水間 俊
| 薬学部 薬学科 | 教授 |
Last Updated :2025/10/07
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論文
- Kinetic Assessment of Luminal Degradation of Orally Effective Prodrugs for Rational Drug Development
Takashi Mizuma
JOURNAL OF PHARMACEUTICAL SCIENCES, 2010年02月, ［査読有り］ - Intestinal glucuronidation metabolism may have a greater impact on oral bioavailability than hepatic glucuronidation metabolism in humans: A study with raloxifene, substrate for UGT1A1, 1A8, 1A9, and 1A10
Takashi Mizuma
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2009年08月, ［査読有り］ - Assessment of Presystemic and Systemic Intestinal Availability of Orally Administered Drugs Using In Vitro and In Vivo Data in Humans: Intestinal Sulfation Metabolism Impacts Presystemic Availability Much More Than Systemic Availability of Salbutamol, SULT1A3 Substrate
Takashi Mizuma
JOURNAL OF PHARMACEUTICAL SCIENCES, 2008年12月, ［査読有り］ - 糖トランスポーターを利用したDDS
水間 俊
Drug delivery system, 2006年03月10日
糖トランスポーターを利用したDDSについて, これまでの知見をまとめた. 糖トランスポーターを利用した"薬物"のデリバリーの報告例は少ない. 腸管においては, SGLT1を介した各種グリコシドの輸送が報告されている. 糖の種類, 糖と薬物の結合様式によりその動態は異なる. 単糖付加体は, SGLT1を介した新規腸管吸収ルートを通ることの出来るプロドラッグとなるが, 二糖付加体の場合は, さらにプレプロドラッグとして利用できる可能性がある.
一方, 各種ペプチドのグルコシドが脳や腎臓へ移行することが報告されているが, 糖トランスポーターの介在性に関する明確なデータはない. - Kinetic characterization of glycosidase activity from disaccharide conjugate to monosaccharide conjugate in Caco-2 cells.
Mizuma T; Fuseda N; Hayashi M
The Journal of pharmacy and pharmacology, 2005年05月, ［査読有り］ - Differentiation of organ availability by sequential and simultaneous analyses: intestinal conjugative metabolism impacts on intestinal availability in humans.
Mizuma T; Kawashima K; Sakai S; Sakaguchi S; Hayashi M
Journal of pharmaceutical sciences, 2005年03月, ［査読有り］ - Simultaneous HPLC assay of lenampicillin (ampicillin prodrug), ampicillin, and marker compound for high-throughput in vitro assessment of intestinal absorption and metabolism using caco-2 cells
T Mizuma; S Sakaguchi; M Hayashi
JOURNAL OF LIQUID CHROMATOGRAPHY & RELATED TECHNOLOGIES, 2005年, ［査読有り］ - SGLT1-mediated transport of glucoside increase intestinal availability
Y Nakajima; M Nakamura; T Mizuma; H Ina; T Miyazaki; M Hayashi
YAKUGAKU ZASSHI-JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN, 2004年, ［査読有り］ - Concentration-dependent atypical intestinal absorption of cyclic phenylalanylserine: Small intestine acts as an interface between the body and ingested compounds
T Mizuma; T Narasaka; S Awazu
BIOLOGICAL & PHARMACEUTICAL BULLETIN, 2003年11月, ［査読有り］ - Uptake of cyclic dipeptide by PEPT1 in Caco-2 cells: phenolic hydroxyl group of substrate enhances affinity for PEPT1
T Mizuma; T Narasaka; S Awazu
JOURNAL OF PHARMACY AND PHARMACOLOGY, 2002年09月, ［査読有り］ - 輸送担体および代謝酵素が関わる薬物腸管吸収の連続的過程と競合的過程 ＳＧＬＴ１，二糖分解酵素，ペプチダーゼ，グルクロン酸抱合代謝酵素について
水間 俊; 松本 誠一; 萩 桂; 小柳 晶裕; 奈良坂 琢央; 布施田 典彦; 林 正弘; 粟津 荘司
薬物動態, 2001年
We have studied intestinal metabolism and transport, which is considered to be sequential (1) or competitive (2) process in absorption (Scheme 1). (1) Disaccharide (maltose, cellobiose, lactose) conjugates of p-nitrophenol were hydrolyzed to p-nitrophenyl β-glucosides (p-NPβglc) on the mucosal side. p-NPβglc was transported by Na+/glucose cotransporter (SGLT1). Transport clearance of p-NPβglc formed from cellobiose and lactose conjugates of p-NP were higher than that from maltose or of p-NPβglc itself. These results suggest that SGLT1 is cooperatively coupled with lactase/phloridzin hydrolase catalyzing hydrolysis of cellobiose