骨冷足;肌 =炎、陳舊性跌打損傷疼 術治瘅fg _广 種疾病弓丨 療頌椎病,腰椎病,肌 的原理完全一致, 嫣 斗ΛΑ Μ 肌肉’筋膜, 強力牵拉而產生的腫脹疼痛 症消除而恢復正常。 ,,其中的主要活性治療成分 ^劑^上可接受的輔劑,輔劑的 》、於藥物的最終劑型,按照常規 口服劑、注射劑和外用製劑。其 皮吸收的流浸貧劑、硬膏劑栓 劑型。該藥物中的製備可以直接 中提取分離出的白頭翁素,也可 已經公開的方法進行提取操作, 中草藥成分化學」( 1 9 77),226 純的白頭翁素結晶體製作注射 使用從含毛茛脊的天然植物中得 藥劑(其中的主要成分為白頭翁1277420 V. INSTRUCTIONS (7) Belt, muscle relaxation, adhesion of blood vessels to increase, and blood pressure, periorbital inflammation, humeral pain, migraine, strain, osteoarthritis, tenosynovitis, pain caused by the syndrome Light-stressed vaginal adhesions and dyskinesias are also based on the use of Pulsatilla, with or without the use of pharmaceutical methods, in this topic, topical agents, liniments, coatings using synthetic or natural drugs such as scientific publication pages The prescriptions, oral preparations, and pulsatilla to a large amount of blood expansion exudate to reduce the sterility and eliminate phlegm, muscle tendons, stomach pain, inflammation, aseptic multiple nerves, and the hands of 'elimination of stimulation The exercise may also include the selected type of the medicine provided by the aseptic inflammation. The invention may be made into a variety of materials, such as a translucent agent, which can be used as a raw material. The liquid is made into a metabolite that enters the muscles and causes the treasure to have fy σ, such as the shape of the sputum: after the circulation is improved, the muscle tension is stimulated and the sleeves of the muscles are compressed. The more cervical spondylosis, the knowledge of the sputum, the spleen spleen, the shoulder W syndrome, the sciatic arthritis, the muscle cold bone cold feet; muscle = inflammation, old bruises, pain, pain, treatment, fg _ wide-ranging disease The principle of sacral spondylosis, lumbar spondylosis, and muscle is completely the same. The swelling and pain caused by strong pulling of the muscles of the sacral sputum Μ 恢复 消除 恢复 恢复 恢复 恢复 恢复 恢复 , , , , , , 肿 肿 肿 肿 肿 肿 肿 肿 肿 肿 肿 肿 肿 肿 肿 肿The auxiliary agent, the auxiliary agent, the final dosage form of the drug, according to the conventional oral preparation, the injection and the external preparation, the skin absorption immersion agent and the plaster suppository dosage form. The preparation in the medicine can be directly extracted and separated. The pulverizer can also be extracted by an open method, Chinese herbal medicine chemistry" (1 9 77), 226 pure pulsatilla crystals are produced by injection from natural plants containing edgy ridges (the main ingredient is Pulsatilla)
1277420 五、發明說明(8) 發揮對盔菌性’火'广々 各化千成伤的影響而獨 ::無邊性炎症各種疾病的治療作用。::穩疋地 、w <表現在:白頭翁素提取液在各種嚴萨产、羽素的穩定 〉皿、霉變、腐爛發臭時,其對益菌性° 如高溫、低 的治愈作用不會衰減。 疒各種疾病高快逮 根據本發明優選的實施方案,該户 :天直物或令草為原'料,使用有“劑:二性:症的物 油、::醋或無機酸作浸提劑進行浸提而得取j直物 植物油、釀造醋或無機酸作用水、動、 的任何天然植物或中草藥在密封條;=碩或其 取液經過濾、澄清等精製過程,得到白頭翁素’提 使用原:有毛κ科植物其包括:^括:’ 打破碗粑花、白頭翁、竹節香附、九:^、 及選自威靈仙中含有白頭翁素的威靈仙:山:n哉 ϊ蓮毛九:花鐵線蓮、毛蕊鐵線^柱= ί禾本和打破:花花的變種秋牡丹等; 物、哿蓮m分U有毛茛苷的毛茛科鐵筷子屬植 :的植物、擇耳細辛屬植物…族 等,也可使用中藥飲片,如白頭翠:::中頭1277420 V. INSTRUCTIONS (8) To play a role in the treatment of various diseases such as infinite inflammation. :: Steady, w < manifested in: Pulsatilla extract in a variety of strict production, feather stability, dish, mildew, rot and smell, its beneficial bacteria such as high temperature, low cure Will not decay. According to a preferred embodiment of the present invention, the household: the straight or the grass is the original material, and the "agent: amphoteric: disease oil,: vinegar or inorganic acid is used for leaching" The agent is leached to obtain the water, the vinegar or the inorganic acid to act on the water, the movement, any natural plant or Chinese herbal medicine in the sealing strip; = the master or its liquid is filtered, clarified and other refining processes to obtain the pulverizer Use the original: Phyllostachys pubescens including: ^ Breaking the bowl of flowers, Pulsatilla, bamboo scent, nine: ^, and from the clematis containing the white-headed sage: Clematis: n哉ϊ莲毛九:花花莲,毛蕊铁线^柱= ί禾本和破:花花的种秋秋牡丹; 物,哿莲 m分U毛毛茛的毛茛科铁子子属: Plants , choose the ear genus genus ... family, etc., you can also use traditional Chinese medicine decoction pieces, such as Baitou Cui::: middle head
