201270 A 6 B 6 經浒部屮央榣準局A工消费合作社印製 五、發明説明（1 ) 本發明偽鼷於性傳染疾病的預防，尤其如愛滋病之類 ,本文以後将用其通常略說語"STD”來表示性傳染疾病 〇 最普遽的STD待別是由於某些病毒Λ細豳、寄生病原 體和真®所引起的。面S這些疾病的Μ延，至今邇沒有 任何足夠有效的預防措施，亦不可能提供對使用保險套 的變換方法，況且人們知道造些預防措施有缺點，使用 亦不便。 事簧上，我們知道某些不同的化學蕖對於引起 STD的病_而言，是具一定果效的，其中最常用的蕖物 ,包括二甲基烷基苄銨氨化物，或氨化苄烷銨、以及士 基粉聚氣乙嫌化合物，或nonoxynol 9。 然而，這些化合物只具有相對的效果，一方面由於它 們僅對引起STD的某些病睹有效，其作用範園狹窄，另 一方面，它們作用所需要的時間長，因而：當用作STD 的預防時，它們是不合適的。 例如，以愛滋病毒和正常黏膜發生沾染的開始幾分》 起，其病毒就可侵入《内。相反，IX濃度的氯化节烷》! 對病《的失活化作用.只有在至少+分fil接《病薄後才 能實施，逭段時間可能會引起联里的沾染。因此，逭種 方法在實際上是不被人接受的。 因此，應用已知的産品不能有效的預防STD ,卽使它 們具有抗病毒的活性，也是如此。 (請先閲讀背面之注意事項再填寫本頁) 裝· *可_ 線- 201270 Λ 6 Β 6 經濟部屮央橾準局β工消费合作社印製 五、發明説明（2 ) 另外，根據歃洲專利ΕΡ-Α-0 113998資料，可以知道 某些膽酸衍生物；主要為脱氣膽酸和脱氫膽酸，可應用 .於治療由Herpes SiBP lex I或1[病毒引起的感染。 然而，此乃涉及治療作用，而非預防作用的問題，而 本發明的目的，確切地是為了提供一種預防措施。在治 療和預防之間界限並不是說是明確的。但是，在此對逭 二種作用方式之間加以區別是主要的，因為S擇何種條 件，它可以決定所用藥物組成的成份、治療或預防的實 施方式、藥物形態、其給藥方式以及使用範匾。治療作 用，正如在歐洲專利ΕΡ-Α-0 113998中所評估的那樣， 與涉及正常人醴的預防作用不同，它是在己經被損害機 體上發揮其效果的。在這些情況中感染是可見的，至少 可測到的，但已被明確診斷後，這些病人可以接受治療 。於是，很明確地診斷Herpes Sinp丨cel或I病棄感染 的部位必須加以治療，並可採用局部治療的方式。 可考嫌兩種給藥方式：非經腸爾道途徑或局部施用途 徑.即在感染的確切部位上非常局限地用藥。 在本發明中，局部給槩方式意味著《用一種藥物組成 物，不局限於明顯感染而K格劃分的匾域，而相反地應 用在一寬*的E域.通常是後合性範園，且始終不確切 的，因為痛要預防的感染不是局限的。因此，在治療例 子中以及在歐洲專利EP-A-0 113998(對己經明確感染的 部位進行治療）中所應的”局部用藥"的含義不應和逋裡 (請先閱讀背面之注意事項再塡寫本頁) 裝- 線_ -4 - 201270 A 6 B 6 經濟部屮央橾準局β工消赀合作社印製 五、發明説明（3 ) 預防情況下使用的相同名稱加以混淆。追裡的含義，正 如上述，是完全不同的。 另外，對於預防STD目的而言，局部施用途徑較非經 賜胃道途徑為佳。逭是由於目前某些_物具有實際效果 ，但它們不蠹被引入機藤内。事實上，酋它們在大劑量 被吸收時變成有毒的物質，然後被機賭新陳化謝掉。 最後，須指出的，在歐洲專利ΕΡ-Α-0 113998中僅 Herpes Simplex I和1Γ被提及，而本發明是預防引起 STD的廣譜病表，其中主要病毒的種類，例如為： ----生殖性Her pes I及I病毒 ----愛滋病HIV I及HIV Π病毒 ----B型肝炎病毒 ——乳實狀《病 為此，本發明涉及廣泛複雜匾域的保薄。 至於歃洲専利ΕΡ-Α-0 113998,其介紹的内容並不鼓 勵内行人使用譫酸衍生物任何一種： 一方面.對於在數小時内能起有效的預防作用而言， 它必需把一傾均勻足夠藥劑量的形式的藥物組成物*用 在一鏑不明確限定的E域上，或者在正常而易沾污的部 位，或者已被感染的，且易沾污對方的部位。 另一方面，對於對《[於Herpes S丨hpUx細胞不間表現 的廣_病*言.其作用範園是非常普通的。 陰道是鲇膜類組嫌，一些物霣自然地易於通遇，或者 —5 - (請先閲讀背面之注意事項再塡寫本頁) 裝· *ΐτ- 太认後R泞iA m Ψ Κ Η它i,ti达（CNS) Ψ4姐枋（210乂297公货） 201270 A 6 B 6 經濟部肀央橾準局貝工消费合作社印製 五、發明説明（4 ) 向體外擠泄，或者被鳢内器官吸收。 然而，對於有效預防STD來說，一種或多種活性成份 _不應被機賭所吸收的，特別不能通過陰道黏膜。 事實上，至今人們邇不可能應用某些藥物來達成此預 防目的雖然這些藥物是有效的，但它們能在釀内器官很 快地擴散吸收。 於是.本發明涉及包含一種或多種對STD具有效預防 作用的活性成份的槩物組成物。 本專利發明同樣涉及一項能通過局部用藥來保_如處 女陰道那樣高度危險部位的藥物組成物。 ^為此，本發明目的是提供製備一種預防因黏膜接觸而 引起性傳染疾病的藥物組成物，其特微在於包括：一方 面，至少一種能對抗引起上述性傳染疾病病毒或細菌的 活性成分，B —方面.一種抑制上述活性成分滲透通過 黏膜的試劑，與_理許可的且適合於此組成物的局部給 藥途徑的賦形劑相配合。 本發明内容將由詳細介紹的、淸楚而非對其限制的例 子來描述。 滲透抑制劑是一_惟性而無毒的試劑，且易形成一鹤 隔離性薄禊，也是黏膜或皮虜上保護性膜。 另外，為了足夠程度地抑制滲透，應自陰道口起加以 有效的保讓，且覆蓋整傾黏禊.疽足很_實現的，因為 後者有許多折叠牖蔽處。 -6- (請先閱讀背面之注意事項再填寫本頁) 裝· 線- 太认？6 R 泞 i* m Ψ 因 H ’dtilMCNS) H74ta^i21fly297公-好） 經濟部屮央槛準而只工消费合作社印製 20似Ο Λ6 _Β_6_ 五、發明説明（5 ) 根據本發明的藥物組成物，有利地含有一種惰性無毒 試劑，它能分散一種或一些活性成分，以得到上述藥物 組成物的足夠劑量，均勻的塗藥。 在本發明組成物中採用的滲透抑制雨和分散劑最好是 由相同化合物組成.尤其是矽酮屬化合物。 根據本發明的藥物組成物含有膽酸鹽可作為所臁用活 性成分的一籲例子。 眾所皆知，膽酸是膽汁中天然成分，及其藥理許可鹽 ，實際上鼴用於臨床用做為利膽蕖劑。 根據歐洲專利申請ΕΡ-Α-0 285285,其中所介紹分散 劑的應用，正如所有能在水性介質中降低界面張力的試 劑。它和膽酸配合使用，可以治療赛性感染。知道病泰 利用它所寄生的细胞蛋白質在其核酸（DKA或RHA)鍵四周 形成一艢外殼。在歟洲專利申謓EP-A-0 285285,中 提出的分散劑，其抗病毒作用在於斷裂病毒的外敕，使 其不再侵犯其他细睢，因此而被消滅。 逭裡重要的是使其明確.即具有以上作用的分散劑是 包含在經非腸苗道途徑給槩的第物組成物之中，含上述 分敝劑的藥物組成物是直接注射到循環之血掖中。 根據本發明的藥物組成物中，和一種或多種活性成分 結合的分敝劑，其作用是完全不同於上述情況。 逭裡，事《上逭匍分散劑不直接干預病毒.逭不同於 上述專利所介紹的分散_。 -7 - (請先閲讀背面之注意事項再填寫本頁) 裝. 訂· 線· 太认牦Rm Ψ囚03 Ψ4拟格（210x297公货） 經濟部屮央標準局KX工消費合作社印製 201270 Λ 6 _Β_6_ 五、發明説明（6 ) 根據本發明的组成物是指定通通局部途徑來給藥的， 造不同於歐洲專利申請ΕΡ-Α-0285285,敘述的給藥方式 (非經腸胃道途徑和口服）。 在本發明的ffi成物中所含有的形成薄膜試爾，其主要 待性是在所有需保譜的區域表面上形成一傾均勻而隔離 的膜，它可發揮屏障的作用。 --它抑制活性成分滲透入機體，防止在醱内新陳代謝 掉，在塗藥後，可保持上述活性成分發揮作用所痛的時 間〇 --它防止引起STD的病棄通過黏膜向其他部位擴散。 因此，致病性病毒被保持和活性成份進行接嫌，後者可 將其殺死。 --它的隔離和保護作用是雙重的；一方面，它保護健 康的嫌女避免被同伴患者可能引起的病竃沾染，另一方 面，當婦女已患病的情況下，它亦以同樣隔離效果來保 謾對方。 形成薄膜試劑和分敝劑的二者效果之間配合，可以在 構成陰道黏膜的皺襞所有表面上形成一種薄醭。 本專利的_物組成物中應用的膽酸鹽，較佳為膽酸納 〇 膽酸納是一種強殺病毒和殺細®的藥物。此化合物S 生物物質，不具毒性，甚至在小劑*時亦有殺《活性。 本發明藥物組成物中所用的膽酸納的劑最，較有益的在 -8- (請先閱讀背面之注意事項再填寫本頁) 裝- 訂 線- 太认铬尺泞ifi 1?! Ψ K a定ita(CNS) Ψ4姐松（2丨0乂297公好） 201270201270 A 6 B 6 Printed by A Department of Consumers and Cooperatives of the Central Bureau of the Ministry of Justice, V. Description of the invention (1) The present invention is false for the prevention of sexually transmitted diseases, especially such as AIDS, which will be used in this article. Say " STD ”to indicate sexually transmitted diseases. The most common STDs are caused by certain viruses such as larvae, parasitic pathogens and Zhen®. In the face of these diseases, there is not enough to date Effective preventive measures can not provide a conversion method for using condoms, and people know that there are shortcomings in making these preventive measures, and it is also inconvenient to use. It is said to be effective, and the most commonly used medicaments include dimethyl alkyl benzyl ammonium amide, or benzalkonium amide, and Shiji powder polymethine, or nonoxynol 9. However, These compounds only have relative effects. On the one hand, because they are only effective against certain diseases that cause STD, their scope of action is narrow, on the other hand, they take a long time to act, so: when used as a prevention of STD , They are not suitable. For example, from the beginning of the infection of HIV and normal mucosa, the virus can invade "inside. On the contrary, IX concentration of chlorinated benzane"! Chemical effect. It can only be implemented after at least + minutes of connection to the disease, and it may cause contamination of Lianli in a short period of time. Therefore, the seeding method is actually not accepted by people. Therefore, use known products Can not effectively prevent STD, so that they have anti-viral activity, too. (Please read the precautions on the back before filling out this page) 装 · * 可 _ 线-201270 Λ 6 Β 6 Ministry of Economic Affairs Printed by β Industry Consumer Cooperative V. Description of invention (2) In addition, according to the data of Pizhou Patent ΕΡ-Α-0 113998, we can know certain cholic acid derivatives; mainly degassed cholic acid and dehydrocholic acid, which can be applied . In the treatment of infections caused by Herpes SiBP lex I or 1 [virus. However, this is a problem involving therapeutic effects, not preventive effects, and the purpose of the present invention is precisely to provide a preventive measure. In the treatment and prevention Between boundaries and It is said to be clear. However, the distinction between the two modes of action is the main one here, because S chooses what conditions it can determine the composition of the drug used, the implementation of treatment or prevention, the form of the drug, The method of administration and the use of plaque. The therapeutic effect, as evaluated in European Patent ΕΡ-Α-0 113998, is different from the preventive effect involving normal human sweets, it exerts its effect on the already damaged body In these cases, the infection