AIM: A new HPLC-MS method was developed to determine finasteride in human plasma. METHODS: Two formulations of finasteride tablets were given to 20 healthy male volunteers according to a randomized 2-way cross-over design. The samples were extracted by ethyl acetate under basic conditions, then were separated by C18 column and determined by mass detector. RESULTS: The calibration curve of finasteride was linear and intra-day and inter-day RSD were less than 10 %. The pharmacokinetics parameters of the two formulations (4.5 ± 0.5) h for t1/2; (3.0 ± 0.7) and (2.8 ± 0.9) h for tmax, respectively. The results indicated that there was no significant difference on cmax, A UC0-24, t1/2 or tmax values between the two formulations. CONCLUTION: The relative bioavailability of tablets I with respect to tablets Ⅱ is (99.3 ± 9.2) % by the A UC0-24 measurement, and bioe quivalence is observed between the two tablets.

AIM: To determine the distribution and frequency of functionally important allelic variants in the cytochromes P450 (CYP) 2C19, arylamine N-acetyltransferase 2 (NAT2), and thiopurine S-methyltransferase (TPMT) genes in the Han Chinese population and compare them with those of other ethnic populations.METHODS: Genotyping was carried out in a total of 210 unrelated Han Chinese volunteers derived from He-nan area. CYP2C19 variants ( * 2 and * 3), NAT2 variants ( * 6 and * 7), and TPMT variants ( * 3A, * 3B, and * 3C) were detected using polymerase chain reaction/restriction fragment length polymorphism (PCR-RFLP)assays. Detection of NA T2 * 5 and TPMT * 2 were performed using allele-specific polymerase chain reaction assays. RESULTS: Allele frequencies of CYP2C19 * 2 and * 3 occurred with 34.76 % and 6.4 %, respectively.Thirty-one persons ( 14.8 % ) carried two of these CYP2C19 alleles responsible for poor metabolizing activity.The frequencies of specif ic NAT2 alleles were 59.1%, 4.1%, 26.4 %, and 9.5 % for * 4 (wild-type), * 5(341C), * 6 (590A), and * 7 (857A), respectively. Genotyping of three different single nucleotide polymorphisms in the NA T2 gene revealed that the frequency of slow acetylators was 19.5 %. TPMT * 3C had an allelic frequency of 1.2 %. TPMT* 2, TPMT * 3A, or TPMT* 3B was not detected in the analysed samples. CONCLUSION: The overview of allele distribution for drug-metabolizing enzymes CYP2C19, NAT2, and TPMT among a Han Chinese population shows obvious difference to Caucasians. The data will be useful for clinical pharmacokinetic investigation and drug dosage administration to Han Chinese population.

AIM: To discuss the effects of phytoestrogenic-genistein on cathepsin K (CK) expression stimulated by interleukin-1α (IL-1α) in osteoclast-like cells (OCLs) . METHODS: The OCLs were isolated from tissue of human giant cell tumor of bone (GCT) . The cells treated with reagents were divided into 7 groups including control (treated with phenol red-free-DMEM), vehicle (treated with 1.2 nmol· L-1 IL- 1α), 10-10-10-6genistein, genistein+ ICI 182.780, and 17[β-estrodiol (17β-E2) group. The cells were treated with 1.2 nmol· L-1IL-1α after pre-treated with genistein or 17β-E2 for 48 h (excluded the control group) . Expression of CK wasdetermined by reverse transcriptase-polymerase chain reaction (RT-PCR) and Western blot in OCLs stimulated by IL-1α in the presence of genistein or 17[β-E2. RESULTS: The obvious increase of expression of CK by IL1α in vehicle group was noted in comparing with control group (P ＜ 0.01 ) . Genistein down-regulated CK gene expression stimulated by IL-1α at the transcription level in a dose-dependent manner (r = 0.68, P ＜ 0.01 ) .Genistein down-regulated CK protein expression stimulated by IL-1α also in a dose-dependent manner (r = 0.61,P ＜ 0.01 ). The effects of genistein were abrogated partly after treatment with the estrogen receptor antagonist ICI 182.780. CONCLUSION: Genistein inhibits CK expression stimulated by IL-1α partly through estrogen receptor in OCLs.