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I 5163-4131-Pf.ptd 第11頁 1277420 五、發明說明(9) 所用有機溶劑包括乙醇、甲醇、丙二 其混合物等。本發明所說的冷浸方甘油、氯仿、或 溫下用浸提劑進行浸提^本是指將原料藥在常 熱浸方法’即,將原料藥可採用 提。 Γ的次提劑中進行浸 所以本發明提供的製備方法 效的處理方法將原料藥中的原白f ^之一就在於通過有 經聚合轉化成白頭翁素: 構發生改變’ 無菌,”症有顯著療效的ίΐ翁炎仙,尤其對 度的ΐί際ii8考個慮月’優選的方案可以是採用約3〇,%濃 反的〇畔 今個月以上,式趑甘a也 ^ m ^ ^ ^ ^ A將其加熱至沸點後加入原 枓樂繼繽加熱至沸點,密封浸提6個月以上。 根據本發明的製備方本,担 部位,如新鮮毛声=;直,可選擇原料藥的有效 比例加入浸提劍;根粉碎後放入提取罐,按 ϊΐ: ίί 轉化成白頭翁素溶於溶劑中,然後 扩1=公過濾和澄清等步驟,得到黃色透明的澄清 法進行檢測)。 甲的白頭羽素可通過常規方 挺山如tΠ’本發明該優選方案的特微就在於摸索並 中的原白頭翁素在-定條件下被轉化成為 崩素的以’即使原#藥與適當㈣量的浸提劑一起 :封久放的過程。浸提劑的選擇如以上所列舉,甲醇可以 疋30%左右溪度的熱甲醇或冷甲醇,植物油可以是例如麻I 5163-4131-Pf.ptd Page 11 1277420 V. INSTRUCTIONS (9) The organic solvent used includes ethanol, methanol, propylene glycol, and the like. The immersion of the cold-immersed glycerin, chloroform or the extracting agent under the temperature of the present invention means that the raw material drug is subjected to the usual hot dip method, i.e., the raw material drug can be used. The method of the preparation method provided by the present invention is carried out by the method of the preparation method provided by the present invention. One of the raw white materials in the raw material medicine is that it is converted into a pulverizer by polymerization: a structural change 'sterile,' Significant curative effect of ΐ ΐ 炎 仙 , , , , , , , , , , , , , , , , , , , , , , , , , , , iii ii ii ii ii ii ii ii ii ii ii ii ii ii ii ii ii ii ii ii ii ii ii ii ii ii After heating it to the boiling point, it is added to the original 枓乐继彬 to heat to the boiling point, and the sealing leaching is carried out for more than 6 months. According to the preparation method of the invention, the supporting part, such as fresh hair sound = straight, the effective selection of the raw material medicine can be selected. The proportion is added to the dip sword; after the root is crushed, it is put into the extraction tank, and the ϊΐ: ίί is converted into a pulsatilla dissolved in a solvent, and then expanded by 1 = male filtration and clarification, and a yellow transparent clarification method is obtained for detection). The white-headed feather can be passed through the conventional formula, such as tΠ'. The special feature of the preferred embodiment of the present invention lies in the fact that the original protothecin is converted into a disintegrating substance under the condition of 'the original #药与适(四)量The extracting agent together: sealing for a long time Process. Leaching agent selected as listed above, may Cloth hot methanol or methanol with cold methanol 30% degree Creek, vegetable oil, for example, may be hemp
1277420 五、發明說明(10) 油、茶油、花生油等’優選使用乙醇、甲醇或水,原料藥 可以使用一種或多種混合提取。例如:按重量比計算,選 · 新鮮毛茛:乙醇約為1 : 1的比例,取鮮毛貧全草,根或僅 用全草,粉碎後裝入容器内,將適度濃度例如4〇%左右的 - 乙醇加熱後倒入裝有鮮毛茛的容P内繼續加熱,密封存 放,使毛茛中的原白頭翁素充分聚合成白頭翁素溶於溶劑 中,然後壓汁,去渣,過濾,澄清,取黃色透明澄清液即 得白頭翁素提取液;也可以按重量比計算,選新鮮毛茛: 乙醇約為1 ·· 1的比例,取鮮毛茛全草,根或僅用全草,粉 碎後裝入容器内,用冷浸法將適度濃度例如40%的乙醇或 p 30%左右濃度的甲醇直接倒入該裝鮮毛茛的容器内,密封 鲁1277420 V. DESCRIPTION OF THE INVENTION (10) Oil, tea oil, peanut oil, etc. 'Ethanol, methanol or water is preferably used, and the drug substance can be extracted by one or more kinds of mixing. For example: according to the weight ratio, choose fresh 茛: ethanol ratio of about 1:1, take fresh hair, whole grass, root or only whole grass, crushed and put into the container, the moderate concentration, for example, about 4% - After heating with ethanol, pour it into the volume P containing fresh bristles, continue to heat, seal and store, so that the original pulsatilla in the edulis is fully polymerized into pulsatilla dissolved in the solvent, then pressed, slag, filtered, clarified, taken The yellow transparent clear liquid is the extract of Pulsatillae; the fresh buttercup can also be selected according to the weight ratio: the ratio of ethanol is about 1 ··1, the whole grass is taken from the whole grass, the root or only the whole grass is used, and the container is crushed and put into the container. Inside, use a cold soak method to directly pour a moderate concentration of, for example, 40% ethanol or a concentration of about 30% of methanol into the container of the freshly colored donkey.
