Bioequivalence of metformin hydrochloride sustained-release tablets under fed condition in healthy subjects / 中国药科大学学报

@#To evaluate bioequivalence and safety of two kinds of metformin hydrochloride sustained-release tablets (test preparation vs reference preparation) under the condition of fed and single administration.A single center, randomized, open, single-dose, two-period, two-sequence, and double-crossover design was used.32 healthy subjects took 0.5 g of test preparation or reference preparation under fed and single-dose administration.4 mL of venous blood was collected from before administration (0 h) to 1, 3, 4, 4.5, 5, 5.5, 6, 7, 8, 9, 10, 12, 15, 24, 36 and 48 h after administration.The concentration of metformin in plasma samples was detected, and then the pharmacokinetic parameters were calculated by WinNonlin 7.0 software.When the 90% confidence intervals of cmax, AUC0-t and AUC0-∞ geometric mean ratio of test preparation and reference preparation were within 80.00%-125.00% equivalent intervals respectively, the bioequivalence of the two preparations was proved.One subject fell off due to adverse events.The main pharmacokinetic parameters of test preparation and reference preparation as follows: cmax were (0.68 ± 0.14) and (0.65 ± 0.11) mg/L, AUC0-t were (7.33 ± 1.65) and (7.00 ± 1.89) h·mg/L, AUC0-∞ were (7.39 ± 1.67) and (7.06 ± 1.91) h·mg/L, respectively.The 90% confidence intervals of the geometric mean ratio of the two main pharmacokinetic parameters were 101.45%-109.14%, 100.08%-112.32% and 100.24%-112.28%, respectively, which fell within the bioequivalence interval of 80.00%-125.00%.There were no serious adverse events and unexpected adverse events during the trial.The results show that test preparation and reference preparation are bioequivalent under fed and single-dose administration, safe and well tolerated in healthy subjects.

Development and validation of the Knowledge-Attitude-Practice Scale for Prevention of Occupational Low Back Pain for Nurses / 中国职业医学

Objective To develop and validate the Knowledge-Attitude-Practice Scale for Prevention of Occupational Low Back Pain for Nurses (hereinafter referred to as KAP). Methods Based on the knowledge, attitudes and practice theory, a list of 48 potential items were developed by reviewing literatures related to the prevention of occupational low back pain in nurses. The Delphi expert consultation method was used to conduct two rounds of consultation on the items, and the KAP (draft) with 31 items was formed. A total of 269 nurses in a hospital in Guangdong Province were selected as study subjects by convenience sampling method and investigated with the KAP (draft). The list was selected and its validity tested using SPSS 25.0 software. Results The authority degrees of two rounds of expert consultation were 0.919 and 0.922. All of the recovery rates of valid questionnaires were >80.0%, with the coefficients of variation ranged from 0.07 to 0.40 and 0.05 to 0.28. The Kendall's concordance coefficients were 0.198 and 0.274, respectively (all P<0.05). After item selection, five items were removed, resulting in the KAP with 28-item including three dimensions： knowledge, attitude and behavior. The scale-level content validity index/average was 0.976, and the item-level content validity index ranged from 0.833 to 1.000, as assessed by experts. The scale demonstrated 100.0% for convergent and discriminative validity of the three dimensions. The exploratory factor analysis revealed three factors with a cumulative variance contribution rate of 51.0%. Cronbach's alpha coefficients for the overall scale and knowledge, attitude, and behavior dimensions were 0.880, 0.878, 0.895, and 0.877, respectively. Split-half reliability coefficients were 0.922, 0.863, 0.852, and 0.820, respectively. Conclusion The KAP shows good reliability and validity and can be used to assess knowledge, attitude and practice levels related to occupational low back pain prevention among nurses.

High-throughput screening identifies established drugs as SARS-CoV-2 PLpro inhibitors

A new coronavirus (SARS-CoV-2) has been identified as the etiologic agent for the COVID-19 outbreak. Currently, effective treatment options remain very limited for this disease; therefore, there is an urgent need to identify new anti-COVID-19 agents. In this study, we screened over 6,000 compounds that included approved drugs, drug candidates in clinical trials, and pharmacologically active compounds to identify leads that target the SARS-CoV-2 papain-like protease (PLpro). Together with main protease (M

Pharmacokinetics/Pharmacodynamics models of veterinary antimicrobial agents

Misuse and abuse of veterinary antimicrobial agents have led to an alarming increase in bacterial resistance, clinical treatment failure, and drug residues. To address these problems, consistent and appropriate dosage regimens for veterinary antimicrobial agents are needed. Pharmacokinetics/Pharmacodynamics (PK/PD) models have been widely used to establish rational dosage regimens for veterinary antimicrobial agents that can achieve effective prevention and treatment of bacterial diseases and avoid the development of bacterial resistance. This review introduces building methods for PK/PD models and describes current PK/PD research progress toward rational dosage regimens for veterinary antimicrobial agents. Finally, the challenges and prospects of PK/PD models in the design of dosage regimens for veterinary antimicrobial agents are reviewed. This review will help to increase awareness of PK/PD modeling among veterinarians and hopefully promote its development and future use.

Efficacy of chemical thoracic sympathetic nerve modulation combined with pulsed radiofrequency in treating upper limb postherpetic neuralgia / 中华麻醉学杂志

Objective To evaluate the efficacy of chemical thoracic sympathetic nerve modulation combined with pulsed radiofrequency in treating upper limb postherpetic neuralgia ( PHN). Methods Forty-two patients of both sexes with upper limb PHN, aged 48-75 yr, were divided into 2 groups ( n=21 each) using a random number table method: chemical thoracic sympathetic nerve modulation combined with pulsed radiofrequency group ( TSNM+PR group) and pulsed radiofrequency group ( PR group) . TSNM+PR group was treated using chemical thoracic sympathetic nerve modulation combined with pulsed radiofrequen-cy, and PR group received pulsed radiofrequency alone. The occurrence of treatment-related adverse reac-tions was recorded. Numeric rating scale scores were recorded preoperatively and at 1 day and 1 and 3 months after operation, and the efficacy was graded. The effective treatment and pain recurrence were re-corded 3 months after operation. Quantitative sensory nerve tests were performed to record the current per-ception threshold before operation and on 1 day, 1 month and 3 months after operation. Results Compared with PR group, numeric rating scale score was significantly decreased, the therapeutic effect was en-hanced, the rate of effective treatment was increased, the recurrence rate of pain was decreased at 1 and 3 months after surgery, the current perception threshold at 250 and 5 Hz on the ipsilateral side was increased at 1 and 3 months after surgery in TSNM+PR group ( P<0. 05) . No treatment-related adverse reactions were found in two groups. Conclusion Chemical thoracic sympathetic nerve modulation combined with pulsed radiofrequency provides reliable therapeutic effect and higher safety for upper limb PHN.