and lactose conjugates. There might be cooperative relationship between peptidase and H+/oligopeptide cotransporter or amino acid transporter as well. (2) Kyotorphin (KTP) was too unstable in intestine to be absorbed. KTP appeared on the serosal side in the presence of peptidase inhibitors. Meanwhile, cyclic KTP was stable in intestine to be absorbed. Absorption clearance of cyclic KTP was higher than the overall transport clearance of KTP, which was calculated according to the metabolic inhibition model. Competitive process was observed in intestinal absorption of α-naphthol as well. These results indicate that metabolism degradation and membrane transport are competitive. Unless drug is stabilized against metabolic enzyme, intestinal absorption of drug can not be improved even if membrane transport is increased. - ROLE OF TRANSPORTER AND METAOBLIC ENZYME IN INTESTINAL DRUG ABSORPTION
水間 俊; 松本 誠一; 萩 桂; 小柳 晶裕; 奈良坂 琢央; 布施田 典彦; 林 正弘; 粟津 荘司
薬物動態, 2000年
We have studied intestinal metabolism and transport, which is considered as sequential (1) or competitive (2) process in absorption (Scheme 1). (1) Disaccharide (maltose, cellobiose, lactose) conjugates of p-nitrophenol were hydrolyzed to p-nitrophenyl β-glucosides (p-NPβglc) on the mucosal side. p-NPβglc was transported by Na+/glucose cotransporter (SGLT1). Transport clearance of p-NPβglc formed from cellobiose and lactose conjugates of p-NP were higher than that from maltose or of p-NPβglc itself. These results suggest that SGLT1 may be cooperatively coupled with lactase/phloridzin hydrolase catalizing hydrolysis of cellobiose and lactose conjugates. There might be cooperative relationship between peptidase and H+/oligopeptide cotransporter or amino acid transporter as well. (2) Kyotorphin (KTP) was too unstable in intestine to be absorbed. KTP appeared on the serosal side in the presence of peptidase inhibitors. Meanwhile, cyclic KTP was stable in intestine to be absorbed. Absorption clearance of cyclic KTP was higher than the overall transport clearance of KTP, which was calculated according to the metabolic inhibition model. These results indicate that metabolism degradation and membrane transport are competitive. Unless drug is stabilized against metabolic enzyme, intestinal absorption of drug can not be improved even if membrane transport is increased. - Transportability and recognizability of SGLT1 for alkyl glucosides: TRN (Transportable, Recognizable, Non-interactive) classification of glucose conjugates
T Mizuma; S Matsumoto; S Awazu
CONTROL AND DISEASES OF SODIUM DEPENDENT TRANSPORT PROTEINS AND ION CHANNELS, 2000年, ［査読有り］ - Intestinal absorption of acyclovir beta-glucoside: Comparative study with acyclovir, guanosine, and kinetin beta-glucoside
T Mizuma; S Masubuchi; S Awazu
PHARMACEUTICAL RESEARCH, 1999年01月, ［査読有り］ - Intestinal absorption and analgesic activity of aminopeptidase-resistant cellobiose-coupled leucine enkephalinamide
T Mizuma; K Ohta; S Awazu
BIOPHARMACEUTICS & DRUG DISPOSITION, 1998年12月, ［査読有り］ - Intestinal Na+/glucose cotransporter-mediated transport of glucose conjugate formed from disaccharide conjugate
T Mizuma; S Awazu
BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS, 1998年01月, ［査読有り］ - ACTION MECHANISM OF PERMEATION ENHANCERS IN PARACELLULAR PATHWAY
M HAYASHI; M CHIDA; T OGAWA; T MIZUMA; T HORIE; S AWAZU
JOURNAL OF PHARMACOBIO-DYNAMICS, 1992年02月, ［査読有り］
MISC
- Does the well-stirred model assess the intestinal first-pass effect well?
