TWM294946U - Delivery system - Google Patents

Delivery system Download PDF

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Publication number
TWM294946U
TWM294946U TW093211316U TW93211316U TWM294946U TW M294946 U TWM294946 U TW M294946U TW 093211316 U TW093211316 U TW 093211316U TW 93211316 U TW93211316 U TW 93211316U TW M294946 U TWM294946 U TW M294946U
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TW
Taiwan
Prior art keywords
delivery
delivery device
delivery system
weight
ratio
Prior art date
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TW093211316U
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Chinese (zh)
Inventor
Robert C Cuca
Thomas C Riley
R Saul Levinson
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Drugtech Corp
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Priority claimed from PCT/US2004/022058 external-priority patent/WO2006016869A1/en
Application filed by Drugtech Corp filed Critical Drugtech Corp
Publication of TWM294946U publication Critical patent/TWM294946U/en

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  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Infusion, Injection, And Reservoir Apparatuses (AREA)

Description

M294946 =沒有表現出以最佳安全方式釋放醫藥活性藥劑長達3小 τ或更長之日守間’而沒有遭遇與生物黏附性或過度釋放活 性醫藥成分有關之問題。例如,一般可用之輪送裝置幾乎 旦插入陰運腔内,便立即開始溶解、分散或者液化。因 此,此等輸送裝置典型地具有對陰道壁之最小生物黏附性。 在周配物中具有較大比例丙二醇之傳統輸送裝置已細用 來增強併入之藥物之可用性。所採用之優勢為活性醫;化 口物在洛劑狀分子(諸如丙二醇)中之可能溶解作用,以及藉 由丙二醇通過生物膜提供之增強之滲透可能性。此等對用曰 =黏=輸送裝置之推斷可被誇大,尤其^於陰道腔 J % 之水性本性為裝置吸收已溶解之活性醫藥化合物 θ七、了取適條件。包含高濃度之溶解活性醫藥藥劑之化合 增:装置對該藥劑之吸收可能性。儘管在某些實例 中希望獲得此效應,伸η力 、 、 1一疋在治療局部黏膜感染時,從接近 區域去除有益藥物可以 , 、 、抆/口療方案,亚且在某些情況下 可以導致活性醫藥化合物之I置吸收達到無益之含量。 此外,輸送裝置之物裡能摄 心樣可由包含適量至過量之丙二 =而損害。對於傳統乳劑’適量至過量之丙二醇可以增加 輸送裝置在陰道腔親水性環境中之溶解性和液化作用。對 2獨特之礼劑裝置’在環境溫度和升高溫度下包含較高 U之丙二醇都可以導致物理不穩定性。 結果,傳統和獨特輸送裝 田&、 置之乳劑無法在陰道腔中提供 ^ ^對方、提供陰逼疾病和痛苦之最佳治療之控釋輸 所需。因此,提供持續釋放醫 94057.doc M294946 :置於其遠側端。-種伸縮活塞桿組件與推動器裝置相 ’该組件具有料限制活塞桿組件伸長和防止活 件縮回有關之彳A I @ w t 、、 、、曰 7 、置。抓握裝置係提供用於操作該伸縮 塞才干、、且件。塗藥器係藉由抓住抓握端並將其(首先是封閉 端)插入所需腔中而操作。藉由抓握裝置將該活塞組件細 到分止裝置之限度,然後將該活塞組件相對於細長主體推 近由此產生堡力而打開封閉室並從儲存器中分配該藥物。 本創作之其他特μ將結合附圖而瞭解。本創作之盆他優 點和新穎特徵也將藉由檢視以下或由本發明實務學習而更 佳地被熟悉此項技藝者所瞭解。 【實施方式】 如圖1和2中所演示,醫藥物塗藥器20具有一分配末端22 和一抓握末端24。一圓筒構件26充當塗藥器之主體,其具 有—醫藥物儲存器部分、-活塞組件外殼部分、以及一抓 f ^面部分32。封閉構件34係在圓筒構件26之-縮減外獲 部分36之上滑動地接收。活塞組件38係在圓筒構件%内滑 =地接收,該活塞組件38具有一帶有活塞部分42之第一活 基構件40和-第二活塞構件44 ;該活塞部分42位於醫藥物 儲存器部分28内’並且活塞組件38之其餘部分位於活塞組 件外殼部分30内。一抓握構件46係提供用於第二柱塞構件 4 4 〇 本創作提供—種具有70%至90%間之高内部乳劑比率之 輪送裝置,較佳為其中非類脂相構成該裝置體積之約7〇〇/。 至90 /。。本創作之調配物與先前技藝之調配物相比,丙二 94057.doc M294946 醇之量減少約20%至約80%, 樣高之7〇%至90%的内部乳劑比率/ 7°而仍然保持同 此外,本創作可在86卞之溫度 大於-個月,更佳為大;^ —個月,較佳為 以及再更佳為大於-年,例如3至5年。 ^们月, 創作可被儲存於易受氣候變曰穩疋性使本 此等改良—般被認為是”改良之 本創作提供一種用於陰道腔之輸送裝置 控=式長時間輸送醫藥活性藥劑至陰道腔。在本= 間可以持續長達1〇天或更長。該輸送穿置以=下亥時 率為特徵。該輸送裝置較佳為種部乳劑比 鳩之親水性組分之乳^ 種包料置體積之至少 =送W純、維“及料料料腔之 或痛古之藥劑。該"陰道腔”也包括接近區域,例如… 括陰這、女性泌尿道(諸如尿道口)、陰道腔開口處之哭= 組織、以及藉由該腔可到達之生殖器官。該輸送裝置也以° =夠黏附(另外稱作,,生物黏附”)到陰道腔壁以及接近區域 (匕括上皮細胞、組織及器官)為特徵。 該輸送裝置不僅釋放活性藥劑,還以控制之方式釋 劑以獲得最佳吸收。因此,該活性藥劑可用於吸收、在吸 收。Ρ位產生樂理學或其他效應或以足以造成與藥劑之固有 性質:致之所需回應及提供將此回應維持適度程度所需時 門之里作用。本創作之輸送裝置較佳地以控制釋放活性藥 94057.doc M294946 劑至X體部位、作用部位、吸收部位或應用部位以及在該 邛位獲得希望之效應為特徵。該輸送裝置較佳為不與水互 溶’並且在陰道腔内使用無害。 本創作之輸送裝置可包括活性和非活性醫藥成分(也就 是本文一般稱作之”賦形劑”)之組合。例如非活性成分用以 將活性成分溶解、懸浮、加濃、稀釋、乳化、穩定、防腐、 保4、著色、調味,以及製成安全、方便、及使用上可接 文之適用的和有效的製劑。