TW201838624A - Pharmaceutical carrier for transdermal drug delivery and pharmaceutical composition containing the same - Google Patents
Pharmaceutical carrier for transdermal drug delivery and pharmaceutical composition containing the same Download PDFInfo
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本發明攸關一種醫藥載體,且特別攸關一種用於經皮遞送藥物的醫藥載體及包含有此載體的醫藥組合物。The present invention is directed to a pharmaceutical carrier and, in particular, to a pharmaceutical carrier for transdermal delivery of a medicament and a pharmaceutical composition comprising the carrier.
兒茶素(catechin)具有低口服生物利用率,這導致其於體內的濃度低於有效濃度(請參照Mol Pharm. 2007 Nov-Dec;4(6):819-25),從而無法發揮有效的生物功能。目前已知以下方式可提升兒茶素的口服生物利用率:禁食狀態下服用兒茶素,或者與胡椒鹼共同服用。Catechin has a low oral bioavailability, which results in its concentration in the body being lower than the effective concentration (please refer to Mol Pharm. 2007 Nov-Dec; 4(6): 819-25), so that it cannot be effective. Biological function. The following methods are known to enhance the oral bioavailability of catechins: taking catechins in a fasted state or taking them with piperine.
職是之故,如何解決兒茶素等黃烷-3-醇(flavan-3-ol)之低生物利用率的問題確實為本發明所屬技術領域人士積極解決的課題之一。For the sake of the job, how to solve the problem of low bioavailability of flavin-3-ol such as catechin is one of the problems actively solved by those skilled in the art.
本發明之一目的在於提出一種新穎的醫藥載體,其包含:一水相組份、一油相組份、一界面活性劑、以及一輔助界面活性劑;而水相組份含有水,油相組份含有C10至C20脂肪酸,界面活性劑含有Tween 80/Span 20或Brij 35/Brij 30,輔助界面活性劑含有C2至C6醇。An object of the present invention is to provide a novel pharmaceutical carrier comprising: an aqueous phase component, an oil phase component, a surfactant, and an auxiliary surfactant; and the aqueous component contains water, oil phase The component contains a C10 to C20 fatty acid, the surfactant contains Tween 80/Span 20 or Brij 35/Brij 30, and the co-surfactant contains a C2 to C6 alcohol.
本發明之另一目的在於提出一種新穎的醫藥組合物,其包含:前述的醫藥載體、以及一黃烷-3-醇;而黃烷-3-醇為包含於水相組份中。Another object of the present invention is to provide a novel pharmaceutical composition comprising: the aforementioned pharmaceutical carrier, and a flavan-3-ol; and the flavan-3-ol is contained in the aqueous phase component.
本發明之再一目的在於提出一種前述之醫藥組合物的用途,其為用於製備治療或預防阿茲海默症(Alzheimer's disease)的乳劑,其中黃烷-3-醇為兒茶素。A further object of the present invention is to provide a use of the aforementioned pharmaceutical composition for the preparation of an emulsion for the treatment or prevention of Alzheimer's disease, wherein the flavan-3-ol is catechin.
本發明之又一目的在於提出一種前述之醫藥組合物的用途,其為用於製備抗氧化的乳劑,其中黃烷-3-醇為兒茶素。A further object of the present invention is to provide a use of the aforementioned pharmaceutical composition which is an emulsion for the preparation of an antioxidant, wherein the flavan-3-ol is catechin.
本發明之更一目的在於提出一種前述之醫藥組合物的用途,其為用於製備清除自由基的乳劑,其中黃烷-3-醇為兒茶素。A further object of the present invention is to provide a use of the aforementioned pharmaceutical composition for preparing a free radical scavenging emulsion wherein the flavan-3-ol is catechin.
本發明之仍一目的在於提出一種前述之醫藥組合物的用途,其為用於製備抗癌的乳劑,其中黃烷-3-醇為兒茶素。Still another object of the present invention is to provide a use of the aforementioned pharmaceutical composition for the preparation of an anticancer emulsion wherein the flavan-3-ol is catechin.
