UPENDRA MARATHI,マラティ,ウペンドラ,SUSANN CHILDRESS,チャイルドレス,スーザン,SHAUN GAMMILL,ガミル,シャウン,ROBERT W STROZIER,ストロージャー,ロバート ダブリュ.,マラティ,ウペンドラ,チャイルドレス,スーザン,ガミル,シャウン,ストロージャー,ロバート ダブリュ.
申请号:
JP2017114115
公开号:
JP2017222650A
申请日:
2017.06.09
申请国别(地区):
JP
年份:
2017
代理人:
摘要:
PROBLEM TO BE SOLVED: To provide a composition for delivering a bioactive agent to the gastrointestinal (GI), eyes, urinary tract, or reproductive tract, the bioactive agent having problems of (a) being injurious to the upper GI tract (esophagus, stomach, and duodenum), (b) being acid labile, (c) being impermeable/insoluble compounds in GI fluids, (d) being susceptible to first pass metabolism, and (e) causing stomach irritation, upset, or dyspepsia.SOLUTION: According to the present invention, there is provided a pharmaceutical composition comprising a bioactive agent, such as a weak acid non-steroidal anti-inflammatory drug (NSAID); and a carrier comprising a pH dependent release agent, such as at least 5% by weight of a biocompatible free fatty acid having at least 8 carbon atoms, less than 10% by weight phospholipid, etc. Here, the carrier can controllably release the bioactive agent in a pH sensitive manner. Preferably, the composition further comprises a water immiscible neutral lipid. According to the present invention, there is provided a composition for targeted release of a bioactive agent to the small intestine.SELECTED DRAWING: Figure 12【課題】(a)上部GI管(食道、胃、及び十二指腸)に対して傷害性であり、(b)酸に不安定であり、(c)GI液中で不透過性/不溶性であり、(d)初回通過代謝の影響を受け易く、(e)胃の刺激作用、不調、又は消化不良をもたらす等の問題点を有する生物活性剤を、胃腸(GI)、眼、尿路、又は生殖管へと送達する組成物の提供。【解決手段】弱酸の非ステロイド性抗炎症薬(NSAID)剤等の生物活性剤と、少なくとも8個の炭素原子を有する生体適合性遊離脂肪酸を、少なくとも5重量%、リン脂質を10重量%未満等のpH依存性放出剤を含む担体と、を含む医薬組成物であって、担体が、生物活性剤をpH感受性の様式で制御可能に放出することが可能な組成物。さらに水不混和性の中性脂質を含むことが好ましい。小腸への生物活性剤の標的放出のための、組成物。【選択図】図12