舉例而言,活性成分可以構成 輸送裝置總重量百分比之^㈣至抓’較佳為約15%至M294946 = No indication of the release of a pharmaceutically active agent in an optimally safe manner for up to 3 hours τ or longer on the day of the day' without encountering problems associated with bioadhesive or over-release active pharmaceutical ingredients. For example, a generally available wheeling device is inserted into the inhalation chamber almost immediately, and begins to dissolve, disperse or liquefy immediately. Therefore, such delivery devices typically have minimal bioadhesion to the vaginal wall. Conventional delivery devices having a greater proportion of propylene glycol in the weekly formulation have been used to enhance the availability of the incorporated drug. The advantages employed are active physicians; the potential solubility of the pharmaceutically acceptable substances in the lozenges (such as propylene glycol), and the enhanced penetration potential provided by propylene glycol through the biofilm. These inferences about the use of 曰 = sticky = delivery device can be exaggerated, especially in the vaginal cavity J % of the water nature of the device to absorb the dissolved active pharmaceutical compound θ VII, the appropriate conditions. A combination of a high concentration of a lytic active pharmaceutical agent: the likelihood of absorption of the agent by the device. Although in some instances it is desirable to achieve this effect, the extension of the force, 1 疋 in the treatment of local mucosal infections, the removal of beneficial drugs from the vicinity of the area, can be, in some cases, can lead to The I-intake of the active pharmaceutical compound reaches an unfavorable content. In addition, the contents of the delivery device can be damaged by containing an appropriate amount to an excess of Cyan =. For conventional emulsions, an appropriate amount to an excess of propylene glycol can increase the solubility and liquefaction of the delivery device in the hydrophilic environment of the vaginal canal. The inclusion of a higher U propylene glycol at ambient and elevated temperatures can cause physical instability. As a result, traditional and unique delivery fields & emulsions are not required to provide the optimal delivery of the best treatment in the vaginal canal, providing the best treatment for the disease and pain. Therefore, a continuous release physician 94057.doc M294946 is provided: placed at its distal end. - Telescopic piston rod assembly and pusher device 'This assembly has a material to limit the piston rod assembly elongation and prevent the workpiece from retracting 彳A I @ w t , , , , 7 . The gripping device is provided for operating the telescopic plug, and the member. The applicator operates by grasping the grip end and inserting it (first, the closed end) into the desired cavity. The piston assembly is fined to the extent of the dispensing device by the gripping device, and then the piston assembly is pushed closer to the elongated body thereby creating a fortune to open the closed chamber and dispense the medicament from the reservoir. Other features of this creation will be understood in conjunction with the drawings. The advantages and novel features of the present invention will also be better understood by those skilled in the art by reviewing the following or the practice of the present invention. [Embodiment] As demonstrated in Figures 1 and 2, the pharmaceutical applicator 20 has a dispensing tip 22 and a gripping end 24. A cylindrical member 26 serves as the body of the applicator having a medicinal reservoir portion, a piston assembly housing portion, and a gripping portion 32. The closure member 34 is slidably received over the reduced outer portion 36 of the cylindrical member 26. The piston assembly 38 is slidably received within the cylindrical member %, the piston assembly 38 having a first living base member 40 and a second piston member 44 with a piston portion 42; the piston portion 42 is located in the medical reservoir portion The inner portion 28 is 'and the remainder of the piston assembly 38 is located within the piston assembly outer casing