JP2012529451A - 5−アミノレブリン酸を含む固体組成物 - Google Patents
5−アミノレブリン酸を含む固体組成物 Download PDFInfo
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- 125000000400 lauroyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 230000002475 laxative effect Effects 0.000 description 1
- 229940049918 linoleate Drugs 0.000 description 1
- 235000020888 liquid diet Nutrition 0.000 description 1
- 238000011068 loading method Methods 0.000 description 1
- 235000010420 locust bean gum Nutrition 0.000 description 1
- 239000000711 locust bean gum Substances 0.000 description 1
- 239000008176 lyophilized powder Substances 0.000 description 1
- 239000011777 magnesium Substances 0.000 description 1
- 229910052749 magnesium Inorganic materials 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 230000037353 metabolic pathway Effects 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 229910021645 metal ion Inorganic materials 0.000 description 1
- 150000002739 metals Chemical class 0.000 description 1
- 230000009401 metastasis Effects 0.000 description 1
- YUUAYBAIHCDHHD-UHFFFAOYSA-N methyl 5-aminolevulinate Chemical compound COC(=O)CCC(=O)CN YUUAYBAIHCDHHD-UHFFFAOYSA-N 0.000 description 1
- 239000011859 microparticle Substances 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 238000012544 monitoring process Methods 0.000 description 1
- RZRNAYUHWVFMIP-UHFFFAOYSA-N monoelaidin Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC(O)CO RZRNAYUHWVFMIP-UHFFFAOYSA-N 0.000 description 1
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- 210000004877 mucosa Anatomy 0.000 description 1
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- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
- 239000002105 nanoparticle Substances 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 1
- FBUKVWPVBMHYJY-UHFFFAOYSA-N nonanoic acid Chemical compound CCCCCCCCC(O)=O FBUKVWPVBMHYJY-UHFFFAOYSA-N 0.000 description 1
- 239000007764 o/w emulsion Substances 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
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- 229940049964 oleate Drugs 0.000 description 1
- 235000021313 oleic acid Nutrition 0.000 description 1
- 229940055577 oleyl alcohol Drugs 0.000 description 1
- XMLQWXUVTXCDDL-UHFFFAOYSA-N oleyl alcohol Natural products CCCCCCC=CCCCCCCCCCCO XMLQWXUVTXCDDL-UHFFFAOYSA-N 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 239000001301 oxygen Chemical group 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 238000010979 pH adjustment Methods 0.000 description 1
