Effect of chromatographic conditions on enantioseparation of bovine serum albumin chiral stationary phase in HPLC and thermodynamic studies.

Twelve chiral compounds were enantiomerically resolved on bovine serum albumin chiral stationary phase (BSA-CSP) by high-performance liquid chromatography (HPLC) in reversed-phase modes. Chromatographic conditions such as mobile phase pH, the percentage of organic modifier, and concentration of analyte were optimized for separation of enantiomers. For N-(2, 4-dinitrophenyl)-serine (DNP-ser), the retention factors (k) greatly increase from 0.81 to 6.23 as the pH decreasing from 7.21 to 5.14, and the resolution factor (R(s)) exhibited a similar increasing trend (from 0 to 1.34). More interestingly, the retention factors for N-(2, 4-dinitrophenyl)-proline (DNP-pro) decrease along with increasing 1-propanol in mobile phase (3%, 5%, 7% and 9% by volume), whereas the resolution factor shows an upward trend (from 0.96 to 2.04). Moreover, chiral recognition mechanisms for chiral analytes were further investigated through thermodynamic methods.

[Comparative study on acupoint pressing and medication for angina pectoris due to coronary heart disease].

OBJECTIVE: To observe the differences of therapeutic effect of acupoint pressing, Nitroglycerin and Suxiaojiuxin pill on angina pectoris (AP) due to coronary heart disease (CHD). METHODS: One hundred and six ty-eight patients with AP due to CHD were randomly divided into an acupoint pressing group (n = 58), a Nitro glycerin group (n = 56) and a Suxiaojiuxin pill group (n = 54) and were treated with acupoint pressing at Danzhong (CV 17) for 5-10 minutes, sublingual administration of Nitroglycerin and sublingual administration of Suxiaojiuxin pill, respectively. Symptoms, improvements in ECG, the time of producing effectiveness and adverse effects in all the groups were observed. RESULTS: The total effective rate and the effective rate of ECG were 93.1% (54/58) and 86.2% (50/58) in the acupoint pressing group respectively, 92.9% (52/56) and 85.7% (48/56) in the Nitroglycerin group, and 87.0% (47/54) and 75.9% (41/54) in the Suxiaojiuxin pill group, with no significant differences among the three groups (all P > 0.05). The average time of producing effectiveness was (1.67 +/- 2.45) min in the acupoint pressing group which was shorter than (2.89 +/- 2.64) min in the Nitroglycerin group and (3.75 +/- 2.99) min in the Suxiaojiuxin pill group (P < 0.05, P < 0.001). During the treatment, there were no adverse effects in the acupoint pressing group, which less than 19 cases in the Nitroglycerin group and 12 cases in the Suxiaojiuxin pill group (both P < 0.05). CONCLUSION: Acupoint pressing can significantly improve symptoms of AP patients with a similar therapeutic effect to Nitroglycerin and Suxiaojiuxin pill, but it has more rapid therapeutic effect without adverse effects.

[Clinical observation on acupuncture for treatment of abdominal postoperative pain].

OBJECTIVE: To compare the therapeutic effects between acupuncture based on syndrome differentiation and analgesic on abdominal postoperative pain. METHODS: One hundred cases of abdominal postoperative pain were randomly divided into two groups, 50 cases in each one. In acupuncture group, the treatment was applied according to meridian differentiation and point selection on the affected meridian. Ashi points near to the incision as the main points and those closely connected with Zangfu functions were selected, such as Yanglingquan (GB 34), Taichong (LR 3) and Zusanli (ST 36), etc. In medication group, muscular injection of Bucinnazine was administered. The severity of pain was evaluated with Visual Analogue Scale (VAS) before and after treatment. RESULTS: The remarkably effective rate in acupuncture group was 60.0% (30/50), which was markedly better than that 28.0% (14/50) in medication group (P < 0.01). VAS scores in 30 min and 4 h after treatment as well as 24 h after operation in two groups were all reduced remarkably as compared with those before treatment (all P < 0.01), indicating the satisfactory analgesia in treatment. VAS scores in acupuncture group were lower apparently than those in medication group in 30 min and 4 h after treatment (P < 0.01,P < 0.05). CONCLUSION: Acupuncture has quick analgesia in treatment of abdominal postoperative pain, which is superior to muscular injection of Bucinnazine because of its advantages of long-term and significant efficacy.

Preparation of liposomal brucine and its pharmaceutical/pharmacodynamic characterization.

AIM: To prepare a novel transdermal preparation of liposomal brucine (LB) and investigate its pharmaceutical/pharmacodynamic characterization. METHODS: LB was prepared by a modified ethanol-dripping method. Its drug encapsulation efficiency (EE), particle size, in vitro release, and skin permeation were studied. Furthermore, a safety evaluation and pharmacodynamic analysis of LB, including acute dermal toxicity, skin irritation, and analgesic and anti-inflammatory effects were investigated. RESULTS: the EE of LB was 72% and the mean particle size of the liposomes was 55.4 nm. The in vitro release profile indicated that less than 68% of the encapsulated brucine was released in 10 h. A skin permeation study showed that compared with the free brucine, LB exhibited higher cumulative drug permeation through the skin and lower drug accumulation in skin tissue, indicative of an obvious promotion of skin permeation with liposomal encapsulation. The acute dermal LD50 of LB was greater than 100 mg/kg (brucine content) and skin irritation tests revealed that LB had no irritation to both integrity and broken skin. A pharmacodynamic evaluation of LB was performed by xylene-induced mouse ear edema test and acetic acid-induced writhing test at the dosage of 1.5, 3, and 6 mg/kg, respectively. The results showed that anti-inflammatory activities and analgesic effects of brucine encapsulated were significantly higher than that of the free brucine (P<0.01). Moreover, LB maintained a remarkably longer antiinflammatory and analgesic duration. CONCLUSION: It can be proposed that LB prepared here could represent a safe, effective and promising transdermal formulation for analgesic and anti-inflammatory effects.

[Observation on therapeutic effect of electroacupuncture at points of different channels at different stages on hemiplagia after apoplexy].

OBJECTIVE: To compare the therapeutic effects at points of different channels at different stages on hemiplegia after apoplexy. METHODS: One hundred and twenty-eight cases of hemiplegia after apoplexy were randomly divided into a treatment group and a control group, 64 cases in each group. The Brunnstrom cerebral apoplexy motor recovery six-stages scale was used as criterion for division of stages in treatment of the treatment group, and different points were selected according to different stages, and the brief Fugl-Meyer motor scale was used as criterion for assessment of the therapeutic effect; the control group were treated with routine acupuncture. RESULTS: The total effective rate was 93.8% in the treatment group and 57.9% in the control group, the treatment group being better than the control group (P < 0.01). CONCLUSION: Electroacupuncture at points of different channels at different stages has a good therapeutic effect on hemiplegia after apoplexy.