本發明之復一目的在於提出一種前述之醫藥組合物的用途,其為用於製備抗病毒的乳劑,其中黃烷-3-醇為兒茶素。A further object of the present invention is to provide a use of the aforementioned pharmaceutical composition for the preparation of an antiviral emulsion wherein the flavan-3-ol is catechin.
本發明之另一目的在於提出一種前述之醫藥組合物的用途,其為用於製備降血壓的乳劑,其中黃烷-3-醇為兒茶素。Another object of the present invention is to provide a use of the aforementioned pharmaceutical composition for the preparation of a blood pressure lowering emulsion wherein the flavan-3-ol is catechin.
本發明之再一目的在於提出一種前述之醫藥組合物的用途,其為用於製備預防UV傷害的乳劑,其中黃烷-3-醇為兒茶素。A further object of the present invention is to provide a use of the aforementioned pharmaceutical composition for preparing an emulsion for preventing UV damage, wherein the flavan-3-ol is catechin.
為讓本發明上述及/或其他目的、功效、特徵更明顯易懂,下文特舉較佳實施方式,並配合所附圖式,作詳細說明如下:In order to make the above and/or other objects, functions and features of the present invention more comprehensible, the following detailed description of the preferred embodiments,
本發明之第一實施方式提出一種醫藥載體,其可呈乳劑形式並可經皮遞送藥物至生物體內;更具體地說,其可有效地經皮遞送黃烷-3-醇至生物體內,以解決黃烷-3-醇口服生物利用率低的問題。所述的醫藥載體至少含有:一水相組份、一油相組份、一界面活性劑、及一輔助界面活性劑。水相組份含有水;油相組份含有C10至C20脂肪酸,其實例可以為但不限於肉荳蔻酸異丙酯(isopropyl myristate,IPM)或油酸(oleic acid);界面活性劑含有Tween 80/Span 20或Brij 35/Brij 30;輔助界面活性劑含有C2至C6醇,其實例可以為但不限於乙醇、異丙醇、二甘醇-乙醚、或丙二醇。須說明的是,符號「/」表示連接的物質為相互混合的;亦即,「Tween 80/Span 20」代表Tween 80與Span 20的混合物,其餘依此類推。術語「Tween 80」的同義字為「聚山梨醇酯80(polysorbate 80)」;術語「Span 20」的同義字為「山梨醇單月桂酸酯(sorbitan monolaurate);術語「Brij 35」的同義字為「聚氧乙烯(23)十二烷醚(poly(oxyethylene)(23) lauryl ether)」;術語「Brij 30」的同義字為「聚氧乙烯(4)十二烷醚(poly(oxyethylene)(4) lauryl ether)」。A first embodiment of the present invention provides a pharmaceutical carrier which can be in the form of an emulsion and which can deliver a drug to a living body transdermally; more specifically, it can effectively deliver flavan-3-ol to a living body transdermally, Solve the problem of low bioavailability of flavan-3-ol. The pharmaceutical carrier comprises at least: an aqueous phase component, an oil phase component, a surfactant, and an auxiliary surfactant. The aqueous phase component contains water; the oil phase component contains C10 to C20 fatty acids, examples of which may be, but are not limited to, isopropyl myristate (IPM) or oleic acid; surfactants contain Tween 80 /Span 20 or Brij 35/Brij 30; the co-surfactant contains a C2 to C6 alcohol, examples of which may be, but are not limited to, ethanol, isopropanol, diethylene glycol-diethyl ether, or propylene glycol. It should be noted that the symbol "/" indicates that the connected substances are intermixed; that is, "Tween 80/Span 20" represents a mixture of Tween 80 and Span 20, and so on. The synonym for the term "Tween 80" is "polysorbate 80"; the synonym for the term "Span 20" is "sorbitan monolaurate"; the synonym for the term "Brij 35" "poly(oxy)(23) lauryl ether"; the synonym for the term "Brij 30" is "polyoxyethylene (4) dodecyl ether (poly(oxy)) (4) lauryl ether)".