- 230000005298 paramagnetic effect Effects 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000006072 paste Substances 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 229960003330 pentetic acid Drugs 0.000 description 1
- 230000002572 peristaltic effect Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 239000008363 phosphate buffer Substances 0.000 description 1
- 239000002953 phosphate buffered saline Substances 0.000 description 1
- 230000036211 photosensitivity Effects 0.000 description 1
- 239000010665 pine oil Substances 0.000 description 1
- 229920001993 poloxamer 188 Polymers 0.000 description 1
- 229920001515 polyalkylene glycol Polymers 0.000 description 1
- 229920000193 polymethacrylate Polymers 0.000 description 1
- 229940100528 polyoxyl 8 stearate Drugs 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- 229940068965 polysorbates Drugs 0.000 description 1
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- 150000004032 porphyrins Chemical class 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 238000004393 prognosis Methods 0.000 description 1
- 230000001737 promoting effect Effects 0.000 description 1
- 239000001944 prunus armeniaca kernel oil Substances 0.000 description 1
- 238000001407 pulse-discharge detection Methods 0.000 description 1
- 150000004040 pyrrolidinones Chemical class 0.000 description 1
- 125000001453 quaternary ammonium group Chemical group 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- WBHHMMIMDMUBKC-QJWNTBNXSA-M ricinoleate Chemical compound CCCCCC[C@@H](O)C\C=C/CCCCCCCC([O-])=O WBHHMMIMDMUBKC-QJWNTBNXSA-M 0.000 description 1
- 229940066675 ricinoleate Drugs 0.000 description 1
- 235000005713 safflower oil Nutrition 0.000 description 1
- 239000003813 safflower oil Substances 0.000 description 1
- 229940057910 shea butter Drugs 0.000 description 1
- 150000004666 short chain fatty acids Chemical class 0.000 description 1
- 235000021391 short chain fatty acids Nutrition 0.000 description 1
- 208000017520 skin disease Diseases 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- APSBXTVYXVQYAB-UHFFFAOYSA-M sodium docusate Chemical compound [Na+].CCCCC(CC)COC(=O)CC(S([O-])(=O)=O)C(=O)OCC(CC)CCCC APSBXTVYXVQYAB-UHFFFAOYSA-M 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- 229910000162 sodium phosphate Inorganic materials 0.000 description 1
- 239000011343 solid material Substances 0.000 description 1
- 239000012265 solid product Substances 0.000 description 1
- 229940035044 sorbitan monolaurate Drugs 0.000 description 1
- 235000011071 sorbitan monopalmitate Nutrition 0.000 description 1