久放,使毛茛中的原白頭翁素充分聚合成白頭翁素溶於溶 劑中,然後壓汁,去潰,過渡,澄清,取黃色透明澄清液 即得白頭翁素提取液;也可以使用中藥飲片提取,如用中 藥威靈仙飲片、白頭翁飲片,用乙醇熱浸法或冷浸法提取 白頭翁素提取液,則按重量比計算,乙醇:藥材約3 : 1的 比例’用適度濃度例如4 0%的乙醇熱浸法或冷浸法浸潰三 至三個月,每日拌一次,使含於中藥威靈仙或白頭翁中的 白頭翁素充分溶解於乙醇中,過濾澄清即得棕色白頭翁素 提取液;若用水作溶劑,則按重量比計算,新鮮毛茛粉 細:水約1 : 1,加適量防腐劑(食品級),採用冷浸法或熱 浸法將水直接倒入裝 '有鮮毛茛粉細的容器内,密封存放\ 使毛笑中的原白頭翁素充分聚合成白頭翁素溶於溶劑中, 然後壓汁,去渣,過濾,澄清,收取黃色透明澄清液即得Long-term release, so that the original pulsatilla in the edulis is fully polymerized into a pulsatilla dissolved in a solvent, then pressed, decomposed, transitioned, clarified, and the yellow transparent clarified liquid is obtained as a extract of Pulsatilla; or can be extracted using traditional Chinese medicine pieces. For example, if the traditional Chinese medicine Weilingxian decoction pieces, Pulsatilla decoction pieces, and the extract of Pulsatillae by ethanol hot dip or cold soaking method, the ratio of ethanol: the ratio of medicinal materials is about 3:1 'with a moderate concentration such as 40% Ethanol hot dip method or cold soak method for three to three months, once a day to mix, so that the Chinese medicine Wolverine or Pulsatilla can be fully dissolved in ethanol, filtered to clear the brown pulsatilla extract; If water is used as the solvent, the fresh ranunculus powder is finely calculated according to the weight ratio: water is about 1:1, and an appropriate amount of preservative (food grade) is added. The water is poured directly into the package by the cold soaking method or hot dip method. In a thin container, sealed and stored\The original Pulsatilla in the hairy hair is fully polymerized into Pulsatilla in the solvent, then pressed, slag, filtered, clarified, and the yellow transparent clear liquid is obtained.
5163-4131-Pf.ptd 第13頁 !277420 明通過 原料中 白頭翁 «ΧΙΟ ArAr 1 * 调即成 ,所以 格限定 施方案 中草藥 配伍的 無菌性 ,本發 案,工 可以選 使用從 上所述 超臨界 離提取 無菌性 翁素化 按照常 其中, 五、發明說明(Η) 白頭翁素提取液。 需要說明的是,本發 求操作’目的在於提取出 頭翁素’並使提取出的原 得到白頭翁素提取液,經 用’或加工成需要的劑型 例在製備過程中不需要嚴 根據本發明的優選實 翁素提取液與一種或多種 素的穩定性不受多種與之 景> 響而獨立穩定地發揮對 用。長時間放置試驗表明 性在5年以上。 根據本發明的實施方 況,選擇生產的方法,即 翁素化合物為原料,也可 素提取液,提取方法除以 提取罐強制循環工藝,或 術、或中草藥有效成份分 法。 本發明還提供了治療 括治療有效量的上述▲頭 的辅劑(如果需要的話), 劑、注射劑和外用製劑。 使用適當的浸提劑按照要 所含有的原白頭翁素和白 素完全聚合成白頭翁素, 需要濃度即可供治療使 浸提劑與原料藥的加入比 〇 ,提取的白頭翁素或白頭 或化學藥混合時,白頭翁 中草藥及所含化學成份的 炎症各種疾病的治療作 明藥物中白頭翁素的穩定 業生產中可以依據實際情 擇事先合成或精製的白頭 所述原料中提取的白頭翁 還可以選用滲濾法, 萃取技術、或動態提取技 技術提取,也可使用蒸餾 炎症的藥物組合物,其包 合物,和藥劑學上可接受 規製藥方法,製成口服 外用劑型包括可被透皮吸5163-4131-Pf.ptd Page 13! 277420 Ming through the raw materials in the Pulsatilla «ΧΙΟ ArAr 1 * tune, so the grid is limited to the sterility of the Chinese herbal medicine compatibility, this case, the workers can choose to use from the above super The critical separation of the aseptic auxin is normalized according to the five, invention description (Η) Pulsatilla extract. It should be noted that the operation of the present invention is aimed at extracting the ointment and extracting the original extract of Pulsatilla, which is used in the preparation of the desired dosage form, and does not need to be strictly in accordance with the present invention in the preparation process. It is preferred that the stability of the extract of the solid and one or more of the hormones is not independently and stably utilized independently of the various effects. Long-term placement tests have shown that the sex is more than 5 years. According to the embodiment of the present invention, the method of production is selected, that is, the lysin compound is used as a raw material, and the extract is also extracted, and the extraction method is divided by the forced circulation process of the extraction tank, or the active ingredient fraction of the Chinese herbal medicine. The present invention also provides an adjuvant, if necessary, for the treatment of a therapeutically effective amount of the above-mentioned ▲ head, an agent, an injection, and an external preparation. Use a suitable leaching agent to completely polymerize the original pulsatilla and white pigment into a pulsatilla, and the concentration is required to treat the leaching agent and the drug substance. The extracted pulverizer or whitehead or chemical When mixing, the Chinese medicine of Pulsatilla chinensis and its chemical components are treated in various diseases. In the stable production of Pulsatilla, the Pulsatilla extract can be selected according to the actual conditions. Extraction by extraction, extraction techniques, or dynamic extraction techniques, or the use of a pharmaceutical composition for distilling inflammation, a clathrate thereof, and a pharmaceutically acceptable pharmaceutical method to prepare an oral external dosage form including transdermal absorption
