KR100287626B1 - Pharmaceutical composition for treatment of erectile dysfunction and device for transdermal administration of formulation - Google Patents

Pharmaceutical composition for treatment of erectile dysfunction and device for transdermal administration of formulation Download PDF

Info

Publication number
KR100287626B1
KR100287626B1 KR1019950043422A KR19950043422A KR100287626B1 KR 100287626 B1 KR100287626 B1 KR 100287626B1 KR 1019950043422 A KR1019950043422 A KR 1019950043422A KR 19950043422 A KR19950043422 A KR 19950043422A KR 100287626 B1 KR100287626 B1 KR 100287626B1
Authority
KR
South Korea
Prior art keywords
patch
weight
composition
acid
erectile dysfunction
Prior art date
Application number
KR1019950043422A
Other languages
Korean (ko)
Other versions
KR970025609A (en
Inventor
이헌한
조중웅
백재승
Original Assignee
김윤
주식회사삼양사
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 김윤, 주식회사삼양사 filed Critical 김윤
Priority to KR1019950043422A priority Critical patent/KR100287626B1/en
Priority to US08/627,805 priority patent/US5741511A/en
Priority to CN96193170A priority patent/CN1181022A/en
Priority to EP96909389A priority patent/EP0831942A1/en
Priority to JP8530906A priority patent/JPH10512173A/en
Priority to PCT/KR1996/000052 priority patent/WO1996032141A1/en
Publication of KR970025609A publication Critical patent/KR970025609A/en
Application granted granted Critical
Publication of KR100287626B1 publication Critical patent/KR100287626B1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins

Abstract

PURPOSE: A patch composition for treatment of erectile impotence comprising prostaglandin E1, a stabilizer and a penetration enhancer is provided. Also provided is a patch device comprising a patch composition-containing patch, a supporter for supporting the patch and a compression ring. The patch device helps treat erectile dysfunction and stimulates erection effectively. CONSTITUTION: The patch composition comprises 5 to 30% by weight of an erection-inducing composition such as prostaglandin E1, minoxidil or linsidomine, 1 to 60% by weight of one or more stabilizers such as polyethylene glycol, triacetin, propylene glycol or ethanol and 1 to 50% by weight of one or more skin penetration enhancers selected from cetyl alcohol, stearyl alcohol, 1-dodecanol, oleyl alcohol, lactic acid, oleic acid, salicylic acid, lecithin, linoleic acid, linolenic acid, bile salt, monoolein, 1-menthol or ethanol. The patch device comprises a patch(20) containing the patch composition, a band type supporter and a ring(30) for compressing the base part of the genitals, wherein the patch comprises a backing layer, a matrix or a drug layer, a porous membrane and a removable film.

Description

발기부전 치료용 약물조성 및 경피투여제형Drug composition and transdermal drug formulation for erectile dysfunction

제1도는 본 발명의 패취기구 사용 상태를 나타내는 개략도이다.1 is a schematic view showing a state of using the patch mechanism of the present invention.

제2도는 본 발명의 밴드형 지지체와 패취의 평면도이다.2 is a plan view of the band-like support and the patch of the present invention.

제3도는 본 발명의 패취를 밴드형 지지체에 결합하여 사용할때 패취기구의 평면도이다.3 is a plan view of a patch mechanism when the patch of the present invention is used in conjunction with a band-like support.

제4도(A)는 제거용 필름을 제거하지 않았을 경우 제3도의 A-A' 선 단면도이다.4A is a cross-sectional view taken along the line A-A 'of FIG. 3 when the removal film is not removed.

제4도(B)는 제거용 필름을 제거하였을 경우 제3도의 A-A' 선 단면도이다.FIG. 4B is a cross-sectional view taken along the line A-A 'of FIG. 3 when the removal film is removed.

* 도면에서 부호의 설명 *Explanation of symbols in the drawing

1. 성기의 귀두 10. 밴드형 지지체1. Genital glans 10. Band-shaped support

11. 점착제 층 20. 패취11.Adhesive layer 20. Patch

21. 패취의 손잡이 부분 30. 압박고리21. Handle part of patch 30. Pressing ring

101. 제거용 필름 102. 다공성 막101. Removal film 102. Porous membrane

103. 매트릭스 또는 레져보형 약물 층 104. 백킹레이어103. Matrix or leisure drug layer 104. Backing layer