- 239000001570 sorbitan monopalmitate Substances 0.000 description 1
- 229940031953 sorbitan monopalmitate Drugs 0.000 description 1
- 235000011076 sorbitan monostearate Nutrition 0.000 description 1
- 239000001587 sorbitan monostearate Substances 0.000 description 1
- 229940035048 sorbitan monostearate Drugs 0.000 description 1
- 235000019337 sorbitan trioleate Nutrition 0.000 description 1
- 229960000391 sorbitan trioleate Drugs 0.000 description 1
- 235000011078 sorbitan tristearate Nutrition 0.000 description 1
- 239000001589 sorbitan tristearate Substances 0.000 description 1
- 229960004129 sorbitan tristearate Drugs 0.000 description 1
- 239000008347 soybean phospholipid Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000008174 sterile solution Substances 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 239000001384 succinic acid Substances 0.000 description 1
- 150000008054 sulfonate salts Chemical class 0.000 description 1
- 239000011593 sulfur Chemical group 0.000 description 1
- 229910052717 sulfur Chemical group 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 208000011580 syndromic disease Diseases 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- OULAJFUGPPVRBK-UHFFFAOYSA-N tetratriacontyl alcohol Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCO OULAJFUGPPVRBK-UHFFFAOYSA-N 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 231100000027 toxicology Toxicity 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 229920000428 triblock copolymer Polymers 0.000 description 1
- 150000005691 triesters Chemical class 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- PHYFQTYBJUILEZ-IUPFWZBJSA-N triolein Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(OC(=O)CCCCCCC\C=C/CCCCCCCC)COC(=O)CCCCCCC\C=C/CCCCCCCC PHYFQTYBJUILEZ-IUPFWZBJSA-N 0.000 description 1
- HRXKRNGNAMMEHJ-UHFFFAOYSA-K trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 description 1
- 229940038773 trisodium citrate Drugs 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
- 125000004417 unsaturated alkyl group Chemical group 0.000 description 1
- 210000002438 upper gastrointestinal tract Anatomy 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
- 235000013311 vegetables Nutrition 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 229920003176 water-insoluble polymer Polymers 0.000 description 1
- 230000004580 weight loss Effects 0.000 description 1
Classifications
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- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
