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首页> 美国卫生研究院文献>AAPS PharmSciTech >Increased In Situ Intestinal Absorption of Phytoestrogenic Diarylheptanoids from Curcuma comosa in Nanoemulsions
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Increased In Situ Intestinal Absorption of Phytoestrogenic Diarylheptanoids from Curcuma comosa in Nanoemulsions

机译：纳米乳液中姜黄中植物雌激素二芳基庚烷类化合物的原位肠道吸收增加

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Curcuma comosa has long been used as a gynecological medicine. Several diarylheptanoids have been purified from this plant, and their pharmacological effects were proven. However, there is no information about the absorption of C. comosa components to support the formulation usage. In the present study, C. comosa hexane extract and the mixture of its two major compounds, (4E,6E)-1,7-diphenylhepta-4,6-dien-3-ol (DA1) and (6E)-1,7-diphenylhept-6-en-3-ol (DA2), were formulated into nanoemulsions. The physical properties of the nanoemulsions and the in situ intestinal absorptions of DA1 and DA2 were evaluated. The results demonstrated the mean particle sizes at 0.207 ± 0.001 and 0.408 ± 0.014 μm, and the zeta potential at −14.57 ± 0.85 and −10.47 ± 0.32 mV for C. comosa nanoemulsion (C.c-Nano) and mixture of diarlylheptanoid nanoemulsions (DA-Nano), respectively. The entrapments of DA1 and DA2 were 76.61% and 75.41%, and 71.91% and 71.63% for C.c-Nano and DA-Nano, respectively. The drug loading ratios of DA1 and DA2 were 351.47 and 614.53 μg/mg, and 59.48 and 126.72 μg/mg for C.c-Nano and DA-Nano. The intestinal absorption rates of DA1 and DA2 were 0.329 ± 0.015 and 0.519 ± 0.026 μg/min/cm2 in C.c-Nano, and 0.380 ± 0.006 and 0.428 ± 0.036 μg/min/cm2 in DA-Nano, which were five to ten times faster than those in oil. In conclusion, the formulation in nanoemulsion forms obviously increased the intestinal absorption rate of diarylheptanoids.
机译：姜黄长期以来一直被用作妇科药物。已经从该植物中纯化了几种二芳基庚烷，并证明了它们的药理作用。但是，没有有关吸收角果衣原体成分以支持制剂使用的信息。在本研究中，毛角梭菌己烷提取物及其两种主要化合物（4E，6E）-1,7-二苯庚基-4,6-dien-3-ol（DA1）和（6E）-1的混合物将7-二苯基庚-6-烯-3-醇（DA2）配制成纳米乳剂。评价了纳米乳液的物理性质以及DA1和DA2的原位肠道吸收。结果表明，C。comosa纳米乳液（Cc-Nano）和双芳基庚类纳米乳剂（DA-纳米）。 C.c-Nano和DA-Nano的DA1和DA2的包封率分别为76.61％和75.41％，以及71.91％和71.63％。 DA1和DA2的载药率为351.47和614.53μg/ mg，C.c-Nano和DA-Nano的载药率为59.48和126.72μg/ mg。在Cc-Nano中，DA1和DA2的肠道吸收率为0.329 0.3±0.015和0.519±0.026μg/ min / cm 2 ，分别为0.380±0.006和0.428±0.036μg/ min / cm DA-Nano中的2 ，比石油中的速度快五到十倍。总之，纳米乳液形式的制剂明显增加了二芳基庚烷的肠吸收率。

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