Journal of Chinese Pharmaceutical Sciences

A New Natural Product from Cistanche deserticola Y.C.Ma.

Xu Zhaohui, Yang Junshan, Lu Ruimian, Lu Yang, Zhou Junguo, Zheng Qitai, Yang Songsong

1999, 8(2): 61-63.

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One new natural Preduct, (2, 5-dioxo-4-imidazolidiny1)-carbamic acid was iso-lated from C. deserticola Y.C. Ma. Its chemical Structure and stereochemistry were finally conifrmedby single-crystal X-ray diffraction in addition to conventional spectroscopic methods.

Synthesis and Antifungal Activities of Some 6,8-Dichlorothiochromanone Derivatives

Guo Chun, Fang Lin

1999, 8(2): 64-67.

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A series of 6,8-dichlorothiochromanones was designed and synthesized. Twelve of them had not been reported in the literature. The antifungal activities of these compounds were also tested. Some of them displayed good activities against six tested fungi in vitro.

The Dissolution Properties of Nimodipine Solid Dispersion Used in Fast Release Formulations

Zhao Ganlin, Shen Xiaobin

1999, 8(2): 68-72.

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In the Present study, nimodipine-PVP solid dispersion was investigated to enhance the dissolution rate of nimodipine (NMDP), a poorly water-soluble substance, and to formulate the dosage forms with fast-release properties. The dissolution properties of NMDP-PVP coprecipitate and physical mixture were compared. The physical states of NMDP in both newly-made and one-yak-old samples of solid dispersion were also investigated by X-ray diffraction analysis. The dissolution rate of NMDP from the tablets and capsules of coprecipitate was compared with that of two kinds of commercial tablets. The results showed that solid dispersion gave much higher improvement than Physical mixture in the dissolution rate. In 5 min, 89% of the ding was released from solid dispersion, and 45% from physical mixture. Powder X-ray diffraction pattern showed that NMDP was present in amorphous or molecular form in the solid dispersion while it was in crystal line form in physical mixture. There was no appearance of crystallization in solid dispersion after one-year storage in a sealed glass bottle under room temperature. Capsules and tablets of coprecipitate both showed fast-release properties, and the drug dissolution fate from the former was greater than that from the latter, suggesting that the compressing pressure could influence the dissolution rate. It was also demonstrated that the dissolution rate of NMDP from the selected capsules was much greater (about three to four times) than that from the two kinds of commercial tablets.

Transdermal Iontophoretic Delivery of Ondansetron HCI

Ding Pingtian, Li Wei, Zheng Junmin

1999, 8(2): 73-77.

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The permeability of ondansetron at different current densities applied across the full-thickness mouse skin in vitro is reported. The steady state flux of ondansetron was increased from 30.29 μg·cm^-2·h^-1 to 160.70 μg.cm^-2·h^-1 When the current density changed from 0.05 mA·cm^-2 to 0.3 mA·cm^-2. But there was no strict linear relationship. Discoloration of ondansetron solution was found when platinum electrode was used in the donor compartment, which would be overcome by using Ag as electrode. The PH values in both donor and receptor compartments were changed in the study when platinum electrode was applied. The problems mentioned above and the keys to them were discussed.

Determination of Relative Bioavailability of Cefaclor in Healthy Human Volunteers by High Performance Liquid Chromatography

Lu Wanliang, Zhang Qiang, Sun Huadong, Wang Xinhong

1999, 8(2): 78-81.

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To evaluate the bioavailability of cefaclor, we established a reverse phase high performance liquid chromatographic method (HPLC). Ten healthy male volunteers were included in this randomized crossover study of bioavailability. Each was orally administered cefaclor capsule preparation (Keflor, 250 mg) or commercial one (Ceclor as a control, 250 mg), respectively. Venous blood samples were drawn at different times after dosing, and determined by HPLC. The results showed that the mean recovery of cefaclor from serum was 98.0%, and relative standard deviations of within-day and of between-day were observed from 0. 1% to 4.0%. The pharmacokinetic parameters of test preparation (Keflor), Tmax, Cmax, AUC0-∞, t1/2 were 0.55±0.11 h, 5.61±1.27 μg.ml^-1, 11.13±1.64 μg.h.ml^-1, 0.9 h, respectively. The relative bioavailability of Keflor was calculated to be 105.29±19.13%, as compared with control preparation (Ceclor). No statistically significant differences were observed in AUC0-∞, etc, by the two one-sided t-test procedures.

CGC Measurement of Propylene Glycol Content with Bentport Programmed Temperature Vaporizing (PTV) Injector

Ling Xiaomei, Xu Bingjiu

1999, 8(2): 82-85.

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This paper describes a CGC method to measure propylene glycol content in injection of 8-chloro-adenosine by injecting into a new PTV injector with bent-port vaporizing tube. This new method has the following advantages over split injection: it results in higher accuracy and precision (RSD ca. 2%, recovery ca. 99%), its analytical Period is short (<7 min), pretreatment of the sample is not necessary, and capillary column is not damaged after hundreds of samples injected. In comparison with PTV techniques published so far, this novel injector is superior in several respects.