portion 30. A grip member 46 is provided for the second plunger member to provide a high delivery ratio of between 70% and 90% of the internal emulsion ratio, preferably wherein the non-lipid phase constitutes the device The volume is about 7 〇〇 /. To 90 /. . The formulation of the present invention is reduced by about 20% to about 80% of the amount of alcohol, compared to the prior art formulation, and the internal emulsion ratio of 7% to 90% of the sample height / 7° is still In addition, the creation may be at a temperature of 86 大于 greater than -month, more preferably greater; ^ - month, preferably and more preferably greater than - year, for example 3 to 5 years. ^月月, Creations can be stored in a climate-sensitive and stable environment, so that these improvements are generally considered to be "improved. This creation provides a delivery device for the vaginal cavity. To the vaginal cavity. It can last up to 1 day or longer between the times. The delivery is characterized by a rate of =down. The delivery device is preferably a milk of the seed emulsion than the hydrophilic component of the sputum ^ At least the volume of the material is set to be sent to the product of pure, dimensional, and material. The "vaginal cavity" also includes access areas such as: yin, female urinary tract (such as the urethral opening), crying at the opening of the vaginal cavity = tissue, and the reproductive organs reachable through the cavity. It is characterized by ° = enough adhesion (also called, bioadhesion) to the vaginal wall and the proximal area (including epithelial cells, tissues and organs). The delivery device not only releases the active agent, but also releases it in a controlled manner for optimal absorption. Therefore, the active agent can be used for absorption and absorption. The sputum produces ethics or other effects or is sufficient to cause the inherent nature of the pharmacy: to respond to the desired response and to provide the role needed to maintain this response to a moderate degree. The delivery device of the present invention is preferably characterized by controlled release of the active agent 94057.doc M294946 to the X body site, site of action, absorption site or site of application and the desired effect at the site. Preferably, the delivery device is non-miscible with water & is harmless for use within the vaginal canal. The delivery device of the present invention may comprise a combination of active and inactive pharmaceutical ingredients (also referred to herein as "excipients"). For example, the inactive ingredients are used to dissolve, suspend, concentrate, dilute, emulsify, stabilize, preserve, protect, color, season, and make the active, convenient, and usable applications effective and effective. preparation. For example, the active ingredient may constitute a total weight percent of the delivery device from (4) to grab' preferably from about 15% to

2.5%,更佳為約2.0%之,可提供陰道腔之醫藥或化學治療 此等活性成分被調配成以控制方式釋放。包括活性藥劑二 活性成分可以為任何被認可或應用於治療、預防、治癒^ 緩解陰道腔之任#疾病之成分。纟創作之輸送裝置之主^ 活性成分為咪唑衍生物,其本質上為抗真菌劑和抗㈣ 劑。該口米唾衍生物可以醫藥可接受鹽或靖酸鹽之形式名2.5%, more preferably about 2.0%, may provide medical or chemical treatment of the vaginal cavity. These active ingredients are formulated to be released in a controlled manner. Including active agent II The active ingredient can be any ingredient that is approved or applied to treat, prevent, cure, relieve the vaginal cavity. The main active ingredient of the delivery device is an imidazole derivative which is essentially an antifungal agent and an anti-(four) agent. The rice saliva derivative may be in the form of a pharmaceutically acceptable salt or a salt of the acid salt.