於本實施方式,所述的醫藥載體可為一油包水(W/O)形式的載體或一水包油(O/W)形式的載體。術語「油包水」意指油相組份透過界面活性劑與輔助界面活性劑包覆水相組份以形成水滴,水滴較佳地為微米級水滴;術語「水包油」意指水相組份透過界面活性劑與輔助界面活性劑包覆油相組份以形成油滴,油滴較佳地為微米級油滴。於微米級水滴或微米級油滴形成的條件下,所述的醫藥載體可視為一微米級載體。In this embodiment, the pharmaceutical carrier can be a carrier in the form of a water-in-oil (W/O) or a carrier in the form of an oil-in-water (O/W). The term "water-in-oil" means that the oil phase component coats the aqueous phase component with the surfactant and the auxiliary surfactant to form water droplets, and the water droplets are preferably micron-sized water droplets; the term "oil-in-water" means the water phase The component coats the oil phase component with the surfactant and the auxiliary surfactant to form oil droplets, which are preferably micron oil droplets. The pharmaceutical carrier can be considered to be a one-micron carrier under conditions in which micron-sized water droplets or micron-sized oil droplets are formed.
於本實施方式,Tween 80與Span 20間的重量比可為1:2至1:1,較佳地為2:3;Brij 35與Brij 30間的重量比可為1:4至1:2,較佳地為1:3.7。In this embodiment, the weight ratio between Tween 80 and Span 20 may be 1:2 to 1:1, preferably 2:3; the weight ratio between Brij 35 and Brij 30 may be 1:4 to 1:2. Preferably, it is 1:3.7.
於本實施方式,以所述之醫藥載體的總重量計,水相組份、油相組份、界面活性劑、與輔助界面活性劑的重量百分比可各為10.00%至50.00%、2.00%至53.00%、10.00%至30.00%、5.00%至35.00%,較佳地各為15.00%至48.00%、3.02%至50.00%、15.00%至25.30%、10.00%至32.00%,更佳地各為40.02%至46.39%、5.00%至10.31%、15.17%至25.00%、26.83%至30.93%。In this embodiment, the weight percentage of the aqueous phase component, the oil phase component, the surfactant, and the auxiliary surfactant may be 10.00% to 50.00% and 2.00%, respectively, based on the total weight of the pharmaceutical carrier. 53.00%, 10.00% to 30.00%, 5.00% to 35.00%, preferably 15.00% to 48.00%, 3.02% to 50.00%, 15.00% to 25.30%, 10.00% to 32.00%, and more preferably 40.02 each. % to 46.39%, 5.00% to 10.31%, 15.17% to 25.00%, 26.83% to 30.93%.
本發明之第二實施方式提出一種醫藥組合物,其可呈乳劑形式並至少含有:如第一實施方式所述的醫藥載體、以及一黃烷-3-醇;黃烷-3-醇為包含於醫藥載體的水相組份中,其實例可以為但不限於兒茶素、表兒茶素(epicatechin)、表沒食子兒茶素(epigallocatechin)、表兒茶素沒食子酸酯(epicatechin gallate)、表沒食子兒茶素沒食子酸酯(epigallocatechin gallate)、表阿夫兒茶精(epiafzelechin)、非瑟酮醇(fisetinidol)、喹色亭酚(guibourtinidol)、牧豆樹醇(mesquitol)、或刺槐亭醇(robinetinidol)。如前所述,於醫藥組合物塗抹於生物體的皮膚上時,可透過醫藥載體經皮遞送組合物中的黃烷-3-醇至體內。又如前所述,於醫藥載體為油包水形式之載體的條件下,所述的醫藥組合物為一油包水形式的組合物;於醫藥載體為水包油形式之載體的條件下,所述的醫藥組合物為一水包油形式的組合物。更如前所述,於微米級水滴或微米級油滴形成的條件下,所述的醫藥組合物可視為一微乳劑。A second embodiment of the present invention provides a pharmaceutical composition which may be in the form of an emulsion and which comprises at least: a pharmaceutical carrier according to the first embodiment, and a flavan-3-ol; the flavan-3-ol is included In the aqueous phase component of the pharmaceutical carrier, examples thereof may be, but not limited to, catechin, epicatechin, epigallocatechin, epicatechin gallate ( Epicatechin gallate), epigallocatechin gallate, epiafzelechin, fisetinidol, guibourtinidol, mesquite Mesquitol, or robintinidol. As described above, when the pharmaceutical composition is applied to the skin of a living body, the flavan-3-ol in the composition can be transdermally delivered to the body through a pharmaceutical carrier. Further, as described above, the pharmaceutical composition is a water-in-oil form of the composition under the condition that the pharmaceutical carrier is in the form of a water-in-oil form; and the pharmaceutical carrier is in the form of a carrier in the form of an oil-in-water, The pharmaceutical composition is a composition in the form of an oil-in-water. Further, as described above, the pharmaceutical composition can be regarded as a microemulsion under the conditions of formation of micron-sized water droplets or micron-sized oil droplets.