is visible and at least measurable, but after a clear diagnosis, these patients can receive treatment. Therefore, it is very clear that the site of infection of Herpes Sinpícel or I must be treated. , And can use local treatment. Two methods of administration can be considered: non-enteric route or topical application. That is, the drug is very limited to the exact site of infection. In the present invention, the local administration method means that "with a pharmaceutical composition, it is not limited to the plaque domain divided by the K grid with obvious infection, but is instead applied to a wide * E domain. It is usually a post-combination model. , And is always inaccurate, because the infection to be prevented by pain is not limited. Therefore, the meaning of "topical medicine" in the treatment example and in the European patent EP-A-0 113998 (treatment of a site that has been clearly infected) should not be in harmony (please read the notes on the back first Matters will be written on this page) Installed-Line _ -4-201270 A 6 B 6 Printed by the Ministry of Economic Affairs, Central Bureau of Industry and Commerce, βWork Consumers Cooperative Co., Ltd. 5. Description of the invention (3) The same name used in the case of prevention is to be confused. The meaning of chali, as mentioned above, is completely different. In addition, for the purpose of preventing STD, the topical route is better than the non-gastrointestinal route. It is due to the fact that certain substances have practical effects, but they The codling was introduced into the machine vine. In fact, the chieftains became toxic substances when they were absorbed in large doses, and then they were discarded by machine gambling. Finally, it should be pointed out that in the European patent ΕΡ-Α-0 113998 only Herpes Simplex I and 1Γ are mentioned, and the present invention is to prevent the broad spectrum of diseases caused by STD. The main types of viruses are, for example: ---- Reproductive Her pes I and I virus ---- AIDS HIV I and HIV Π virus-Hepatitis B virus-milk For this reason, the present invention relates to the preservation of a wide range of complex plaque domains. As for Shizhou Zili ΕΡ-Α-0 113998, the content of its introduction does not encourage any expert to use any of the derivatives of delanoic acid: On the one hand. For effective prevention within a few hours, it is necessary to apply a pharmaceutical composition in the form of an even and sufficient dose of medicine * on an undefined E domain, or in a normal and easily contaminated area, Or it has been infected and easily contaminates the other party's part. On the other hand, it is very common for the wide range of diseases that are not manifested in Herpes S 丨 hpUx cells. Its role is very common. The vagina is catfish Membrane group is suspected, some things are naturally easy to encounter, or -5-(please read the precautions on the back before writing this page) installed · * lτ- after recognition, R 択 iA m Ψ Κ Η 其 i, tiDa (CNS) Ψ4 elder sister (210 to 297 public goods) 201270 A 6 B 6 Printed by the Ministry of Economic Affairs of the Central Bureau of Industry and Fisheries Beigong Consumer Cooperatives V. Description of invention (4) Squeezed out of the body, or internal organs of snakeheads Absorption. However, for effective prevention of STD, one or more active ingredients should not be The gambling can not be absorbed through the vaginal mucosa. In fact, it has not been possible to use certain drugs to achieve this prevention purpose. Although these drugs are effective, they can quickly diffuse and absorb in the internal organs. The present invention relates to a chamotte composition containing one or more active ingredients having an effective preventive effect on STD. The invention of the present patent also relates to a pharmaceutical composition that can protect _ highly dangerous parts like virgin vagina by topical administration. Therefore, the object of the present invention is to provide a pharmaceutical composition for preventing sexually transmitted diseases caused by contact with mucous membranes. Aspect. An agent that inhibits the penetration of the above active ingredient through the mucosa, and is compatible with excipients approved by the law and suitable for the topical route of administration of the composition. The content of the present invention will be described by the examples introduced in detail and not by limitation. Penetration inhibitor is a unique and non-toxic reagent, and it is easy to form a thin, isolated, and protective film on the mucous membrane or skin. In addition, in order to suppress penetration to a sufficient degree, it should be effectively guaranteed from the vaginal opening, and covered with the inclination and stickiness. The gangrene foot is very achievable, because the latter has many folding and covering places. -6- (please read the precautions on the back before filling in this page) 装 · 线-Too recognition? 6 R 泞 i * m Ψ Due to H'dtilMCNS) H74ta ^ i21fly297 (good-)) The Ministry of Economic Affairs, the central government ’s standards, only the industrial and consumer cooperatives printed 20 similar Ο Λ6 _Β_6_ V. Description of the invention (5) The composition of the drug according to the present invention The substance advantageously contains an inert non-toxic agent that can disperse one or some active ingredients to obtain a sufficient dose of the above-mentioned pharmaceutical composition for uniform application. The penetration-inhibiting rain and dispersant used in the composition of the present invention are preferably composed of the same compound, especially a silicone compound. The pharmaceutical composition according to the present invention contains cholate as an example of the active ingredient used. As everyone knows, bile acid is a natural ingredient in bile and its pharmacologically approved salt. In fact, mole is used clinically as a gall bladder. According to the European patent application EP-Α-0 285285, the application of the dispersant described therein is just like all agents that can reduce the interfacial tension in aqueous media. It is used in combination with bile acid to treat race infections. Knowing that Tyrant uses its parasitic cell protein to form a shell around its nucleic acid (DKA or RHA) bond. The dispersant proposed in EP-A-0 285285, patented by Xizhou Patent, has an antiviral effect that breaks the outer virions of the virus, so that it no longer infringes on other fine eyes, so it is eliminated. The important thing is to make it clear. That is, the dispersing agent