在。可被用於本創作之㈣衍生物包括此項技藝中盆他高 知之藥劑中之口米康唾硝酸鹽、布康唾石肖酸鹽、奥昔康: ㈣conazoie)确酸鹽、甲硝唾硝酸鹽、特康唾硝酸鹽以及声 黴唾餐鹽。本創作之輸置之較㈣㈣生物 唑硝酸鹽0 〇 該輸送裝置可包含單位管。此等單位管為該裝置之基本 的、不可再分之重複單位。該單位管具有内相和外相,其 分別代表輪送裝置之内相與外相。該内相可以為非類脂性 的’亦即’與水互溶’以及可以包括水、甘油或其組合物。 94057.doc -10- M294946 該内相可以為多相,並且可以 組合,並且可以包含至少1分洋液、乳劑或其 -連續相並且為親脂性的,亦:劑。該外相可以為 括中性月曰肪、脂肪酸、壤 〃、匕 酉夂酉曰以及不溶於水但溶於醇 、知之月曰肪 礦物油。 、、虱仿或其他脂肪溶劑之 該輸送裝置習知上分類為 雔^丨 > 為例如,乳劑、乳劑/分散劑、 又礼鈉、乳劑内之懸浮劑、於 才^、泡沫劑或此項技藝中所 熟知之其他分類。因&,在 IT所 ^ ^ 丨作之具體實施例中,該輸 运l置可在形式上變化。在 ^ 狀罢& 本創作之一具體實施例中,該 衣置為礼貧劑形式之乳化成分。 勹4工、土 V +钔作之其他具體貫施例 包括洗液、凝膠劑、泡沫劑 不及各種乳化形式。此外, 創作之其他具體實施例包括 ^ 括黏度乾圍從約5,000至750 〇〇〇 厘泊’較佳為350,000至55〇 〇 ’ ^ n 〇,000厘泊之液體、半固體和固 體。最佳之黏度可以使續於、' 灸°亥輪迗叙置在陰道腔上獲得最大生 物黏附性。 較佳地該輸送裝置换用姿丨^ & 礼化介貝或高内相比率(其為外 相和内相之間之比率)之彤彳 _ t /式。该比率值代表内相佔該裝置 體積之百分比。在本創作 + 乍之具體貫施例中,該比率可以為 至少70%體積比,較佳為5丨 、 平乂仏馮至少75%,更佳為至少8〇%,以及 再更佳為多達約90%。 本創作之控制釋放特徵A太為丨a ^ θ Α 寸仪马本創作所展示之咼内相乳劑之 產物。乳化劑、輔助劑、乳化藥劑或其他賦形劑(諸如單硬 月曰酉夂甘油酉曰、單異硬脂酸甘油醋、對經苯甲酸甲酷、對羥 94057.doc M294946 酐酉/夂=&曰、以及一般之油、甘油醋、嚴糠醋、山梨糖醇 -人夕山木醇§日、乳酸硬脂酸鹽、卵磷脂以及其他類似 、#)產生出由非活性成分組成之乳化小球。該小球包含 藥J之儲存為。此等小球在塗佈時緩慢地分散,亦即, Γ、球傾向於尋找能夠容納它之表面或膜,而且該小球局 口p擴散(亦即,在昤指日允向、//Λ 隹u逗l内),從而形成一包含小球之,,膜,,, 制釋放方式隨時間經過釋放活性藥劑。該過程發生 丰又日可間’諸如,例如3丨日车 ή 例如3小時至多達ίο天或更多,並且因此 一般稱為’’控制釋放”。 之吝::作之生物黏附性特徵為本創作所展示之高内相乳劑 点2。該乳化之小球,其由賦形劑(其實例列於以上)組 成,為體積小但是具有相當 牲Wt _L 之表面積。^表面積和表面 使小球與人類組織藉由許多種物理結合分子力(諸如 凡得瓦力或氫鍵)相互作用。此輩沾人U 力(為如 比垄而用此寺結合力由於乳劑之高内相 Μ ’與包括乳劑之小體積連續相或外相相比,此 等非常小之小球之數量極大。 相相比此 本案將Riley,jr之哀女丨 ΓΚΠ直„ 就為5,266,329號之美國專利 (Rdey專利,,)全部以引用 生η Β μ 飞彳开入本文,该專利係於1999 日㈣。摘作之輸料置”知料 如ey專利所揭示者)之間之至少、括 穩定性。 矛文化為邊輪送裝置之 丙:醇可影響該細置之穩定性及擴散速 可包括於該輪送裝置之調 —% 之活性成分(例如㈣,諸如布:作為帛助洛解該輪送裝置 f 。者如布康唑硝酸鹽)之溶劑。已知在 94057.doc M294946 習知調配物中使用5〇〇重量%之丙二醇。 在本創作之具體## ^ 、騣只細例中,丙二醇可以約丨〇 量%,更佳為約3·5__至約3 至均4.0重 量%之量存在,亦f 1且最佳為約3.75重 'Λ ί7,與據信先前輪送裝置所t 相比,丙二醇之量減少約25%。 斤而之5.00重量% 本創作之至少—些具體實施例之輸送 配物中丙二醇之量 系错由減少調 、隹〇 項技藝中已熟知之輪送拿置改 進。丙二醇之減少廿旦 < 衣置改 亚不杉響内相乳劑比率, 鳩,也不阻止乳劑之形成。而且 =率大於 獲得料想不到的处果j a ^ 丙—醇之減少可 和有益。L果,该結果對醫藥和醫療技藝高度有利 本創作之輸送裝置香月g 了 | 少丙-醇之C 局限性。例如,減 二丙-私之里改進輪送裝置中活性w藥藥. 亚保持其有益之醫藥性質和效力。 ㈠'“’ 此外,本創作之具體實施例之輸送裝置已_ 附性之物理屬性和可能增加之與相分離相關之物; :Γ晋’二及長時間固定地保持抗分散之能力。本創作輸 、、置之總體增加物理屬性為消費者提供了— ▲則 之:品,以及較適當之陰道腔内治療’亦即,該; :且已經改進了對活性醫藥成分擴散速率之控制,因 有效。最後’該增強之穩定性在無法控 了儲存壽命,並且使更多人使用該輸送震置。又的&域增加 H之例示具體實施例現在已經依照上述優點進行描 ,"應瞭解此等實例僅用於説明本創作。許多變化和修改 94057.doc -13 - M294946 將為所屬技術領域之技術人員所明白 【圖式簡單說明】 在附圖中: 即用之位 圖1係醫藥物塗藥器之側視圖,其展示以緊密 置顯示之本創作之原理; 之分解圖,其顯示封閉部分 第二活塞構件(共同形成活塞in. (4) Derivatives that can be used in this creation include the medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicinal medicin , Tecom salicylate and Aspergillus saliva salt. Comparison of the creation of this creation (4) (4) Bioazole nitrate 0 〇 The delivery device can contain a unit tube. These unit tubes are the basic, non-reproducible repeating units of the device. The unit tube has an inner phase and an outer phase, which respectively represent the inner and outer phases of the wheeling device. The internal phase may be non-lipid', i.e., miscible with water' and may include water, glycerin or combinations thereof. 