AIM: To study the protective effects of baicalin on myocardial ischemia-reperfusion injury in rats. METHODS: The models of myocardial ischemia-reperfusion injury were established by occluding left anterior descending coronary artery (LAD) for 30 min, followed by reperfusion for 120 min. The rate of rise and decline of left ventricular pressure (±dp/dtmax) and end-diastolic pressure of left ventricle (LVEDP) were monitored continuously with polygraph. After reperfusion, the blood and myocardium samples were taken for determination of malondialdehyde (MDA) content, superoxide dismutase (SOD), Na+-K+-ATPase, Ca2+-ATPase activities in myocardium, creatine kinase (CK) and lactate dehydrogenase (LDH) in serum with spectrophotometer. The ultrastructural changes in ischemic myocardium were assessed by transmission electron microscope. RESULTS:dtmax and LVEDP, decreased plasma CK and LDH levels, reduced myocardial MDA content, and increased the activities of SOD, Na+-K+-ATPase, and Ca2+-ATPase in myocardium following ischemia-reperfusion. The ultrastructural injury in reperfused myocardium was relieved. CONCLUSION: Baicalin possesses a protective effect against myocardial ischnemia-reperfusion injury through scavenging oxide radicals and improving Na+-K+-ATPase and Ca2+-ATPase activities.

AIM: To investigate the effect of soybean isoflavones (SI) on ventricular remodeling induced by myocardial infarction (MI). METHODS: MI was induced by permanent ligation of the left anterior descending coronary artery (LAD) in male Sprague-Dawley (SD)rats. Rats were randomly divided into six groups: shamThree hours after the operation, the drugs or solvent were administrated ig qd for 35 d. Twenty-four hours after the last administration, heart rate (HR), left ventricular end-diastolic pressure (LVEDP), peak systolic left ventricular pressure (Peak), maximal rate of left ventricular pressure rising (+dp/dtmax), maximal rate of left ventricular pressure declining (-dp/dtmax) and myocardial maximal shortening velocity (Vmax) were measured. After above hemodynamic parameters were measured, hearts were extracted. The ratio of total ventricle weight to body weight(TVW/BW) was calculated. Myocardial collagen was shown with the collagen-specific picrosirius red stain,myocardial interstitial collagen volume fraction(ICVF), perivascular collagen volume fraction(PCVF), infarct size,septal thickness (ST) and left ventricular diameter (LVD) were measured by image analysis system. RESULTS:(31 ± 5) %, respectively, all of which were significantly smaller than that in MI group (( 38.9 ± 2.9) %, P ＜ 0.01 ).In MI group, TVW/BW, LVD, ICVF and PCVF were remarkably increased compared with those in sham group (P ＜ 0.01 ). The increased TVW/BW, LVD, ICVF and PCVF were significantly reduced by treatment with eaprats in MI group was significantly decreased than that in sham group (P ＜ 0.01 ). The reduced ST could be in-dp/dtmax and Vmax were decreased (P ＜ 0.01 ), while LVEDP was increased (P ＜ 0.01 ), significantly. The reSION: SI can improve cardiac function and ventricular remodeling induced by myocardial infarction in the rat.

AIM:To establish HPLC method for the determination of amodiaquine in human plasma.METHODS: Amodiaquine and internal standard(hydroxychloroquine) were analyzed on C18 column(150 mm ×4.6 mm, 5 μm) with methanol: water:triethylamine: orthophosphoric acid (21:77.5:1:0.5 )as mobile phase at the flow rate of 1.0 mL · min-1The UV detector was set at 294 nm. RESULTS: The retention times of amodiaquine and internal standard were 5.82, 8.56 min, respectively. The calibration curve was linear in the range from 10 to 1 000 μg ·L- 1 ( r = 0.999 8, n = 9 ). The limit of quantitation was5 μg· L-1. The extraction recovery was between 75.5 % and 82.7 %, and the methodological recovery was between 97.0 % and 104.8 %. The intra-day and inter-day RSD were less than 6.0 % and 7.5 %, respectively. CONCLUSION: This HPLC method is simple, sensitive and suitable for pharmacokinetic study of amodiaquine.