본 발명은 성기능 장애인 발기부전, 임포텐스 환자에게 인위적으로 발기를 유발시키는 약물, 특히 프로스타글란딘 E1, 린시도민, 미녹시딜 등의 약물의 액체, 반-액체, 크림, 서스펜션, 젤, 연고, 젤-연고, 고형질 등에 균일하게 혼합하거나 용매에 녹여서 만든 패취제형이나 또는 약물을 고분자 젤에 분포시켜서 만든 패취를 남성 성기의 귀두 부위에 직접 적용시켜서 발기를 유발시키는 패취, 남성 성기의 기저부위를 압박하는 고리, 환 등으로 구성된 발기부전 치료용 고안물에 관한 것이다. 또한 이러한 고안물에 사용되는 패취내에 약물안정화제로서 글리세롤류 특히 트리아세틴(글리세롤 트리아세테이트), 프로필렌글리콜, 폴리에틸렌 글리콜 또는 에탄올을 사용하고 피부침투증강제로는 지방족 산이나 지방족 알코올류로서 특히 세틸알코올, 스테아릴알코올, 1-도데칸올, 올레일알코올, 유산, 올레산, 살리실산, 미리스틴산, 미네랄오일, 담즙염, 모노올레인, 리놀레익산, 리놀레닉산, 레시틴 및 테르펜 유도체인 1-멘솔, 에탄올을 사용함을 특징으로 하는 패취의 조성에 관한 것이다.The present invention is a liquid, semi-liquid, cream, suspension, gel, ointment, gel-ointment, high-dose drugs, such as prostaglandin E1, lincidomin, minoxidil, drugs that cause artificial erection in patients with impotence and impotence Patches that are made by uniformly mixing traits or dissolved in a solvent, or patches made by distributing drugs in a polymer gel, are applied directly to the glans of the male genitals to induce erections, and rings that press the base of the male genitals. The present invention relates to a design for treating erectile dysfunction. In addition, glycerol, in particular triacetin (glycerol triacetate), propylene glycol, polyethylene glycol, or ethanol, is used as a patch stabilizer in the patch used in the present invention, and as a skin penetration enhancer, in particular cetyl alcohol, Stearyl alcohol, 1-dodecanol, oleyl alcohol, lactic acid, oleic acid, salicylic acid, myristic acid, mineral oil, bile salt, monoolein, linoleic acid, linolenic acid, lecithin and terpene derivatives 1-menthol, It relates to the composition of a patch characterized by the use of ethanol.

프로스타글란딘 E1을 이용하여 발기부전 및 임포턴스를 치료하는데 쓰이는 기존제형으로는 주로 주사제가 대부분이며 최근에 개발된 제형으로는 남성 성기의 요도를 통해서 약물을 전달하는 방법(MUSE)이 개발되고 있다. 일본 공개특허 평2-264,725호에는 고혈압 및 말초혈액장애 치료를 위한 프로스타글란딘 E1의 경피투여제형이 개시되어 있고, 일본 공개특허 평3-83,926호에는 괴저병 피부궤양 치료를 위해 지방족알코올과 사이클로덱스트린 유도체를 약물안정화제로 쓰는 제형이, 미국특허 제5,082,664호에는 프로스타글란딘 E1을 리포솜에 도입한 제형이 개시되어 있다. 한편 국제특허 제95-37,787호에는 비페이직 멀티라멜라 리피드 비씨클(biphasic multilamellar lipid vesicles, MLV)을 이용하여 임포턴스치료를 위해 프로스타글란딘 E1을 경피적으로 투여하는 방법이 개시되어 있다.Existing formulations mainly used to treat erectile dysfunction and impurity using prostaglandin E1 are mainly injections, and recently developed formulations (MUSE) have been developed to deliver drugs through the urethra of male genitalia. Japanese Patent Laid-Open No. 2-264,725 discloses a transdermal dosage form of prostaglandin E1 for treating hypertension and peripheral blood disorders, and Japanese Patent Laid-Open No. 3-83,926 discloses aliphatic alcohols and cyclodextrin derivatives for the treatment of necrotic skin ulcers. Formulations for use as drug stabilizers, US Pat. No. 5,082,664 discloses formulations in which prostaglandin E1 is introduced into liposomes. Meanwhile, International Patent No. 95-37,787 discloses a method for transdermal administration of prostaglandin E1 for impartance treatment using biphasic multilamellar lipid vesicles (MLV).

그러나 상기의 선행기술에 개시된 프로스타글란딘 E1의 경피투여 제형은 성기세포에 프로스타글란딘 E1 약물흡수가 용이하지 않고, 그 사용이 간편하지 못하여 실용화되기가 어려웠다.However, the transdermal dosage form of prostaglandin E1 disclosed in the above prior art has not been easy to absorb prostaglandin E1 drug into the genital cells, and its use is not easy to be practical.

따라서 본 발명의 목적은 프로스타글란딘 E1에 약물안정화제와 피부침투증강제를 혼합한 약물조성을 함유한 패취, 이 패취를 지지하는 밴드형 지지체 및 압박고리로 구성된 발기부전 치료를 위한 고안물을 제공하는데 있다.Accordingly, an object of the present invention is to provide a design for the treatment of erectile dysfunction consisting of a patch containing a drug composition in which a prostaglandin E1 is mixed with a drug stabilizer and a skin penetration enhancer, a band-like support and a compression ring supporting the patch.