於本實施方式,以所述之醫藥組合物的總重量計,醫藥載體的重量百分比可為96.00%至99.90%,黃烷-3-醇的重量百分比可為0.10%至4.00%;較佳地,醫藥載體的重量百分比為97.00%至99.50%,黃烷-3-醇的重量百分比為0.50%至3.00%。更具體地說,以所述之醫藥組合物的總重量計,水相組份、油相組份、界面活性劑、輔助界面活性劑、與黃烷-3-醇的重量百分比可分別為9.60%至49.95%、1.92%至52.95%、9.60%至29.97%、4.80%至34.97%、與0.10%至4.00%,而較佳地分別為14.55%至47.76%、2.93%至49.75%、14.55%至25.17%、9.70%至31.84%、與0.50%至3.00%。In this embodiment, the weight percentage of the pharmaceutical carrier may be from 96.00% to 99.90%, and the weight percentage of flavan-3-ol may be from 0.10% to 4.00%, based on the total weight of the pharmaceutical composition. The weight percentage of the pharmaceutical carrier is from 97.00% to 99.50%, and the weight percentage of flavan-3-ol is from 0.50% to 3.00%. More specifically, the weight percentage of the aqueous phase component, the oil phase component, the surfactant, the auxiliary surfactant, and the flavan-3-ol may be 9.60, respectively, based on the total weight of the pharmaceutical composition. % to 49.95%, 1.92% to 52.95%, 9.60% to 29.97%, 4.80% to 34.97%, and 0.10% to 4.00%, and preferably 14.55% to 47.76%, 2.93% to 49.75%, 14.55%, respectively. To 25.17%, 9.70% to 31.84%, and 0.50% to 3.00%.
依J Nutr Biochem. 2013 Jul;24(7):1302-13所述,綠茶兒茶素能整體地改善NSE/hAPP-C105轉殖鼠的阿茲海默症相關表型。基於此,本發明之第三實施方式提出一種如第二實施方式所述之醫藥組合物的用途,其為用於製備治療或預防阿茲海默症的乳劑,其中黃烷-3-醇為兒茶素。如前所述,所製的乳劑塗抹於有此需求之生物體的皮膚上時,可透過醫藥載體經皮遞送兒茶素至體內,以達到治療或預防阿茲海默症的目的。According to J Nutr Biochem. 2013 Jul;24(7):1302-13, green tea catechins can improve the Alzheimer's-related phenotype of NSE/hAPP-C105 transgenic mice as a whole. Based on this, a third embodiment of the present invention provides the use of the pharmaceutical composition according to the second embodiment, which is an emulsion for preparing or treating Alzheimer's disease, wherein flavan-3-ol is Catechin. As described above, when the prepared emulsion is applied to the skin of a living body in need thereof, the catechin can be delivered to the body through a medical carrier to achieve the purpose of treating or preventing Alzheimer's disease.