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- A61K41/00—Medicinal preparations obtained by treating materials with wave energy or particle radiation ; Therapies using these preparations
- A61K41/0057—Photodynamic therapy with a photosensitizer, i.e. agent able to produce reactive oxygen species upon exposure to light or radiation, e.g. UV or visible light; photocleavage of nucleic acids with an agent
- A61K41/0061—5-aminolevulinic acid-based PDT: 5-ALA-PDT involving porphyrins or precursors of protoporphyrins generated in vivo from 5-ALA
-
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
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- A61K49/001—Preparation for luminescence or biological staining
- A61K49/0013—Luminescence
- A61K49/0017—Fluorescence in vivo
- A61K49/0019—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules
- A61K49/0021—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules the fluorescent group being a small organic molecule
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Abstract
【選択図】なし
Description
a) 5-ALA、5-ALAの前駆体又は5-ALAの誘導体、及び、その薬学的に許容可能な塩から選ばれる活性成分;
b) 1種類以上のトリグリセリド;及び、
c) 1種類以上の乳化剤、
を含む、固体薬品を提供する。
R2 2N-CH2COCH2-CH2CO-OR1(I)
上式において、
R1は、置換又は非置換アルキル基を表し;且つ、
R2は、それぞれ独立に、水素原子又はR1基を表す。
a) 5-ALA及びその薬学的に許容可能な塩、好ましくは、5-ALAエステル又はその薬学的に許容可能な塩;
b) 一つ以上のトリグリセリド;及び、
c) 一つ以上の乳化剤、
を含む、固体薬品である。
d) 必要に応じて一つ以上の粘性接着剤;
e) 必要に応じて、b)及びc)以外の、一つ以上の薬学的に許容可能な賦形剤;
f) 必要に応じて、一つ以上の表面浸透剤;及び、
g) 必要に応じて、一つ以上のキレート剤
を含む。
本発明による固体薬品が、必要に応じて、一つ以上の薬学的に許容される溶媒を含む場合、その溶媒は、遊離脂肪酸、遊離脂肪性アルコール、水溶液、例えば、バッファー又は水であってもよい。しかしながら、本発明による固体薬品は、まったく水を含まないこと、すなわち、無水であることが好ましい。無水であるとは、その固体薬品に水が添加されないこと、及び、製品において何らかの測定可能な水分含量があるとしても、それは、成分a)-g)のいずれかに偶発的に含まれる可能性のある水分によるものであることを意味する。
下部消化管における癌、前癌、及び非癌状態の光力学診断に使用するための固体組成物又は固体薬品の製造における、
a) 5-ALA、5-ALAの前駆体、又は5-ALAの誘導体、及びその薬学的に許容可能な塩から選ばれる活性成分;
b) 一つ以上のトリグリセリド;及び
c) 一つ以上の乳化剤
の使用を提供する。
下部消化管、特に、結腸及び直腸における癌及び前癌状態の光力学診断に使用するための固体組成物又は固体薬品の製造における、
a) 5-ALA、5-ALAの前駆体、又は5-ALAの誘導体、及びその薬学的に許容可能な塩から選ばれる活性成分;
b) 一つ以上のトリグリセリド;及び
c) 一つ以上の乳化剤
の使用を提供する。
下部消化管における癌、前癌、及び非癌状態の光力学診断法であって、
(a) 対象、例えば、ヒト又は非ヒト動物に対し、本明細書に定義される固体薬品又は固体組成物を投与すること;
(b) 上記薬品内の活性成分が光感受性物質に変換され、下部消化管の所望部位において有効組織濃度を実現するのに必要な期間待機すること;
(c) 光感受性物質を光活性化すること;及び、
(d) 上記光感受性物質から、癌、前癌、及び非癌状態を示す蛍光を検出すること、
を含む上記方法を提供する。
a) 5-ALA、5-ALAの前駆体、又は5-ALAの誘導体、及びその薬学的に許容可能な塩から選ばれる活性成分;
b) 一つ以上のトリグセリド;及び
c) 一つ以上の乳化剤
を含む固体組成物を提供する。
a) 5-ALA、5-ALAの前駆体、又は5-ALAの誘導体、及びその薬学的に許容可能な塩から選ばれる活性成分;
b) 一つ以上のトリグリセリド;及び
c) 一つ以上の乳化剤
からなる。
本発明による固体組成物