1277420 五、發明說明(12) 型的二π «劑、硬高劑、检劑、擦劑、塗佈劑等多種劑 得到二:頭2:: 3 0 - 4 0 %濃度左右的乙醇按照本發明方法 布吸附後敷2ΐ:液:為流劑,可用於塗擦患部或以紗 算,新鮮革貧/… 右用乙醇作防腐劑,按重量比計 的乙醇直接初細:乙醇大約3 :1的比例,將濃度為95% 長時id入ί有鮮毛笑粉細的容器内充分拌句,密封 ϊ成熱:子放’使鮮毛笑中的原白頭翁素充分聚 翁飲片、=由本即传白頭翁素軟膏。用威靈仙飲片、白頭 精製成中Uif ’同樣方法提取,提取液經煎濃縮, θ i成τ樂讓、%顆粒劑(雲i 主要成份為白適當的添加劑), 病。Ϊ二:1每2=或外用於治療無菌性炎症疾 取液中約,白頭翁素=白f翁素藥液或白頭翁素提 25毫升白頭今去姆南、.笔克,每星期只需用紗布吸附約 疼痛區域透:敷貼一J在:菌性炎症各種疾病病變位置或 小時,三次為-療程?=積約為100㈣2’每次四 間即有止痛作用一次= ί就高達9〇%’短時 敷貼即可治愈,無紅腫、起療效,部分病人-次 用,安全範圍極大,毒性m水、過敏、疼痛等副作 製作流浸膏劑,硬膏劑,栓:=頭翁素藥液或提取液可 劑型,白頭翁素還可製作: ^劑,塗佈劑等多種外用 滴丸、口服液、藥酒棼。片蜊,注射劑等,亦可製成 本發明提供的藥物或藥物組 該化合物配伍而起輔助治療=中退可包括任何忐與 ’、 糸&取物。所述中藥可以1277420 V. Invention description (12) type of two π «agent, hard high agent, test agent, smear, coating agent and other agents get two: head 2:: 3 0 - 40% concentration of ethanol according to this The invention method is applied after the adsorption of the cloth 2: liquid: as a flow agent, can be used for rubbing the affected part or by the yarn, fresh leather is poor /... Right with ethanol as a preservative, the ethanol by weight ratio is directly fine: ethanol is about 3:1 The ratio will be 95% long when the id is filled into the container with a small hairy smiley powder, and the seal is smashed into heat: the child puts the original white-headed sage in the fresh hair and laughs. That is to pass the white-headed ointment ointment. It is extracted by the same method as the Uif ‘ 威 饮 、 , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , , Ϊ二:1 every 2= or outside for the treatment of aseptic inflammatory disease liquid, about 1, pulsatilla = white f yin liquid or white-headed scented 25 ml white head now to Mnan, pike, only need to use every week Gauze absorbs about the pain area: Apply a J in: bacterial inflammation, various disease lesions or hours, three times - treatment? = product is about 100 (four) 2' each time there is an analgesic effect in four rooms = ί is as high as 9〇%' short-term application can be cured, no redness, efficacy, some patients - secondary use, safety range, toxicity m water , allergies, pain and other by-products to make a flow extract, plaster, plug: = cephalosporin liquid or extract can be formulated, pulsatilla can also be made: ^ agent, coating agent and other external use pills, oral liquid, Medicinal wine cellar. Tablets, injections, and the like, may also be formulated into a drug or a drug group provided by the present invention. The compound is compatible with adjuvant treatment = the intermediate withdrawal may include any sputum and ‘, 糸 & The traditional Chinese medicine can
!277420 五、發明說明(13) 5自雞血藤、大血藤、山枝 子、路邊金等。 應該理解的是,本發明 了白頭翁素以及含有白頭翁 症中的用述,同時通過有效 頭翁素發生聚合,改變了化 實現了從原白頭翁素向白頭 對肌體特別是對皮膚的刺激 方式,有效治療無菌性炎症 斷為頸椎病、腰椎病、肩周 痛、陳舊性跌打損傷、無菌 固性胃痛、膽囊炎等辨證為 本發明通過含有白頭翁辛 各種無菌性炎症的有 物在治療無菌性炎症(疼痛 1 上,確實具有清熱解毒、舒 使用本發明作為活性成 的急毒性和長期毒性試驗, 腹腔給藥時天竺鼠的最 起動物中毒或死亡;以動物 進行皮膚給藥,未能引起動 4周’未能引起天竺鼠、體重、 腎功能、内臟器官以及皮膚 動物試驗的結果還可得 茶、岩武加、夜關門根、 鐵筷 的主要特徵就在於私 >現和接φ 素的藥物成分在治療無菌性炎 的手段促使原料中所含的原 學結構,成為白頭翁素,由於 翁素的轉&,消除了原白頭翁 性,通過外數#、底^ p r默/D療的最佳給藥 的各類病症,例如對於西醫診 火、風濕性關節炎、坐骨神經 性前列腺炎、支氣管哮喘、頑 「痒痛」者均有明顯療效,即 藥物的研究和應用,實現了對 ,經床試驗證明,本發明藥 方面療效顯著,達到8 5 %以 筋活絡、消腫止痛之功效。 分的白頭翁素提取液做了動物 結果 · 大耐受量為266 g/kg,未能引 體表面積的1 0%作為給藥面積 物中毒或死亡。連續皮膚給条 内臟系數、血象、肝功能、 的異常和病理改變。 