BACKGROUND Aceclofenac(ACF),a widely used nonsteroidal anti-inflammatory drug,has been associated with a number of severe cases of clinical hepatotoxicity.Terminalia bellirica,an evergreen tree,is known to have severa...BACKGROUND Aceclofenac(ACF),a widely used nonsteroidal anti-inflammatory drug,has been associated with a number of severe cases of clinical hepatotoxicity.Terminalia bellirica,an evergreen tree,is known to have several ethnomedicinal uses including antioxidant and hepatoprotective effects.Hence T.bellirica fruit extracts and its phytoconstituent ellagic acid(EA)are expected to provide protection against oxidative stress and liver damage produced by long-term use of ACF.AIM To evaluate the antioxidant and hepatoprotective activities of T.bellirica fruit extracts and EA against ACF-induced toxicity in albino Wistar rats.METHODS The in vitro antioxidant activities of T.bellirica fruit ethyl acetate and aqueous extracts were measured by metal ion chelation and nitric oxide radical scavenging assays.The in vivo antioxidant and hepatoprotective effects of T.bellirica extracts(200 mg/kg)and EA(40 mg/kg)in ACF-induced hepatotoxic rats were assessed in serum and liver tissue after oral administration for 21 d.Silymarin(40 mg/kg)was used as a standard control.Oxidative stress markers in the blood(ferric reducing ability of plasma and lipid peroxidation inhibition)and liver tissues(superoxide dismutase,catalase and malondialdehyde)were analyzed using standard protocols.Liver function markers such as alkaline phosphatase,glutamic pyruvic transaminase,glutamic oxaloacetic transaminase,lactate dehydrogenase,γ-glutamyl transferase,creatinine,total protein,and uric acid were evaluated in rat serum.RESULTS The T.bellirica fruit ethyl acetate extract exhibited superior metal ion chelating and nitric oxide radical scavenging abilities during in vitro antioxidant assays as compared to aqueous extracts.Oral administration of ACF in rats(15 mg/kg)for 21 d produced oxidative stress and adversely affected liver function suggesting liver injury.Treatment with extracts(ethyl acetate and aqueous),EA and silymarin accounted for a significant reduction in the adverse effects of ACF on oxidative stress and liver function markers in serum and hepatic tissue in rats.Histopathological evaluation of the liver indicated that the extracts and EA significantly decreased the degree of liver damage.The in vivo efficacy of EA was higher than T.bellirica fruit extracts.Of these extracts,ethyl acetate extract revealed comparatively better antioxidant and hepatoprotective activity.CONCLUSION Ellagic acid and T.bellirica fruit extracts exhibited considerable hepatoprotective and antioxidant activities in long-term ACF-treated rats.展开更多
The objective of the study was to develop film coated tablets of aceclofenac using wet granulation technique. Possible drug-excipient interaction was evaluated by HPLC （high performance liquid chromatography） and FT...The objective of the study was to develop film coated tablets of aceclofenac using wet granulation technique. Possible drug-excipient interaction was evaluated by HPLC （high performance liquid chromatography） and FTIR （fourier infrared spectroscopy）. The tablets prepared were assessed for their physicochemical, in vitro dissolution at pH 1.2, 4.5, 6.8 and 7.5 and stability characteristics. Comparison with a commercial aceclofenac product was made in vitro and in vitro studies. There was no interaction between aceclofenac and used excipients. Furthermore, the physicochemical properties of the tablets were satisfactory. The dissolution profile of one of the formulated aceclofenac tablets （D07） was statistically similar （p 〈 0.05） to that of the commercial aceclofenac brand in all the dissolution media. The formulated products ware stable and showed no changes in physical appearance, drug content, or dissolution pattern after storage at 40 ℃/75% RH for 6 months. The results indicate that it is feasible to achieve a stable aceclofenac tablet formulation by using wet granulation technique.展开更多
Aceclofenac is a new generational Non-Steroidal Anti-Inflammatory Drug (NSAID), and is considered a better alternative to the popular pain-killer diclofenac, as it overcomes some of the adverse gastrointestinal and ca...Aceclofenac is a new generational Non-Steroidal Anti-Inflammatory Drug (NSAID), and is considered a better alternative to the popular pain-killer diclofenac, as it overcomes some of the adverse gastrointestinal and cardiac side effects associated with the latter. However, the bioavailability of the drug remains limited due to low aqueous solubility (0.058 μg/mL) and poor dissolution characteristics. Hence, improving its dissolution characteristics is of prime significance in order to establish its optimal therapeutic efficacy. In an effort to tackle this issue, we report the use of