또한 본 발명에서 사용되는 약물의 조성은 주성분약인 프로스타글란딘 E1과 같은 남성 성기의 발기를 인위적으로 유발시키는 약물 5~30 중량%에 대하여, 약물안정화제로서 글리세롤류인 폴리에틸렌 글리콜, 트리아세틴, 프로필렌글리콜 또는 에탄올 중에서 선택된 1종 이상을 1~60 중량% 사용하고, 피부침투증강제로는 지방족산이나 알코올류, 특히 세틸알코올, 스테아릴알코올, 1-도데칸올, 올레일알코올, 유산, 올레산, 살리실산, 미리스틴산, 레시틴, 리놀레익산, 리놀레닉산, 담즙염, 모노올레인 및 테르펜 유도체인 1-멘솔 또는 에탄올 중에서 선택된 1종 이상을 1~50 중량% 사용하여 조성된 패취 조성물인 것이다.In addition, the composition of the drug used in the present invention is glycerol-based polyethylene glycol, triacetin, propylene glycol or ethanol as a drug stabilizing agent with respect to 5-30% by weight of a drug that artificially causes an erection of male genitalia, such as prostaglandin E1, the main ingredient. 1 to 60% by weight of one or more selected from among them, and skin penetration enhancers include aliphatic acids and alcohols, especially cetyl alcohol, stearyl alcohol, 1-dodecanol, oleyl alcohol, lactic acid, oleic acid, salicylic acid, myristic It is a patch composition composed of 1 to 50% by weight of at least one selected from 1-menthol or ethanol which is acid, lecithin, linoleic acid, linolenic acid, bile salt, monoolein and terpene derivatives.

이때 약물의 안정화제로 쓰이는 폴리에틸렌 글리콜은 분자량이 200, 400, 600, 1000, 2000, 4000, 8000 등을 1~60 중량%로 사용하며 특히 15~35 중량%를 사용하는 것이 바람직하다. 또다른 약물안정화제인 프로필렌글리콜 1~50 중량%로 사용하며 특히 5~20 중량%로 하는 것이 바람직하다.In this case, polyethylene glycol, which is used as a stabilizer of the drug, has a molecular weight of 200, 400, 600, 1000, 2000, 4000, 8000, etc., using 1 to 60% by weight, and particularly preferably 15 to 35% by weight. Another drug stabilizer is used in an amount of 1 to 50% by weight of propylene glycol, and particularly preferably 5 to 20% by weight.

피부침투증강제인 에탄올은 1~40 중량%를 사용하며, 특히 5~35 중량%를 사용함이 바람직하고, 1-멘솔은 1~15 중량%를 사용하고 특히 1~10 중량%를 사용함이 바람직하다.Ethanol, a skin penetration enhancer, is used in an amount of 1 to 40% by weight, particularly preferably 5 to 35% by weight, and 1-menthol is preferably used in an amount of 1 to 15% by weight, in particular, 1 to 10% by weight. .

또다른 피부침투증강제로는 쓰이는 지방족산이나 알코올 특히 세틸알코올, 스테아릴알코올, 미리스틴산, 1-도데카놀, 올레일알코올, 유산, 올레산, 살리실산 및 레시틴, 담즙염, 모노올레인, 리놀레익산, 리놀레닉산 등은 1~50 중량%로 사용하며, 특히 5~50 중량%로 사용함이 바람직하다.Other skin penetration enhancers include fatty acids and alcohols, especially cetyl alcohol, stearyl alcohol, myristic acid, 1-dodecanol, oleyl alcohol, lactic acid, oleic acid, salicylic acid and lecithin, bile salts, monoolein, linoleic Iksan, linolenic acid and the like are used in an amount of 1 to 50% by weight, and particularly preferably in an amount of 5 to 50% by weight.

이하 본 발명의 패취고안물의 구성을 도면을 참조하여 더욱 상세히 설명한다.Hereinafter, the configuration of the patched object of the present invention will be described in more detail with reference to the drawings.

기본적으로, 본 발명은 약물조성을 함유한 패취, 이를 지지시키는 지지체 및 압박고리 등으로 구성된 패취 고안물에 관한 것으로, 본 발명의 패취 고안물은 점착제층이 없는 3층 구조로된 패취 또는 점착제층이 있는 4층 구조로된 패취로 구성되어 있다.Basically, the present invention relates to a patch design consisting of a patch containing the drug composition, a support for supporting it, and a pressure ring, etc. The patch design of the present invention is a patch or pressure-sensitive adhesive layer having a three-layer structure without an adhesive layer. It consists of a patch of four layers.