出··本發明藥物是無刺激性、!277420 V. Description of invention (13) 5 From spatholobus, big blood vine, mountain branch, roadside gold, etc. It should be understood that the present invention has the use of Pulsatilla and the use of Pulsatilla chinensis, and at the same time, by the polymerization of the effective cephalosporin, the stimuli are improved from the original pulsatilla to the whitehead, especially to the skin. The treatment of aseptic inflammation is cervical spondylosis, lumbar spondylosis, shoulder pain, old bruises, aseptic solid stomach pain, cholecystitis, etc. The invention is based on the treatment of aseptic inflammation by various kinds of aseptic inflammation containing Pulsatilla. (In pain 1, there is indeed an acute toxicity and long-term toxicity test using the present invention as an active agent, and the most priming poisoning or death of guinea pigs during intraperitoneal administration; dermal administration to animals fails to cause motion 4 Zhou's failure to cause guinea pigs, body weight, kidney function, internal organs and skin animal test results can also be obtained from tea, Yanwujia, Yemenmengen, iron chopsticks, the main feature is the private > Ingredients in the treatment of aseptic inflammation promote the original structure contained in the raw materials, become the ginseng, due to the transfer of Mp;, eliminates the original Pulsatilla sex, through the external number #, bottom ^ pr / D treatment of the best dose of various diseases, such as Western medicine, rheumatoid arthritis, sciatic prostatitis, bronchial asthma, The stubborn "itchy" has obvious curative effect, that is, the research and application of the drug has achieved the right, and the bed test proves that the effect of the medicine of the invention is remarkable, and the effect of the muscles of the muscles is relieved, the swelling and the pain are relieved. The results were obtained from the extract of Pulsatilla chinensis. The large tolerated dose was 266 g/kg, and 10% of the surface area of the unexposed body was used as the poisoning or death of the administered area. The continuous skin gave the visceral coefficient, blood picture, liver function, Abnormal and pathological changes. The drug of the present invention is non-irritating,
5163-4131-Pf.Ptd 第16頁 1277420 五、發明說明(14) 非致敏物質,對皮膚無刺激性、無過敏反應, 用不會引起破損皮膚病理改變,故不妨礙;膚傷口 =使 有關本發明的具體實施方案和功效通過實施例進〜 說明,但本發明的實施應以權利要求書的保護範圍界二步 任何基於本發明的思想所完成的方案,即採用各種可=, 手段改變原頭翁素的化學結構,冑之聚合成為白:的 不同形式含有白頭翁素或相關成分的藥物對所 疋、…、囷性炎症的治療均應涊為是屬於本發明的 範圍。 耳施 實施例 實施例1 於四至九月採取新鮮毛茛全草及根或僅用全草,於 細’科100斤裝入陶瓷器或塑料桶,40%濃度的乙醇 加熱至沸點,然後倒入裝有鮮毛茛容器内埶 密封存放半年以上,使原白頭翁素充分聚合:白頭 於溶劑中,壓汁,去潰,過渡,澄清,取黃色透明澄清液 即得白頭翁素提取液,常規方法檢測,提取物的有效成分 中白頭翁素含量約為90%左右’用乙醇調配至每25亳升提 取液中含12· 5毫克白頭翁素,即製成外敷劑供外用治療。 或用乙醇冷浸法k 一年以上久置後提取白頭翁素提取 液05163-4131-Pf.Ptd Page 16 1277420 V. Description of invention (14) Non-sensitizing substances, non-irritating to the skin, no allergic reaction, no damage to the skin pathology, so it does not hinder; skin wound = make The specific embodiments and functions of the present invention are described by way of example, but the implementation of the present invention should be based on the scope of the claims, and any solution based on the idea of the present invention, that is, using various means, It is within the scope of the present invention to change the chemical structure of the protochrome, and to polymerize the sputum into white: different forms of the drug containing pulsatilla or related ingredients for the treatment of sputum, ..., sputum inflammation. Example of ear application Example 1 Take fresh buttercup whole grass and root or only whole grass from April to September, put 100 kg of fine powder into a ceramic or plastic bucket, heat 40% ethanol to boiling point, then pour It is sealed in a container with fresh bristles for more than half a year, so that the original pulsatilla can be fully polymerized: whitehead in solvent, pressed juice, decomposed, transitioned, clarified, and taken yellow transparent clarified liquid to obtain Pulsatilla extract, routine method test, The active ingredient of the extract contains about 20% of the pulverizer content. It is formulated with ethanol to contain 12. 5 mg of pulverulent per 25 liters of extract, which is made into an external preparation for external treatment. Or use ethanol cold dipping method k for more than one year after the long-term extraction of Pulsatilla extract 0
麵 5163-4131-Pf.ptd 第17頁 1277420Face 5163-4131-Pf.ptd Page 17 1277420