依Crit Rev Food Sci Nutr. 2003;43(1):89-143所述,於動物模式綠茶與綠茶兒茶素對氧化壓力的生物標記影響相當具有潛力,特別是氧化DNA傷害。基於此,本發明之第四實施方式提出一種如第二實施方式所述之醫藥組合物的用途,其為用於製備抗氧化的乳劑,其中黃烷-3-醇為兒茶素。如前所述,所製的乳劑塗抹於有此需求之生物體的皮膚上時,可透過醫藥載體經皮遞送兒茶素至體內,以達到抗氧化目的。According to Crit Rev Food Sci Nutr. 2003; 43(1): 89-143, the effect of green tea and green tea catechins on the biomarker of oxidative stress in animal models is quite potential, especially oxidative DNA damage. Based on this, a fourth embodiment of the present invention provides a use of the pharmaceutical composition according to the second embodiment, which is an emulsion for preparing an antioxidant, wherein the flavan-3-ol is catechin. As described above, when the prepared emulsion is applied to the skin of a living organism in need thereof, the catechin can be delivered to the body through a medical carrier to achieve antioxidant effects.
依Biosci Biotechnol Biochem. 1999 Sep;63(9):1621-3所述,綠茶兒茶素及其相關化合物具有自由基清除活性。基於此,本發明之第五實施方式提出一種如第二實施方式所述之醫藥組合物的用途,其為用於製備清除自由基的乳劑,其中黃烷-3-醇為兒茶素。如前所述,所製的乳劑塗抹於有此需求之生物體的皮膚上時,可透過醫藥載體經皮遞送兒茶素至體內,以達到清除自由基的目的。According to Biosci Biotechnol Biochem. 1999 Sep; 63(9): 1621-3, green tea catechins and related compounds have free radical scavenging activity. Based on this, a fifth embodiment of the present invention provides a use of the pharmaceutical composition according to the second embodiment, which is an emulsion for preparing a radical scavenging agent, wherein the flavan-3-ol is catechin. As described above, when the prepared emulsion is applied to the skin of the organism in need thereof, the catechin can be delivered to the body through the medical carrier to achieve the purpose of scavenging free radicals.
依Curr Med Chem Anticancer Agents. 2002 Jul;2(4):441-63所述,兒茶素為新穎的抗癌與抗血管新生化合物。基於此,本發明之第六實施方式提出一種如第二實施方式所述之醫藥組合物的用途,其為用於製備抗癌的乳劑,其中黃烷-3-醇為兒茶素。如前所述,所製的乳劑塗抹於有此需求之生物體的皮膚上時,可透過醫藥載體經皮遞送兒茶素至體內,以達到抗癌目的。According to Curr Med Chem Anticancer Agents. 2002 Jul; 2(4): 441-43, catechins are novel anti-cancer and anti-angiogenic compounds. Based on this, a sixth embodiment of the present invention provides a use of the pharmaceutical composition according to the second embodiment, which is an emulsion for preparing an anticancer, wherein the flavan-3-ol is catechin. As described above, when the prepared emulsion is applied to the skin of a living body in need thereof, the catechin can be delivered to the body through a medical carrier to achieve anticancer effects.
依Antiviral Res. 2005 Nov;68(2):66-74所述,綠茶兒茶素可透過與紅血球凝集素(hemagglutinin,HA)間的作用並改變病毒外膜來對抗病毒,特別是流感病毒。基於此,本發明之第七實施方式提出一種如第二實施方式所述之醫藥組合物的用途,其為用於製備抗病毒的乳劑,其中黃烷-3-醇為兒茶素。如前所述,所製的乳劑塗抹於有此需求之生物體的皮膚上時,可透過醫藥載體經皮遞送兒茶素至體內,以達到抗病毒目的。According to Antiviral Res. 2005 Nov;68(2):66-74, green tea catechins can fight viruses, especially influenza viruses, by interacting with hemagglutinin (HA) and altering the outer membrane of the virus. Based on this, a seventh embodiment of the present invention provides a use of the pharmaceutical composition according to the second embodiment, which is an emulsion for preparing an antiviral, wherein the flavan-3-ol is catechin. As described above, when the prepared emulsion is applied to the skin of the organism in need thereof, the catechin can be delivered to the body through the medical carrier to achieve antiviral purpose.
