Journal of Chinese Pharmaceutical Sciences

Studies on Adriamycin Magnetic Gelatin Microspheres

Chuan-Bin Wu, Shu-Li We, Wei Lu, Su-Mei He, Wen-Wei Gao, Tian-Li Wang, Xuan Li, Jing-Xia Xie

1995, 4(1): 1-7.

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The preparation and properties of adriamycin magnetic gelatin microspheres (Adr-MG-ms) were reported. The synthesis of magnetic iron oxide ultrafine particle and embolization effects of magnetic gelatin microspheres (MG-ms) in dog were studied. Adr-MG-ms consist of 2% (w/w) of adriamycin (Adr) as the core, and 68% of gelatin and 30% of magnetite as the shell with a mean particle size of 22 μm. In vitro experiment, the release rate of drug demonstrated that the microspheres have sustained-release properties. The average diameter of magnetic iron oxide was approximately l0 nm. Transcatheter embolization with MG-ms and ^99mTc-labelled MG-ms was performed under external magenet control in dog liver, respectively. Gamma photography and angiogram revealed that MG-ms level was almost equal both in left and right hepatic arteries without magnet, while with magnet (1200 Gs), MG-ms level in left hepatic artery (target site) was about 2.25 fold higher than in right hepatic artery, and few MG-ms in thyroid gland, brain and heart was observed. Results showed that the MG-ms is a promising embolic agent for treatment of hepatic cancer under external magnet control.

Pharmacokinetics and Relative Bioavailability ofsustained-release Tablets of Diclofenac Sodiumin Male Volunteers

Ai-Min Ji, Heng-Qin Zou, Zhong-Yi Zhang, Ou Che

1995, 4(1): 8-11.

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The pharmacokinetics of a sustained- release formulation and an enteric-coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open, randomized crossover study. Drug level in serum was assayed by HPLC method. The changes in serum concentration were conformed to a l-compartment open model. The t1/2 (Ke) averaged 2.15±0.17 and 11.60±l.95 h, and the areas under the drug concentration curves were 5.87±0.67 and 5.55±0.57 μg·h/ml for enteric-coated and sustained-release tablet of diclofenac sodium, respectively. The mean relative bioavailability of sustained-release tablet was 0.95 to that of enteric-coated tablet.

Effects of 2-[p-(Dimethylamino)Styrl] PyridineMethiodide on Slow Response Action Potentialand Slow lnward Current of Guinea Pig Papillary Muscles

Xin-Min Mao, Di-Min Li, Cheng-Ming Zhou, Xiao-Wen Wang, Ke-Jing Zhang

1995, 4(1): 12-16.

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The effects of 2-[p-(Dimethylamino)styryl] pyridine methiodide (DSPM) on slow response action potential (SRAP) and slow inward current (Isi) of guinea pig papillary muscles were studied by intracellular microelectrodes and voltage clamp techniques. The APA and Vmax of SRAP induced by high K⁺ were decreased after 50 min of perfusion with DSPM solution. Isi was suppressed from a peak value of 8.8±1.6 μA to 5.7±1.8 μA, The results indicated that DSPM has a selective blocking effect on calcium channel.

Effects of Diazepam on Rat Cholinesterase and Membrane Stability of Red Cell in vitro

Zhi-Yi Liu, Bao-Guo Liu, Cai-Li Zhang

1995, 4(1): 17-21.

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The results confirmed that diazepam inhibits the cholinesterase in rat serum, red cell, corpus striatum and diaphragm in vitro, that the higher the diazepam concentration, the stronger the cholinesterase inhibition, and that diazepam is a reversible inhibitor to acetylcholinesterase and diazepam has a stabilizing action on red cell membranes. The role of these effects of diazepam in the treatment of organic phosphate poisoning is discussed.

Preliminary Studies on High-performance Liquid Chro-matography-Chemiluminescence Determination of the Saturated Fatty Acids (C16, C18) in Human Serum

Geng-Li Duan, Kenichiro Nakashima, Naotaka Kuroda, Shuzo Akiyama

1995, 4(1): 22-29.

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The peroxyoxalate chemiluminescence (CL) detection of fatty acids in human serum combined with high-performance liquid chromatography (HPLC) is described. Some fatty acids in serum were extracted with a 1:1 (v/v) mixture of chloroform-n-heptane. 2-(4-Hydrazinocarbonyl- phenyl)-4,5-diphenylimidazole (HCPI) was used as a fluorescent labelling reagent of the fatty acids. The labelling reaction was carried out at 30 ºC for 1 h at pH 6.5 and the resulting reaction mixture was subjected to HPLC. The labelled fatty acid C17 (P-C17) was used as the internal standard. The labelled fatty acids C16 and C18 were separated within 18 min on an ODS-80TM column (150 mm×6 mm ID, 5 μm, Tosoh Japan). The calibration curves of fatty acids from the spiked control serum were Y1 = -0.0037 + 0.0028X1, r = 0.994 for FA C16 and Y2 = 0.0012 + 0.00098X2, r = 0.999 for FA C18, respectively. The average recoveries of facids from the spiked control serum were 107.2% (n = 8, RSD = 4.3%)for FA C16 and 97.35%(n=8, RSD=4.0%) for FA C18, respectively. The lower detection limits of fatty acids after reaction were 12μmol per 20 μl injection for FA C16 and 18 μmol per 20 μl injection for FA C18, respectively (signal to noise ratio, S/N = 2). The HPLC/CL method was applied to the determination of FA C16 and FA C18 in normal human serum and the results showed that the concentrations of fatty acids in normal human serum were 0.134±0.009 μ mol/ml serum (n = 5) for FA C16 and 0.052±0.028 μmol/ml serum (n = 5) for FA C18, respectively.

Chemical Constituents of Silene jenisseensis Root

Zhen-Hua Cui, Liang Qiao, Cong-Yuan Gao, Zhi-Cen Lou

1995, 4(1): 30-31.

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Effect of Cu(II)-Salicylate in Micellar Systems on Scavenging Superoxide Ion Released by Cultured Macrophages

Yu-Hui Ying, Ying Zhang, Chun-Su Lu

1995, 4(1): 32-36.

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