• Journal of Pharmaceutical Investigation
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• 제30권4호
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• pp.235-239
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• 2000

Ipriflavone (3-phenyl-7-isopropoxy-4H-1-benzopyran-4-one, IP) is a well-known antiosteoporotic drug with poor bioavailability. In the previous study, we reported that the IP formulation prepared by spray-drying method with polyvinylpyrrolidone (PVP) (SIP) was very effective in improving the bioavailability of IP. In this study, we examined the effects of molecular weight and mixture ratios of PVP to IP on the systemic absorption of IP following oral administration of SIP at a dose of 50 mg/kg to rats. In the effect of molecular weight, the Cmax of spray-dried IP with PVP K30 (SIP-K30) was significantly higher than those of spray-dried IP with PVP 360 (SIP-360), spray-dried IP with PVP K90 (SIP-K90), and spray-dried IP with PVP K17 (SIP-K17) (p<0.05). The AUC of SIP-K30 was about 2, 3, and 5.5 times higher than those of SIP-360, SIP-K90, and SIP-K17, respectively. The AUC value of SIP-K30 was significantly greater than those of SIP-K17 and SIP-K90 (p<0.05) except for SIP-360. In the ratio of PVP K30 to drug, the $C_{max}$ and the AUC value of 3 : 7 IP-PVP solid dispersion were similar to those of 5 : 5 IP-PVP and significantly higher than those of the other solid dispersions (p<0.05). It was concluded that the spray-dried IP with PVP K30 at the ratio of 3:7 (w/w) was the best formulation for improving the bioavailability of IP.

• 대한화장품학회지
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• 제32권4호
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• pp.227-231
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• 2006

주름생성의 주요 원인은 자외선, 공기 오염, 담배 연기, 스트레스 등을 들 수 있다. 특히, 자외선은 피부에 다양한 형태로 영향을 주어 깊은 주름, 잔주름, 피부거침, 피부건조와 같은 현상을 발생시켜 피부노화를 유발시킨다. 이러한 주름 생성 해결 및 피부 노화 문제의 해결은 화장품에서 가장 활발하게 연구되는 분야 중 하나이다. 최근에 열대 식물인 노니로부터 추출한 유효성분이 주름 개선에서 가장 중요한 콜라겐 생합성을 촉진하는 효과를 확인하였으며, 특히 노니 추출물로부터 분리한 스코폴레틴(scopoletin)이 이러한 효과를 주는 활성 성분임을 확인하였다. 스코폴레틴은 인체 섬유아 세포를 이용한 콜라겐 합성 촉진 효과 시험에서 농도 의존적으로 콜라겐 합성을 촉진하는 활성을 보였다($0.2{\mu}g/mL-89.5%$ 콜라겐 생합성 촉진. 또한, 주름 개선 효과를 확인하기 위해 3% (v/v) 노니 추출물을 함유한 크림을 이용하여 12주 동안 임상연구를 수행하여, 안면의 주름 감소 정도를 측정하였으며 이 제품이 주름을 감소시켜주는 뛰어난 효과가 있다는 것을 확인하였다. 이러한 결과들은 노니 추출물이 주름 개선효과가 매우 높으며, 노화 방지 원료로서 이용 가능성이 매우 높다는 것을 보여주는 것이라 할 수 있다.

• The Korean Journal of Physiology and Pharmacology
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• 제1권6호
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• pp.759-767
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• 1997

In the present study, we characterized the non-vascular smooth muscle relaxant effects of a novel benzoyran derivative ,SKP-450 (2-[2'(1',3'-dioxolone)-2-methyl-4- (2'-oxo-1'-pyrrolidinyl) -6-nitro-2H-1- benzopyran) and its metabolite, SKP-310, in comparison with levcromakalim (LCRK). In the rat stomach fundus, the spontaneous motility stimulated by $10^{-6.5}\;M$ bethanechol was completely eliminated not only by $10^{-7}\;M$ SKP-450 but also by $10^{-6}\;M$ LCRK, which were blocked by $10^{-6}\;M$ glibenclamide. The inhibitory effect of SKP-450 $pD_2,\;3.94{\pm}0.66)$ was much less than LCRK $(pD2,\;5.73{\pm}0.38,\;p<0.05)$. In the bethanechol $(10{-6.5 }\;M)-stimulated$ urinary bladder, the tonus was decreased in association with elimination of spontaneous motility by $10^{-7}\;M$ M SKP-450 and $10^{-6}\;M\;LCRK\;(pD2,\;6.77{\pm}0.06)\;(P<0.05)$, which were inhibitable by $10^{-6}\;M$ glibenclamide. The inhibitory effect of SKP-450 $(pD2,\;7.66{\pm}0.05)$ was significantly more potent than that of LCRK $(pD2,\;6.77{\pm}0.06,\;p<0.05)$. In the rat uterus stimulated by $PGF_{2\alpha}\;(10^{-7}\;M)$, both increased tonus and spontaneous motility were eliminated by $10^{-6}\;M$ LCRK with slight depression of the tonus, but not by SKP-450 $(10^{-5}\;M)$. The stimulated trachea of guinea-pig by $10^{-6.5}\;M$ bethanechol was moderately suppressed by SKP-450 $(10^{-6}{sim}10^{-5}\;M)$ but little by SKP-310. In association with the relaxant effects, SKP-450 $(10^{-6}\;M)$ and LCRK $(10^{-5}\;M)$ caused a significant stimulation of the $^{86}Rb$ efflux from rat urinary bladder and stomach fundus, which were antagonized by $10^{-5}\;M$ glibenclamide, whereas the $K^+$ channel openers could not exert a stimulation of the $^{86}Rb$ efflux from rat uterus. In conclusion, it is suggested that SKP-450 exerts potent relaxant effects on the urinary bladder detrusor muscle and duodenum, whereas it shows much less effect on stomach fundus and uterus as contrasted to LCRK.