College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 426-791, South Korea.
J Microencapsul. 2012;29(4):323-30. doi: 10.3109/02652048.2011.651497. Epub 2012 Jan 10.
To develop a novel flurbiprofen-loaded solid self-microemulsifying drug delivery system (solid SMEDDS) with improved oral bioavailability using gelatin as a solid carrier, the solid SMEDDS formulation was prepared by spray-drying the solutions containing liquid SMEDDS and gelatin. The liquid SMEDDS, composed of Labrafil M 1944 CS/Labrasol/Transcutol HP (12.5/80/7.5%) with 2% w/v flurbiprofen, gave a z-average diameter of about 100 nm. The flurbiprofen-loaded solid SMEDDS formulation gave a larger emulsion droplet size compared to liquid SMEDDS. Unlike conventional solid SMEDDS, it produced a kind of microcapsule in which liquid SMEDDS was not absorbed onto the surfaces of carrier but formed together with carrier in it. However, the drug was in an amorphous state in it like conventional solid SMEDDS. It greatly improved the oral bioavailability of flurbiprofen in rats. Thus, gelatin could be used as a carrier in the development of solid SMEDDS with improved oral bioavailability of poorly water-soluble drug.
为了开发一种新型的负载氟比洛芬的固体自微乳药物传递系统（固体自微乳），以提高口服生物利用度，采用明胶作为固体载体，通过喷雾干燥含有液体自微乳和明胶的溶液来制备固体自微乳制剂。液体自微乳由 Labrafil M 1944 CS/Labrasol/Transcutol HP（12.5/80/7.5%）和 2% w/v 的氟比洛芬组成，粒径约为 100nm。与液体自微乳相比，负载氟比洛芬的固体自微乳制剂的乳滴粒径更大。与传统的固体自微乳不同，它产生了一种微胶囊，其中液体自微乳没有被吸收到载体的表面上，而是与载体一起形成。然而，药物在其中呈无定形状态，与传统的固体自微乳一样。它大大提高了氟比洛芬在大鼠体内的口服生物利用度。因此，明胶可用作固体自微乳的载体，以提高难溶性药物的口服生物利用度。