n-ヘキシルアミノレブリン酸エステル(HAL)塩酸塩(HAL HCl)(フォトキュアASA、ノルウェー)を含むコートされたカプセルは、「カプセル組成物」の下に列挙される化合物同士を、それらの融点よりも高い温度で混ぜ合わせることによって調製した。この混合物を、白色HPMCカプセル中に注入し、HPMC(3.1 mg)、ジェランガム(0.015 mg)、及びクエン酸三ナトリウム(0.05 mg)の水溶液によって結合させた。このカプセルを、湿度耐性コーティング(6.3 mg/cm2、Opadry AMB)によってコートし、次いで、腸溶コーティング(8 mg/cm2、共に水中に分散させた、80% Eudragit(登録商標) L30 D-55及び20% Eudragit(登録商標) FS 30Dの混合物による)によってコートし、6.5以上のpHで崩壊するpH感受性フィルムを得た。
HALの溶解
実施例1に従って調製されたカプセルA-Hはインビトロ溶解実験に用いた。ヒトの胃内状態を模倣するために、カプセルを先ず、500 mlの0.1M HClの溶解媒体(1)中に37°Cで1時間浸漬させた。次に、カプセルをこの媒体から取り出し、ヒトの末端回腸の状態、すなわち、水性環境及びpHを模倣すべく、pH 6.5、37°Cの温度を有する、500 mlの水性リン酸バッファーの溶解媒体(2)に浸漬させた。両浸漬において、パドル及びシンカーを備えた穏やかな溶解装置"USP 711"を用いた。カプセルをシンカーに置き、溶解媒体中に沈めた。75 rpmの回転速度を選んだ。5、15、30、60、120、及び180分において、溶解媒体の2 mlサンプルを手で取りだした。このサンプルをろ過し(40 μm HDPEフィルター)、HAL含量をHPLCによって定量した。このサンプルのHAL含量は、標準曲線との比較によって計算した。六つのカプセルA-HのHAL放出を分析した。下記の表は平均放出を示す。
溶解媒体(1)ではHAL放出は観察されなかった。
インビボにおけるHAL HClの放出
腸溶コートカプセル、すなわち、本発明による固体薬品の消化器移送の評価において、上記腸溶コートカプセルから組成物が放出される部位、及び、空っぽの、すなわち、洗浄後の結腸におけるHAL HClの分布を決定するために、健康な男性ボランティアにおいてガンマ・シンチグラフィー実験を実施した。
6名の検査対象から成る群に対して処置Aを施した。すなわち、1 MBq以下の111In-DTPAによって放射線標識した水性処方(処方A)を、EnterionTMカプセルを介して末端回腸/盲腸に送達させ、その部においてカプセルの内容物を放出させた。EnterionTMカプセルは、4 MBq以下の99mTc-DTPAによって放射線標識した、合計500 mLの水と共に送達された。この99mTc-標識水は、250 mLから成る、二つの分液として投与された、すなわち、第1分液はカプセルの投与時で、第2分液は、カプセルが胃から排出された後である。ガンマ・シンチグラフィーを実行し、結腸全体における処方Aの分布程度を決定した。活性化1時間後では、分布は狭く、盲腸及び上行結腸に限局していた。最大分布、すなわち、結腸全体への分布は、活性化後平均7時間後に観察された。図1a-cは、活性化後2、6、及び12時間における分布を示す。
4名の検査対象から成る群に対し処置Bを施した。すなわち、1 MBq以下の111In-DTPAによって放射線標識した、200 mgのMiglyol(登録商標) 812及び100 mgのGelucire(登録商標) 44/14に溶解させた100 mgのHAL HClからなる組成物(組成物B)を、EnterionTMカプセルを介して末端回腸/盲腸に送達させ、その部においてカプセルの内容物を放出させた。EnterionTMカプセルは、4 MBq以下の99mTc-DTPAによって放射線標識した、合計500 mLの水と共に送達された。この99mTc-標識水は、250 mLから成る、二つの分液として投与された、すなわち、第1分液はカプセルの投与時で、第2分液は、カプセルが胃から排出された後である。ガンマ・シンチグラフィーを実行し、結腸全体における処方Bの分布程度を決定した。活性化1時間後では、組成物の結腸到着は、1名の検査対象にしか見られなかった。最大分布、すなわち、結腸全体への分布は、活性化後平均10時間後に観察された。組成物Bの分布は、処方Aのものと同様である、すなわち、水の分布に匹敵することが認められた。図2a-c参照。同図は、活性化後2、6、及び12時間における分布を示す。
6名の検査対象から成る群に対し処置Cを施した。すなわち、1 MBq以下の111In-DTPAによって放射線標識した、200 mgのMiglyol(登録商標) 812及び100 mgのGelucire(登録商標) 44/14に溶解した100 mgのHAL HClから成る組成物(組成物C)を、実施例1で記述した通りの腸溶コートカプセルを介して送達させた。この腸溶コートカプセルは、4 MBq以下の99mTc-DTPAによって放射線標識した、合計500 mLの水と共に送達された。この99mTc-標識水は、250 mLから成る、二つの分液として投与された、すなわち、第1分液はカプセルの投与時で、第2分液は、カプセルが胃から排出された後である。ガンマ・シンチグラフィーを実行し、結腸全体における処方Cの分布程度を決定した。組成物Cの分布は、処方Aのものと同様である、すなわち、水の分布に匹敵することが認められた。図3a-c参照。同図は、放出後2、6、及び12時間における分布を示す。
Claims (15)
- 下部消化管における癌、前癌、及び非癌状態の光力学診断に使用するための固体薬品であって、
a) 5-ALA、5-ALAの前駆体、又は5-ALAの誘導体、及びその薬学的に許容可能な塩から選ばれる活性成分;
b) 一つ以上のトリグリセリド;及び
c) 一つ以上の乳化剤
を含む固体薬品。 - 前記活性成分が、5-ALAの誘導体、好ましくは5-ALAエステル又はその薬学的に許容可能な塩であることを特徴とする、請求項1に記載の固体薬品。