Studies on Quantitative Determination of Antibiotics by the Derivative Differential Pulse Polarography

Liang Yunai, Wang Jie

1999, 8(2): 86-92.

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Quantitative determinations of streptomycin, benzylpeincillin and oxytetracycline by the first derivative differential pulse polarography (FDDPP), and of chloralnphenicol, kanamycin and ribostamycin by the second derivative differential Pulse polarography (SDDPP) were respectively studied. They showed very good linear relationship to the polarographic Peak heights (amplitudes) in the concentration ranges of 200~700 μg·ml^-1 (streptomycin), 35~210 μg·ml^-1 (benzylpenicillin), 10~60 μg·ml^-1 (oxytetracycline), 32~192 μg·ml^-1 (chloramphenicol), 150~900 μg·ml^-1 (kanamycin), and 80~480 μg·ml^-1 (ribostamycin) (p<0.01). The peak potentials and detection limits of streptomycin, benzylpenicillin, oxytetracycline, chloramphenicol, kanamycin and ribostamycin are 0. 100V, 5.6×10^-8 mol·L^-1, -1.400V, 8.0×10^-9 mol·L^-1, -1.536V, 6.9×10^-7 mol·L^-1,-0.060V, 6.0×10^-9 mol·L^-1, -0.370V, 4.6×10^-8 mol·L^-1, and -0.105V, 7.2×10^-9 mol·L^-1, respectively. This method is simple, rapid and sensitive, and the results are accurate.

Anti-inflammatory Activity of Berbamine

Cao Li, Luo Chongnian, Bian Qingya, Xiao Peigen

1999, 8(2): 93-94.

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Berbamine, a kind of alkaloid, was studied for anti-inflammatory activity. The drug was tested on carrageenan-induced rat paw oedema and kaolin-induced arthritis in rats. Berbamine has shown significant anti-inflammatory and anti-arthritic activities.

Effect of 3-n-Butylphthalide on Reperfusion induced Lipid Peroxidation Following Cerebral Ischemia in Rats and Superoxide Radical Formation In Vitro

Chong Zhaozhong, Feng Yipu

1999, 8(2): 95-99.

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Reperfusion after focal cerebral ischemia induced an increase in the content of malondialdehyde (MDA), a product of lipid peroxidation, in ischemic brain. dl-3-n-Butylphthalide (dl-NBP, 20 mg.kg^-1, ip). was shown to decrease the content of MDA in cerebral cortex of rats subjected to 1 h reperfusion following 6 h MCAO. dl-NBP, d-NBP and l-NBP were also shown to inhibit the production of superoxide boon in xanthine-xanthine oxidase reaction system in vitro. The effect of dl-NBP, d-NBP and l-NBP on superoxide anion may be due to their capability of inhibiting the activity of xanthine oxidase. The results suggest that dl-NBP may possess inhibiting effect on the formation of superoxide anion and reducing effect on lipid peroxidation during reperfusion after cerebral ischemia.

A Comparative Study of the Dose-Response and Recovery Time Course of Atracurium and Vecuronium

Xue Fushan, Liu Jianhua, Zhang Yanming, Liao Xu, An Gang

1999, 8(2): 100-104.

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To compare the characteristics of the dose-response and the time-course of action between atracurium and veculonium, sixty Chinese patients, ASA grade I, aped 17~50 (28.2±8.3) years, scheduled for elective plastic surgery were studied. All the patients were randomly and equally divided to either atracurium or vecuronium group. General anesthesia was maintained with 60% nitrous oxide in oxygen, thiopentone, and fentanyl. Neuromuscular function was assessed using an accelerometer with train-of-four (TOF) stimulation at the wrist every 12 s, and the depression percentage of first botch (T1) was used as the study parameter. The dose-response relationships of atracurium and vecuronium were determined by the cumulative dose-response technique. According to the dose-response curves established by led squares linear regression, the neuromuscular blocking potency of atracurium was only approximately 17% that of vecuronium. There were significant differences in the ED50, ED90, and ED95 between the two drugs. After the intravenous administration of equipotent doses of the two drugs (1.5×ED95), the duration of peak effect, clinical duration, recovery index, and total duration showed no significant differences between them. It is concluded that atracurium is a low-potency muscle relaxant and vecuronium is a high-potency muscle relaxant. The potency ratio of vecuronium: atracurium is 1:6 on the basis of ED95, and the recovery time course of the two drugs showed no significant differences following administration of equipotent doses.

Studies on the Chemical Constituents of the Roots from Bupleurum scorzonerifolium

Bat Yaming, Zhao Yuying, Tan Li, Zhang Ruyi

1999, 8(2): 105-107.

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Synthesis of Spin Labeled Carbocyclic Lignan Analogue Related to Podophyllotoxin

Lu Kuanke, Lin Shujing, Guan Zuowu, Chen Yaozu

1999, 8(2): 108-110.

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