with the above effect is included in the composition of the substance given to the intestine through the non-intestinal tract, and the pharmaceutical composition containing the above-mentioned dispensing agent is directly injected into the circulation. Blood tucked in. In the pharmaceutical composition according to the present invention, the effect of the splitting agent combined with one or more active ingredients is completely different from that described above. Weili, the matter "Shangyao dispersant does not directly interfere with the virus. Weishi is different from the dispersion described in the above patent." -7-(Please read the precautions on the back before filling in this page) Packing. Order · Thread · Taiyin Rm Ψ Prisoner 03 Ψ4 draft (210x297 public goods) Printed by KX Industrial and Consumer Cooperatives, Bureau of Standards, Ministry of Economic Affairs, 2012 Λ 6 _Β_6_ V. Description of the invention (6) The composition according to the present invention is prescribed for administration via a local route, which is different from the European Patent Application EP-Α-0285285, which describes the mode of administration (non-gastrointestinal route and oral). The thin film forming agent contained in the ffi product of the present invention has the main requirement of forming a uniform and isolating film on the surface of all areas where spectrum preservation is required, and it can act as a barrier. -It inhibits the penetration of active ingredients into the body and prevents metabolism in the body. After application, it can maintain the time for which the above active ingredients are painful.-It prevents the spread of STD disease to other parts through the mucosa. Therefore, the pathogenic virus is kept in contact with the active ingredient, which can kill it. -Its isolation and protection are twofold; on the one hand, it protects healthy suspects from contaminants that may be caused by companion patients; on the other hand, when women are already ill, it is also isolated Effect to protect the other party. The combination of the effects of the thin-film forming agent and the split agent can form a thin layer on all surfaces of the folds constituting the vaginal mucosa. The bile salt used in the composition of this patent is preferably sodium cholate. Sodium cholate is a strong virus-killing and cytotoxic drug. This compound S biological substance is not toxic, and it has killing activity even in small doses *. The sodium cholate agent used in the pharmaceutical composition of the present invention is the most beneficial. It is more beneficial at -8- (please read the precautions on the back and then fill out this page) Packing-Strapping-Too chromium ruler ifi 1 ?! Ψ Ka Dingita (CNS) Ψ4 sister loose (2 丨 0 侂 297 public good) 201270
Λ 6 Β 6 五、發明説明（7 ) 0 . 2 - 1 . 5 X範圍，較 根據本發明的目 甲基聚矽氣烷，其 的隔離效果。 根據本發明目的 氣烷的置，是在组 依照本發明，可 較，形成薄膜試剤 此乃由於追求薄 有範圍（在陰道黏 而且為了得到有效 即逹到以下兩锃目 --減少（而我們 性，谙是致病因子 --避免輿薄膜结 所述部位上保留了 佳在组成物绝重董的0.25和U之間。 的較佳的形成薄膜試和分敗劑是二 同樣具有抗黏附效果，因而增強薄膜 在藥物组成物中所含有的二甲基聚矽 成物缌重量的3·5χ範圍内。 以注意到，輿活性成分的所用置相比 的量是很大的。 膜的形成，不僅要在受保護表面的所 膜的例子中這是大的表面）上》施， 的隔雎屏障效果，成膜應足夠緊密， 的： 希望完全阻止）致病因子轉移的危險 或來至鲇膜，或朝向鲇膜方向。 合的活性成分被fc膜所吸收，因此在 活性成分.那裡其局部作用足必要的 η 先 閱 讀 背 面 之 事 項 再 ή 本 裝 線 經濟部十央找準XJA工消货合作社印^. 0 於合 體 成 合適 掖 形 《 劑 然 為 .铤 天 因 c ϋ - 和 是高用中 可 逭增習子 . ，於足例 性 少向ββ的 鲇 滅傾擴腴 具 要而物鲇 其 不加椠道 . 而增的險 體 ,度接誤 0 些濃可保 性 加劑.在。水 增式的，用擇 可著明fie使 S 定随®縝部好 0 ，本的内最 用果於蕖和人 使效合用期行 此的適部長内 膜 局於 i<6 R /i ii m Ψ Η K it m i CNS) Ή 4 Wf 21 n y 297it) 經濟部屮央#準工消赀合作社印製 201^0 A 6 _B 6 五、發明説明（8 ) 進行稀釋。 根據本發明組成物優先考慮的實施方法，可以含有如 _鹽酸類缓衝劑，以調整pH為4.7左右，這姮pH值可以不 影雄陰道内g族和多徳W ( D 〇 e d e r 1 e ί η )捍g。不破壤多 徳蘭桿菌是很重的。因為它具有對抗生殯糸統感染的重 要保護功能，所以必箱保留這些菌種。 根據本發明的_物組成物可呈現溶液（陰道沖劑）、乳 劑、凝謬等形式。 内行人可S擇一種適合於預定提出的可接受的_物摘 體。 本發明的组成物所呈現出的形式，是輿使用方式相鼷 的。另外，這_組成物應具有適合於使用方式的黏度。 為此目的，本發明的藥物組成物另外包含一種增櫊劑 ，它使能播得合睦的流變學行為。 在習用的增稠劑中，本發明優先考«的是羥丙基甲基 繼維素，以其商品名” Methloes 60 SH 4000”由SEPPIC 公司（法國，巴黎，香舒利大街70號）出售。 此增稠劑可調節黏度，直至適合於組成物形式的最佳 程度（溶液、乳劑、凝®等）。如此得到的貼度，在製備 第物組成物遇程中pH不同時；亦不發生明顯的變化。 在以後的敍述的應用例子中能更好地理解迪傾試《的 重要性。 根據本發明的藥物組成物.其濃度最常用劑量嫌納在 -1 0 - (請先閱讀背面之注意事項再塡寫本頁) 裝· 訂_ 線_ 太认汴尺泞1Λ Ψ K H 姐柊m〇x297公分） 201270 修正於 補充 Λ 6 ,, Β 6 五、發明説明（9 ) 表I中： --0.25-1J：重量比例的腾酸納。 _ --3·5 3：重置比例的二甲基聚矽氧烷。 --43；重量比例的羥丙基甲基餓雒素。 --鹽酸：調整至pH-4.7所必需的量。 --水：加到100Χ所裔的童。 根據本發明的更精心擬定的實施方式，將數種活性成 分配在一起；尤其可增強轚酸銷的作用，待別對某茔細 菌的作用。 因此，根據本發明的組成物可含有一種或多種另外具 有殺精子作用的抗病毒和抗细®藥物與瞭酸銷和成禊劑 、分散劑结合。在這些抗病毐、抗细®和殺精子藥物中 ,較佳為氮化苄烷銨及/或nonoxynl 9。 瑄裡可注意到，K用nonoxynol 9的可能性說明了本 發明所帶來的®點。事實上，酋大劑贵η ο η ο X y η 〇丨9縿 透入機腌内，可形成某空毒性，逭由於它主要積聚在聚 釅内。另外，它穿透陰道鲇膜能力可提离到80Χ左右。 然而.根搣本發明的组成物中應用nonoxynol 9S完全 可能的及没有危險性，此多虧在此組成物中所含有的成 睽削形成一《隔_薄禊之故，上述成睽ffl亦足一棰對抗 活性成分躱透入機體内的抑制削。 對於氮化苄烷枝和η ο η ο X y η ο丨9來説，所用的劑置較 佳為在組成物绝重ft的0.5-13：和0.25-15!的茧懂比例之 -η - (請先閲讀背面之注意事項再填寫本頁) 裝. 訂 經濟邰屮央梂芈乃Μ工消赀合作社印3i 太认认 R 冷 Li rn Ψ ffi K 婭以（210乂297公讣） 201270 修正81.1 •本年月曰 補充 Λ 6 13 6 五、發明説明（工〇) 間 成 组 有 含 物 成 組 物 藥 之 的 ： 目的 明.明 發説 本所 於 I 合表 適下 別如 待為 , 佳 是較 於 ， 置 9 。素量 1 ^ ^ W o R Μ yn*織需 X ^ 必 0X& 基& n5g3s所 no基 7 基 4 例 S S B-HH4 fchbfcfcfc二丙 P X s i I 3 羥至0¾ 量量量的？？ ο Eltlwb 的整 1 .v, 3 3 -j-i 表 xxxifcb調到 Π 有它 Ills _ _ - I 量：加表常 ， 5 ο 5 3 r . ί 252Χ 重酸：述非上 • U 鹽水上得寅 __ I 依楢事 能 。銨 納烷 酸苄 臛化 的氛 和 Ο 〇 性 D 的 0 ^ ^ 待防细 其預和 於於子 由合精 -適 ’ 物別毒 '成恃病 组故抗 。物，對 量藥用時 的的作同 需施護是 所» 保用 例的作 比效的 且病 而述 -上 化在 活 0 去效 失有 毒搛 病同 的 ， 有其 D 和 Τ ! S2B: 與细類 使的幾 地關下 C 效有以10 有D述hy C3 T - P 闭 S 弓 a 儀輿可St 不茔 .* 它那中 對阌 Π ΰ 球 0 ) 色閑 黄珠 金念 S 色 Θ 白 Γ ( u S a η a s c u i c b ο 1 (請先閱讀背面之注意事項再填寫本頁) 裝 訂 線. 經濟部十央找半iJM工消t合作社印製 s u c 閉 球 m 乳 無 M 氏 0 奈 病 /(\ e a e ο h Γ Γ ο η ο n Π Γ ϋ nal s a n o re o 蟲 滴 0 陰 太认讣尺冷J ΙΠ屮β 03 丨0><297公炒） 201270 Λ6 _B6_ 五、發明説明（11) 在表I中的组成物中合併的三種活性槩劑，以相互補 充的方式來發揮作用，因而具有很廣》的活性。 , 例如，nonoxynol 9對 Chlamidia Trachomatis (沙眼 依原體）有效，然而它可引起Candida Albicans(白色念 珠菌）感染的鼹重擴散。而在细成物中同時出現的氨化苄 烷銨，對Candida Albicans (白色念珠菌）具有非常明確 的作用。 為了預防STD.根據發明的_物組成物，可方梗地輿 陰道栓塞結合使用，如同發明者在法國專利FR-A-2614525 中所介紹的。這傾栓塞彌補了在避孕習用栓塞所固有的 不便之處：難以拔抽、剌激性、缺乏自由處理性。此在 栓塞體上至少有一槽構做抓取的裝置及拔除術所引起的 〇 按照本發明.對於有利實施藥物組成物來説，栓塞邏 應具有輿其组成、輿其製備方式相對《的特擻。 因此，用作預防STD的藥物組成物的載體的栓塞，是 由開孔型泡決塑料來構成，其密度較佳地在15和28之間 Ο 經濟部屮央楳準而β工消费合作社印製 (請先閱讀背面之注意事項再塡寫本頁) 另一方面，聚胺酯醚泡沫塑料具有的斷裂強度，較佳 在70-100Kpa範園内。 最後，在聚胺酯醚泡沫塑料中所含»孔的平均直徑， 較佳在0.67-0.53·ιη之間。 為了成功地實施本發明方法，在裂備栓塞時，使其不 -1 3 - 201270 經濟部屮央梂準局貝工消t合作社印製 A 6 _B6_ 五、發明説明（12) 形成”皮層”也就是説，一傾外表面多少會延鑛，實際上 並沒有開孔。 為此，用鋸切操作來清除泡洙塑料塊外表的”皮層” 再以其切剌成一猶適當厚度的丨1材，再以此塑料Η材中 切剪成栓塞。 内行人考盧到前述的準則，蘧擇適合於女使用者解剖 學特點的栓塞形式和大小。 根據本發明的藥物組成物，較佳為呈現一霍水性凝謬 形式，這因為栓塞應用的身釅部位是水性的。事實上， 這涉及在非常敏感區域中内部使用，即在陰道黏贌上， 它不應被剌瀲和損壤。另一方面，這凝謬是完好地保留在 栓塞内。事際上，當使用者將栓塞放入陰道内，由於壓 塞時的壓力，藥物組成物不應太多的泄出。另外，栓塞 窸該保留在陰道内，尤其在足夠畏的時間，至少幾小時 内能有效地滯留住，栓塞内浸漬的蕖物組成物劑型應是 這樣：它在使用的開始幾分鐘中不能發生太多的槩物釋 放。應用一種凝謬劑型是重要的，因它彌補了逭健彩埵 效果的不足之疼。造掴凝膠型式，由於其特別的黏度， 能和鲇膜很好的接以至在鲇膜上形成一傾均匀而足 蛋的塗膜。 對於浸潰栓塞中的凝®醮必須有的鲇度來説，逭同樣 強諏了增稠劑作用的重要性。 