1994 Fiscal Year Final Research Report Summary
Development of Oral Dosage form for Poorly Absorbable Drugs
| Project/Area Number |
05557102
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| Research Category |
Grant-in-Aid for Developmental Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Research Field |
Physical pharmacy
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| Research Institution | Tokyo University of Pharmacy and Life Science |
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Principal Investigator |
AWAZU Shojii School of Pharmacy Professor, 薬学部, 教授 (60012621)
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| Co-Investigator(Kenkyū-buntansha) |
HOSOI Kaoru Meiji Seika K.K.Shinier Researcher, 薬品総合研・製剤研究所, 室長
HAYASHI Masahiro Science University of Tokyo Professor, 薬学部, 教授 (20012669)
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| Project Period (FY) |
1993 – 1994
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| Keywords | Caco-2 / Absorption enhancement / Bioadhensive / Microsphere / Peptide / Intestinal / Concanvaline A / Peyer's Patch |
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| Research Abstract |
Assessment System of Drug Absorption by Cultured Cells, and Control of Whole Study. Caco-2 cell monolayr system for absorption was established. The absorptions were well correlated with the results in human colon. The absorption from the bioadhesive microsphere (MS) developed by Meiji Seika group was determined in this system. Polycarbophil (PCP) that is used for adhesive coating exhibited absorption enhancement. MS coated with decanoyl carnitine(absorption enhancer)and PCP showed more 10 times absorbability than control, showing the promise of adhesive MS.Cationic polyamino acids showed the possibility to be used as adhesive coating material with absorption enhancement. Absorbability of Polypeptides and Prodrug in Peyer's Patch. Concanavalin (Con A) , a rectin, that is expected to target to Peyer's patch (PP) was conjugated with BSA in the ratio 1/1 (maleimide method) . This conjugate showed higher permeability in PP than BSA itself. This showed the possibility to use rectin protein conjugate as a prodrug for absorption enhancement. Polylacetic acid Polyglycolic acid copolymer MS was prepared as DDS for PP.The absorption of BSA,HRP and SOD from the MS was examined, but the determination of transported amounts of these compounds in this system remained as future problem. Development of Membrane Adhesive Micorosphere (MC) and MS targeted to PP.The adhesive MC was not prepared because of surface activity of the enhancers encapsulated in MC.since MS can be substituted, the adhesive MS preparation was examined. PVP as base was found unsuitable, because the prepared MS shapes were not uniform. Gelatine MS coated with PCP exhibited enough adhesiveness with good release.
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