94057.doc -10- M294946 The internal phase may be heterogeneous and may be combined and may comprise at least one cent fluid, emulsion or its - continuous phase and is lipophilic, also: agent. The external phase may include neutral moon fat, fatty acids, earthworms, earthworms, and mineral oils that are insoluble in water but soluble in alcohol and know the moon. The delivery device of, or imitation or other fatty solvent is conventionally classified as 雔^丨> for example, an emulsion, an emulsion/dispersant, a sodium sulphate, a suspending agent in an emulsion, a emulsifier, a foaming agent or the like Other classifications well known in the art. Because of &, in the specific embodiment of IT, the transport can be changed in form. In one embodiment of the present invention, the garment is in the form of an emulsified component in the form of a remedy. Other specific examples of 勹4 work, soil V + 钔, including lotion, gel, foaming agent and various emulsified forms. In addition, other specific embodiments of the creation include liquid, semi-solid and solids having a viscosity dry circumference of from about 5,000 to 750 psi, preferably from 350,000 to 55 〇 ’ ^ 〇 10,000 psi. The best viscosity can be continued, 'the moxibustion of the sea rim is placed on the vaginal cavity to obtain the maximum bioadhesion. Preferably, the transport device is replaced by a 丨 t & & 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 、 This ratio value represents the percentage of the internal phase that accounts for the volume of the device. In the specific embodiment of the present creation + 乍, the ratio may be at least 70% by volume, preferably 5 丨, 乂仏 乂仏 von at least 75%, more preferably at least 8%, and even more preferably Up to about 90%. The controlled release feature A of this creation is too much of the product of the internal phase emulsion exhibited by 丨a ^ θ 寸 仪 马 马 马. Emulsifiers, adjuvants, emulsifiers or other excipients (such as monostearyl glycerol, monoisostearic acid glycerol, benzoic acid, hydroxy 94057.doc M294946 anhydride 酉/夂=&曰, and general oil, glycerin vinegar, sulphuric acid vinegar, sorbitol-human sorbitol § day, lactic acid stearate, lecithin and the like, #) produced by inactive ingredients Emulsified pellets. The pellet contains the storage of the drug J. These pellets are slowly dispersed during coating, that is, the spheres tend to look for a surface or film that can hold it, and the ball is diffused (i.e., at the fingertips, // Λ 隹u teasing l), thereby forming a globule-containing, film, and release means to release the active agent over time. The process occurs in abundance, such as, for example, 3 丨 ή, such as 3 hours to as many as ίο days or more, and is therefore generally referred to as ''controlled release'.) 吝:: The bioadhesive characteristic is The present invention shows a high internal phase emulsion point 2. The emulsified pellet consists of excipients (examples of which are listed above) which are small in size but have a surface area comparable to Wt_L. ^ Surface area and surface area are small The ball interacts with human tissue through a variety of physical binding molecular forces (such as van der Waals or hydrogen bonds). This generation is smeared with U force (for the use of this temple as a ridge, due to the high internal phase of the emulsion Μ ' Compared with the small volume continuous phase or external phase including the emulsion, the number of such very small pellets is extremely large. In contrast, this case will be Riley, the female sorrow of jr, which is the US patent of 5,266,329 (Rdey patent) ,,) All of them are cited in the reference η Β μ 彳 , , , , , , , , , , , , , , , , , , , , , , , 1999 1999 1999 1999 1999 1999 1999 1999 1999 1999 1999 1999 1999 1999 1999 1999 