為浸濟栓塞所需水性凝腰的《，逭取決於栓塞的《積 -1 4 - (請先閲讀背面之注意事項再填寫本頁) 裝· 訂 線_ 太认牦κ泞iA丨ί! Ψ S3 Η它过迆（CNM Ψ4妈枱（2〗0乂297公婊） 經濟部屮央橾準而货工消费合作社印製 201270 Λ 6 _Β6_ 五、發明説明（13) 和組成。但是，經驗表明，最好栓塞不被完金浸潰。另 一方面；則因在使用者把栓塞壓入陰道内時産生大量凝 ，膠排出，另一方面對於液體之天然流醱來說，可能被吸收 (以置換方式）或被中和。為了’浸漬栓塞，所必須的凝 繆體用量取決於上述先決條件，與栓塞總吸收的體稹相 比，睽醭的用量為其2 5%左右。 毎餾栓塞劑分別包裝在一值密封的膠囊内。 對於直徑45m*、厚度20a*的栓塞剤而言，可以遘用一 個内徑46bb、高度2 4min的醪囊。如此自由度的間隙是適 於本發明中栓塞浸漬的方式。 這種膠囊具有一倍5·»寬的四周翻邊，使蓋子輿上述 顴邊密缝結合，而将膠囊封蓋好。 由於膠囊（直徑24BB)和拴塞（直徑20··)大小不同，則 利用上述存在的自由小空隙，可方便地把膠囊封蓋好 〇 醪囊可由聚乙烯類材料製成。至於蓋子，則由鋁合金 製成，後者通常用於塑料容器的封蓋。 按照本發明法，浸潰足按以下方式寊施的： 将所箱最凝騵放置於睡囊的底部，對於45*20n«的栓 塞來説，大約需5s睬體。將此膠狀物傾斜，使在睇囊的 所有表而上形成一鏟小薄層膠體。 然後將栓塞於在謬賄上，再將膠囊封蓋。 此醪體通過毛細管現象猱透入栓垂内。 -1 5 - (請先閲讀背面之注意事項再填寫本頁) 裝· 訂 線· 太认汴疳iA m Ψ S3 Μ定过迆（CNSVK4坦坊（2〗0乂297公婊） 201270 A6 B6 經濟部屮央榣準而员工消t合作社印製 五、發明説明（14) 如果放置栓塞後能立即方便地在幾秒鐽内封蓋好，貝IJ 浸漬時間在30秒範圍内，也就是説在栓塞本身浸潰結束 .之前就封蕃好了。 因此.浸漬是在以後包裝搡作通程中加以完成的。換 句話説，浸漬是在”擯蔽時間”内«得的。 逆向操作，即把謬體放在栓塞上，而不是放在騵囊的 底部，如果驂囊的内部鱧積接近於栓塞外部醴積，正如 邐輯上考慮那樣，這是不合適的。在逭種情況下，實際 上在封蓋時，醪體很可能意外地黏附到謬囊邊上。由於 蓋子一般通過焊接方式固定在謬囊的《邊上，而醪體介 於此兩者之間，則阻止這種焊接。謬體越含有矽氣烷， 這種情況越為睦重。很少的不明顯置的謬體，就足夠使 封蓋得不完好，也就是説，騵囊是不密封的。 另外，對栓塞消番是不必需的，因其中含有高容量的 抗病毒劑和殺阑_。 因此，使用幾種有效成份組成物來浸潰的栓塞，由於 它們相互補充的活性.刖顯示出適合於預防STD的新而 獨特的優點。 實際上，由於栓塞的所有表面上具有開孔，它可使栓 塞内所浸潰的水性凝謬，一旦在使用栓壅時，就會流動 出現，以進入陰道口，而且伴随其推進，逐漸覆器 了除的所有鲇膜，因而保證了即刻而而稟實的保護。 當栓塞推進時，從栓塞中抽提出的水性凝瞜部份，由 -1 6 - 人請先閱讀背面之注意事項再塡寫本頁) 裝- 線 經濟部十央榣準局β工消费合作社印製 201270 A 6 _B_6 五、發明説明（15) 於開孔之間的溝通，在栓塞四周它被中心區域的撇孔中 原先含有的凝睡所置換。另外，由於其内部轉移，當發 _生性關傜時，流出的凝醪量顥得更重要，因性鬭偽意味 著運動，待別有利於殺死在陰道介質、精子和精掖中存 在的病原菌。 凝謬的物理性塗展顯示其流動是穩定而有規律的，此 優點在使用普通栓塞時不可能播得的。達增強了二甲基 聚矽氣烷的作用。後者和其分散劑性霣相平行，可在黏 膜和皮虜上形成一種保譁性膜。二甲基聚矽氧院屬於矽 氣烷類.因其待性，可使隔離和疏水兩者效果結合在一 起。 由於凝睽内含低濃度活性成分，以及成膜劃具有抑制 這些活性成分滲透人體内的效果，按照本發明的方法， 凝謬可以逹重後，長期使用的目的。 因此，使用者可以如同她希望那樣經常地更換浸潰過 的栓塞。同一姮栓塞可留在陰道内幾小時，而不産生對 黏膜剌激的危險性.甚至忘記取出時，也如此。 另外，建謙在最後一次性交後，至少將栓《滯留六小 時，以保證最好的；可能的保護效果。 按照表I.在配方中之氯化苄烷«可以增強膽酸納作 用，以防止發生”中毒性休克綜合症”的危險。 當其他病原龆被殺死時."中《性休克綜合症"來源於 Stapylococus aureus (金黃色酿朦葡萄球® )的ffi速繁 - 17- (請先閱讀背面之注意事項再塡寫本頁) 裝- 訂- 線· 經濟部屮央#準局β工消费合作社印製 20似Ο Α6 _ Β 6 五、發明説明（16) 殖。這傾發展的重要性起源於此種事寅；BJStaphyloc-ocus aursus (金黃色酿釀ίδ萄球S)産生一些強烈的毒 _素，它能非常快地導致中毒者死亡。因而，氮化苄烷较 正如膽酸納，對這種十分危險的病原體具有明顯的作用 〇 如前所述的被浸漬過的栓塞提供了雙重性保諶。例如 ，對於愛滋病來說，下列數種情況可考盧使用： --在健康婦女和一 te有明顯或血淸陽性疾病的男性發 生性願傜；女性機醴通過覆蓋陰道黏膜的薄膜而得陽離 和保護。栓塞中有效成分殺死在精子中，或由男性患者 帶來的致病因子。 --在患明顯或血清陽性疾病的婦女和健康男性之間發 生性鬭係；陰道腔被凝_禊覆蓋，使陰道黏膜和病毒可 能侵》途徑黏（侵蝕、破壤屏障）加以隔離。病毒不能 離開患病女性機構。由栓塞射出的凝膝同樣凝留在男性 伙伴的陰埜上，於是形成的薄膜可通過直接接«以及通 過皮虜上殘留藥物的效果來保護男性。 --在均患明願或血淸陽性疾病的男女雙方之間發生性 藺傜；凝繆的作用可防止血淸陽性症的联重而重後性感 染，此作用通常交叉隔離以及殺死兩铒來源的致病阑來 w現。 因此.本發明的漫*栓塞特別適合於煑滋病的預防。 除了習用的避孕措施（避孕丸，避孕用具等）外，前 -1 8 - (請先閲讀背面之注意事項再填寫本頁) 裝- 線_ 2〇i27〇Λ 6 Β 6 V. Description of the invention (7) 0. 2-1.5 X range, compared with the objective methyl polysilane according to the present invention, its isolation effect. According to the purpose of the present invention, the placement of gas is in accordance with the present invention. It is comparable to the formation of a thin film. This is due to the pursuit of thinness and a range (sticky in the vagina and in order to be effective, it is to the following two targets-reduction (and we Sex is a pathogenic factor-to avoid the retention of the best part of the composition between 0.25 and U. The best film forming test and dispersing agent is that it also has anti-adhesion Effect, and thus enhance the thin film in the range of 3.5 x the weight of the dimethyl polysilicon compound contained in the pharmaceutical composition. It is noted that the amount of the active ingredient used in comparison with the film is very large. The formation, not only in the case of the film on the protected surface, which is a large surface), the barrier effect of the barrier is applied, the film formation should be close enough, the: hope to completely prevent) the risk of the transfer of pathogenic factors or come To the catfish membrane, or toward the direction of the catfish membrane. The active ingredient is absorbed by the fc film, so the active ingredient is there. The local effect is sufficient. First read the matters on the back of the book. Then Shiyang, the Ministry of Economic Affairs of the assembly line, finds the XJA Gongxiaohuo Cooperative Society. ^. 0 于 合体Formed into a suitable shape. "The agent is. The tian tian is due to c ϋ-and it is a high-use medium, which can be used to increase the Xizi. It is necessary to expand the scorpion to the ββ catfish, but the catfish does not add it. And the increased risk body, the connection error is some thick insurable additives. Water-increased, using selective fie to make S Dingsui® 缜 部 good 0, the most useful in this book is the suitable endometrium for the period of the combination of the effect of human and human use i < 6 R / i ii m Ψ Η K it mi CNS) Ή 4 Wf 21 ny 297it) Printed by the Ministry of Economic Affairs # 揮 央 # 華工 消 貀 cooperatives 201 ^ 0 A 6 _B 6 V. Invention description (8) Dilute. According to the preferred implementation method of the composition of the present invention, a buffer such as hydrochloric acid may be included to adjust the pH to about 4.7. This pH value does not affect the g-group and dodeol in the male vagina (D 〇eder 1 e ί η) defend g. It is very heavy without breaking the soil. Because it has an important protective function against infections in the funeral system, these strains must be kept in the box. The composition according to the present invention may take the form of a solution (vaginal granule), emulsion, coagulation, etc. The insider can choose an acceptable abstract suitable for the proposed proposal. The form of the composition of the present invention depends on the way of use. In addition, the composition should have a viscosity suitable for the mode of use. For this purpose, the pharmaceutical composition of the present invention additionally contains a soothing agent, which enables a consistent rheological behavior. Among the conventional thickeners, the preferred test of the present invention is hydroxypropyl methyl ketone, sold under the trade name "Methloes 60 SH 4000" by SEPPIC (Paris, France, No. 70, Champs-Élysées Avenue) . This thickener adjusts the viscosity until it is optimal for the composition form (solution, emulsion, gel®, etc.). The adhesion thus obtained did not change significantly when the pH was different during the preparation of the first composition. In the application examples described later, the importance of Di Qingshi can be better understood. According to the pharmaceutical composition of the present invention, the concentration of the most commonly used dose is suspected to be -1 0-(please read the precautions on the back and then write this page) Pack · Book_ _ Thread _ Recognize 汴 尺 泞 1Λ Ψ KH 姐 柊m〇x297 cm) 201270 amended to supplement