Ammoury N, Fessi H, Devissaguet J P, Dubrasquet M, Benita S
Laboratoire de Pharmacie Galénique et Biopharmacie, URA CNRS 1218, Centre d'Etudes Pharmaceutiques, Chatenay-Malabry, France.
Pharm Res. 1991 Jan;8(1):101-5. doi: 10.1023/a:1015846810474.
The jejunal absorption of indomethacin nanocapsules was studied using an in vivo infusion technique. Jejunal absorption of indomethacin from the nanocapsules was slightly delayed as compared to a commercial indomethacin solution. The plasma and jejunal mucosa indomethacin concentrations were similar in both cases. However, the nanocapsules protected the rat jejunum from the ulcerating effect of indomethacin, probably by avoiding direct contact of the free drug with the surface of the mucosa. The pharmacokinetic profile of indomethacin nanocapsule formulations was compared to a solution of free drug following oral administration of 5 mg/kg in rats; no difference in the mean concentration-time profiles of the drug was observed. Blood levels of thromboxane showed a sustained biological activity, over a period of 24 hr, of indomethacin-loaded nanocapsules, relative to the drug in solution, following oral administration.
采用体内输注技术研究了吲哚美辛纳米胶囊的空肠吸收情况。与市售吲哚美辛溶液相比，纳米胶囊中吲哚美辛的空肠吸收略有延迟。两种情况下血浆和空肠黏膜中吲哚美辛的浓度相似。然而，纳米胶囊可能通过避免游离药物与黏膜表面直接接触，保护大鼠空肠免受吲哚美辛的溃疡作用。在大鼠口服5mg/kg后，将吲哚美辛纳米胶囊制剂的药代动力学特征与游离药物溶液进行了比较；未观察到药物平均浓度-时间曲线的差异。口服给药后，相对于溶液中的药物，载有吲哚美辛的纳米胶囊在24小时内血栓素的血药水平显示出持续的生物活性。