依Eur J Nutr. 2014 Sep;53(6):1299-311所述,統合分析(meta-analysis)證實綠茶及其兒茶素可改善血壓。基於此,本發明之第八實施方式提出一種如第二實施方式所述之醫藥組合物的用途,其為用於製備降血壓的乳劑,其中黃烷-3-醇為兒茶素。如前所述,所製的乳劑塗抹於有此需求之生物體的皮膚上時,可透過醫藥載體經皮遞送兒茶素至體內,以達到降血壓目的。According to Eur J Nutr. 2014 Sep;53(6):1299-311, meta-analysis confirmed that green tea and its catechins can improve blood pressure. Based on this, an eighth embodiment of the present invention provides a use of the pharmaceutical composition according to the second embodiment, which is an emulsion for preparing a blood pressure lowering, wherein the flavan-3-ol is catechin. As described above, when the prepared emulsion is applied to the skin of the organism in need thereof, the catechin can be delivered to the body through the medical carrier to achieve the purpose of lowering blood pressure.
依Pharm Dev Technol. 2014 Jun;19(4):395-400所述,兒茶素的乳化作用可影響皮膚穿透與UV保護。基於此,本發明之第九實施方式提出一種如第二實施方式所述之醫藥組合物的用途,其為用於製備預防UV傷害的乳劑,其中黃烷-3-醇為兒茶素。如前所述,所製的乳劑塗抹於有此需求之生物體的皮膚上時,可透過醫藥載體經皮遞送兒茶素至體內,以達到預防UV傷害的目的。According to Pharm Dev Technol. 2014 Jun;19(4):395-400, the emulsification of catechins can affect skin penetration and UV protection. Based on this, a ninth embodiment of the present invention provides a use of the pharmaceutical composition according to the second embodiment, which is an emulsion for preparing for preventing UV damage, wherein the flavan-3-ol is catechin. As described above, when the prepared emulsion is applied to the skin of the living body in need thereof, the catechin can be delivered to the body through the medical carrier to prevent UV damage.
茲以下述實施例,以詳細說明本發明的上述實施方式:The above embodiments of the present invention are described in detail by the following examples:
<實施例01至14><Examples 01 to 14>
將水相組份、油相組份、界面活性劑、與輔助界面活性劑混合後,渦漩攪拌所得的混合液20秒以得到醫藥載體。接著,加入(+)-兒茶素至所得的醫藥載體中,並將所得的混合物渦漩攪拌1分鐘以得到乳劑。實施例01至14中所選用的水相組份、油相組份、界面活性劑、與輔助界面活性劑比例、及(+)-兒茶素比例如表1所示。 表1、實施例01至14之乳劑的成分及其比例
利用Franz擴散器(diffusion cell)進行以下試驗,試驗時搭配循環水槽控制水溫。首先,將鼠皮自-20℃冰箱中取出並回溫至室溫。將鼠皮裁切成適當尺寸後,置於供應腔室(donor chamber)與接受腔室(receptor chamber)間的平面上。接著,緊密供應腔室與接受腔室後,Na2 HPO3 .2H2 O-檸檬酸緩衝液(pH5.5)經取樣口(sampling port)填入接受腔室,且接受腔室配置有攪拌子。於供應腔室給1毫升所得的乳劑後,以parafilm封口膜密封供應腔室的上開口。最後,於給藥後的特定時間點,自接受腔室取0.5毫升緩衝液進行高效液相色譜法(high performance liquid chromatography,HPLC)分析以進行成分分析,並於取出後立即加入0.5毫升新鮮緩衝液至接受腔室內。The following test was carried out using a Franz diffuser cell, which was controlled with a circulating water tank to control the water temperature. First, the mouse skin was taken out from the -20 ° C refrigerator and warmed to room temperature. After the mouse skin is cut to an appropriate size, it is placed on a plane between the donor chamber and the receptor chamber. Next, after tightly supplying the chamber to the receiving chamber, Na 2 HPO 3 . 2H 2 O-citrate buffer (pH 5.5) was filled into the receiving chamber through a sampling port, and the receiving chamber was equipped with a stir bar. After 1 ml of the resulting emulsion was supplied to the supply chamber, the upper opening of the supply chamber was sealed with a parafilm sealing film. Finally, at a specific time point after administration, 0.5 ml of buffer was taken from the receiving chamber for high performance liquid chromatography (HPLC) analysis for component analysis, and 0.5 ml of fresh buffer was added immediately after removal. Liquid into the receiving chamber.