제1도는 본 발명의 발기부전 치료를 위한 기구의 전체구성을 나타낸 것으로, 점착제를 사용하지 않은 패취(20), 패취를 성기의 귀두 부위에 지지시킬 수 있는 밴드형 지지체(10)와 성기의 기저 부위를 압박하는 압박고리(30)로 구성되어 있다.Figure 1 shows the overall configuration of the apparatus for the treatment of erectile dysfunction of the present invention, the patch 20, the band-like support 10 and the base of the genital that can support the patch on the glans of the genitals Compression ring 30 for pressing the site is composed.

제2도는 본 발명의 밴드형 지지체(10)과 패취(20)의 평면도로서 밴드형 지지체 점착제 층(11)을 지니고 있으며 사용시 점착제 층위의 제거용 필름을 제거하여 사용한다. 또한 패취(20)의 가장자리에 제거용 필름(101)을 손쉽게 제거할 수 있는 손잡이 부위(21)가 있어, 사용시 쉽게 제거용 필름(101)을 제거한다.2 is a plan view of the band-like support 10 and the patch 20 of the present invention having a band-like support pressure-sensitive adhesive layer 11 and used to remove the film for removal on the pressure-sensitive adhesive layer in use. In addition, there is a handle portion 21 that can easily remove the removal film 101 on the edge of the patch 20, it is easy to remove the removal film 101 in use.

제3도는 본 발명의 패취(20)와 밴드형 지지체(10)이 결합된 상태를 나타낸 것이다. 또한 제4도는 제3도의 A-A' 선 단면도를 나타내는 것으로 제4도(A)는 패취(20)의 제거용 필름(101)을 제거하지 않은 경우이고, 제4도(B)는 패취(20)의 제거용 필름(101)을 제거한 경우이다. 제4도에 나타난 바와 같이 제거용 필름(101) 하부에는 다공성 막(102)이 있고 그 하부에 매트릭스 또는 레져보형의 약물층(103)이 있으며, 그 밑에 백킹레이어(104)와 밴드형 지지체(10)가 존재한다.3 shows a state in which the patch 20 and the band-shaped support 10 of the present invention are combined. 4 is a cross-sectional view taken along the line AA ′ of FIG. 3, and FIG. 4A illustrates a case where the removal film 101 of the patch 20 is not removed, and FIG. 4B illustrates the patch 20. This is the case where the film 101 for removal of is removed. As shown in FIG. 4, there is a porous membrane 102 under the removal film 101, and there is a matrix or leisure-type drug layer 103 under the backing layer 104, and a backing layer 104 and a band-shaped support (below). 10) exists.

본 발명의 패취기구의 사용은 제1도에 나타난 바와 같이, 점착제가 있는 밴드형 지지체를 이용하여 패취를 성기의 귀두부위에 고정시키고, 성기의 기저부위를 압박하는 압박고리와 함께 사용한다. 본 발명에서 사용되는 패취의 형태는 특히 유선형으로서 성기의 귀두와 패취를 최대한 밀착시킬 수 있는 형태로서 본 발명의 고유한 특징중의 하나이다.Use of the patch mechanism of the present invention, as shown in Figure 1, using a pressure-sensitive adhesive band-like support to fix the patch to the head of the genitals, it is used in conjunction with the compression ring for pressing the base of the genitals. The form of the patch used in the present invention is one of the inherent features of the present invention, in particular, in the form of a streamlined form that can close the genitals and the patch.

레저보형 패취의 제조는 약물투과성이 없는 필름 특히 폴리에스터 백킹필름 또는 알루미늄 코팅된 폴리에스터 필름을 100~150℃ 온도 범위에서 진공/열 성형하고 여기에 약물안정화제와 피부침투증강제를 포함하는 약물조성을 100~1000㎕ 정도 가하고 약물투과성인 다공성 막을 위에 놓고 100~150℃ 온도범위에서 1차 열압착한다. 제2도에서 빗금친 부분(21)은 제거용 필름을 떼어내는 손잡이를 나타낸 것으로서 백킹필름과 다공성막의 1차 열압착시 패취의 테두리뿐만 아니라 손잡이 부분도 함께 열압착하여 제조한다.The production of leisure-type patches is carried out by vacuum / thermoforming a film having no drug permeability, particularly a polyester backing film or an aluminum coated polyester film, in a temperature range of 100 to 150 ° C., and comprising a drug stabilizer and a skin penetration enhancer. Add about 100 ~ 1000µl and place the drug-permeable porous membrane on the first thermocompression bonding at the temperature range of 100 ~ 150 ℃. The hatched portion 21 in FIG. 2 shows a handle for removing the removal film, and is manufactured by thermocompression bonding the handle portion as well as the edge of the patch during the first thermal compression of the backing film and the porous membrane.