J Pharm Pharmacol, 2004年 - Caco-2細胞を用いた薬物の第2相代謝と吸収に関する検討 (第25回生体膜と薬物の相互作用シンポジウム--ダイナミックインターフェイスとしての生体膜 講演要旨集)
水間 俊; 川島 弘之; 林 正弘
薬学雑誌, 2003年11月13日
日本薬学会 - 糖付加体の吸収動態と体内分布 : 梅肉含有 Benzylglucoside について
中村 摩耶; 水間 俊; 林 正弘
薬剤学 = Journal of Pharmaceutical Science and Technology, Japan, 2003年03月05日 - Caco-2細胞を用いたグルクロン酸抱合代謝活性評価及び代謝阻害効果の検討
川島 弘之; 水間 俊; 林 正弘
薬剤学 = Journal of Pharmaceutical Science and Technology, Japan, 2003年03月05日 - Caco-2細胞におけるグルクロン酸抱合代謝活性の変動とその要因
百田 亮一; 水間 俊; 芳賀 信; 林 正弘
薬物動態 = Xenobiotic metabolism and disposition, 2001年09月17日 - 糖付加体に対するNa^+/glucose共輸送担体の認識性と輸送性: aryl glucoside と alkyl glucoside との比較検討
古代 晃士; 布施田 典彦; 水間 俊; 林 正弘; 栗津 荘司
薬物動態 = Xenobiotic metabolism and disposition, 2001年09月17日 - Caco-2細胞におけるグルクロン酸抱合代謝の各種要因の検討
百田 亮一; 水間 俊; 芳賀 信; 林 正弘
薬剤学 = Journal of Pharmaceutical Science and Technology, Japan, 2001年03月05日 - Factors that cause β-anomeric preference of Na+/glucose cotransporter for intestinal transport of monosaccharide conjugates
Biochim. Biophys. Acta. ,, 1998年08月 - Intestinal Na+/glucose cotransporter-mediated transport of glucose conjugate formed from disaccharide conjugate
MIZUMA T; AWAZU S
Biochim. Biophys. Acta. ,, 1998年 - Photo-Stability of Drugs in Enteral Hyperalimentation Solutions and Its Influence on the Dose Given by a Continuous Infusion :
MIZUMA TAKASHI; NAKAJIMA SAYURI; TAKASE HIROSHI; KUROSAKI TOSHIMI; HORIKOSHI ISAMU
病院薬学, 1991年
日本病院薬剤師会 - IRREVERSIBLE BINDING OF FUROSEMIDE TO HUMAN SERUM ALBUMIN BY METABOLIC ACTIVATION, PHOTOACTIVATION AND BOTH ACTIVATIONS
MIZUMA Takashi; BENET Leslie Z.; McDONAGH Anthony F.; LIN Emil T.
Journal of pharmacobio-dynamics, 1990年
公益社団法人日本薬学会
書籍等出版物
- 生物薬剤学 ドラッグデリバリーシステム：プロドラッグ（化学修飾）化による方法
南江堂, 2001年 - Transportability and recognizability of SGLTI for alkyl glucosides : TRN (Transportable, Recognizable ; Non-interactive) classification of glucose conjugates
Control and disease of Sodium dependent transport proteins and ion channels, 2000年 - Transportability and recognizability of SGLTI for alkyl glucosides : TRNC Transportable, Recognizable ; Non-interactive classification of glucose conjugates
Control and disease of Sodium dependent transport proteins and ion channels, 2000年
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