1999 1999 1999 1999 Culture is the side of the wheel transfer device: alcohol can be shadow The stability of the fineness and the speed of diffusion may be included in the adjustment of the transfer device to %% of the active ingredient (for example, (d), such as cloth: as a help to solve the transfer device f. Such as butoconazole nitrate) Solvent. It is known to use 5% by weight of propylene glycol in the conventional formula of 94057.doc M294946. In the specific example of the present invention, propylene glycol can be about 5% by weight, more preferably about 5% by weight. The amount of 3·5__ to about 3 to 4.0% by weight is present, and also f 1 and most preferably about 3.75, which is a reduction of about 25% of the amount of propylene glycol as compared to the previous transfer apparatus. 5.00% by weight of the present invention At least the amount of propylene glycol in the delivery formulation of at least some embodiments is improved by the reduction of the well-known rotation of the art. The reduction of propylene glycol is < The ratio of the clothes to the sub-phase emulsion is not to prevent the formation of the emulsion. Moreover, the rate is greater than the unexpected result. The reduction of gamma-co-alcohol can be beneficial. L. The result is for medicine and Medical technology is highly beneficial to the delivery device of the creation of the fragrance month g | less C-alcohol C Limitations. For example, the reduction of the activity of the active drug in the delivery device. The maintenance of its beneficial medical properties and efficacy. (a) '"' In addition, the delivery device of the specific embodiment of the present invention has been attached The physical properties of sex and the substances that may be associated with the separation of phases; :Γ晋'2 and the ability to maintain anti-dispersion fixedly for a long time. The overall physical attributes of the creation and delivery of the creation provide consumers with - ▲ then: the product, and the appropriate appropriate intravaginal treatment 'that is, that; and has improved the control of the diffusion rate of active pharmaceutical ingredients Because it is effective. Finally, the stability of this enhancement is beyond the control of shelf life and allows more people to use the conveyor to settling. The exemplification of the & field addition H has now been described in terms of the above advantages, " should be understood that these examples are only used to illustrate the creation. Many variations and modifications will be made to those skilled in the art. [Brief Description] In the drawings: Figure 1 is a side view of a pharmaceutical applicator, showing The principle of the present invention in a compact display; an exploded view showing the closed second piston member (to form a piston together)

圖2係圖1之醫藥物塗藥器 圓筒部分、第一活塞構件和 件),以及抓握構件。 【主要元件符號說明】 2〇 醫藥物塗藥器 22 分配末端 24 抓握末端 26 圓筒構件 28 醫藥物儲存器部分 3 0 活塞組件外殼部分 32 抓握表面部分 34 封閉構件 36 縮減外徑部分 38 活塞組件 40 第一活塞構件 42 活塞部分 44 弟^活基構件 46 抓握構件 94057.doc -14-Fig. 2 is a view showing the cylindrical portion of the medical applicator of Fig. 1, the first piston member and the member, and the gripping member. [Main component symbol description] 2 〇 medicine applicator 22 dispensing end 24 grip end 26 cylindrical member 28 medicinal reservoir portion 3 0 piston assembly outer casing portion 32 grip surface portion 34 closing member 36 reduced outer diameter portion 38 Piston assembly 40 first piston member 42 piston portion 44 mate member 46 grip member 94057.doc -14-

