To provide an external preparation or injectable preparation that exerts the effect of enabling transdermal or transmucosal in vivo absorption of fat-soluble drugs and water-soluble drugs not having been satisfactorily attained hitherto and that contains a highly absorbable fat-soluble/water-soluble drug, the injectable preparation especially aiming at sustained-release and target effects.
In particular, drug-containing nanoparticles (secondary nanoparticles) are provided by causing primary nanoparticles containing a fat-soluble drug or fat-solubilized water-soluble drug to act with a bivalent or trivalent metal salt. Further, drug-containing nanoparticles (tertiary nanoparticles) are provided by first causing primary nanoparticles containing a fat-soluble drug or fat-solubilized water-soluble drug to act with a bivalent or trivalent metal salt to thereby obtain secondary nanoparticles and thereafter causing a monovalent to trivalent basic salt to act on the secondary nanoparticles. Still further, there are provided a process for producing these nanoparticles, and a transdermal or transmucosal external preparation or injectable preparation in which these nanoparticles are contained.
提供一种外用制剂或注射制剂,该制剂能够发挥迄今为止尚未令人满意地实现的脂溶性药物和
水溶性药物透皮或透粘膜体内吸收的效果,并且含有高吸收性脂溶性/
水溶性药物,该注射制剂尤其以持续释放和靶向效应为目标。
特别是,通过使含有脂溶性药物或脂溶性
水溶性药物的初级纳米颗粒与二价或三价
金属盐作用,提供了含药纳米颗粒(次级纳米颗粒)。更进一步,通过首先使含有脂溶性药物或脂溶性
水溶性药物的一级纳米粒子与二价或三价
金属盐作用,从而获得二级纳米粒子,然后使一价至三价碱性盐作用于二级纳米粒子,从而提供含药物的纳米粒子(三级纳米粒子)。此外,还提供了生产这些纳米颗粒的工艺,以及包含这些纳米颗粒的透皮或透粘膜外用制剂或注射制剂。