- 前記活性成分が、式Iの化合物、又は、その許容可能な塩であり、
R2 2N-CH2COCH2-CH2CO-OR1(I)
上式において、
R1は、置換又は非置換アルキル基を表し;且つ、
R2は、それぞれ独立に、水素原子又はR1基を表す、
ことを特徴とする、請求項1及び2に記載の固体薬品。 - 前記一つ以上のトリグリセリドが、グリセロールと、三つの同じか又は異なるC2-C22脂肪酸、より好ましくは三つの同じか又は異なるC4-C18脂肪酸、さらに好ましくは三つの同じか又は異なるC6-C18脂肪酸、及びもっとも好ましくは三つの同じか又は異なるC6-C12脂肪酸とからなるトリグリセリドであることを特徴とする、前項のいずれにも記載の固体薬品。
- 前記一つ以上のトリグリセリドが、ココアバター、木蝋、ハードファット、水素添加ココ-グリセリド、水素添加パーム油、トリステアリン、トリパルミチン及びトリミリスチンから選ばれる固体トリグリセリドであるか、又は、トリカプリリン、トリカプロイン、トリヘプタノイン、カプリル酸/カプリン酸トリグリセリド、カプリル酸/カプリン酸/リノレン酸トリグリセリドから選ばれる液体トリグリセリドであることを特徴とする、前項のいずれにも記載の固体薬品。
- 前記一つ以上の乳化剤が非イオン性であることを特徴とする、前項のいずれにも記載の固体薬品。
- 前記一つ以上の乳化剤が、ポリエチレングリコールと、天然又は水素添加油脂との反応から得られる非イオン性乳化剤であることを特徴とする、前項のいずれにも記載の固体薬品。
- d) 必要に応じて一つ以上の粘性接着剤;
e) 必要に応じて、b)、c)及びd)以外の、一つ以上の薬学的に許容可能な賦形剤;
f) 必要に応じて、一つ以上の表面浸透剤;及び、
g) 必要に応じて、一つ以上のキレート剤
をさらに含むことを特徴とする、前項のいずれにも記載の固体薬品。 - 前記薬品が、坐剤、又は、一つ以上の腸溶コーティングを含む経口用固体薬品であって、pH 6.5からpH 7.5の範囲において活性成分a)のpH調節放出を実現する薬品であることを特徴とする、前項のいずれにも記載の固体薬品。
- 前記固体薬品が水を含まないことを特徴とする、前項のいずれにも記載の固体薬品。
- a) 5-ALA、5-ALAの前駆体又は5-ALAの誘導体、及びその薬学的に許容可能な塩から選ばれる活性成分;
b) 一つ以上のトリグリセリド;及び
c) 一つ以上の乳化剤
を含む固体組成物。 - 前記活性成分が、5-ALAの誘導体、好ましくは、5-ALAエステル又はその薬学的に許容可能な塩であり、前記一つ以上のトリグリセリドが、ココアバター、木蝋、ハードファット、水素添加ココ-グリセリド、水素添加パーム油、トリステアリン、トリパルミチン及びトリミリスチンから選ばれる固体トリグリセリドであるか、又は、グリセロールと、三つの同じか又は異なるC2-C22脂肪酸、より好ましくは、三つの同じか又は異なるC4-C18脂肪酸、さらに好ましくは、三つの同じか又は異なるC6-C18脂肪酸、及びもっとも好ましくは、三つの同じか又は異なるC6-C12脂肪酸からなるトリグリセリドから選ばれる液体トリグリセリドであり、且つ、前記一つ以上の乳化剤が、ポリエチレングリコールと、天然又は水素添加油脂との反応から得られる非イオン性乳化剤である、ことを特徴とする請求項11に記載の固体組成物。
- 薬剤として使用される、請求項11及び12に記載の固体組成物。
- 下部消化管における癌、前癌、及び非癌状態の光力学診断において使用される、請求項11及び12に記載の固体組成物。
- 下部消化管における癌、前癌、及び非癌状態の光力学診断法において使用され、前記方法が:
(a) 対象、例えば、ヒト又は非ヒト動物に対し、請求項1〜10に記載の固体薬品、又は請求項11〜14に記載の固体組成物を投与すること;
(b) 前記薬品内の活性成分が光感受性物質に変換され、下部消化管の所望部位において有効組織濃度を達成するのに必要な期間待機すること;
(c) 該光感受性物質を光活性化すること;及び、
(d) 前記光感受性物質から、癌、前癌、及び非癌状態を示す蛍光を検出すること、
を含む、請求項1〜10に記載の固体薬品、又は請求項11〜14に記載の固体組成物。
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BRPI1011650A2 (pt) | 2016-03-22 |
CO6480960A2 (es) | 2012-07-16 |
RU2527328C2 (ru) | 2014-08-27 |
AU2010257752B2 (en) | 2015-04-09 |
PE20120858A1 (es) | 2012-08-01 |
CL2011003115A1 (es) | 2012-06-22 |
US20120134921A1 (en) | 2012-05-31 |
ZA201108850B (en) | 2013-02-27 |
WO2010142456A1 (en) | 2010-12-16 |
CA2763837A1 (en) | 2010-12-16 |
SG176687A1 (en) | 2012-01-30 |
EP2440188A1 (en) | 2012-04-18 |
RU2011150920A (ru) | 2013-07-20 |
CR20110649A (es) | 2012-03-22 |
NZ596946A (en) | 2014-07-25 |
CN102802612A (zh) | 2012-11-28 |
KR20140014401A (ko) | 2014-02-06 |
MX2011013069A (es) | 2012-02-01 |
AU2010257752A1 (en) | 2012-01-12 |
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