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METHOD FOR PRODUCING GELATINOUS COMPOSITION, AND GELATINOUS COMPOSITION

Foreign code F210010303
File No. (S2019-0508-N0)
Posted date Jan 29, 2021
Country WIPO
International application number 2020JP025280
International publication number WO 2020262625
Date of international filing Jun 26, 2020
Date of international publication Dec 30, 2020
Priority data
  • P2019-119814 (Jun 27, 2019) JP
Title METHOD FOR PRODUCING GELATINOUS COMPOSITION, AND GELATINOUS COMPOSITION
Abstract Provided is a method for producing a gelatinous composition, the method including: a step for mixing lecithin that has been dissolved or dispersed in water and an organic compound (excluding lecithin) having a molecular weight of 500 or more that has been dissolved or dispersed in water to obtain a mixed liquid containing the lecithin and the organic compound; a step for freeze-drying or heat-drying the mixed liquid to obtain a solid mixture containing the lecithin and the organic compound; and a step for mixing the solid mixture, an oil component and a polar liquid to obtain a gelatinous composition. Also provided is a gelatinous composition produced using the production method.
Outline of related art and contending technology BACKGROUND ART
Because protein formulations are poorly absorbed from the gastrointestinal mucosa upon oral administration and degrade before being absorbed, most of the formulations have been developed as injectables that do not undergo first-pass effects. However, injectables also have many disadvantages such as being invasive, requiring the technique of a medicator, requiring sterile preparation, and the like.
Routes of administration that do not undergo first-pass effects include transdermal administration. Transdermal preparations have advantages such as simple administration methods, easy maintenance of blood levels, simple interruption of administration, and direct confirmation of medication compliance. However, the keratinous layer of the outermost layer of the skin is a strong barrier, and a water-soluble polymer having a molecular weight of 500 or greater is difficult to penetrate the skin. Therefore, preparations containing water-soluble polymers such as protein preparations cannot usually be administered as transdermal preparations.
Physical promotion methods such as microneedle methods and iontophoresis, nanoparticles, liposomes, surfactant vesicles, microemulsions, and the like have been investigated as methods for enhancing migration of drugs to the skin. Microneedle approach is a method of delivering drugs directly into the skin with fine needles, but is not painful compared to injections, but does not change in needle passage through the skin, which has problems with actual use, such as assurance of sterility. In addition, iontophoresis is a method of promoting absorption of drugs from the skin using electrical energy, but requires specialized devices and is suspected of effectiveness in polymers. In the method using nanoparticles, only appendages such as hair follicles and sweat glands are targeted because the nanoparticles are large to penetrate the stratum corneum. Liposomes have limited formulation in which it is difficult to efficiently and stably encapsulate the drug and can change shape so that it permeates between corner layers. Surfactant vesicles and microemulsions leave safety issues when the surfactant concentration is high or alcohol is needed.
On the other hand, gel-like formulations are widely used in various fields such as cosmetics, pharmaceuticals, foods, paints, inks, lubricants, and the like. There are various methods for preparing gel-like preparations, but the preparation of gel-like preparations by reverse string-like micelles has also been reported (NpL 1). A reversed string-like micelle is a type of self-assembly formed by a surfactant, and is known to induce gelation in order to form a network structure in oil.
The present inventors have found that in the past, lecithin/sucrose fatty acid ester (Patent Document 1), lecithin/saccharide (Patent Document 2), lecithin/urea (Patent Document 3), lecithin/polyglycerol (Patent Document 4); Gel-like compositions by reverse string-like micelles of lecithin/ascorbic acid or a derivative thereof (Patent Document 5) and lecithin/aliphatic carboxylic acid (Patent Document 6) have been developed. In addition, (Non-Patent Document 2) reports attempts to percutaneously absorb hydrophobic low molecules using gel-like compositions by reverse string-like micelles. In addition, the present inventors reported (Patent Document 7) a gel-like composition with enhanced skin migration properties of a water-soluble polymer having a molecular weight of 500 or greater by using reverse string-like micelles.
Scope of claims (In Japanese)[請求項1]
 水に溶解又は分散させたレシチンと、水に溶解又は分散させた分子量500以上の有機化合物(但し、レシチンを除く)とを混合し、前記レシチンと前記有機化合物とを含む混合液を得る工程と、
 前記混合液を凍結乾燥又は加熱乾燥し、前記レシチンと前記有機化合物とを含む固体混合物を得る工程と、
 前記固体混合物と、オイル成分と、極性液体とを混合し、ゲル状組成物を得る工程と、
 を含む、ゲル状組成物の製造方法。

