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Physicochemical Characterization and an Injection Formulation Study of Water Insoluble $ZCVI_4$-2, a Novel NO-Donor Anticancer Compound
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  • Physicochemical Characterization and an Injection Formulation Study of Water Insoluble $ZCVI_4$-2, a Novel NO-Donor Anticancer Compound
  • Physicochemical Characterization and an Injection Formulation Study of Water Insoluble $ZCVI_4$-2, a Novel NO-Donor Anticancer Compound
저자명
Gao. Yuan,Li. Li,Zhang. Jianjun,Su. Feng,Gong. Zhenhua,Lai. Yisheng,Zhang. Yihua
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2012년|35권 7호|pp.1177-1186 (10 pages)
발행정보
대한약학회
파일정보
정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

$ZCVI_4$-2 was a novel nitric oxide-releasing glycosyl derivative of oleanolic acid that displayed strong cytotoxicity selectively against human hepatocellular carcinoma in vitro and in vivo. In this study, $ZCVI_4$-2 was characterized by FT-IR spectroscopy, differential scanning calorimetry, powder X-ray diffractometry, Raman spectroscopy, hygroscopicity and stability. A high performance liquid chromatography method was also established for the quantitative determination of solubility and additional stability profile of $ZCVI_4$-2. $ZCVI_4$-2 was found to be an amorphous and stable solid with low solubility of less than 10 ${mu}g/mL$. Based on the solubilization tests that included methods of cosolvency and micellization, the solution mixture of 5% Solutol HS-15, 5% 1, 2-propylene glycol and 5% anhydrous ethanol was determined to be the system for the preparation of the $ZCVI_4$-2 early injection solution. The effect of pH, temperature, light and injectable isotonic glucose or NaCl solution on $ZCVI_4$-2 injection was also investigated. Good stability was observed at all testing conditions. Under the conditions studied, the NO-releasing rate and amount of $ZCVI_4$-2 from the early injection solution in rat plasma demonstrated a promising therapeutic efficacy while maintaining a good safety profile.