Journal of Chinese Pharmaceutical Sciences

Chemical and Pharmacological Research Progress of Chinese Drug

Zhao Qian, Guo Jixian, Zhang Yunyi

2000, 9(1): 1-5.

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JiangXiang is the dried heartwood of trunk and root of Dalbergia odorifera T. Chen. In this paper, the chemical and pharmacological research progress of "JiangXiang" has been reviewed with 24 references According to its pharmacological activities, some suggestions for further research and development have been made.

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Journal of Chinese Pharmaceutical Sciences

2000, 9(1): 1-01.

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Chemical Constituents of Chaenomeles sinensis (Thouin.) Koehne

Sun Lianna, Hong Yongfu

2000, 9(1): 6-9.

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From the dried fruits of Chaenomeles sinensis (Thouin.) Koehne, a new pentacyclic triterpenoid, ursolic acid-3-O-behenate, along with eighteen known compounds was isolated. Their structures were elucidated by spectral analysis and chemical properties.

New Non-peptide Angiotensin II Antagonists, 2. Quinazolinone and Quinazoline Derivatives

Jiang Xuntian, Xu Tianlin, Hua Weiyi, Zhu Dongya, Yu Jing, Liang Shaomei

2000, 9(1): 10-14.

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The design, synthesis, and angiotensin II (AII) antagonist activities of several quinazolinone (IV) and quinazoline phenoxyphenylacetic acids (V) are described. Quinazolinone ring was used to replace the quinoline moiety of quinoline phenoxyphenylacetic acids (III) which have been discovered as potent AII antagonists, to give a new series of antagonists (IV), while their quinazoline analogs (V) were obtained as isomers during the synthesis of (IV). However, both series of compounds were not found to increase the potencies. In a test for antagonizing AII in vitro using isolated rabbit aorta rings, all the compounds exerted competitive antagonism. The most potent quinazolinone (IVb) and quinazoline (Vb) had pA2 values of 7.0 and 5.9, respectively.

Synthesis and Antifungal Activities of 2-(2,4-Difluorophenyl)-3-(N-Methyl-N-Substituted Sulfonamido)-1-(1H-1,2,4-Triazol-1-yl)-2-Propanol

Zhong Wu, Zhang Wannian, Li Ke, Zhou Youjun, Zhu Ju, Lu Jiaguo

2000, 9(1): 15-18.

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Ten new antifungal triazoles, 3-sulfonamido-2-aryl-1-triazoly-2-propanol derivatives were designed and synthesized as potential inhibitors of the fungal cytochrome P-450 14α-demethylase. Results of antifungal tests in vitro showed that compounds 1b, 1c and 1g had high activity, especially against Candida albicans, Candida parapsilosis and Fonsecaea pedrosor, but less active in comparison with ketoconazole. Compared with fluconazole, compound 1b was thirty-two times more active against Candida parapsilosis and four times more active against Fonsecaea pedrosor, compound 1c was sixteen times more active against Candida parapsilosis and eight times more active against Fonsecaea pedrosor, compound 1g was four times and eight times more active against Candida parapsilosis and Fonsecaea pedrosor respectively.

Study on the Configuration of Nucleoside Analogues Containing Disaccharide by ¹H NMR

Liu Zhongjie, Cui Yuxin^*, Liu Xuehui, Min Jimei, Zhang Lihe

2000, 9(1): 19-21.

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A new kind of nucleoside analogues containing disaccharide resulting from Ferrier reaction of glycal was synthesized. Their (a, b, c, d) ¹H NMR signals were assigned by GCOSY and GNOESY, the configuration was also determined. The results are in accord with computer-aided molecular simulation.

Pulmonary Delivery of Insulin: Absorption Enhancement of Insulin by Various Absorption Promoters in Rats

Shen Zancong, Cheng Yi, Zhang Qiang^*, Wei Shun, Wang Kui

2000, 9(1): 22-25.

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The effects of absorption promoters on the pulmonary absorption of insulin were examined by intratracheal administration of insulin solution in rats. The absorption of insulin from the lung was evaluated by its pharmacological bioavailability (PA%). Results revealed that the coadministration of insulin with 20 mmol·L^-1 sodium cholate (PA% = 69.1%), 1% sodium caprilate (PA% = 40.4%), 1% Brij 35 (PA% = 46.6%). 1% Brij 78 (PA% = 53.6%) or GdCl3(PA% = 32.2% at 0.04 mg.kg^-1 and 36.3% at 0.2 mg·kg^-1) (lanthanide compound) induced a significantly greater decline in blood glucose levels, while coadministration of insulin with adjunvants such as 1% EDIA (PA% = 19.1%), 5% oleic acid (PA% = 20.8%) or LuCl3 (PA% = 25.1%,at 0.2 mg.kg^-1) (lanthanide compound) appeared to have no enhancement effect. These observations indicated that the use of proper absorption promoters would be useful for improving the pulmonary absorption of insulin.

