Detail of "816-94-4"

Reference

Transmucosal passage of liposomally-entrapped drugs in rat small intestine

Transmucosal passage of liposomally-entrapped drugs in rat small intestine. Kimura, Toshikiro; Higaki, Kazutaka; Sezaki, Hitoshi (Fac. Pharm. Sci., Okayama Univ., Okayama 700, Japan). Pharm. Res., (5), 221-4 (English) 1984. CODEN: PHREEB. DOCUMENT TYPE: Journal CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1 Intestinal absorption of liposomally-entrapped drugs was investigated for egg yolk phosphatidylcholine-cholesterol [57-88-5] (2:1 by molar ratio) liposomes (EggPC liposome) and L-distearoylphosphatidylcholine [816-94-4]-cholesterol (2:1) liposomes (DSPC liposome). The release of carboxyfluorescein, an aq. phase marker, induced by the presence of everted rat intestine was 40% and 6% in 1 h from DSPC liposomes and EggPC liposomes, resp., and it is suggested that EggPC liposomes are more stable in the intestinal lumen. The transport of a liposomally-entrapped drug was examd. with fluorescein isothiocyanate-conjugated dextran (FITC-D) as a model drug that has a small mucosal-to-serosal clearance because of its high av. mol. wt. (64200). The clearance of FITC-D entrapped in DSPC liposomes was largely reduced and could be accounted for by the clearance of the extraliposomal FITC-D concn. in the prepn. On the other hand, the calcd. clearance of EggPC liposome-assocd. FITC-D was similar to or even higher than that of free FITC-D. The serosal appearance of the EggPC liposome-assocd. drug was inhibited by colchicine, cytochalasin B, and iodoacetate, suggesting that the liposome was incorporated into the epithelial cells by endocytosis. However, the observation that a lipid phase marker, 14C-dipalmitoylphosphatidylcholine, failed to be transported into the serosal fluid indicates the absence of the penetration by an intact liposomal form.

Liposomes containing FK 565

Liposomes containing FK 565. (Fujisawa Pharmaceutical Co., Ltd., Japan). Jpn. Kokai Tokkyo Koho JP 59076021 A2 28 Apr 1984 Showa, 4 pp. (Japanese). (Japan). CODEN: JKXXAF. CLASS: IC: A61K037-02. ICA: A61K009-10; C07C103-52. APPLICATION: JP 82-186642 22 Oct 1982. DOCUMENT TYPE: Patent CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 1 Liposomes contg. the oligopeptide FK 565 [79335-75-4] which have greater antitumor activities than FK 565 alone are prepd. Thus, L-a-distearoylphosphatidylcholine [816-94-4] was dissolved in CHCl3 in a flask and the solvent was removed under reduced pressure to form a thin film on the inner wall of the flask. Then, a phosphate buffer (pH 7.4) contg. FK 565 (4.3 mg/mL) was added and stirred until all of the thin film was used for the encapsulation of FK 565. The liq. was centrifuged at 100,000 ′ g for 15 min, and the residue isolated and washed with a saline-phosphate buffer to obtain the FK-565 encapsulated with liposomes. The liposomes administered s.c. at 100 mg/kg to mice bearing P815 tumor decreased the size of the tumor by 50% in 10 days, whereas FK 505 alone decreased only 15%.