• 제목/요약/키워드: Bioanalysis

검색결과 227건 처리시간 0.038초

Identification of Metabolites of Phytosterols in Rat Feces Using GC/MS

  • Song, Yun-Seon;Jin, Chang-bae;Park, Eun-Hee
    • Archives of Pharmacal Research
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    • 제23권6호
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    • pp.599-604
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    • 2000

  • $\beta$-Sitosterol, campesterol and stigmasterol have been known to the phytosterols the most frequently found in plants. Metabolism of phytosterols was investigated using rat feces and liver microsomes. Feces were collected after phytosterols (a well characterized mixture of $\beta$-sitosterol 40%, campesterol 30% and dihydrobrasicasterol) were administered orally (0.5 ${g/kg$) to rats. Metabolites of phytosterols were identified using GC/MS. Three peaks were eluted at 12.47, 12.65, 12.87 min and had characteristic molecular ions m/z 428, 430, 432, respectively. Three fecal metabolites were identified as androstadienedione, androstenedione, and androstanedione. No metabolites could be detected in the rat liver microsomal reaction mixture. The results suggest that the metabolites of phytosterols in rat feces are formed by oxidation at 3- position, saturation at 5- and 6- position, and 17- side chain cleavage in the rat large intestine.

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Metabolism of Rutaecarpine by Rat Liver Microsomes

  • Lee, Sang-Kyu;Lee, Jae-Ick;Jahng, Young-Dong;Chang, Hyeun-Wook;Lee, Eung-Seok;Kim, Dong-Hyun;Jeong, Tae-Cheon
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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    • pp.127.2-128
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    • 2003

  • Rutaecarpine is an alkaloid originally isolated from the unripe fruit of Evodia rutaecarpa. In addition to its traditional use in treatment of gastrointestinal disorders, rutaecarpine has recently been characterized to have anti-inflammatory activity through cyclooxygenase-2 inhibition. More recently, to develop rutaecarpine as an anti-inflammatory agent, total synthesis of rutaecarpine has successfully been established in our group. (omitted)

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GLP Bioanalysis from the US FDA Perspective

  • Wilkinson, Tames M.
    • 한국독성학회:학술대회논문집
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    • 한국독성학회 2006년도 추계학술대회
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    • pp.75-79
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    • 2006

  • The United States Food and Drug Administration is responsible for ensuring US residents receive safe and effective medicines. Since blood levels of drugs are correlated with pharmacological effect, FDA closely regulates how those blood levels are measured. The FDA has established requirements for bioanalytical analyses such as minimum method validation, SOP, and reporting criteria. The FDA also has standards for computer validation which must be followed to ensure the data are reliable. Data presented to the Agency are scrutinized to ensure they are accurate and a true reflection of the raw data generated in a study. To verify the quality of data, FDA has developed an inspection program. The specific requirements of the FDA related to bioanalysis will be discussed.

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Pharmacokinetics of Propentofylline and the Quantitation of Its Metaolite Hydroxypropentofylline in Human Volunteers

  • Kwon, Oh-Seung;Chung, Youn-Bok;Kim, Min-Hee;Hahn, Hoh-Gyu;Rhee, Hee-Kyung;Ryu, Jae-Chun
    • Archives of Pharmacal Research
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    • 제21권6호
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    • pp.698-702
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    • 1998

  • Propentofylline (PPF, 3-methyl-1-(5-oxohexyl)-7-propylxanthine) has been reported to be effective for the treatment of both vascular dementia and dementia of the Alzheimer type. The pharmacological effects of PPF may be exerted via the stimulation of nerve growth factor, increased cerebral blood flow, and inhibition of adenosine uptake. The objectives of this experiment are to determine the kinetic behavior of PPF, to identify, and to quantify its metabolite in human. Blood samples were obtained from human volunteers following oral administration of 200mg of PPF tablets. For the identification and quantification of the metabolite, 3-methyl-1-(5-hydroxyhexyl)-7-propylxanthine (PPFOH), PPFOH was synthesized and identified by gas chromatography/mass spectroscopy (GC/MS) and $^1H$-nuclear magnetic resonance spectroscopy. The molecular weight of synthesized metabolite is 308 dalton. The PPF and PPFOH in plasma were extracted with diethyl ether and identified by electron impact GC/MS. The plasma concentrations of PPF and PPFOH were determined by gas chromatography/nitrogen phosphorus detector in plasma and their pharmacokinetic parameters were determined. The mean half-life of PPF was 0.74 hr. The areas under the curve (AUCs) of PPF and PPFOH were 508 and 460ng.hr/ml, respectively. $C_{max}$ of PPF was about 828.4ng/ml and the peak concentration was achieved at about 2.2 hr ($T_{max}$). These results indicate that PPF is rapidly disappeared from blood due to extensive metabolism into PPFOH.

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