Λ 6 ,, Β 6 V. Description of the invention (9) In Table I: --0.25-1J: weight ratio of tenacic acid sodium. _ --3 · 5 3: Reset ratio of dimethyl polysiloxane. --43; weight ratio of hydroxypropylmethyl hunger. -Hydrochloric acid: the amount necessary to adjust to pH-4.7. -Water: Add to the child of 100X. According to a more elaborate embodiment of the present invention, several active ingredients are distributed together; in particular, the effect of antacid can be enhanced and the effect on a certain bacterium is to be determined. Therefore, the composition according to the present invention may contain one or more anti-viral and anti-fine® drugs which additionally have spermicidal action in combination with an acid selling agent, an endogenous agent, and a dispersing agent. Among these anti-disease, anti-fine® and spermicidal drugs, benzalkonium nitride and / or nonoxynl 9 are preferred. Xuan Li can note that the possibility of K using nonoxynol 9 illustrates the ® point brought by the present invention. In fact, the chief agent is expensive η ο η ο X y η 〇 丨 9 縿 penetrated into the machine salting, can form a certain empty toxicity, even if it mainly accumulates in the vinegar. In addition, its ability to penetrate the vaginal catfish membrane can be lifted to about 80X. However, it is entirely possible and non-hazardous to use nonoxynol 9S in the composition of the present invention, thanks to the formation of a thin film contained in this composition, the above-mentioned fine powder is sufficient. The anti-inhibition of the active ingredient into the body. For benzyl nitride and η ο η ο X y η ο 丨 9, the agent used is preferably in the composition absolute weight ft 0.5-13: and 0.25-15! Cocoon understand the ratio of -η -(Please read the precautions on the back and then fill out this page) Pack. Order the economical Taiyang central 銈 是 M industrial consumer cooperative cooperative printing 3i too recognized R cold Li rn Ψ ffi K Ya Yi (210 to 297 public obituary) 201270 Amendment 81.1 • Supplement Λ 6 13 6 on the month of this year V. Description of the invention (work 〇) If there is a group of medicines with contents in the group: The purpose is clear. , Better than, set to 9. Prime amount 1 ^ ^ W o R Μ yn * Weaving needs X ^ Must 0X & base & n5g3s no base 7 base 4 cases S S B-HH4 fchbfcfcfc dipropylene P X s i I 3 hydroxy to 0¾ quantity? ? ο Eltlwb's whole 1. v, 3 3 -ji table xxxifcb is adjusted to Π has it Ills _ _-I Quantity: add table constant, 5 ο 5 3 r. ί 252Χ Heavy acid: Shufeishang • U brine Shangdeyin __ I According to the last thing. The atmosphere of ammonium naphthenic acid benzyl oxide and the 0 ^ ^ of D of 〇 〇 To be fine-grained, it should be preliminarily blended with Yu Zi by Hejing-suitable ‘good poison’ into the disease group. For the amount of medicine used, it is necessary to take care of the same thing as the protection of the case »The case of the use case is compared and the disease is described-Shanghua in the live 0 to lose the effect of the poisonous disease, there are its D and T! S2B : A few places to close the C with the sub-category, the effect is 10 with D hy hy C3 T-P closed S bow a Yi Yu Ke St not tomb. * It's in the middle of the ball ⅰ ball 0) color leisure yellow beads gold read S Color Θ White Γ (u S a η ascuicb ο 1 (Please read the precautions on the back before filling out this page) Binding line. The Ministry of Economic Affairs Shiyang finds half iJM Gongxiaot Cooperative Society to print suc closed ball m milkless M's 0 Nai disease / (\ eae ο h Γ Γ ο η ο n Π Γ ϋ nal sano re o 虫 滴 0 阴 太 recognize the ruler cold J ΙΠ 屮 β 03 丨 0 > < 297 public stir) 201270 Λ6 _B6_ V. Invention Explanation (11) The three active agents incorporated in the composition in Table I act in a complementary manner and therefore have a wide range of activities. For example, nonoxynol 9 is effective against Chlamidia Trachomatis Effective, however, it can cause the spread of Candida Albicans (Candida albicans) infection. The present ammonium benzalkonium chloride has a very clear effect on Candida Albicans (Candida albicans). In order to prevent STD. According to the composition of the invention, it can be used in combination with local vaginal embolism, as the inventor patented in France Introduced in FR-A-2614525. This tilted embolism makes up for the inconveniences inherent in contraceptive embolism: difficult to extract, irritability, lack of free handling. This has at least one groove on the embolization body According to the present invention, the device and the removal technique are taken. According to the present invention, for the advantageous implementation of the pharmaceutical composition, the embolization logic should have a special composition and a relatively different preparation method. Therefore, it is used as a pharmaceutical composition for preventing STD The embolization of the carrier of the object is made of open-cell blister plastic, and its density is preferably between 15 and 28. Printed by the β-Consumer Cooperative Co., Ltd. of the Ministry of Economic Affairs (Please read the notes on the back first (Further writing this page) On the other hand, the breaking strength of polyurethane foams is preferably in the range of 70-100Kpa. Finally, the average diameter of the pores contained in the polyurethane foams is preferably 0.67-0.53 · ιη. In order to successfully implement the method of the present invention, when the embolism is prepared, it will not be -1 3-201270 The Ministry of Economic Affairs, the Central Bureau of Industry and Commerce Co., Ltd. printed A 6 _B6_ V. Explanation (12) The formation of a "cortex" means that the tilted outer surface will somewhat extend ore, and in fact there is no opening. For this purpose, a sawing operation is used to remove the "skin" on the outer surface of the plastic block of foam, and then cut into a material with an appropriate thickness, and then cut into an embolism with this plastic material. Insider Kaulu went to the aforementioned criteria and chose the embolization form and size suitable for the anatomical characteristics of female users. The pharmaceutical composition according to the present invention preferably exhibits an aqueous coagulation form because the body part to which the embolism is applied is aqueous. In fact, this involves internal use in very sensitive areas, ie on the vaginal mucosa, it should not be scratched and damaged. On the other hand, this absurdity remains intact in the embolism. In fact, when the user puts the embolism into the vagina, due to the pressure during the embolization, the