[請求項2]
 前記極性液体が水である、請求項1に記載のゲル状組成物の製造方法。

[請求項3]
 レシチンと、分子量500以上の有機化合物(但し、レシチンを除く)と、常温で固体の極性物質と、水とを混合し、前記レシチンと前記有機化合物と前記極性物質とを含む混合液を得る工程と、
 前記混合液を凍結乾燥又は加熱乾燥し、前記レシチンと前記有機化合物と前記極性物質とを含む固体混合物を得る工程と、
 前記固体混合物と、オイル成分とを混合し、ゲル状組成物を得る工程と、
 を含む、ゲル状組成物の製造方法。

[請求項4]
 前記有機化合物が、分子量500以上の水溶性分子である、請求項1~3のいずれか一項に記載のゲル状組成物の製造方法。

[請求項5]
 前記ゲル状組成物が逆紐状ミセル構造を含む、請求項1~4のいずれか一項に記載のゲル状組成物の製造方法。

[請求項6]
 前記ゲル状組成物における前記レシチンの含有量が5~70質量%である、請求項1~5のいずれか一項に記載のゲル状組成物の製造方法。

[請求項7]
 前記ゲル状組成物における前記有機化合物の含有量が0.1~10質量%である、請求項1~6のいずれか一項に記載のゲル状組成物の製造方法。

[請求項8]
 (a)レシチンと、(b)分子量500以上の有機化合物と、(c)オイル成分と、(d)極性物質と、を含むゲル状組成物であって、
 前記ゲル状組成物中で可溶化している前記(b)分子量500以上の有機化合物の量が、前記ゲル状組成物に含まれる前記(d)極性物質に溶解可能な量より多い、
 ゲル状組成物。

[請求項9]
 前記(b))分子量500以上の有機化合物が、分子量500以上の水溶性分子である、請求項8に記載のゲル状組成物。

[請求項10]
 逆紐状ミセル構造を含む、請求項8又は9に記載のゲル状組成物。

[請求項11]
 前記(a)レシチンの含有量が5~70質量%である、請求項8~10のいずれか一項に記載のゲル状組成物。

[請求項12]
 前記(d)極性物質が水である、請求項8~11のいずれか一項に記載のゲル状組成物。

[請求項13]
 前記(b)分子量500以上の有機化合物の含有量が、0.1~10質量%である、請求項8~12のいずれか一項に記載のゲル状組成物。

[請求項14]
 1μm以上の懸濁粒子が存在しない、請求項8~13のいずれか一項に記載のゲル状組成物。

[請求項15]
 請求項1~7のいずれか一項に記載のゲル状組成物の製造方法により製造される、ゲル状組成物。

[請求項16]
 経皮吸収型製剤である、請求項8~15のいずれか一項に記載のゲル状組成物。

[請求項17]
 請求項8~16のいずれか一項に記載のゲル状組成物を含む医薬組成物。

[請求項18]
 請求項8~16のいずれか一項に記載のゲル状組成物を含む化粧料。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • NIHON UNIVERSITY
  • Inventor
  • HASHIZAKI Kaname
  • FUJII Makiko
  • TAGUCHI Hiroyuki
IPC(International Patent Classification)
Specified countries National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DJ DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JO JP KE KG KH KN KP KR KW KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN WS ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL ST SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN TD TG
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