Efficacy and safety of flurbiprofen cataplasms versus loxoprofen sodium cataplasms in knee osteoarthritis: a randomized controlled trial / 中华医学杂志(英文版)

BACKGROUND@#Clinical trial evidence is limited to identify better topical non-steroidal anti-inflammatory drugs (NSAIDs) for treating knee osteoarthritis (OA). We aimed to compare the clinical efficacy and safety of flurbiprofen cataplasms (FPC) with loxoprofen sodium cataplasms (LSC) in treating patients with knee OA.@*METHODS@#This is an open-label, non-inferiority randomized controlled trial conducted at Peking University Shougang Hospital. Overall, 250 patients with knee OA admitted from October 2021 to April 2022 were randomly assigned to FPC and LSC treatment groups in a 1:1 ratio. Both medications were administered to patients for 28 days. The primary outcome was the change of pain measured by visual analog scale (VAS) score from baseline to day 28 (range, 0-10 points; higher score indicates worse pain; non-inferiority margin: 1 point; superiority margin: 0 point). There were four secondary outcomes, including the extent of pain relief, the change trends of VAS scores, joint function scores measured by the Western Ontario and McMaster University Osteoarthritis Index (WOMAC), and adverse events.@*RESULTS@#Among 250 randomized patients (One patient without complete baseline record in the flurbiprofen cataplasms was excluded; age, 62.8 ± 10.5 years; 61.4% [153/249] women), 234 (93.6%) finally completed the trial. In the intention-to-treat analysis, the decline of the VAS score for the 24-h most intense pain in the FPC group was non-inferior, and also superior to that in the LSC group (differences and 95% confidence interval, 0.414 (0.147-0.681); P <0.001 for non-inferiority; P = 0.001 for superiority). Similar results were observed of the VAS scores for the current pain and pain during exercise. WOMAC scores were also lower in the FPC group at week 4 (12.50 [8.00-22.50] vs . 16.00 [11.00-27.00], P = 0.010), mainly driven by the dimension of daily activity difficulty. In addition, the FPC group experienced a significantly lower incidence of adverse events (5.6% [7/124] vs . 33.6% [42/125], P <0.001), including irritation, rash and pain of the skin, and sticky hair uncovering pain.@*CONCLUSIONS@#This study suggested that FPC is superior to LSC for treating patients with knee OA in pain relief, joint function improvement, and safety profile.

Effects of Rutin Combined with Quercetin with Different Compatibility Ratios on the Pharmacokinetics of Rutin in Rats in vivo / 中国药房

OBJECTIVE:To explore the effects of the different compatibility ratios of rutin with quercetin on the pharmacoki-netics of rutin in rats in vivo. METHODS:30 rats were randomly divided into rutin group(rutin-quercetin molar ratio of 4:0,the same below),quercetin group(rutin-quercetin ratio of 0:4),BL1 group(rutin-quercetin ratio of 3:1),BL2 group(rutin-quercetin ratio of 2:2)and BL3 group(rutin-quercetin ratio of 1:3),6 rats in each group,all group was administrated 10 mg/kg(calculat-ed by quercetin core of rutin and quercetin) intragastrically. The blood sample 0.3 mL was respectively taken from tail vein after 0.25,0.5,0.75,1,1.5,2,3,4,6,8,10,12,16,20,24 h of administration,the plasma concentration of quercetin(rutin me-tabolite) was determined by HPLC. DAS 2.0 software was used to calculate the pharmacokinetic parameters. RESULTS:The AUC0-24 h in rutin group,quercetin group,BL1 group,BL2 group and BL3 group were (4.908 ± 0.877),(8.382 ± 3.671), (8.473 ± 0.709),(4.366 ± 2.297),(8.914 ± 2.642)μg·h/L;MRT0-24 h were (9.675 ± 1.359),(3.142 ± 0.489),(3.517 ± 1.128), (3.376 ± 1.046),(4.494 ± 1.653) h;tmax were (5.726 ± 5.645),(1.375 ± 0.703),(1.125 ± 1.438),(1.417 ± 2.300),(1.292 ± 0.954) h;and cmax were (0.609 ± 0.202),(2.341 ± 0.539),(2.425 ± 1.217),(1.464 ± 0.677),(3.325 ± 2.425)μg/L. Compared with rutin group,AUC0-24 h and cmax in quercetin group,BL1 group and BL3 group were significantly increased(P0.05). CONCLUSIONS:Quercetin can inhance the related indexes of rutin in rats in vivo.

The impact of MIPO combined with locking plate fixation for the prognosis of patients with fractures of the tibia and Pilon / 中国基层医药

Objective To investigate the impact of minimally invasive osteosynthesis (MIPO)combined with locking plate fixation for the prognosis of patients with fractures of the tibia and Pilon.Methods 84 patients with CT or X -ray diagnosis of tibial Pilon fracture were randomly divided into group A (n =42)and group B (n =42). The group A were threatment with MIPO combination locking plate fixation and group B were threatment with reduction and internal fixation.The following -up clinical and radiological data of the two groups were compared. Results The blood loss of group A were less than group B(t =8.963,P <0.05),postoperative pain score were lower than group B(t =10.789,P <0.05),while the satisfaction score was higher than group A (t =8.963,P <0.05), postoperative hospital stay,healing time were shorter than group B (t =9.362,10.556,all P <0.05).The Conroy scoring system and Tenny scoring system of A group of excellent rates were 95.24%,76.19% were higher than 92.86% and 71.43% of group B(χ2 =6.222,6.574,all P <0.05).The overall complication rate of A group was lower than the group B(χ2 =7.265,P <0.05 ).Conclusion MIPO combination of locking plate fixation Pilon fractures can reduce soft tissue dissection,reduce surgical trauma to the patient,reduce postoperative complications in patients,in favor of patients recover as soon as possible.