Water Penetration, Matrix Swell and Drug Release Property Studies of Hydroxypropylmethyl Cellulose Matrix Tablets

Xu Guojie, Zhang Ruhua, Chu Wei, Hisakazu Sunada

2000, 9(1): 26-30.

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Water penetration into HPMC matrices may be observed when they are brought into contact with water. The effects of HPMC substitute type on the water penetration are concentrated on the initially short time, which is considered to be the time for HPMC to form a hydrogel. After hydrogel is formed, the water penetration rate is identical. The effect of HPMC on water penetration depends on its molecular weight. When a drug is added into HPMC matrix, the ability of water penetration into matrix is weakened. As the water penetrates, a considerable swelling of the HPMC matrix is also observed, axial swelling is greater than radial swelling, and the swelling of matrix is mainly produced by HPMC. High HPMC level produces large swelling of matrix. Linear relations exist between water penetration, matrix swelling and drug release.

Study on Pharmacokinetics and Relative Bioavailability of A Sustained-release Preparation of Albuterol

Wang Jianxin, Chen Deguang, Cai Chuanzhen, Li Tongling, Qin Yongping, Li Tun

2000, 9(1): 31-34.

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The pharmacokinetics and relative bioavailability of a sustained-release capsule of albuterol (Salbuta) made by CDDA (China) were investigated following a single and multiple oral dose given to 20 healthy male volunteers in a randomized 2-way cross-over study. The controlled-release tablet of albuterol (Volmax) made by Glaxo (U.K.) was used as reference preparation. Plasma concentration of albuterol was determined by a newly developed HPLC method with UV detection. After a single oral dose the peak concentrations Cmax were 10.6±3.94 ng·mL^-1 and 10.52±2.59 ng·mL^-1 at 5.50±0.85 h and 5.30±0.95 h and the AUC0-∞ were 124.74±33.86 h·ng·mL^-1 and 126.02±38. 17 h.ng·mL-1 for Salbuta and Volmax respectively. The relative bioavailability of Salbuta was 98.98±12.04%. Following multiple dosing, mean steady state C^ssmax values were 12.94±3.35 ng·mL^-1 and 12.60±3.36 ng.mL^-1, mean C^ssmin values were 5.84±1.34 ng.mL^-1 and 6.16±1.33 ng·mL^-1, the degree of fluctuation (DF) was 81.82±17.74% and 76.03±20.48% for the two formulations respectively. The results of statistical comparison showed that the two preparations were bioequivalent.

Study of the Bioequivalence of Four Formulations of Nimodipine in Healthy Volunteers

Xu Xiaowei, Fu Qiang, Li Dakui, Charles H Nightingale

2000, 9(1): 35-38.

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Aim: The objective was to compare the rate and extent of absorption of three generic formulations with that of a reference formulation when administered in equal doses. Methods: The study design was a singledose, randomized four-way crossover with a 1-week washout period between each phase of the experiment dosing. Plasma concentration-time profiles were determined and the bioavailability of different formulations of nimodipine tablets (A, B, C and D) following oral administration of a 120 mg nimodipine single dose was compared. Results: The Tmax of the tablet A, B, C and D was 0.6±0.2 h,1.1±1.2 h,0.5±0.1 h and 0.5±0.2 h, respectively, the Cmax was 108.8±59.5 ng·ml^-1, 56.1±30.7 ng·ml^-1, 73.2±34.9 ng·ml^-1 and 94.7±41.1 ng.ml^-1, respectively; and the AUC was 175.4±77.9 ng·h·ml^-1, 135.8±62.4 ng.h.ml^-1, 154.8±69.5 ng.h.ml^-1 and 154.5±51.6ng·h·ml^-1, respectively. The relative bioavailabilities of tablets B, C and D compared with tablet A were 83.7%, 93.1% and 97.6%, respectively. The 90% confidence interval for the AUC shown for tablets B and C were 66.7-88.8% and 77.2-102.7%, respectively, less than 80% compared to the reference at the low-range estimate, tablet D was 80.5-107. 1%, greater than 80% compared to the reference at the low-range estimate. Conclusion: The 90% confidence interval with respect to AUC was between 80% and 125%, the formulations B and C were not considered bioequivalent, formulation D was considered bioequivalent compared with formulation A.

