Analysis of medication regularity of classical prescription in treatment of COPD based on multi-target efficacy evaluation system of Chinese medicine / 中国中药杂志

Effective drugs for chronic obstructive pulmonary disease(COPD), a complex chronic lung disease, have long been difficultly determined, while traditional Chinese medicine(TCM) has played a critical effect in the treatment of such disease. A new approach for the prediction based on data analysis by integrating TCM basic theories and modern science is urgently needed apart from clinical experiments. In this study, an efficacy evaluation system of COPD was established based on the multi-target efficacy evaluation system of Chinese medicine to analyze the medication regularity and characteristics, such as efficacies, properties, meridian tropism,and core combinations of Chinese medicines. The characteristics of classical prescriptions in the intervention of COPD were explored from modern pharmacology. The results showed that the Chinese medicines in the classical prescriptions in the treatment of COPD were dominated by heat-clearing, phlegm-resolving, dampness-dispelling, exterior-releasing, deficiency-tonifying, and interior-warming drugs. Among them, dampness-dispelling, interior-warming, and heat-clearing drugs resulted in higher perturbation efficiency in the disease network than some western medicines on the market, suggesting that these drugs possessed better efficacies in the treatment of COPD. In the classic prescriptions, warm-heat drugs were equivalent to cold-cool drugs in number, while the proportion of warm-heat drugs gradually raised with the increase in the perturbation efficiency. Additionally, core combinations in the classical prescriptions,such as heat-clearing/heat-clearing, dampness-dispelling/dampness-dispelling, and phlegm-resolving/heat-clearing, could achieve better efficacy for COPD. The present study preliminarily screened out the efficacies of Chinese medicines in the treatment of COPD based on scientific data through the multi-target efficacy evaluation system to explore the effect of Chinese medicine on COPD from modern pharmacology, explain the mechanism of TCM treatment of lung diseases, and provide references for the development of drugs targeting COPD.

Bioequivalence evaluation of acarbose tablet in healthy chinese volunteers with pharmacodynamic endpoints / 中国药学杂志

OBJECTIVE: To evaluate the bioequivalence of acarbose tablet in healthy Chinese volunteers through the use of pharmacodynamics endpoint parameters of serum glucose. METHODS: Following the Food and Drug Administration (FDA) guidance, a single oral dose of test and reference formulations was given to 32 healthy Chinese volunteers according to a randomized crossover design. Serum glucose concentrations after sucrose administration and co-administration of sucrose and acarbose on the following day were both determined. The reduction of serum glucose concentration were calculated following treatment with acarbose and sucrose together relative to the baseline serum glucose concentration observed. The parameters of Δcmax and AUEC0-4 h recommended by the FDA were used for bioequivalence evaluation. Four pharmacodynamics parameters of AUEC0-2 h,AUEC0-1.5 h, AUEC0-1.0 hand ΔGE were also tested in the evaluation. RESULTS: The main pharmacodynamics parameters of serum glucose in test and reference formulations were as follows:Δcmax (1.169±0.719) and (0.878±0.571) mmol·L-1, AUEC0-2 h(46±25) and (50±21) mmol·min·L-1, AUEC0-1.5 h(62±42) and (70±29) mmol·min·L-1, AUEC0-1 h(59±52) and (73±32) mmol·min·L-1, ΔGE(1.829±0.952) and (1.656±0.764) mmol·L-1, respectively. The parameter AUEC0-4 h could not be evaluated due to the presence of negative values. CONCLUSION: Acarbose tablet is bioinequivalent to the reference tablet.This might be related to acarbose dose, the 50 mg dose of acarbose tablet is inadequate. Pharmacodynamics parameters which is suitable to demonstrate acarbose bioequivalence might also need to be optimized.

Anti-tumor activity of long-circulation thermosensitive liposome-loaded vincristine / 国际药学研究杂志

Objective To investigate the anti- tumor activity of long- circulation thermosensitive liposom- loaded vincristine (VTSL) in vivo and in vitro. Methods The inhibitory effects of VTSL and vincristine injection (VCR) on sw620 cell and PANC cell were detected by MTT assay. The uptake capacity of HT-1080 was studied by using Cou-6-loaded liposome. Different xenograft nude mice models of HepG-2 and MCF-7 were established. To study anti-tumor effect of VTSL, drugs were given via tail and heat therapeutic area for 30 minutes, mice weight and tumor weight were recorded. To study anti-tumor effect of VTSL, drugs were given via tail vein and heat therapeutic areas for 30 min, mice body mass and tumor mass were recorded. Results After VTSL was given 72 h, the activity of sw620 and PANC was less than 5% and 20%, respectively. VTSL showed stronger cytotoxic effect than vincristine. At the same dose, tumor inhibitory rate of VCR and VTSL on HepG-2 and MCF-7 bearing nude mice was 50%, 69.7%, 47.8% and 76.1%, respectively. There were significant differences in tumor weight after treatment. Conclusion VTSL enhances the cytotoxicity by heating. Loading vincristine into TSL increased cytotoxicity, and heating could promote the fusion of liposomes and cell membrane. Under the same dosage, VTSL showed much higher tumor inhibition rate than VCR, and there was a certain dose dependence. The results show that VTSL can be used in treatment of solid tumor and has the potential to expand vincristine clinical application.

Anti-tumor activity of long-circulation thermosensitive liposome-loaded vincristine / 国际药学研究杂志

Objective To investigate the anti-tumor activity of long-circulation thermosensitive liposom-loaded vincristine (VTSL)in vivo and in vitro. Methods The inhibitory effects of VTSL and vincristine injection(VCR)on sw620 cell and PANC cell were detected by MTT assay. The uptake capacity of HT-1080 was studied by using Cou-6-loaded liposome. Different xenograft nude mice models of HepG-2 and MCF-7 were established. To study anti-tumor effect of VTSL,drugs were given via tail and heat therapeu?tic area for 30 minutes,mice weight and tumor weight were recorded. To study anti-tumor effect of VTSL,drugs were given via tail vein and heat therapeutic areas for 30 min,mice body mass and tumor mass were recorded. Results After VTSL was given 72 h,the activ?ity of sw620 and PANC was less than 5%and 20%,respectively. VTSL showed stronger cytotoxic effect than vincristine. At the same dose,tumor inhibitory rate of VCR and VTSL on HepG-2 and MCF-7 bearing nude mice was 50%,69.7%,47.8%and 76.1%,respec?tively. There were significant differences in tumor weight after treatment. Conclusion VTSL enhances the cytotoxicity by heating. Loading vincristine into TSL increased cytotoxicity,and heating could promote the fusion of liposomes and cell membrane. Under the same dosage,VTSL showed much higher tumor inhibition rate than VCR,and there was a certain dose dependence. The results show that VTSL can be used in treatment of solid tumor and has the potential to expand vincristine clinical application.