Journal of Chinese Pharmaceutical Sciences

Study on the Equivalent Conformation of Retinoids

Zong-Ru Guo, Quan-Zhi Liu, Min-Min Wang

1997, 6(4): 173-177.

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N-(4-Carboxy-phenyl)-3,5-di-t-butyl-4-hydroxy-benzamide (2) possesses structural prerequisite for cell-differentiation inducing activity, which constitutes the therapeutic basis of all-trans-retinoic acid (ATRA) and analogues for the treatment of cancer and dermatosis. In addition to the similarity of the disposition of functional groups with ATRA, 2 shows a conformational equivalence to ATRA in terms of molecular shape, size, as well as the spatial arrangement of functional groups. However, the N-methylated compound (3) is devoid of the activity. It owes the biological behavior to the conformational difference, because of the steric interference between N-methyl group and the hydrogen atom of a phenyl ring. X-ray crystallography, UV, and NMR were performed to investigate the difference.

A New Phenylethanoid Glucoside from Buddleia officinalis

Jiao-She Li, Yu-Ying Zhao^*, Li-Bin Ma

1997, 6(4): 178-181.

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A new phenylethanoid glycoside, neobudofficide B was isolated from Buddleia officinalis. On the basis of spectral and chemical evidence, the glycoside was identified as-β-(3',4'-dihydroxy, 6'-N-pyridinechloride-phenyl )-ethyl-O-α-L-rhamnopyranosyl-( 1→3 )-β-D-( 4''-O-caffeoyl )glucopyranoside.

A New Flavone C-glycoside from Scutellaria baicalensis

Yong-Yu Zhang, Yun-Zhen Guo, Hiroyuki Ageta, Yoshihiro Harigaya, Masayuki Onda, Kadsunori Hashimoto, Yukinobu Ikeya, Minoru Okada, Masao Maruno

1997, 6(4): 182-186.

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A new flavone C-glycoside, chrysin-8-C-β-D-glucoside (1) and a known phenethyl alcohol glycoside, acteoside (2), were isolated for the first time from the roots of Scutellaria baicalensis (Labiatae).

A Novel Angular Furanocoumarin Isolated from Cnidium monnieri Fruit

Zheng-Tao Wang, Jin Na Cai, Guo-Jun Xu, Chun-Tao Che

1997, 6(4): 187-191.

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A new angular furanocoumarin, 2'-acetylangelicin (8), along with oroselone (1), columbianadin (3), bergapten (4),Oacetyl columbianetin (5), cniforin A (6), edultin (7) and β-sitosterol (2), was isolated from the fruit of Cnidium monnieri. The structures were elucidated by spectral methods. Compound 1 was isolated from this plant for the first time.

Triterpenoids from the Fruiting Body of Ganoderma lucidum

Fang-Sheng Wang, Hui Cai, Jun-Shan Yang^*, Yu-Mei Zhang, Ying-Ju Zhao

1997, 6(4): 192-197.

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A new triterpenoid, named ganolactone, was isolated from the CH2Cl2 soluble fraction of the fruiting body of Ganoderma lucidum. Its structure was deduced as 7β-hydroxy-3,11,15-trioxo-lanosta-8-en-24→20s lactone (1) on the basis of spectral analysis (UV, IR, MS, ¹H NMR, ¹³C NMR and 2D NMR) and was confirmed by X-ray diffraction. In addition, three known compounds, ganoderiol A (2), ganoderiol B (3) and ganodermatriol (4), were obtained.

Study on Liposomes of Mimetic Red Cell

Xin-Pu Hou, Yong Qiu, Jun-Mei Zhang

1997, 6(4): 198-202.

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Liposomes were prepared by adding hydrophilic agents PEG-PE, rigidity agent SM in the bilayer membrane for mimetic red cell membrane. In PBS or serum, release of calcein content from liposomes dramatically decreased, which demonstrated increasing membrane stability by adding PEG-PE or SM. The ratio b/R of the remains of liposomes in blood to that in RES was used as a parameter of biodistribution in vivo. At 2 h after iv injection, b/R of modified liposomes was enhanced 6.5~13.1 fold. Their clearance half-life from blood circulation was delayed 1.6~5.8 fold. The modification of liposome membrane by PEG-PE or SM is the favorable condition for drug-liposomes to target the non-RES.

Influence of Preparation Factors on the Sustained Release of Nifedipine from Eudragit RL/RS Microspheres

Chong-Dong Fu, Xue-Tao Jiang, Jin-Hong Hu, Wan-Guo Zhang

1997, 6(4): 203-210.

