In vivo effects of highly purified docosahexaenoic acid on rectal insulin absorption.
In vivo effects of highly purified docosahexaenoic acid on rectal insulin absorption.
复制标题
高纯度二十二碳六烯酸对直肠胰岛素吸收的体内影响。
DOI：
10.1016/s0378-5173(99)00471-8
复制
发表时间：
2000
影响因子：
5.8
通讯作者：
T. Nagai
中科院分区：
文献类型：
--
作者：
Y. Onuki;M. Morishita;K. Takayama;S. Tokiwa;Y. Chiba;K. Isowa;T. Nagai
本研究的目的是评价油酸、二十碳五烯酸(EPA)和二十二碳六烯酸(DHA)等多不饱和脂肪酸作为胰岛素直肠给药促进剂的有效性和毒性。在单次给药研究中，直肠胰岛素吸收显著增强，并以与胰岛素剂量相关的方式加入各种脂肪酸的乳剂诱导了显著的低血糖。含2%油酸、环氧乙烷和二羟甲基丙酸的乳剂药理利用度分别为≈7.7%、11.0%和25.4%。当乳剂中DHA含量为1%时，促进胰岛素吸收的效果并不随乳剂中DHA含量的增加而增加。此外，通过在乳剂中加入Pluronic F127(PF 127)，血清葡萄糖-时间曲线的平均Tmax可以延长到不含PF 127的乳剂的两倍。在一项多次给药研究中，含有DHA的乳剂在第一天和第十天的平均AUC葡萄糖价值几乎相同。从粘膜表面的形态观察，添加DHA的乳剂未引起或仅有轻微的粘膜损伤。结果表明，DHA具有较强的促进胰岛素通透性作用，毒性较小。因此，DHA是一种很有吸引力的肠道胰岛素吸收促进剂。
The purpose of this study was to evaluate the effectiveness and the toxicity of polyunsaturated fatty acid, such as oleic acid, eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA), as a potential absorption enhancer for rectal delivery of insulin, using a water-in-oil-in-water (W/O/W) multiple emulsion. In a single administration study, rectal insulin absorption was enhanced markedly, and marked hypoglycemia was induced by the emulsion incorporating various fatty acids in an insulin dose-related fashion. The pharmacological availability of the emulsion incorporating 2% oleic acid, EPA and DHA was ≈7.7, 11.0 and 25.4%, respectively. The insulin absorption enhancement effect was not increased in proportion to the amount of DHA in the emulsion at >1%. In addition, by incorporating Pluronic F 127 (PF 127) into the emulsion, the mean Tmaxvalue of the serum glucose–time curve could be extended to twice that of the emulsion without PF 127. In a multiple administration study, the mean AUCglucosevalues of the emulsion incorporating DHA showed almost the same value on the first and the tenth day. From the morphological appearance of the mucosal surface, the emulsion incorporating DHA induced no or little mucosal damage. Our findings demonstrated that DHA has a strong insulin permeability enhancement effect and little toxicity. Thus, DHA is an attractive candidate as an absorption enhancer for intestinal delivery of insulin.
DOI：
10.1152/ajpgi.1994.267.6.g1067
发表时间：
1994-12-01
影响因子：
4.5
作者：
ISHIKAWA, S;CEPINSKAS, G;KVIETYS, PR
通讯作者：
KVIETYS, PR
DOI：
10.1152/ajpgi.1993.264.3.g576
发表时间：
1993-03
期刊：
The American journal of physiology
影响因子：
--
作者：
O. R. Velásquez;K. Henninger;M. Fowler;P. Tso;K. Crissinger
通讯作者：
O. R. Velásquez;K. Henninger;M. Fowler;P. Tso;K. Crissinger
结肠上皮细胞粘膜表面胰岛素受体的鉴定。
DOI：
--
发表时间：
1985
期刊：
The Journal of biological chemistry
影响因子：
--
作者：
Pillion,DJ;Ganapathy,V;Leibach,FH
通讯作者：
Leibach,FH