pharmaceutical composition should not be discharged too much. In addition, the embolism should be retained in the vagina, especially for a sufficient period of time, and can be effectively retained for at least a few hours. The dosage form of the phlebium composition impregnated in the embolism should be as follows: it cannot occur within a few minutes of the beginning of use Too much casket is released. It is important to apply a coagulation dosage form, because it makes up for the lack of effect of Weijian Caisi. The slap gel type, due to its special viscosity, can be well connected with the catfish film to form a uniform and sufficient coating film on the catfish film. For the degree of coagulation necessary for the embolization of embolization embolism, Yau also emphasizes the importance of the role of thickener. The water-based solidification waist needed for embolization depends on the embolization of "Ji-1 4-(please read the precautions on the back and then fill out this page) 装 · 线 线 _ 太 譚 質 κ 泞 iA 丨 ί! Ψ S3 Η It has passed (CNM Ψ4 Matai (2〗 0 侂 297 public bitch). The Ministry of Economic Affairs, the central government and the cargo and consumer cooperatives printed 201270 Λ 6 _Β6_ V. Invention description (13) and composition. However, experience It shows that it is best not to impregnate the embolism with gold. On the other hand, when the user presses the embolism into the vagina, a lot of clot is generated and the gel is discharged. On the other hand, for the natural flow of liquid, it may be absorbed (In replacement mode) or neutralized. In order to 'impregnate embolism, the amount of coagulation body required depends on the above prerequisites. Compared with the total absorption of the embolism, the amount of 熽 醭 is about 2 5%. Distillation embolic agents are packaged in one-value sealed capsules. For embolic plugs with a diameter of 45m * and a thickness of 20a *, a mash sac with an inner diameter of 46bb and a height of 24min can be used. The gap of such freedom is suitable The method of embolization in the present invention. This kind of capsule has twice the width Flanging all around to make the lid and the above zygomatic edge tightly joined together to seal the capsule. Since the size of the capsule (diameter 24BB) and the plug (diameter 20 ··) are different, it is convenient to use the free small gaps mentioned above Cover the capsules well. The mash can be made of polyethylene. As for the lid, it is made of aluminum alloy, which is usually used for the closure of plastic containers. According to the method of the present invention, the impregnated foot is applied as follows Of: Place the box of the most condensed jelly on the bottom of the sleeping sac. For the embolism of 45 * 20n «, it takes about 5s. The tilt of this jelly is to form a one on all the surfaces of the sac Shovel a small thin layer of colloid. Then embolize on the bribe, and then cap the capsule. The mash penetrates into the sag through the capillary phenomenon. -1 5-(Please read the precautions on the back before filling this page ) Installation · Threading · Taishen Bianyi iA m Ψ S3 Μ Dingguo (CNSVK4 Tanfang (2〗 0 297 public bitch) 201270 A6 B6 Ministry of Economic Affairs Biyang Bizhong and staff elimination cooperative printing 5. Co-production Instructions (14) If the embolism can be placed and sealed in a few seconds immediately, The IJ immersion time is within 30 seconds, which means that the embolization itself is sealed before the immersion of the embolism itself. Therefore, the immersion is completed in the subsequent packaging process. In other words, the immersion is in " Obtained within the "masking time". Reverse operation, that is, put the fallacid on the embolism instead of the bottom of the sac, if the internal volume of the sac is close to the external volume of the embolism, as considered in the series , This is not suitable. In the case of actually, in fact, when sealing, the mash is likely to accidentally adhere to the edge of the sac. Because the cover is generally fixed by welding to the edge of the sac, and the mash If the body is between these two, this welding is prevented. The more absurd body contains silazane, the more serious this situation is. A few non-obvious fallacies are enough to make the cover incomplete, that is to say, the pouch is not sealed. In addition, the elimination of embolism is not necessary, because it contains high-capacity antiviral agents and killing _. Therefore, the embolization of embolization using several active ingredient compositions, due to their complementary activities, shows new and unique advantages suitable for the prevention of STD. In fact, due to the openings on all surfaces of the embolism, it can make the water-based gel impregnated in the embolism, once the embolism is used, it will flow to enter the vaginal opening, and as it advances, it gradually covers All catfish membranes are removed, thus ensuring immediate and practical protection. When the embolism advances, the water-based condensate part extracted from the embolism is from -1 6-people please read the precautions on the back before writing this page) Printed 201270 A 6 _B_6 5. Description of the invention (15) In the communication between the openings, it was replaced by the solidified sleep originally contained in the skimming holes in the central area around the embolism. In addition, due to its internal transfer, the amount of condensed mash that flows out is more important when it occurs, because sexual hypocrisy means exercise, and it is beneficial to kill those that exist in vaginal media, sperm, and sperm. Pathogens. The condensed physical spread shows that the flow is stable and regular, which is not possible when using ordinary embolism. Tat enhances the role of dimethyl polysilane. The latter is parallel to its dispersant, and it can form a protective film on the mucous membrane and skin. Dimethicone is a kind of silane. Because of its waitability, it can combine the effects of isolation and hydrophobicity. Due to the low concentration of active ingredients contained in the ganoderma lucidum and the effect of film formation to inhibit the penetration of these active ingredients into the human body, according to the method of the present invention, the ganoderma can be used for a long period of time after weight loss. Therefore, the user can change the impregnated emboli as often as she wishes. The same embolism can be left in the vagina for several hours without the danger of stimulating the mucous membrane. Even when you forget to take it out. In addition, after