여기에 사용직전에 떼어내는 필름인 제거용 필름(101)을 100~160℃ 온도범위에서 2차로 열압착하며, 이때는 패취의 손잡이 부분(21)은 열압착하지 않고, 테두리 부분만 열압착하여 점착제 층이 없는 패취를 제조하며, 이 패취를 유선형 절단기로 절단하여 본 발명의 고유한 형태인 유선형 패취로 제조한다.Here, the film 101 for removal, which is a film to be removed immediately before use, is thermally compressed in a second temperature in a temperature range of 100 to 160 ° C. In this case, the handle portion 21 of the patch is not thermally compressed but only the edge portion is thermally compressed. A layerless patch is prepared, which is cut into a streamlined cutter to produce a streamlined patch which is a unique form of the present invention.

1차 열압착시 패취의 손잡이 부분(21)을 함께 열압착하는 제조방법은 패취 사용직전 제거용필름을 떼어낼때 다공성막(102)이 찢어지는 단점을 보완할 수 있는 본 발명만의 고유한 특징중의 하나이다.The manufacturing method of thermocompression bonding the handle portion 21 of the patch during the first thermocompression is a unique feature of the present invention that can compensate for the disadvantage that the porous membrane 102 is torn off when removing the film for removal immediately before using the patch. Is one of.

이하 본 발명의 실시예를 통하여 본 발명의 패취 약물조성 및 그 제조방법을 설명한다. 본 발명의 실시예는 단지 본 발명을 예시하기 위한 것이며, 본 발명의 범위가 본 실시예들로 한정되는 것은 아니다.Hereinafter, the patch drug composition of the present invention and a method of preparing the same will be described through examples of the present invention. The embodiments of the present invention are merely for illustrating the present invention, and the scope of the present invention is not limited to the embodiments.

[실시예 1]Example 1

(패취조성물의 조성)Composition of Patch Composition

페놀수지로 코팅된 밀폐용기에 폴리에틸렌 글리콜 600 27.3 중량%, 모노올레인 45.2 중량%, 프로필렌 글리콜 7.6 중량%를 넣고 균일하게 혼합한 후, 위의 혼합액에 1-멘솔 4.8 중량%를 첨가하여 완전히 투명해질때까지 녹인다. 프로스타글란딘 E1 용액을 15.1 중량% 첨가하여 균일한 혼합액을 만든다. 패취 제조방법에 따라 1-, 2-차 열압착으로 패취를 제조하고, 프란츠셀과 휴먼 카데버스킨을 사용하여 약물의 피부투과량을 측정한다.27.3% by weight of polyethylene glycol 600, 45.2% by weight of monoolein, 7.6% by weight of propylene glycol were mixed in a closed container coated with a phenolic resin, and then mixed uniformly, and 4.8% by weight of 1-menthol was added to the above mixture to be completely transparent. Melt until sunset. 15.1% by weight of prostaglandin E1 solution is added to form a homogeneous mixture. According to the patch manufacturing method, the patch is prepared by 1-, 2-second thermocompression, and the skin permeation of the drug is measured by using Franzcell and human cadaverskin.

이때 약물의 피부 투과실험은 크라운글라스회사의 프란츠셀과 휴먼 카데버스킨을 사용하였으며, 약물의 피부투과량을 증대시키기 위하여 스킨의 최외각 층을 기존의 알려진 방법인 미국특허 제5,003,987호에 개시된 방법을 개선하여 5~10회 정도 제거하여 본 발명의 여러가지 약물조성을 시험하였다.At this time, the skin permeation experiment of the drug was used Franzcell and Human Cadebuskin of Crown Glass Company, and the method disclosed in US Patent No. 5,003,987, which is a known method of the outermost layer of the skin in order to increase the skin penetration of the drug By improving and removing about 5 to 10 times, various drug compositions of the present invention were tested.

[실시예 2]Example 2

(패취조성물의 조성)Composition of Patch Composition

에탄올에 폴리에틸렌 글리콜 8000을 녹여 폴리에틸렌 글리콜 200 32.4 중량%를 섞고, 모노올레인 32.7 중량%와 트리아세틴 8.3 중량%를 넣고 균일하게 혼합한 후, 위의 혼합액에 1-멘솔 4.8 중량%를 첨가하여 완전히 투명해질때까지 녹인다. 프로스타글란딘 E1 용액을 14.7 중량% 첨가하여 균일한 혼합액을 만든다. 패취 제조방법에 따라 1-, 2-차 열압착으로 패취를 제조하고, 프란츠셀과 휴먼 카데버 스킨을 사용하여 약물의 피부투과량을 측정한다.Dissolve polyethylene glycol 8000 in ethanol, mix 32.4 wt% of polyethylene glycol 200, add 32.7 wt% of monoolein and 8.3 wt% of triacetin, uniformly mix, and add 4.8 wt% of 1-menthol to the mixture. Melt until clear. 14.7% by weight of prostaglandin E1 solution is added to form a homogeneous mixture. According to the patch manufacturing method, the patch is prepared by 1-, 2-second thermocompression, and the skin permeation amount of the drug is measured by using Franzcell and Human Caderber skin.