實施例2 花、2 :植:+Γ鮮毛茛、馬蹄葉、石龍芮、打破碗花 九節富蒲、打破碗花花r 香附、回回蒜、 僅用單-中草帛,採:史種秋牡丹混合後的全草及根或 獲得白頭翁素提取液,;二醇方提法或冷浸久置法 擦劑(也可用這些植物乾V提二的方法製成外敷劑或 實施例3 中藥威靈仙飲片,或威靈仙與白頭 浸提法提取獲得白頭翁素提取液,按乙醇:藥飲片,3 :‘、i 的比例,用40%濃度的乙醇加熱浸提法浸潰三個月,每日 攪拌一次,使含於中藥威靈仙或白頭翁中的白頭翁分 溶解於乙醇中,過濾澄清即得棕色白頭翁素提取液,亦可 經濃縮精製和造粒製成中藥濃縮顆粒劑。 實施例4 濃度為40%的乙醇3〇〇公 斤,用乙醇在常溫下冷浸法 使含於中藥威靈仙中的白頭 澄清即得掠色白頭翁素提取 成中藥濃縮顆粒劑。' 斤,中藥威靈仙飲片100公 浸潰六個月,每曰攪拌一次, 翁素充分溶解於乙醇中,過濾 液,亦可經濃縮精製和造粒製 本實施例也可使用白頭翁飲片或中藥烕靈仙與白頭翁 飲片兩者混合’用乙醇常溫冷浸法提取白頭翁素提取液。Example 2 Flower, 2: Plant: + Γ fresh 茛, horseshoe leaves, stone dragon 芮, break the bowl of flowers, nine sections of Fu Pu, break the bowl of flowers, fragrant, return to garlic, use only single - middle grass, mining: history The whole grass and roots of the mixed autumn peony or the extract of Pulsatillae; the glycol extracting method or the cold soaking long-time rubbing agent (the external coating agent can also be prepared by the method of extracting these plants V or the third embodiment) Chinese herbal medicine Weilingxian decoction tablets, or Clematis and white-head extracting method to obtain the extract of Pulsatillae, according to the ratio of ethanol: decoction pieces, 3: ', i, with 40% concentration of ethanol by heating and leaching method In the month, stir once a day to dissolve the pulsatilla in the Chinese medicine Clematis or Pulsatillae in ethanol, and clarify by filtration to obtain the brown pulverizer extract. It can also be concentrated and refined and granulated to form a concentrated granule of traditional Chinese medicine. Example 4 3 乙醇 kg of ethanol with a concentration of 40%, and cold immersion method with ethanol at room temperature to clarify the whitehead contained in the Chinese medicine Clematis, and then extract the pulverized pulverizer into a concentrated granule of traditional Chinese medicine. 'King, Chinese medicine Willing Xian Pie Tablets 100 immersed for six months, once every time , Weng Su is fully dissolved in ethanol, the filtrate can also be concentrated and refined and granulated. This example can also be used to mix Pulsatilla or Chinese herbal medicine Qilingxian and Baitou Weng Decoction. 'Phosphorus extraction with ethanol at room temperature and cold soaking method liquid.
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貫施例5 用水作溶劑,新鮮毛茛粉細丨〇 0公斤,濃度為9 5%的乙 醇33 f斤直接倒入裝有鮮毛茛粉極細的容器内充分攪拌均 句’ $封,加熱或常溫存放8 —丨2月以上,使鮮毛茛中的原 白,羽素充分聚合成白頭翁素,並視提取物的黏稠度加入 適$凡士林調和均勻,即成為白頭翁素軟膏。 實施例7Example 5: Using water as a solvent, fresh buttercup powder, finely pulverized with 0 kg, and a concentration of 9 5% of ethanol, 33 f kg, directly poured into a very fine container containing fresh glutinous rice powder, and thoroughly stirred, sealed, heated or at room temperature. Store 8 - 丨 for more than 2 months, so that the original white in the fresh edulis, feathers are fully polymerized into pulsatilla, and depending on the consistency of the extract, add Vaseline to make it evenly, that is, it becomes a white-headed ointment. Example 7
參照科學出版社出版的「中草藥 (1 997 ), 剛中記載的方法…頭翁全草為原料進行水蒸氣蒸 餾,蒸餾液經乙驗萃取的萃取液再用乙醇精製,製成白頭 翁素晶體(或外購),it -步製成外敷劑、口服劑、注射 劑、栓劑、擦劑等多種劑型。 實施例8 使用實施例1得到的白頭翁素提取液,配成每25毫升 含白頭翁素約12.5毫克的藥液,用無紡布浸泡後製成面積 在1 00 cm2的濕紙巾。According to the "Chinese herbal medicine (1 997) published by Science Press, the method described in the first... The whole body of the sage is steam distilled, and the extract of the distillate is purified by ethanol and refined with ethanol to make a crystal of pulsatilla ( Or purchased), it-steps are made into various dosage forms such as external preparations, oral preparations, injections, suppositories, liniments, etc. Example 8 Using the extract of Pulsatilla obtained in Example 1, it is formulated into about 12.5 per 1 ml of Pulsatilla containing 25 ml. The milligram of the liquid is soaked in a non-woven fabric to make a wet tissue with an area of 100 cm2.
實施例9 K中,授拌調配成每2 5 治療時每次外敷時間 稱取白頭翁素粉表加入到鮮毛 耄升含白頭翁素1205毫克的軟膏, 5 - 6小時。Example 9 In K, the mixture was mixed into each topical treatment time for every 2 5 treatments. The powder of white pulverizer was weighed and added to the fresh hair. The ointment containing 1205 mg of pulverizer was added for 5-6 hours.