the last one-off payment, Jian Qian will stay for at least six hours to ensure the best; possible protection effect. According to Table I. Benzyl chloride in the formulation can enhance the role of sodium cholate to prevent the risk of "toxic shock syndrome". When other pathogens are killed. "Sexual Shock Syndrome" in the "quote" is derived from Stapylococus aureus (Golden Straw Grape Ball®)-17- (please read the precautions on the back before writing This page) Binding-Order-Thread · Ministry of Economic Affairs # 揮 央 # The quasi-bureau β industry consumer cooperative printed 20 Ο Α6 _ Β 6 V. Description of invention (16) Reproduction. The importance of this development stems from this kind of thing; BJStaphyloc-ocus aursus (golden brewing δδ) produces some strong toxins, which can cause the poisoners to die very quickly. Therefore, benzyl nitride has a significant effect on this very dangerous pathogen as sodium cholate. The impregnated embolization as described above provides a dual protection. For example, for AIDS, the following several situations can be used in Kalu:-In healthy women and men who have obvious or blood-positive diseases, sexual desire is not uncommon; female organs are yang by covering the membrane of the vaginal mucosa Away and protect. The active ingredient in the embolism kills the sperm or the causative agent brought by the male patient. --Sexual infections occur between women with obvious or seropositive diseases and healthy men; the vaginal cavity is covered with coagulation, so that the vaginal mucosa and viruses may invade by viscous (erosion, soil barrier) isolation. The virus cannot leave sick female institutions. The coagulated knee ejected by the embolism is also condensed on the male partner's shadow, so the formed film can protect the male by directly connecting «and through the effect of the residual drug on the skin. -Sexual luxation occurs between men and women who both suffer from a wish or blood-positive disease; the role of coagulation can prevent the combination of blood-positive diseases and subsequent serious infections. This effect usually crosses isolation and kills the two. The erbium-derived pathogenic appendix comes now. Therefore, the diffuse embolism of the present invention is particularly suitable for the prevention of AIDS. In addition to the conventional contraceptive measures (contraceptive pills, contraceptives, etc.), the former -1 8-(please read the precautions on the back before filling out this page) 装-线 _ 2〇i27〇
Λ 6 13 6 經濟部屮央標半沿β工消#合作社印Μ 五、發明説明（17) 述的浸漬栓塞也能用來預防STD 。在應用時尤其不需移 動某些避孕用具。. 它同樣顧示了可以保守秘密的優點^ »際上，和保險套相反，它不被同房者所感覺。在保險套的例子中，在 應用展開過程中此因素是非常有限的。對於本發明來説 ,這值障礙被移除了。 另外，浸漬栓塞安置在單用而可扯破的包裝组内供自 由使用，該包裝正確地保護和保存了栓塞，因而在應用 上提供了很大方便。 上述應用構成了本發明藥物组成物的掲特之處，尤其 可對抗愛滋病的蔓延，但也不是只針對此病的。 借助於以下實例，將詳細地敍述本發明： 寅例 所用的試劑 --雎酸納，由 CIPEC公司出雙，7 「ue Lincoln, 75008 巴黎（法國）。 --氮化苄烷銨，商品名為” REWOQUAT B50”由SCHERING 公司出资.5 rue Le Corbusier, 94150(¾ 琪（法國）。 --Nonoxyno 丨 9,商品名為"SIMULS0L 930 NP"由 SEPPIC公司出售,70 Avenue des Chanps-E 丨 ysees， 7 5 008巴黎（法因）。 --35%二甲基淤矽铒烷.商品為”365 MEDICAL GRADE E M U L SI 0 N ” 由 DO W CORNING CORPORATION. Midland公司出 -1 9 - (請先閲讀背面之注意事項再塡寫本頁) 裝. 訂 線 201270 A 6 B6 經濟部屮央標準局β工消費合作社印製 五、發明説明（18) 售 HichiUan 48640(美國）〇 --羥丙基甲基纖維素，商品名為” METH0L0SE 60 SH .4 000”由5〇(^61^5£卩？10公爾出售，70八¥611115〇65 Champs-Elysees, 75008巴黎（法國）。 實施I :按照表I處方的水性凝騵浸漬的陰道栓塞 栓塞： 由聚胺酯醚的泡沫塑料所構成，其具有以下待點： •密度：大約22。 •斷裂強度：大約130Kpa。 •微孔的平均直徑：0.6·»。 ♦直徑為45i«b,厚度為20bb。 正如法國專利ER-A-2614525所介绍的，在栓塞體上有 兩鍤槽溝。 凝醪·· --為浸潰以上待點的栓塞，必需用5g凝睡（一個如此栓 塞的總吸附體稹為20g) --所用的凝騵組成如下： •膽酸銷 ♦二甲基聚矽氧烷（35X溶液） •羥丙基甲基繼雄素 • 1N鹽酸 •純水 凝皤的裂備 0.025g(0.5X) 0.50g (10% ) 0.20g (4% ) 適量.至PH4 . 7 適量，加至绝重5g止 (請先閲讀背面之注意事項再填寫本頁) 裝· 訂 線 -20 經濟部屮央標準^JKX工消費合作社印製 m J- 81· 12.18 衣年A曰 補电 ^ 6 —— --B 6 五、發明説明（1¾ (此操作方式可用來製備任何量的凝謬） --在一 β不銹鏑捅内（B桶）内，室溫下把膽酸《溶解 .於一半量鈍水中。然後，加人二甲基聚矽氣烷。攪拌混 合此溶液，直至成為均相溶液為止。由於這些産品是表 面活性劑，故混合應以慢速攪拌方式進行。 --在一催雙靥不銹鏑桶（Α桶）内，另一半純水通遇夾 層内蒸汽循琛加熱至70*C。在攪拌下加入羥丙基甲《維 素.直至形成一傾均相腰體為止。以後，通過桶的來層 内冷水循琛而使謬龌冷卻到室溫。 --在攪拌下把B桶内所得溶液，於室溫下不断地加到 A桶内所得膠賭中，直至得到一偟均相膠鱧為止。 --加入足夠量的1N鹽酸溶液，調整pH至4.7。 --加入足夠量純水，調整繆體绝重置為5g為止。 栓塞的浸漬： --把上述得到的凝膠放置於一錮直徑46»b,离度24·· ，且有一傾5·β宽翻邊的睡囊底部。 --把栓塞放在此凝膠上，後者通過毛細管谚透入栓塞 内。 --把羞子焊接在β囊上，使其密封蓋好。 »例丨：按照表I[«方的水性凝睡浸潢的陰道栓塞 栓塞： --它呈現相同於實例I的特擻。 凝繆： -2 1 - (請先閲讀背面之注意事項再塡寫本頁) 裝_ 訂 線- 2012*70 A 6 B 6 經濟部屮央櫺準局貝工消f合作社印製 五、發明説明（20) --為浸潰栓塞必需用5g凝謬。 --所用凝騵的组成如下： .·臛酸納 0.025g (0.5X) •氛化苄烷较 0.50g(lX) • Nonoxyno1 9 0.025g(0.5X) •二甲基聚矽氣烷（355!溶液）0.50g(10S!) •羥丙基甲基纖維素 0 . 20g (4X) •IN鹽酸 適量，調整至pH-4.7 •純水 適量，加至總重 (4-4.2g) 凝睡的製備： --用如同實施例I同樣方法來進行。 --同時加入，氰化苄烷较，Nonoxynol 9和二甲基聚 矽氣烷。 栓塞的浸潰： --輿實例I方法相同。 藥理性質 A-抗病毒活性 在一翻用愛滋病HIV-Ι病籌沾污的溶液中，以測定可 逆性轉錄酶活性為指檬來確定藥物對病毒的抑制： a-在如下實驗條件下用膽酸納的结果： -22- (請先閲讀背面之注意事項再填寫本頁) 太/iiA ΙΑ Ψ 因 Μ 公货） 201270 A 6 B 6 五、發明説明（21) 膽酸納濃度X 可逆性轉錄睛被抑制X 處理時間’分 0 . 04 70 15 0 . 25 90 5 0 . 50 99 1 b-用 實例 I組成物裂得的凝睡： (請先閲讀背面之注意事項再填寫本頁) 凝謬濃度（鱧積/體稹）可逆性轉錄_被抑制X處理時間/分 裝 經濟部屮央橾準而貝工消费合作社印製 10-6 5 1 〇-5 7 1 0-4 99 1 〇-3 100 少 於 2 分 10-2 100 少 於 2 分 B -抗 細闌 活性 按 照實 例Π組成物所製得 的凝睡， 在32 t：時其 抗 活 性如 下： -23- 玎 線 五、發明説明（22) 66 ΛΒ mm 防腐雨濃度（龌稹/體積）必需接觴時間/分Λ 6 13 6 The Ministry of Economic Affairs, the central standard, half along β 工 消 # Cooperative Society Printing Μ 5. The invention description (17) The impregnated embolism can also be used to prevent STD. In particular, it is not necessary to move certain contraceptives during application. . It also shows the advantages of keeping secrets ^ »In fact, contrary to condoms, it is not felt by the same roommates. In the case of condoms, this factor is very limited during application deployment. For the present invention, this value barrier has been removed. In addition, the impregnated plug is placed in a single-use and tearable packaging group for free use. The package correctly protects and preserves the plug, thus providing great convenience in application. The above-mentioned applications constitute the special features of the pharmaceutical composition of the present invention, and are particularly effective against the spread of AIDS, but they are not specific to this disease. The present invention will be described in detail with the help of the following examples: The reagent used in Yin Example-sodium oleate, produced by CIPEC, 7 "ue Lincoln, 75008 Paris (France).-Benzalkonium nitride, trade name Funded by SCHERING for "REWOQUAT B50". 5 rue Le Corbusier, 94150 (¾ Qi (France). --Nonoxyno 丨 9, trade name " SIMULS0L 930 NP " sold by SEPPIC, 70 Avenue des Chanps-E 丨ysees, 7 5 008 Paris (Fin). --35% dimethyl silyl erbium. The product is "365 MEDICAL GRADE EMUL SI 0 N" by DO W CORNING CORPORATION. Midland -1 9-(please first Read the precautions on the back and write this page). Packing. Stranded 201270 A 6 B6 Printed by the β-Consumer Cooperative of the Bureau of Standards and Economics of the Ministry of Economic Affairs V. Invention Instructions (18) HichiUan 48640 (U.S.) 