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Sustained-release Eudragit RL/RS microspheres encapsulating nifedipine were prepared using the acetone/liquid paraffin emulsion-solvent evaporation method. The influence of different preparation factors on release of the drug in vitro was investigated. The release rate of nifedipine from the microspheres increased with increasing Eudragit RL/RS ratio and stirring rate during the preparation, and with decreasing the polymer concentration of internal phase and microsphere size. It was found that a linear relationship existed between the microsphere size and the time of 50% drug release. The drug release rate increased with increasing nifedipine content from 4.2 to 16.7% and was more rapid than the dissolution rate of pure nifedipine particles. However, the release rate of the microspheres with 26.6% drug content decreased significantly and was slower than the dissolution rate of pure drug particles. This was attributed mainly to the nifedipine dispersion state in the microspheres as confirmed by the differential thermal analysis and X-ray diffraction study, which showed that nifedipine was present in an amorphous or molecular state in the microspheres with 4.2, 9.4 and 16.7% drug, whereas partly in the crystalline state in the microspheres with 26.6% drug. The amounts released for less than 70% nifedipine can be fitted to Higuchi square-root of time model, independent of polymer ratio, drug content and microsphere size.

Pharmacokinetics of Controlled Release and Immediate Release Morphine Sulphate Tablets after a Single Dose and Multiple Doses in Chinese Volunteers

Yan-Ping Deng, Kai Wang, Li-Jing Liu, Jing-Wen Liu, Zhi-Ji Cai, Ya-Qing Lou

1997, 6(4): 211-214.

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The pharmacokinetics of morphine sulphate was studied in 10 Chinese healthy volunteers after a single oral dose. Blood samples were collected before and after administration of controlled release tablets (CRMS, 30 mg) and immediate release tablets (IRMS, 20 mg). The plasma concentration of morphine was determined by GC MS. The pharmacokinetic parameters of controlled release tablets and immediate release tablets were calculated: Cmax was 19.38±3.80 and 21.27±6.21 ng/ml, tmax was 2.36 ±0.37 h and 0.56±0.16 h, t1/2β was 3.53±0.87 and 3.03±0.74 h, AUC was 145.15±17.65 and 93.08±16.65 ng/ml, respectively. The steady state plasma concentration of morphine sulphate in cancer patients after multiple doses was achieved, Cmax of CRMS and IRMS was 27.43±0.33 ng/ml and 22.68±0.16 ng/ml, Cmin of CRMS and IRMS was 19.45±1.44 ng/ml and 18.14±0.49 ng/ml, respectively.

The Pharmacokinetics of Pancuronium in Infants, Children and Adults

Fu-Shan Xue, Lai-Kui Luo, Bai-Hua Sun, Qin Zou

1997, 6(4): 215-220.

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In order to determine the effect of age on the pharmacokinetics of pancuronium, twenty-four patients undergoing elective plastic surgery were studied. The patients were divided into three groups by their ages: Group 1-infants, 0.75 to 2.95 years (n = 5); Group 2-children, 4 to 14 years (n = 13); and Group 3-adults, 16 to 27 years (n = 6). After administered a bolus of pancuronium 100 μg/kg, an improved fluorimetric assay was used to measure the plasma concentrations of pancuronium. The pharmacokinetics of pancuronium may be best described mathematically by a two-compartment open model in all patients. The younger the patients, the larger the distribution volumes, the higher the Cl, and the lower the plasma concentrations of pancuronium. There were significant differences among the three groups regarding V1, V2, Vdss, Cl, AUC. T1/2β, MRT in Group 1 were longer than those in Groups 2 and 3. T1/2α and K21 were not significantly different among the three groups.

Further Isolation of Coumarin from Angelica pubescence Maxim f. biserrata Shan et Yuan

Jiang-Hua Liu, Sui-Xu Xu^*, Zhi-Yun Meng, Xin-Sheng Yao, Yu-Qiang Wu

1997, 6(4): 221-224.

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Nine coumarin compounds were further isolated from Angelica pubescence. They were columbianedin (1), osthol (2), bergapten (3), isoimperaterin (4), meranzin hydrate (5), nodakenetin (6), marmesinin (7), columbianin (8) and angelidiol (9). Among them, 5~8 were isolated for the first time from this plant, 9 is a new natural product.

Lucyoside Q, a Triterpenoid Saponin from Leaves of Luffa cylindrica (L.) M. Roem.

Long Liang, Chang-Yu Liu, Guang-Yu Li, Ling-En Lu, Yuan-Cong Cai

1997, 6(4): 225-227.

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A new pentacyclic triterpenoid saponin, named lucyoside Q, was isolated from the leaves of Luffa cylindrica. Its structure was established as 21-β-hydroxyloleanolic acid-28-O-β-D-glucopyranoside by means of the spectral evidence and chemical methods.

Effects of Artesunate on Tracheal Smooth Muscle from the Guinea-pig

Mao-Sheng Yang^*, Jian-Chu Xiao

1997, 6(4): 228-229.

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