Study on stability of major pharmaceutical ingredients of vladimiriae radix before and after being roasted in artificial gastric juice, artificial intestinal juice and isolated rat gastric, intestinal or colonic incubation juice / 中国中药杂志

<p><b>OBJECTIVE</b>To study the stability of costunolide (COS) and dehydrocostus lactone (DEH) of Vladimiriae Radix before and after being roasted in artificial gastric juice, artificial intestinal juice and isolated rat gastric, intestinal or colonic incubation juice.</p><p><b>METHOD</b>The HPLC method was used for the determination of the mass concentration of COS and DEH Vladimiriae Radix before and after being roasted artificial gastric juice, artificial intestinal juice and isolated rat gastric, intestinal or colonic incubation juice. The samples were incubated with isolated rat stomach, small intestine; colon was used to study physical adsorption, absorption or degradation parameters.</p><p><b>RESULT</b>COS of Vladimiriae Radix before or after being roasted was unstable in artificial gastric juice, with the average degradation constants as 0.758 0 and 0.531 1. Having been roasted, it showed an increasing stability with a significant difference (P < 0.01). Both of COS and DEH of Vladimiriae Radix before or after being roasted showed high adsorption, uptake or degradation (2 h), and it had significant difference between different parts.</p><p><b>CONCLUSION</b>COS was unstable in artificial gastric juice (unprocessed Vladimiriae Radix has a higher degradation rate). Isolated rat stomach, small intestine, colon can adsorb, take, degrade COS and DEH of Vladimiriae Radix before or after roasting process obviously and differently. It provides basis for studies on the absorption mechanisms of effective ingredients of Vladimiriae Radix before and after being roasted.</p>

Determination method of muscone in rat intestinal perfusate by GC-MS/MS and its intestinal absorption kinetic characteristics in rats / 中国中药杂志

<p><b>OBJECTIVE</b>To establish the method for determining muscone in rat intestinal perfusate by GC-MS/MS and study its intestinal absorption kinetic characteristics in rats.</p><p><b>METHOD</b>The GC-MS/MS method was used to determine the content of muscone in rat intestinal circulation fluid. In situ intestinal circulation perfusion was adopted to study absorption kinetics of muscone in rats.</p><p><b>RESULT</b>Muscone was proved to be well absorbed in each section of small intestine. Its absorption rate constants (Ka) and the absorption rate (A) in the rat intestine showed duodenum > jejunum (P < 0.05) , duodenum > ileum (P < 0.01). Its Ka, A and t1/2 in rat small intestine was 0.990 h(-1) , 43.58% and 0.705h, respectively.</p><p><b>CONCLUSION</b>Muscone was well absorbed in each intestinal section, with duodenum better than jejunum (Ka, T1/2, P < 0.05) significantly better than ileum (Ka, T1/2, P < 0.01; A, P < 0.05). There is no obvious statistical difference between jejunum and ileum.</p>

Interaction of Baicalin with Berberine for Intestinal Absorption in Rats / 中国药房

OBJECTIVE:To study the interaction of baicalin with berberine for intestinal absorption in rats. METHODS: The mode was induced by in situ intestinal perfusion to observe the absorptive kinetics characteristic in rats’ intestine before and after mixing. RESULTS: The absorption rate constant (ka) and absorption rate (A) of baicalin alone were (0.068?0.002)h-1 and (5.92?1.39)% while those of baicalin mixed with berberine were (0.060?0.002)h-1 and (4.27?1.23)% , respectively. ka and A of berberine alone were (0.044?0.003)h-1 and (3.47?0.64)% while those of berberine mixed with baicalin were (0.057?0.006) h-1 and (5.18?0.83)%, respectively. There were significant difference in the absorption rate constant of baicalin after mixing(P

Application of PK-PD methods based on metabonomics and "FANG-ZHENG Correspondence" to investigating compatibility of Chinese material medica / 中草药

The systematic approaches of metabonomics are similar to the essential attribution in concept of the wholism for traditional Chinese medicine (TCM) theories. The metabonomics had been progressively utilized to study the TCM theories, such as "ZHENG" (synelromes), or the systematic mechanism of Chinese materia medica (CMM) and its formulae by animal models, and toxicology in recent years. These studies almost focused on the responeses of endogenous metabonome to biological stimuli or genetic manipulation (pharmacodynamics and toxicology) by TCM theory of "ZHENG", while less involved the precess of formulae itself and its dynamic changes (pharmacokinetics) by TCM theory of "FANG". The "treatment by differentiating syndrome" and "Correspondence of FANG-ZHANG" is the quintessence of TCM theories. Consequently, in this idea, the application of PK-PD methods based on metabonomics and "FANG-ZHENG correspondence" to investigating the compatibility of the formulae in TCM theory is discussed in this paper.