〇-Hydroxypropyl Methyl cellulose, trade name "METH0L0SE 60 SH .4 000" is sold by 5〇 (^ 61 ^ 5 £ 卩? 10 g, 70 8 ¥ 611115〇65 Champs-Elysees, 75008 Paris (France). Implementation I : Vaginal embolism impregnated with aqueous gelatin impregnated according to the prescription in Table I: by polyurethane The foam is composed of the following points: • Density: about 22. • Breaking strength: about 130Kpa. • Average pore diameter: 0.6 · ». ♦ Diameter 45i« b, thickness 20bb. Just as the French patent As described in ER-A-2614525, there are two grooves on the embolization body. Condensation mash-For embolization of the embolization point above, 5g of condensate must be used (the total adsorption volume of one embolization is 20g )-The composition of the gelatinium used is as follows: • Bile acid ♦ Dimethyl polysiloxane (35X solution) • Hydroxypropyl methyl androgen • 1N hydrochloric acid • Pure water condensate cracking preparation 0.025g (0.5 X) 0.50g (10%) 0.20g (4%) Appropriate amount. To PH4. 7 Appropriate amount, add to the absolute weight of 5g (please read the precautions on the back and then fill out this page) Packing & Booking Line-20 Ministry of Economic Affairs Central Standards ^ Printed by the JKX Industrial and Consumer Cooperatives m J-81 · 12.18 Yi Nian A said to supplement electricity ^ 6 —— --B 6 V. Description of invention (1¾ (This operation method can be used to prepare any amount of condensate)- In a β-stainless dysprosium poke (barrel B), dissolve cholic acid in half the amount of blunt water at room temperature. Then, add dimethyl polysilane. This solution was stirred and mixed until it became a homogeneous solution. Since these products are surfactants, mixing should be done with slow stirring. --In a stainless steel dysprosium barrel (A barrel), the other half of the pure water meets the steam in the interlayer and is heated to 70 * C. Hydroxypropyl methionine is added with stirring until a one-pound homogeneous waist is formed. Afterwards, the cold water in the layer of the barrel followed the water and cooled the room to room temperature. -With stirring, add the solution in barrel B to the glue in barrel A at room temperature until you get a homogeneous gel snake. --Add a sufficient amount of 1N hydrochloric acid solution to adjust the pH to 4.7. --Add sufficient amount of pure water and adjust the body to 5g. Impregnation of embolism: --Place the gel obtained above at the bottom of a sleeping bag with a diameter of 46 »b, a distance of 24 ··, and a 5 · β wide flange. --Place the plug on this gel, which penetrates into the plug through a capillary tube. -Weld the shit on the β capsule to make it tightly sealed. »Example 丨: According to Table I [« Vaginal embolism of water-based coagulation and dip in embolism. Embolism: --It presents the same characteristics as Example I. Ning Miao: -2 1-(Please read the precautions on the back before writing this page) _ _ Line-2012 * 70 A 6 B 6 Printed by the Ministry of Economic Affairs, Pengyang Bureau, Beigongxiao F Cooperative V. Inventions Explanation (20)-5g of coagulation must be used for embolization. --The composition of the tartar used is as follows: · 0.025g (0.5X) of sodium naphthenate • 0.50g (lX) of chlorinated benzane • Nonoxyno1 9 0.025g (0.5X) • Dimethyl polysilane (355 ! Solution) 0.50g (10S!) • Hydroxypropyl methylcellulose 0.20g (4X) • Appropriate amount of IN hydrochloric acid, adjusted to pH-4.7 • Appropriate amount of pure water, added to the total weight (4-4.2g) Preparation:-proceeded in the same way as in Example I. -Added at the same time, compared with benzane cyanide, Nonoxynol 9 and dimethyl polysilane. Embolization:-The method of Example 1 is the same. Pharmacological properties A-Antiviral activity in a solution contaminated with HIV-I disease-fighting drugs, to determine the reversible transcriptase activity as a indicator to determine the drug's inhibition of the virus: a-Use bile under the following experimental conditions Results of acid sodium: -22- (please read the precautions on the back before filling in this page) Tai / iiA ΙΑ Ψ Due to public goods) 201270 A 6 B 6 V. Description of invention (21) sodium cholate concentration X reversibility Transcription eye is inhibited X processing time 'minute 0. 04 70 15 0. 25 90 5 0. 50 99 1 b- the sleeping sleep cracked with the composition of Example I: (please read the precautions on the back before filling this page) Condensation concentration (Zhangji / Yi Zhen) reversible transcription_Suppressed X processing time / packed by the Ministry of Economic Affairs, Yoshihide Yoko, and printed by Beigong Consumer Cooperatives 10-6 5 1 〇-5 7 1 0-4 99 1 〇-3 100 is less than 2 points 10-2 100 is less than 2 points B-anti-aperiolar activity The coagulation prepared according to the composition of Example Π, the anti-activity at 32 t: is as follows: -23- 玎 线 五、 Description of the invention (22) 66 ΛΒ mm anticorrosive rain concentration (Qianzhen / volume) must meet the time / min
Staphylococcus au CIP 53127 Candida albicans CIP 1180.79 Streptococcus agalactiae CIP 55 118 e 9 1 ο s 7 e 7 s n ί p r p a I a I N c G c a 8 «1 11 a 4 1 7 gonorrhoeae vaginal is 0.5¾ 5X 0.5¾ 0. IX 0.5¾ 5分 5分 5分 5分 5分 (請先閱讀背面之注意事項再塡寫本頁) 裝 經濟部屮央橾準而貝工消费合作社印製 以上表格所列豳株代表了引起性傳染陰道感染的细® 種類。 根據法國藥典，最低殺菌濃度應在15分鐘内為5X(克 毫升）〇 C-抗寄生活性 在0.5X(克/毫升>«度水醪溶液中，在37它接《5分饋 時間，此凝睡（其含實例Π所述tb例的各組分）具即刻的 抗寄生效果，使Trichono»a 1/88丨118丨！5(陰道毛滴典）群 體至少減少1 0 0 0倍。 -24- 訂· 線·Staphylococcus au CIP 53127 Candida albicans CIP 1180.79 Streptococcus agalactiae CIP 55 118 e 9 1 ο s 7 e 7 sn ί prpa I a IN c G ca 8 «1 11 a 4 1 7 gonorrhoeae vaginal is 0.5¾ 5X 0.5¾ 0. IX 0.5 ¾ 5 points, 5 points, 5 points, 5 points, 5 points (please read the precautions on the back and then write this page). Pretend that the Ministry of Economic Affairs is quasi and the Beigong Consumer Cooperative printed the vine strains listed in the above table. Variety of vaginal infections. According to the French Pharmacopoeia, the minimum bactericidal concentration should be 5X (gram ml) within 15 minutes. The C-antiparasitic activity is 0.5X (gram / ml) «degree water mash solution, at 37 it is connected to" 5 minutes feed time, This coagulation sleep (which contains the components of the tb example described in Example Π) has an immediate anti-parasitic effect, which reduces the Trichono »a 1/88 丨 118 丨! 5 (vaginal hair drop code) population by at least 100 times. -24- Order · Line ·