[실시예 3]Example 3

(패취조성물의 조성)Composition of Patch Composition

프로필렌 글리콜 43.2 중량%에 담즙염 2.7 중량%를 첨가하여 완전히 투명해질때까지 녹인다. 에탄올에 1-멘솔을 녹이고, 두 용액을 동량 섞어 균일한 혼합물을 만든다. 프로스타글란딘 E1 용액을 17.0 중량% 첨가하여 균일한 혼합액을 만든다. 패취 제조방법에 따라 1-, 2-차 열압착으로 패취를 제조하고, 프란츠셀과 휴먼 카데버 스킨을 사용하여 약물의 피부투과량을 측정한다.Add 43.2% propylene glycol to 2.7% bile salt and dissolve until completely clear. Dissolve 1-menthol in ethanol and mix both solutions in equal amounts to form a uniform mixture. 17.0% by weight of prostaglandin E1 solution is added to form a uniform mixture. According to the patch manufacturing method, the patch is prepared by 1-, 2-second thermocompression, and the skin permeation amount of the drug is measured by using Franzcell and Human Caderber skin.

[실시예 4]Example 4

(패취조성물의 조성)Composition of Patch Composition

분자량 3350인 폴리에틸렌 글리콜 18.6 중량%와 분자량 400인 폴리에틸렌 글리콜 27.9 중량%를 가열하면서 균일하게 혼합한다. 여기에 모노올레인 18.6 중량%, 프로필렌글리콜 11.7 중량%, 1-멘솔 4.6 중량%를 가하여 균일한 액상을 유지할 수 있는 가장 낮은 온도를 유지시킨다.18.6% by weight of polyethylene glycol having a molecular weight of 3350 and 27.9% by weight of polyethylene glycol having a molecular weight of 400 are mixed uniformly while heating. 18.6% by weight of monoolein, 11.7% by weight of propylene glycol, and 4.6% by weight of 1-menthol are added to maintain the lowest temperature to maintain a uniform liquid phase.

프로스타글란딘 E1 용액 18.6 중량%를 위에서 준비한 액상과 균일하게 혼합한다. 패취 제조방법에 따라 1-차, 2-차 열압착으로 패취를 제조하고, 프란츠셀과 휴먼 카데버 스킨을 사용하여 약물의 피부투과량을 측정한다.18.6% by weight of the prostaglandin E1 solution is uniformly mixed with the liquid prepared above. According to the patch manufacturing method, the patch is prepared by first- and second-order thermocompression, and the skin permeation amount of the drug is measured by using Franzcell and Human Caderber skin.

[실시예 5]Example 5

(패취조성물의 조성)Composition of Patch Composition

분자량 3350인 폴리에틸렌 글리콜 18.6 중량%와 분자량 400인 폴리에틸렌 글리콜 27.9 중량%를 가열하면서 균일하게 혼합한다. 여기에 모노올레인 9.2 중량%, 프로필렌 글리콜 11.7 중량%, 20% 에탄올 담즙염 용액 9.4 중량%, 1-멘솔 4.6 중량%를 가하여 균일한 액상을 유지할 수 있는 가장 낮은 온도를 유지시킨다.18.6% by weight of polyethylene glycol having a molecular weight of 3350 and 27.9% by weight of polyethylene glycol having a molecular weight of 400 are mixed uniformly while heating. 9.2% by weight of monoolein, 11.7% by weight of propylene glycol, 9.4% by weight of 20% ethanol bile salt solution and 4.6% by weight of 1-menthol are added to maintain the lowest temperature to maintain a uniform liquid phase.

프로스타 글란딘 E1 용액 18.6 중량%를 위에서 준비한 액상과 균일하게 혼합한다. 패취 제조방법에 따라 1-차, 2-차 열압착으로 패취를 제조하고, 프란츠셀과 휴먼 카데버 스킨을 사용하여 약물의 피부투과량을 측정한다.18.6% by weight of the prostaglandin E1 solution is uniformly mixed with the liquid prepared above. According to the patch manufacturing method, the patch is prepared by first- and second-order thermocompression, and the skin permeation amount of the drug is measured by using Franzcell and Human Caderber skin.

