RESUMO
Objective To investigate celecoxib self-microemulsifying drug delivery system (CXB-SMEDDS) that was developed to increase the dissolution rate and oral bioavailability of celecoxib.Methods The formulation of CXB-SMEDDS was optimized by pseudo-ternary phase diagrams analysis.The appearance, morphology, particle size distribution and in vitro drug release behavior of CXB-SMEDDS were investigated after diluted by water.The bioavailability of CXB-SMEDDS was determined by oral administration to rats compared with CXB suspension.Results An optimized formulation was selected: Medium chain triglycerides as oil phase, Tween 20 as surfactant, Transcutol HP as cosurfactant.The ratio of oil phase, surfactant and cosurfactant was 2∶9∶9.Upon mixing with water, CXB-SMEDDS formed a clear and transparent microemulsion solution with homogeneous small spherical under transmission electron microscopy.For particle size of CXB-SMEDDS was found to be (57.6±14.2) nm.The in vitro dissolution test indicated a significant improvement in release characteristics of CXB.The AUC of CXB-SMEDDS and CXB suspension were (5.54±0.94) and (3.32±0.59) mg·L-1·h, respectively.The relative bioavailability was 166.9%.Conclusion The SMEDDS can significantly increase celecoxib dissolution in vitro and bioavailability in vivo.
RESUMO
Objective To study effects of oxycodone post-operative early analgesia on stress re-sponse with in diabetics undergoing uvulopalatopharyngoplasty (UPPP).Methods Eighty patients undergoing UPPP,53 males,27 females,aged 28-65 years,ASA Ⅰ or Ⅱ were randomly divided in-to two groups(n =40).1 5 minutes before the end of the operation,group O was intravenously given oxycodone 0.07 mg/kg;Group F fentanyl 0.7 μg/kg.The patients of the two groups were sampled venous blood 3 ml in the morning of operation (T1 ),postoperative 1 hour (T2 ),postoperative 3 hours (T3 )for determination of serum cortisol (Cor),serum insulin(Ins),serum C-peptide(C-P)u-sing electrochemical luminescence method.Results Cor at T2 ,T3 was lower than that at T1 , C-P was higher than that at T1 (P <0.05)in group O,respectively;Cor at T2 ,T3 was higher than that at T1 , respectively,C-P was lower than that at T1 (P <0.05);Cor in group F was higher than that in group O,C-P in group F was lower than that in group O(P <0.05).Ins at T2 ,T3 was lower than that at T1 and was lower than that in group O(P <0.05).Conclusion Oxycodone 0.07 mg/kg early analgesia for UPPP significantly inhibits the occurrence of stress response.
RESUMO
OBJECTIVE@#To explore the effects of different analgesia methods after UPPP.@*METHOD@#Ninety cases of patients uvulopalatopharyngoplasty were divided into 3 groups randomly, and 30 cases in each group. The group A was the blank control group without any analgesia measures. The cases in group B were treated with intramuscular injection of parecoxib sodium 40 mg after surgery immediately, and continued injecting 40 mg after 12 hours, 24 hours and 36 hours respectively. 100 mg tramadol replaced 40 mg parecoxib sodium in group C. The VAS scoring was performed after surgery 12, 24, 36, 48, 72, 96 hours in 3 groups, and we observed adverse reaction such as lethargy, nausea, vomiting, dizziness, skin rash and so on.@*RESULT@#The group B and C reduced the pain significantly compared with blank control group. The pain scores in group B were significantly decreased than that in group C (P<. 05).@*CONCLUSION@#The analgesic effect of parecoxib sodium after UPPP is significant and better than tramadol. It is worthy to use widely in clinical due to its better effect and less side effect.