Claims (1)

M29J946 弟093)11316號專利申請案 中文申請專利範圍替換本(95年5月) 九、申請專利範圍: 1. 一種包括一塗单哭夕私、、 殺華物少〆…$廷系統’其包括:—用於將含有 面樂物之輪送裝置分配 即用的塗藥器,該塗荜哭二::預裝填的、 側抓握末端之細長主體:。該主::有τ分配末端和^ 形成-適於包含預定旦=度;細長主體之近側部分 v 預西樂物之儲存器;細長主I#之遠 側部分形成-活塞外殼;在儲存哭“一 接處,封閉梦罟/ σσ ϋ /舌基組合外殼之連 才閉#置位於儲存器之分 其遠端;-盘推動…“ 推動器裝置位於 件且有用” 之伸縮活塞桿組件,該組 H、有用於限制活塞桿組件伸 有關之停止穿署· 、,η 止活基桿組件縮回 1 了止衣置,以及用於操作該伸 握裝置;該醫筚物呈有右1Β 、、基#組件之抓 西+物具有有效置之活性 多種醫藥可接受之賦形劑,該賦形劑;;^ 制方式釋放至陰道腔内之位置,於性藥劑以控 大於70%之内相q π ^ t Ώ + 、 该輸送裝置具有 保存穩定度礼劑比率及在86ΐ溫度下至少—個月之 2.::…之輪送系統’其中該活 總重!百分比之約i · 5 %至3 %。 再成錢达裝置 4·如“们之輪送系統,其中該輪 丁生物。 置體積之至少观之親水性組分。、佔該輪送裳 “求項4之輪送系統,其中該輪送 置體積之至少8G%之親水性組分。、I括佔該輪送裳 94057-950508.doc M294946 6·如請求項5之私、、, 一^一〜二二·::::」 、之輪迗系統,其中該輸送裝置包括佔該輪 置體積之至客从 Ζ祝运1 夕約90%之親水性組分。 7. 如請求項·| 、/ 、之輪送系統,其中該一種或更多種醫藥可接受 之賦开y劑使該輪送裝置黏附於陰道腔壁。 8. 如:求項1之輪送系統,其中該輸送裝置為選自由乳劑、 乳劑/分散劑、雙乳劑、以及㈣或混合物中之料心 成之群組之形式。M29J946 Brother 093) No. 11316 Patent Application Replacement of Chinese Patent Application (May 95) IX. Scope of Application: 1. One type includes a single crying, and a Chinese smuggling... Including: - an applicator for dispensing a carousel containing a facial music, the coughing two:: a pre-filled, slender body with a side grip end:. The main:: having a τ dispensing end and forming - suitable for containing a predetermined denier = degree; a proximal portion of the elongated body v pre-synaptic reservoir; the distal portion of the elongated main I# forming a piston housing; crying in storage "A joint, a closed nightmare / σσ ϋ / a combination of a tongue-and-base combination housing is placed at the distal end of the reservoir; - the disk is pushed..." The pusher device is located and useful" telescopic piston rod assembly, The group H has a stop-stop mechanism for restricting the extension of the piston rod assembly, the η-killing base rod assembly is retracted, and the holding device is operated; the medical article has a right side , the base #component of the grasp of the West + material has an effective setting of a variety of pharmaceutically acceptable excipients, the excipient;; method of release into the vaginal cavity, the control of more than 70% of the drug The internal phase q π ^ t Ώ + , the conveying device has a storage stability ratio and a transfer system of at least - months at a temperature of 86 ' 2. The total weight of the live! 5 % to 3%. Re-into the money device 4 · such as "the wheel of the system, its The round Ding organisms. At least the hydrophilic component of the volume is placed. In the round of the delivery of the "study 4 of the wheel delivery system, which is at least 8G% of the volume of the hydrophilic component of the volume of the delivery. I include the wheel to send skirts 94057-950508.doc M294946 6 · as requested 5 私, , , 一 一 一 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二 二Minute. 7. The delivery system of claim 1, wherein the one or more medically acceptable y agents allow the delivery device to adhere to the vaginal canal wall. 8. The method of claim 1, wherein the delivery device is in the form of a group selected from the group consisting of emulsions, emulsions/dispersants, double emulsions, and (iv) or mixtures. 认长員3之輪送系統,其中該咪唑衍生物係選自由咪康 坐〆布康唑、奥昔康唑(oxiconazole)、甲硝唑、以及克黴 Λ或/、西藥可接受鹽或硝/酸鹽組成之群組。 