[실시예 6]Example 6

(패취조성물의 조성)Composition of Patch Composition

분자량 3350인 폴리에틸렌 글리콜 18.6 중량%와 분자량 400인 폴리에틸렌 글리콜 27.9 중량%를 가열하면서 균일하게 혼합한다. 여기에 모노올레인 9.3 중량%, 올레산 9.3 중량%, 프로필렌글리콜 11.7 중량%, 1-멘솔 4.6 중량%를 가하여 균일하게 액상을 유지할 수 있는 가장 낮은 온도를 유지시킨다.18.6% by weight of polyethylene glycol having a molecular weight of 3350 and 27.9% by weight of polyethylene glycol having a molecular weight of 400 are mixed uniformly while heating. 9.3% by weight of monoolein, 9.3% by weight of oleic acid, 11.7% by weight of propylene glycol, and 4.6% by weight of 1-menthol are added to maintain the lowest temperature to maintain a uniform liquid phase.

프로스타글란딘 E1 용액 18.6 중량%를 위에서 준비한 액상과 균일하게 혼합한다. 패취 제조방법에 따라 1-차, 2-차 열압착으로 패취를 제조하고, 프란츠셀과 휴먼 카데버 스킨을 사용하여 약물의 피부투과량을 측정한다.18.6% by weight of the prostaglandin E1 solution is uniformly mixed with the liquid prepared above. According to the patch manufacturing method, the patch is prepared by first- and second-order thermocompression, and the skin permeation amount of the drug is measured by using Franzcell and Human Caderber skin.

Claims (4)

프로스타글란딘 E1, 미녹시딜 또는 린시도민과 같은 남성 성기의 발기를 인위적으로 유발시키는 약물 5~30 중량%에 대하여, 약물안정화제로 폴리에틸렌 글리콜, 트리아세틴, 프로필렌글리콜 또는 에탄올 중에서 선택된 1종 이상을 1~60 중량% 사용하고, 피부 침투증강제로는 세틸알코올, 스테아릴알코올, 1-도데칸올, 올레일알코올, 유산, 올레산, 살리실산, 미리스틴산, 레시틴, 리놀레익산, 리놀레닉산, 담즙염, 모노올레인, 테르펜 유도체인 1-멘솔 또는 에탄올 중에서 선택된 1종 이상을 1~50 중량% 사용함을 특징으로 하는 성기부착용 발기부전 치료 패취 조성물.1 to 60% by weight of one or more selected from polyethylene glycol, triacetin, propylene glycol or ethanol as a drug stabilizing agent with respect to 5 to 30% by weight of a drug that artificially induces an erection of male genitalia such as prostaglandin E1, minoxidil or lincidomin %, Skin penetration enhancers cetyl alcohol, stearyl alcohol, 1-dodecanol, oleyl alcohol, lactic acid, oleic acid, salicylic acid, myristic acid, lecithin, linoleic acid, linolenic acid, bile salt, monoole 1 to 50% by weight of at least one selected from phosphorus, terpene derivatives 1-menthol or ethanol, erectile dysfunction treatment patch composition characterized in that used. 제1항에 있어서, 약물안정화제인 폴리에틸렌 글리콜은 분자량이 200, 400, 600, 1000, 2000, 4000, 8000인 것을 1~60 중량% 사용하고, 트리아세틴, 프로필렌글리콜은 1~50 중량%를 사용함을 특징으로 하는 성기부착용 발기부전 치료 패취 조성물.According to claim 1, polyethylene glycol is a drug stabilizer of 1 to 60% by weight of the molecular weight of 200, 400, 600, 1000, 2000, 4000, 8000, triacetin, propylene glycol is used 1 to 50% by weight Erectile dysfunction treatment patch composition for genital attachment. 제1항에 있어서, 피부침투증강제인 에탄올은 1~40 중량% 사용하며, 1-멘솔은 1~15 중량% 사용함을 특징으로 하는 성기부착용 발기부전 치료 패취 조성물.The erectile dysfunction treatment patch composition of claim 1, wherein ethanol, a skin penetration enhancer, is used in an amount of 1-40 wt%, and 1-mensol is used in an amount of 1-15 wt%. 제1항의 발기부전 치료용 패취 조성물이 함유된 패취(20), 밴드형 지지체(10) 및 성기의 기저부위를 압박하는 링(30)으로 구성된 발기부전 치료용 패취기구에 있어서, 발기부전 치료용 패취 조성물이 함유된 패취(20)는 백킹레이어(104), 매트릭스 또는 레져보형 약물층(103), 다공성 막(102) 및 제거용 필름(101)로 구성되고, 밴드형 지지체(10)은 점착제 층(11)과 패취의 손잡이 부분(21)로 구성된 것임을 특징으로 하는 성기부착용 발기부전 치료 패취 기구.In the patch device for treating erectile dysfunction comprising a patch 20, a band-like support 10 and a ring 30 for pressing the basal portion of the genital organs, the erectile dysfunction treatment patch The patch 20 containing the patch composition is composed of a backing layer 104, a matrix or leisure drug layer 103, a porous membrane 102 and the removal film 101, the band support 10 is a pressure-sensitive adhesive Erectile dysfunction treatment patch apparatus, characterized in that consisting of the layer 11 and the handle portion 21 of the patch.
KR1019950043422A 1995-04-12 1995-11-24 Pharmaceutical composition for treatment of erectile dysfunction and device for transdermal administration of formulation KR100287626B1 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
KR1019950043422A KR100287626B1 (en) 1995-11-24 1995-11-24 Pharmaceutical composition for treatment of erectile dysfunction and device for transdermal administration of formulation
US08/627,805 US5741511A (en) 1995-04-12 1996-04-10 Transdermal drug delivery device for treating erectile dysfunction
CN96193170A CN1181022A (en) 1995-04-12 1996-04-12 Transdermal drug delivery device for treating erectile dysfunction
EP96909389A EP0831942A1 (en) 1995-04-12 1996-04-12 Transdermal drug delivery device for treating erectile dysfunction
JP8530906A JPH10512173A (en) 1995-04-12 1996-04-12 Transdermal drug delivery device for erectile dysfunction
PCT/KR1996/000052 WO1996032141A1 (en) 1995-04-12 1996-04-12 Transdermal drug delivery device for treating erectile dysfunction