AIM: To evaluate the efficacy and safety of multiple vitamin E, C, B facial mask for the patients with acne vulgaris. METHODS: One hundred and seventeen patients aged over 13 a, with acnes mainly sited on the face and an acne severity rating above grade 2 were enrolled in this study. The mask treatment was used once a day with 8 wk as a course.The primary endpoint included the number and the degree of acne lesions including comedoes, papules, pustules and cysts. The secondary endpoint was the overall efficacy evaluation by the physicians. RESULTS:After 8 wk of treatment with multiple vitamin E, C, B facial mask, the mean number of acne lesions:comedoes, papules, pustules and cysts decreased 13 + s 13,10 ± 12, 5 + 7 and 3 + 3, respectively. These changes were statistically significant (P ＜ 0.01 ). The results of overall efficacy evaluation showed that 7 patients '(6.0 % ) symptom was greatly improved, 44 patients '(37.6 % ) symptoms were moderately improved, 56patients'(47.9 % ) symptoms were slightly improved,and 10 patients' symptoms did not change. Among all 117 patients, 59 patients (50.4 % ) showed no adverse reactions, including swelling, redness, itching,burning or scaling. CONCLUSION: Multiple vitamin E, C, B facial mask is efficacious for the treatment of acne and more than half study subjects experienced in none adverse reaction. Multiple vitamin E, C, B facial mask possesses an alternate therapy in acne vulgaris.

AIM:To study the therapeutic effect of traditional Chinese medicine Reduqing on human cytomegalovirus (HCMV). METHODS:The expression of the HCMV late-mRNA in infected cells was measured by quantitative reverse transcription-polymerase chain reaction(RT-PCR) and the development of cytopathic effect (CPE) caused by HCMV was observed before and after treatment with Reduqing. On the basis of its anti-HCMV activity study in vitro, Reduqing was applied to the child-bearing aged women and pregnant women who were HCMV-IgM positive which indicated the active HCMV infection. The serum levels of tumor necrosis factor-alpha (TNF-α) and interleukin-2 (IL-2) before and after treatment were measured by the ELISA method. RESULTS:The results showed that the Reduqing had a strong inhibitory effect on both HCMV-mRNA and CPE. The level of the TNF-α increased while IL-2 decreased significantly in HCMV-IgM positive serum when compared with HCMV-IgM negative cases. In HCMV-IgM positive patients, after treatment with Reduqing, the serum levels of TNF-α and IL-2 returned to normal, and 73 % of them turned to be HCMV-IgM negative, which was significantly higher than that (14 %) in control group. CONCLUSION:It is suggested that serum TNF-α and IL-2 level are closely related to the activity of HCMV. Reduqing can enhance the immunity of the body and has an obvious inhibition on HCMV in vitro and in vivo, and can thus serve as an effective medicine for active HCMV infection therapy, especially for the pregnant women.

AIM: To establish a method to determine the concentration of indinavir in human plasma and study indinavir bioavailability in Chinese healthy people. METHODS: In a random two-period crossover study, 18 healthy male volunteers received a single dose of indinavir capsules 800 mg of two formulations respectively.A sensitive and specific reversed phase HPLC method was developed to quantitate plasma levels of indinavir. The drug was extracted from plasma with acetonitrile. Analysis was performed on a Hy persil C18 column with a mobile phase of acetonitrile:0.01 mol · L -1 phosphate buffer(pH 5.5 ) (43: 57).The UV detector was set at 210 nm. The standard curve covered the concentration ranged from 0. 03 to 16.38 mg · L-1. RESULTS: The concentration-time curves of reference and tested formulations both fitted to a one-compartment open model. The main pharmacokinetic rameters of tested and reference formulations were (10.6 ±s 2.4) mg· L-1 and (9.8 ±2.2)mg· L-1 for cmax, (0. 71 ± 0. 19) h and (0. 8 ±0.3) h for tmax, (1.30±0.24) h and (1.31 ±0.23) h for t1/2ke, (23±6) mg·h· L-1 and (22±5) mg·h · L-1 forAUC0-10, (24±6) mg · h · L-1 and (22±5) mg · h · L-1 for AUC0-∞, respectively. Two one-sidet test and variance analysis were performed in bioequivalent assessment. No statistically significant difference was found in AUC0-10, AUC0-∞ and cmax values between the tested and reference formulations. CONCLUSION:The reversed phase HPLC is a reliable method to determine the concentration of indinavir in human plasma and the two formulations of indinavir are bioequivalent.

Depressive disorders are relatively common in Hong Kong, and primary care doctors are trained to manage depressed patients appropriately,while more complicated cases are treated by specialists. Nevertheless, comorbid disorders and bipolar disorders are still relatively neglected. A wide variety of antidepressants are now available, but their usage has been limited by their costs, especially in the public medical service.