10· tr求項9之輪送系統,其中該味唾衍生物為布康。坐或盆 西樂可接受鹽或硝酸鹽。 u.如請求们之輪送系統,其中該輸送裝置包含約45重量% 或更少之丙二醇。 12. 如晴求仙之輸送I統,其中該輸送裝置包含約重量% 或更少之丙二醇。 13. =請求項U之輸送系統,其中該輸送裝置包含丙二醇之 I&圍為重量比約10%至約4.〇%。 14. 如請求们之輸送系統,其中該輸送裝置具有大於7〇%之 内相乳劑比率及在86V溫度下至少j個月之保存穩定度。 Μ·如請求項14之輸送系、统,其中該輪送裝置具有大㈣=之 内相乳劑比率及在崎溫度下至少2個月之保存移定度。 16.如請求項15之輸送系統,其中該輸送裝置具有大於獅之 内相乳劑比率及在抑溫度下至少6個月之保存移定度。 94057-950508.doc M294946 fv r d 1 7 ·如請求項16之輸m其巾該輸送裝置 内相乳劑比率及在86V溫度下至少1年之保,7〇%之 18.如請求項1之輸送系、統,其中該輪送裝置可^疋f。 制釋放到陰道腔内部位至少3小時。、、活性藥劑控 Ί求項1之輸送系統,其中該輪送褒置為黏度範圍從約 5,000至約750,〇〇〇厘泊之液體或半固體形式。 請求項19之輸送系統,其中該輸送^為黏度範圍從 約350,〇〇〇至約55〇,〇〇〇厘泊之液體或半固體之形式。 21·如請求項i之輸送系統,其中該活性藥劑係以佔該輸送裝 置總重量百分比之約15%至約3%之範圍存在,並且進— 步包括: 佔該輸送裝置總重量百分比之約! ·〇%至約4 〇%之範圍之 丙二醇。 22·如請求項1之輸送系統,其中該活性藥劑為一抗真菌劑。A system for the identification of a long-term 3, wherein the imidazole derivative is selected from the group consisting of buconazole, oxiconazole, metronidazole, and ketomycin or/or western medicine acceptable salt or nitrate /Group of acid salts. 10 tr The rounding system of Item 9, wherein the taste of the saliva derivative is Bu Kang. Sit or basin Xile can accept salt or nitrate. u. A requesting system for a transfer wherein the delivery device comprises about 45% by weight or less of propylene glycol. 12. In the case of a clear delivery, wherein the delivery device comprises about 5% by weight or less of propylene glycol. 13. The delivery system of claim U, wherein the delivery device comprises propylene glycol in an I&weight ratio of from about 10% to about 4.% by weight. 14. A delivery system as claimed, wherein the delivery device has an internal phase emulsion ratio of greater than 7% and a storage stability of at least j months at 86V. The transport system of claim 14, wherein the transfer device has an internal phase emulsion ratio of a large (four) = and a storage degree of retention at a temperature of at least 2 months. 16. The delivery system of claim 15 wherein the delivery device has a ratio of emulsions greater than the inner phase of the lion and a storage degree of retention at a temperature of at least 6 months. 94057-950508.doc M294946 fv rd 1 7 · In the case of claim 16, the ratio of the phase emulsion in the delivery device and the at least one year warranty at 86V, 7〇% 18. The delivery of claim 1 System, system, wherein the wheeling device can be 疋f. Release to the inside of the vaginal canal for at least 3 hours. The delivery system of the active pharmaceutical product of claim 1, wherein the rotary device is in the form of a liquid or semi-solid having a viscosity ranging from about 5,000 to about 750, 〇〇〇 centipoise. The delivery system of claim 19, wherein the delivery is in the form of a liquid or semi-solid having a viscosity ranging from about 350 Torr to about 55 Torr. 21. The delivery system of claim i, wherein the active agent is present in a range from about 15% to about 3% by weight of the total weight of the delivery device, and further comprising: about a percentage of the total weight of the delivery device ! • 〇% to about 4,000% of propylene glycol. 22. The delivery system of claim 1, wherein the active agent is an antifungal agent. 94057-950508.doc94057-950508.doc M2獅 316號專利申請案 中文圖式替換本(95年5月)M2 Lion 316 Patent Application Chinese Graphic Replacement (May 1995) 94057-950508.doc94057-950508.doc
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