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한규원(Kyu Won Han),정낙신(Lak Shin Jeong),김길수(Kil Soo Kim) 한국약제학회 2000 Journal of Pharmaceutical Investigation Vol.30 No.2
In order to assay the efficacy of newly synthesized antiviral compounds, pyrimidine analogs, pharmacokinetics of those were established as compared with already marketed zidovudine. Zidovudine (15, 20, 25 and 35 ㎎/㎏), LJ142 (18.52 ㎎/㎏) and LJ143 (15, 18.52 and 30 ㎎/㎏) were administered orally and intravenously in rats, blood samples were collected post-injection(i.e., for 360 min) at appropriate time intervals. Those were analyzed by HPLC with UV detection at 265 nm. Pharmacokinetic parameters (C_(max), T_(1/2), MRT, AUC, AUMC, Vd_(ss) Cl_t) were calculated. AUCs of zidovudine and LJ143 following I.V. dosing of 15∼25 ㎎/㎏ and 15∼18.18 ㎎/㎏ were dose-independent. However, AUCs of zidovudine and LJ143 following I.V. dosing of 25∼35 ㎎/㎏ and 18.18∼30 ㎎/㎏ were dose-dependent. The relative bioavailability of zidovudine, LJ142 and LJ143 following oral administration were 61.94, 46.44 and 78.24%, respectively.
Sestamibi 의 신규합성과 제제화에 따른 안정성 비교
손미원(Mi Won Son),임중인(Joong In Lim),장영수(Young Soo Chang),정미영(Mi Young Jung),정낙신(Lak Shin Jeong),김순회(Soon Hoe Kim),김원배(Won Bae Kim),정재민(Jae Min Jeong) 대한핵의학회 2001 핵의학 분자영상 Vol.35 No.5
N/A Purpose: Ascorbic acid is known to act as an antioxidant. Therefore, it can be used in increasing the efficiency of radiochemical labeling of Technetium-99m setamibi by inhibition of oxidation of Sn2+ at low concentration. We intended to estimate the efficiency of radiochemical labeling and the stability of the newly formed formulation when ascorbic acid was added to a commercial kit. Materials and Methods: Synthesis of sestamibi was performed according to Dong-A`s patent procedure (No.10-2001-0012877). First, we undertook a study to evaluate the efficiency of radiochemical labeling of sestamibi containing ascorbic acid. The stability of the vials was assessed using either 7.5 ㎍ or 75 ㎍ of ascorbic acid, added to commercial vials under the accelerated condition(Temp: 40℃, +2℃, Relative humidity: 75±5%). Results: Sestamibi was synthesized in overall 35-40% yield over 5 steps from a commercially available methallyl chloride as a starting material. When ascorbic acid was added, the efficiency of radiochemical labeling was maintained compared to the vial with no ascorbic acid. The accelerated test showed that the addition of ascorbic acid inhibited the oxidation of Sn2+ ion by antioxidation mechanism. Also, the efficiency of radiochemical labeling of this vial after 9 months was nearly the same as the starting point. Therefore, the storage period of the kit is likely to be extended. Taken together, it suggests that the addition of ascorbic acid as a stabilizer is desirable. Conclusion: To increase the stability of a sestamibi cold kit, it is desirable to add ascorbic acid as a stabilizer to the commercial fomulation. (Korean J Nucl Med 2001:35:334-341)
한규원,정낙신,김길수 梨花女子大學校 藥學硏究所 2000 藥學硏究論文集 Vol.- No.9
In order to assay the efficacy of newly synthesized antiviral compounds, pyrimidine analogs, pharmacokinetics of those were established as compared with already marketed zidovudine. Zidovudine (15, 20, 25 and 35 ㎎/㎏), LJ142 (18.52 ㎎/㎏) and LJ143 (15, 18.52 and 30 ㎎/㎏) were administered orally and intravenously in rats, blood samples were collected post-injection(i.e., for 360 min) at appropriate time intervals. Those were analyzed by HPLC with UV detection at 265 ㎚. Pharmacokinetic parameters (C_max, T_(1/2) MRT, AUC, AUMC, Vd_ss, Cl_t) were calculated. AUCs of zidovudine and LJ143 following I.V. dosing of 15∼25 ㎎/㎏ and 15∼18.18 ㎎/㎏ were dose-independent, However, AUCs of zidovudine and LJ143 following I.V. dosing of 25∼35 ㎎/㎏ and 18.18∼30 ㎎/㎏ were dose-dependent. The relative bioavailability of zidovudine, LJ142 and LJ143 following oral administration were 61.94, 46.44 and 78.24%, respectively.