Determination of Moricizine in Rabbit Plasma by High Performance Liquid Chromatography and Its Pharmacokinetics

Hu Ping^*, Zhang Caili

2000, 9(1): 39-42.

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An HPLC assay for moricizine determination in plasma or serum, which is relatively simple, sensitive, selective and rapid. has been developed. Plasma samples were prepared by addition of internal standard (estazolam) followed by dichloromethane extraction. The mobile phase consisted of methanol-water-0.065 mol·L^-1 ammonium acetate-glacial acetic acid (75:24:1:0.015, v/v/v/v). The calibration curve was linear in the range from 50 ng·mL^-1 to 5000 ng·mL^-1 with r = 0.9997. The detection limit of this method was 4 ng·mL^-1. The method showed good precision and the recovery of moricizine from plasma was 96-102%. The relative standard deviations for within-day and between-day were 0.7-3.2% and 2.3-4.0% respectively. The plasma drug concentration-time course in rabbits after intravenous bolus administration conformed to the two-compartment open model. Mean t1/2β value was 6.35±2.23h.

Vasodilatory Effects of a New Nitroderivative of Acetylsalicylic Acid (nitropirin)

Qu Xiangping, Yi Fuxian, Guo Zhaogui

2000, 9(1): 43-45.

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In this study we assessed the vasodilatory effects of nitropirin, a new nitroderivative of aspirin, in vitro. Nitropirin contains a nitric oxide (NO) moiety, which is considered to act both by inhibiting cycloxygenase and by releasing NO in tissues. Nitropirin could relax both the endothelium-intact and endothelium-denuded rabbit aorta rings in a concentration-dependent manner. The values of EC50 were 7.26×10^-6 mol·L^-1 on the endothelium- intact aorta rings and 1.25×10^-5 mol·L^-1 on the endothelium-denuded aorta rings, which were considered insignificant compared with those of nitroglycerin (4.69×10^-6 mol·L^-1 and 5.3×10^-6 mol·L^-1 respectively, P>0.05). Aspirin showed no significant relaxant activity on aorta strips in a wide rang. from 1×10^-8 mol·L^-1 to 1×10^-4 mol·L^-1. The results demonstrate that nitropirin has endothclium-independent relaxant activity on the arteries. The mechanism of this property may be related to the ability of providing NO in target tissues.

Effect of Ganoderma lucidum on Collagen-Induced Arthritis in Rats

Li Hong, Jia Yongfeng, Masao MORI, Zhang Luoxiu

2000, 9(1): 46-49.

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Collagen type II (CII) 1.5 mg was injected intradermally on d0 to induce arthritis (CIA) in rats. Hind paw volumes of rats were measured with a water displacement method. The serum anti-collagen antibody was measured by an enzyme-linked immunosorbent assay. Delayed hypersensitivity was reflected by skin response to CII. Interleukin-1 (IL-1) activities were evaluated by [3H]-TdR uptake and interleukin-2 (IL-2) activity were measured by MTT colorimetric assay. Ganoderma lucidum (leyss. ex Fr.) Karst. (GL) 0.5 and 1.0 g.kg^-1·d^-1, given iP to rats from d0, to d24, suppressed skin response to CII, 1.0 g.kg^-1 GL reduced high level of anti-collagen antibody and improved the lowered IL-2 production in CIA rats. GL had no significant effect on IL-1 production and could not reduce inflammatory swelling of hind paw in CIA rats. As an immunomodulator, GL had shown no significant antiinflammatory activity, but improved the abnormal immune function in CIA.

Recent Progress in Biosynthesis of Rauwolfia Alkaloids

Su Yanfang, Guo Dean

2000, 9(1): 50-54.

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The biogenetic pathways of some Rauwolfia alkaloids including the 29 indole alkaloids isolated from Rauwolfia cell suspension cultures were reviewed. The enzymes related to the biosynthetic pathways were described.

Effect of Starch Microspheres on the Distribution of Cis- Dichlorodiammine Platinum in Mice

Hu Xin, Hou Xinpu

2000, 9(1): 55-56.

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