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五、發明說明(17) 藥效學試驗 使用貫施例1的外敷劑(商品名 試驗: 一、甲醛法鎮痛試驗 觀音露 進行 以下 18122 g小鼠80隻,雌雄各半,隨機 ,、且、中濃度組、低濃度組(分別按照丨 、、且.高濃度 75毫升/25毫升、6·25毫克/25毫升給予^立克^5毫升、8. ίΒ ί 9 R i / 1规曰路)、杜冷丁 、、 克公斤)對照組(給予等量的2 5 %乙醇)。除杜冷V. INSTRUCTIONS (17) Pharmacodynamic test The external application agent of Example 1 was used (trade name test: 1. The formaldehyde method analgesic test Guanyin dew was performed on the following 18122 g mice 80, male and female, random, and Medium concentration group, low concentration group (according to 丨, , and. high concentration 75 ml / 25 ml, 6.25 mg / 25 ml to give ^ 克 ^ 5 ml, 8. ίΒ ί 9 R i / 1 gauge circuit ), Du Lengding, and grams of kg) control group (administer an equal amount of 25% ethanol). In addition to Du Leng
工組動物腹腔注射給藥外,其餘組動物均於左右後足塗抹 藥物。藥後15分鐘,每鼠右後足皮下注射2.5%甲醛〇·〇3 m 1 ’並再塗藥1次,隨即觀察丨5分鐘内小鼠舔後足的次 數0 結果:高濃度的觀音露對甲酸致痛有明顯的鎮痛作 用’小鼠舔右後足次數明顯減少,與對照組比較,ρ < 0 · ,見表1。The animals in the group were administered intraperitoneally, and the other groups were smeared with drugs on the left and right hind legs. 15 minutes after the drug, each mouse was injected subcutaneously with 2.5% formaldehyde 〇·〇3 m 1 ' and the drug was applied once more, and then the number of times of sputum hind foot in the mouse within 5 minutes was observed. 0 Result: High concentration of Guanyinlu There was a significant analgesic effect on the pain caused by formic acid. The number of right hind legs in the mice was significantly reduced. Compared with the control group, ρ < 0 · , see Table 1.
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第20頁 1277420 五、發明說明(18) 表1 觀音露對舔足反應的抑制作用(^=ST>) 组別 動物數 舔後足次錾 p值 性制率 對照组 16 15.68 土 4.13 〜s---------- 高濃度组 16 9_13 土 6.20 <0.05 42 中濃度组 16 12.44 ± 7,20 >0.05 21 低濃度组 16 13.79 ± 5.33 >0.05 12 杜冷丁组 16 0_00 ± 0.00 <0.001 100 一、 熱板法鎮痛試驗 用55 °C熱板篩選出痛反應正 =克’隨機分為4組:觀音露高濃度組^声,重 冷丁、、且、對照組,給藥方式和藥量盥甲醛法鎧 H、枉 邛和左右足塗抹藥物, 勠物均於腹 55。。熱板上,分別測定备,30 60、9〇 “里,將小氣置於 結果:觀音露言μ、鼠痛反應潛住時間。 、 小鼠痛反應潛伏時^ =度對熱板致痛有明顯的鎮痛作用, 增加,與對照組比^,顯延長’小鼠痛閾提高百分率明顯 又’ρ < 〇·05,結果見表2和表3 〇 1ϋ^ 5163-4131-Pf.ptd 第21頁 1277420' 五、發明說明(19) 表2觀音露對痛反應潛伏時間的影響(ISO) 組別 動物數 痛反應潛潛伏時間(秒) 藥前 藥後3〇分藥後分藥後9〇分 對照組 16 29.33±4.12 30.13±5.19 29.69±7.33 29.21±8.18 高泼度組 16 28.46±3.49 31.33±7.21 45.49±9.47 47.34±10.29 P >0.05 <0.05 <0.05 低濃度組 16 30.12±5.03 31.78±6.32 35.26±7.79 36.30±9.74 P >0.05 >0.05 >0.05 杜冷丁組 16 30.08±4.92 49.8615.23 54.29±9.27 58.31±11.23 P <0.01 <0.001 <0.001 表3 觀音露對痛閭提高百分率的影響 组別 動物數- 痛閾提高百分率(%) 藥後30分 藥後60分 藥後90分 對照组 16 3 1 0 高濃度组 16 10 60 66 ί農度组 16 6 17 21 杜冷丁组 16 66 80 94 三、抗大鼠足腫'脹試驗 大鼠40隻,200-250 g,雌雄兼用,隨機分為4組:高 濃度組、低濃度組(12. 5毫克/25毫升、6. 25毫克/2 5毫Page 20 1277420 V. Description of invention (18) Table 1 Inhibition of Guanyin Dew on lameness reaction (^=ST>) Number of animals in the group 舔P. 錾P value rate control group 16 15.68 Soil 4.13 ~s ---------- High concentration group 16 9_13 Soil 6.20 < 0.05 42 Medium concentration group 16 12.44 ± 7,20 > 0.05 21 Low concentration group 16 13.79 ± 5.33 > 0.05 12 Du coldding group 16 0_00 ± 0.00 < 0.001 100 I. Hot plate method Analgesic test using 55 °C hot plate to screen out the pain response positive = gram 'randomly divided into 4 groups: Guanyin high concentration group ^ sound, heavy cold Ding, and, control group, The method of administration and the amount of the drug, the formaldehyde method, the H, the sputum and the left and right feet were applied to the drug, and the sputum was in the abdomen 55. . On the hot plate, measure separately, 30 60, 9 〇 "Li, put the small gas in the result: Guanyin Luyan μ, rat pain reaction stagnation time., mouse pain response latency ^ = degree on the hot plate pain The obvious analgesic effect, increased, compared with the control group ^, prolonged 'the percentage of pain threshold increase in mice is obviously 'ρ < 〇·05, the results are shown in Table 2 and Table 3 〇1ϋ^ 5163-4131-Pf.ptd 21 pages 1277420' V. Description of invention (19) Table 2 Effect of Guanyin dew on latency of pain response (ISO) Number of animals in the group of pain response latent latency (seconds) After drug premedication 3 points after drug dispensing 9 