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR1019950043422A KR100287626B1 (en) 1995-11-24 1995-11-24 Pharmaceutical composition for treatment of erectile dysfunction and device for transdermal administration of formulation

Publications (2)

Publication Number Publication Date
KR970025609A KR970025609A (en) 1997-06-24
KR100287626B1 true KR100287626B1 (en) 2001-04-16

Family

ID=37515026

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019950043422A KR100287626B1 (en) 1995-04-12 1995-11-24 Pharmaceutical composition for treatment of erectile dysfunction and device for transdermal administration of formulation

Country Status (1)

Country Link
KR (1) KR100287626B1 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20010076961A (en) * 2000-01-29 2001-08-17 김제종 A medicament for prevention and treatment of sexual dysfunction

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20010076961A (en) * 2000-01-29 2001-08-17 김제종 A medicament for prevention and treatment of sexual dysfunction

Also Published As

Publication number Publication date
KR970025609A (en) 1997-06-24

Similar Documents

Publication Publication Date Title
KR100445449B1 (en) Skin Permeation Enhancer Compositions Using Acyl Lactylates
CA2135925C (en) Use of glycerin in moderating transdermal drug delivery
AU728797B2 (en) External formulation containing loxoprofen
JP2660839B2 (en) Penetration-enhancing pharmaceutical composition for topical application
US5262165A (en) Transdermal nitroglycerin patch with penetration enhancers
JP2650710B2 (en) Skin permeation enhancer composition using sucrose ester
JP2001503749A (en) Fatty acid esters of glycolic acid and salts thereof as permeation enhancers
ES2239191T3 (en) A STABLE EXTERNAL PREPARATION CONTAINING ACETILSALICILIC ACID.
AU765057B2 (en) A device and method for the treatment of erectile dysfunction
AU785199B2 (en) Transdermal delivery of lasofoxifene
KR100287626B1 (en) Pharmaceutical composition for treatment of erectile dysfunction and device for transdermal administration of formulation
WO1982000005A1 (en) Polymeric diffusion matrix containing a vasodilator
JP2002520352A (en) Transdermal patches and topical compositions containing propylnorapomorphine
US20180360769A1 (en) Systems and methods for transdermal drug delivery
JPH08319234A (en) Percutaneous absorption type antiinflammatory and analgesic plaster
EP0486529A1 (en) Transdermal nitroglycerin patch with penetration enhancers
JP3496169B2 (en) Plaster and production method thereof
JP4237293B2 (en) Transdermal patch
JP5619363B2 (en) Transdermal absorption enhancer, skin treatment preparation containing the same, and transdermal absorption preparation
KR950003696B1 (en) Transdermal nitroglycerin patch with penetration enhancers
KR20030032613A (en) Transdermal delivery patch of matrix type
KR20020066047A (en) Compositions containing ketoprofen and Transdermal delivery matrix system for ketoprofen
FR2685204A1 (en) Pharmaceutical compositions for the transcutaneous administration of fenfluramine
JPH04334327A (en) Absorption-promotive composition
JPH04503519A (en) Transdermal nitroglycerin patch with penetration enhancer

Legal Events

Date Code Title Description
A201 Request for examination
E902 Notification of reason for refusal
E601 Decision to refuse application
J201 Request for trial against refusal decision
J301 Trial decision

Free format text: TRIAL DECISION FOR APPEAL AGAINST DECISION TO DECLINE REFUSAL REQUESTED 19981126

Effective date: 20000331

S901 Examination by remand of revocation
E902 Notification of reason for refusal
GRNO Decision to grant (after opposition)
GRNT Written decision to grant
FPAY Annual fee payment

Payment date: 20051230

Year of fee payment: 6

LAPS Lapse due to unpaid annual fee