如圖1至3所示,分別呈現實施例01至14之乳劑給藥後12小時的(+)-兒茶素累積透過量、遲延時間、及給藥後12小時的(+)-兒茶素皮內沉積量。As shown in Figs. 1 to 3, the (+)-catechin cumulative permeation amount, the delay time, and the (+)-category of 12 hours after the administration of the emulsions of Examples 01 to 14 were respectively exhibited. The amount of deposition in the prime skin.
<實施例15至31><Examples 15 to 31>
參照上述所示的製備流程與試驗流程,製備出實施例15至31的乳劑並分析之。實施例15至31中所選用的水相組份、油相組份、界面活性劑、與輔助界面活性劑比例、以及(+)-兒茶素比例如表2所示。 表2、實施例15至31之乳劑的成分及其比例
如圖4至6所示,分別呈現實施例15至31之乳劑給藥後12小時的(+)-兒茶素累積透過量、遲延時間、及給藥後12小時的(+)-兒茶素皮內沉積量。As shown in Figs. 4 to 6, the (+)-catechin cumulative permeation amount, the delay time, and the (+)-catechin 12 hours after administration of the emulsions of Examples 15 to 31, respectively, were exhibited. The amount of deposition in the prime skin.
綜合以上結果,證實本發明的醫藥載體可增加藥物的經皮透過量與穿透速率,進而提升皮內的藥物沉積量,特別是黃烷-3-醇。Based on the above results, it was confirmed that the pharmaceutical carrier of the present invention can increase the transdermal permeation rate and the penetration rate of the drug, thereby increasing the amount of drug deposition in the skin, particularly flavan-3-ol.
雖然本發明已以較佳實施例揭露於上,然其並非用以限定本發明,本發明所屬技術領域中具有通常知識者,在不脫離本發明之精神及範圍內,當可作些許之更動與潤飾,因此本發明的保護範圍當視後附之申請專利範圍所請求者為準。Although the present invention has been disclosed in its preferred embodiments, it is not intended to limit the invention, and the invention may be modified by those skilled in the art without departing from the spirit and scope of the invention. The scope of the present invention is intended to be in accordance with the scope of the appended claims.
無no
圖1為一統計長條圖,說明著實施例01至14所得之乳劑12小時後的累積透過量(cumulative amount)。 圖2為一統計長條圖,說明著實施例01至14所得之乳劑的遲延時間(lag time)。 圖3為一統計長條圖,說明著實施例01至14所得之乳劑12小時後的皮內沉積量(deposition amount)。 圖4為一統計長條圖,說明著實施例15至31所得之乳劑12小時後的累積透過量。 圖5為一統計長條圖,說明著實施例15至31所得之乳劑的遲延時間。 圖6為一統計長條圖,說明著實施例15至31所得之乳劑12小時後的皮內沉積量。Figure 1 is a statistical bar graph illustrating the cumulative amount of the emulsion obtained in Examples 01 through 14 after 12 hours. Figure 2 is a statistical bar graph illustrating the lag time of the emulsions obtained in Examples 01 through 14. Figure 3 is a statistical bar graph illustrating the amount of deposition of the emulsions obtained in Examples 01 through 14 after 12 hours. Figure 4 is a statistical bar graph showing the cumulative permeation of the emulsions obtained in Examples 15 to 31 after 12 hours. Figure 5 is a statistical bar graph illustrating the delay time of the emulsions obtained in Examples 15 to 31. Figure 6 is a statistical bar graph showing the amount of intradermal deposition of the emulsions obtained in Examples 15 to 31 after 12 hours.
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