Abstrakt
Clinical pharmacokinetics of parecoxib via intravenous and intramuscular injections in Chinese populations
Chenghai Wang, Shaoyan Huang, Jie Li, Wei Shao, Kaoxiang Sun, Mengyuan Zhang
Objective: To study the clinical pharmacokinetics of parecoxib sodium via intravenous and intramuscular injections in Chinese populations.
Methods: A total of 20 patients undergoing unilateral lower limb surgery were selected, and their related parameters were as follows: ASA: Grade I to II, age: 20 to 60 years, and weight: 50 to 80 kg. They were randomly assigned to two groups: the intravenous injection group (IV group) and the intramuscular injection group (IM group), with 10 patients in each group (N=10). Then, they were subjected to intravenous or intramuscular injection of parecoxib at 40 mg (diluted with 2 ml of normal saline) and venous blood sampling (2 ml) at 0, 10, 20, 30, 40, 50, and 60 min, and at 1.5, 2, 4, 6, 8, 12, 16, 20 and 24 h after the injection. After that, the venous blood was added with heparin for anti-coagulation and centrifuged at 3000 rpm for 10min. The plasma was separated and placed in a refrigerator at -20°C. The plasma concentration of levobupivacaine was detected by means of High Performance Liquid Chromatography (HPLC). All statistical analysis was performed using SPSS17.0 statistical software. Measurement data were expressed as mean ± standard deviation (x? ± s), and the t test and repeated measurement analysis of variance were adopted for inter- and intra-group comparisons. The count data were compared using the χ2 test, and P<0.05 was considered statistically significant.
Results: After the intravenous and intramuscular injections of parecoxib, its plasma concentration was increased quickly, with its Cmax at 31.578 ± 13.407 and 21.311 ± 10.160 mg/L, respectively. Then its plasma concentration was decreased rapidly, with no parecoxib detected in the plasma of all patients at 4 h after its administration. Accordingly, the Cmax of valdecoxib in patients from the two groups was reached at 20 min and 1.5 h, respectively, with the values at 0.751 ± 0.290 and 0.543 ± 0.162 mg/L, respectively, and no parecoxib was detected in the plasma of all patients at 24 h after its administration. Processing by the pharmacokinetic software showed that the AUC of parecoxib of patients in Group II was higher than that in Group I (P<0.05) and that CL was lower than that in Group I (P<0.05), whereas the differences in the pharmacokinetic parameters of valdecoxib in patients between the two groups were not statistically significant (P>0.05).
Conclusion: The routes of administration can affect the clinical pharmacokinetic parameters of parecoxib, but not those of valdecoxib.