〇 对照组 control group 16 29.33 ± 4.12 30.13 ± 5.19 29.69 ± 7.33 29.21 ± 8.18 high volatility group 16 28.46 ± 3.49 31.33 ± 7.21 45.49 ± 9.47 47.34 ± 10.29 P > 0.05 < 0.05 < 0.05 low concentration group 16 30.12 ± 5.03 31.78±6.32 35.26±7.79 36.30±9.74 P >0.05 >0.05 >0.05 Du Lengding group 16 30.08±4.92 49.8615.23 54.29±9.27 58.31±11.23 P <0.01 <0.001 <0.001 Table 3 Guanyinlu Effect on the percentage increase of pain mites - Number of animals in the group - Percentage increase in pain threshold (%) 30 points after drug administration After 60 minutes of medicine, 90 points of the control group, 16 3 1 0, high concentration group, 16 10 60 66 ί, agronomic group, 16 6 17 21, dultion group, 16 66 80 94 3. Anti-rat foot swelling, 40 rats, 200 -250 g, both male and female, randomly divided into 4 groups: high concentration group, low concentration group (12.5 mg / 25 ml, 6. 25 mg / 2 5 m
5163-4131-Pf.ptd 第22頁 1277420 五、發明說明(20) 升)、杜冷丁組(2 5毫克/公斤)、膚輕松組、對照組(給予 等量的25%乙醇)。除膚輕松組動物給予〇· 025%膚輕松軟膏 外,其餘組動物均於左右後足塗抹藥物。於每鼠右後足足 瓶皮下注射1 %角叉菜膠〇 · 1 m 1,隨即給右後足塗抹藥物。 分別於給藥後2、3、4、5小時測量每鼠左右後足足跖周 長’以兩足周長差作為腫脹度。每次測量後分別再給大鼠 右後足塗抹藥物。 結果:高濃度觀音露對大鼠足腫脹有明顯的抑制作用, 與對照組比較’ P〈 〇 · 〇 5。見表4。 表4觀音露對足腫脹的抑制作用(适^功 組別 動物數- Μ脹度(cm) 2小時 3小時 4小時 5小時 對照組 10 1.44±0.21 1.48±0.13 1.47±0.19 1.45±0.13 高濃度組 10 1.24±0.23 1.01±0.17 0.97±0.21 0.92±0.18 p值 >0.05 <0.05 <0.05 <0.05 低ί農度組 10 1.37±0.19 1.36±0.21 1.3S±0.24 1.40+0.14 ρ值 >0.05 >0.05 >0.05 >0.05 廣輕松·組 10 0.91 ±〇.2〇 0.92±0.13 0.90+0.18 0.92±0.24 ρ值 <0.01 <0.01 <0.01 <0.015163-4131-Pf.ptd Page 22 1277420 V. Description of invention (20) liter), Du Lengding group (25 mg/kg), skin relaxing group, control group (administer an equal amount of 25% ethanol). The animals in the skin-releasing group were given 〇·025% skin relaxing ointment, and the other groups of animals were applied with drugs on the left and right hind legs. Apply 1% carrageenan 1 1 m 1 to the right hind foot of each rat and then apply the drug to the right hind foot. The circumference of each foot was measured at 2, 3, 4, and 5 hours after administration, respectively, and the difference in circumference between the two feet was used as the degree of swelling. The rats were given a drug to the right hind paw after each measurement. RESULTS: High concentration of Guanyin dew had a significant inhibitory effect on paw swelling in rats, compared with the control group 'P< 〇 · 〇 5. See Table 4. Table 4: Inhibition of foot swelling by the Guanyin dew (the number of animals in the appropriate group) - swelling degree (cm) 2 hours 3 hours 4 hours 5 hours control group 10 1.44 ± 0.21 1.48 ± 0.13 1.47 ± 0.19 1.45 ± 0.13 high concentration Group 10 1.24±0.23 1.01±0.17 0.97±0.21 0.92±0.18 p value>0.05 <0.05 <0.05 <0.05 Low Degree of Agriculture 10 1.37±0.19 1.36±0.21 1.3S±0.24 1.40+0.14 ρ value> ;0.05 >0.05 >0.05 >0.05 Widely relaxing ·Group 10 0.91 ±〇.2〇0.92±0.13 0.90+0.18 0.92±0.24 ρ value <0.01 <0.01 <0.01 <0.01
四、天竺鼠離體、腸肌試驗 天竺鼠4隻,300_350 g,雌雄各2隻,處死後立即取 出迴腸,放入充氧的冷Tyrode’ s液中,沖淨後將腸管剪成4. Tests of guinea pig in vitro and intestinal muscles 4 guinea pigs, 300_350 g, 2 males and 2 females. Immediately after sacrifice, the ileum was taken out and placed in oxygenated cold Tyrode's solution. After rinsing, the intestines were cut into
5163-4131-Pf.ptd 第23頁 1277420, 五、發明說明(21) 2-2. 5 cm的腸段。將兩腸段兩端穿線接扎,一端繫於通氣 鉤上,放入恆溫麥氏浴槽中,另一端繫於拉力換能器上, 連接記錄儀。分別記錄加入觀音露、乙醯膽鹼(1 〇_9)和阿 托品(0 · 0 5% )後腸肌的收縮和舒張情況。 結果··觀音露高濃度對乙醯膽鹼興奮狀態下的腸肌有 明顯鬆弛作用。5163-4131-Pf.ptd Page 23 1277420, V. Description of invention (21) 2-2. 5 cm intestine segment. The two intestine segments are threaded at both ends, one end is attached to the venting hook, placed in a constant temperature Mail's bath, and the other end is attached to a tension transducer to connect to the recorder. The contraction and relaxation of the intestinal muscles were recorded after the addition of Guanyin, acetylcholine (1 〇 _9) and atropine (0 · 0 5%). Results · The high concentration of Guanyin dew has a significant relaxing effect on the intestinal muscles under the excitatory state of acetylcholine.
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