novel Soluplus®-based nanocomposites, prepared from emulsion templates, as effective drug loading agent for aceclofenac. Nanoemulsion templates were prepared by high-shear homogenization using a probe sonicator. The emulsions were subsequently lyophilized to obtain free flowing powders. The amorphization of the drug with increasing polymer content was clearly observed from powder X-ray diffractogram, while the drug-polymer interaction was explored by FTIR spectroscopy. The phase purity and homogeneity of the formulation was characterized using Differential Scanning Calorimetry. The dissolution profiles of the formulations were established by an USP paddle apparatus. Phase solubility study was conducted to evaluate the effect of polymer concentration on aqueous solubility of aceclofenac. The values of Gibbs-free energy (ΔG°tr) associated with the aqueous solubility of aceclofenac in the presence of Soluplus was used to optimize the polymer content. The in vitro dissolution rates of aceclofenac from the nanoparticles were significantly higher compared to the pure drug. Thus, Soluplus nanoparticles provide promising formulations for the improvement of the dissolution profiles and thus, the bioavailability, of aceclofenac.展开更多
Aim:Non-steroidal anti-inflammatory drugs are the most used analgesics for postoperative pain management.Aceclofenac is a newer phenylacetic acid derivative,and being a predominant cyclooxygenase-2 inhibitor,it has be...Aim:Non-steroidal anti-inflammatory drugs are the most used analgesics for postoperative pain management.Aceclofenac is a newer phenylacetic acid derivative,and being a predominant cyclooxygenase-2 inhibitor,it has better gastrointestinal tolerability than diclofenac.The aim was to compare the efficacy and safety of aceclofenac and diclofenac in managing postoperative pain using the Face Legs Activity Cry Consolability(FLACC)score and a visual analog scale(VAS)following composite resection for oral cancer.Methods:Seventy-six patients who underwent composite resection for oral cancer at a tertiary care hospital were randomly assigned to receive either injection of aceclofenac 150 mg or diclofenac 75 mg intramuscularly at 0,12,24,36,48,and 60 h postoperatively.The FLACC score was recorded at 2,4,8,12,and 24 h,and the VAS score was recorded at 24,36,48,60,and 72 h.Intravenous tramadol 100 mg was given as a rescue analgesic if the FLACC or VAS score was>3.The patient satisfaction score was recorded at 72 h.Results:There were 61 female and 15 male patients.Mean surgery durations in the aceclofenac and diclofenac groups were 450.00±116.00 and 416.84±130.63 minutes,respectively.Mean FLACC scores between the two groups were not significantly different.Patients receiving diclofenac had significantly lower mean VAS scores(P=0.005)at 72 than at 24 h.There was no significant difference in mean VAS scores between groups.The amount of rescue analgesic required in both groups was similar(P=0.34).At 72 h,31.57%of patients graded their satisfaction as good in the aceclofenac group and 34.21%in the diclofenac group.Nausea and dyspepsia were common adverse effects in both groups.Conclusion:Aceclofenac was as effective as diclofenac in reducing postoperative pain following composite resection for oral cancer.In individuals with a history of gastritis or peptic ulcer,aceclofenac can be an alternative to diclofenac.展开更多
文摘BACKGROUND Aceclofenac(ACF),a widely used nonsteroidal anti-inflammatory drug,has been associated with a number of severe cases of clinical hepatotoxicity.Terminalia bellirica,an evergreen tree,is known to have several ethnomedicinal uses including antioxidant and hepatoprotective effects.Hence T.bellirica fruit extracts and its phytoconstituent ellagic acid(EA)are expected to provide protection against oxidative stress and liver damage produced by long-term use of ACF.AIM To evaluate the antioxidant and hepatoprotective activities of T.bellirica fruit extracts and EA against ACF-induced toxicity in albino Wistar rats.METHODS The in vitro antioxidant activities of T.bellirica fruit ethyl acetate and aqueous extracts were measured by metal ion chelation and nitric oxide radical scavenging assays.The in vivo antioxidant and hepatoprotective effects of T.bellirica extracts(200 mg/kg)and EA(40 mg/kg)in ACF-induced hepatotoxic rats were assessed in serum and liver tissue after oral administration for 21 d.Silymarin(40 mg/kg)was used as a standard control.Oxidative stress markers in the blood(ferric reducing ability of plasma and lipid peroxidation inhibition)and liver tissues(superoxide dismutase,catalase and malondialdehyde)were analyzed using standard protocols.Liver function markers such as alkaline phosphatase,glutamic pyruvic transaminase,glutamic oxaloacetic transaminase,lactate dehydrogenase,γ-glutamyl transferase,creatinine,total protein,and uric acid were evaluated in rat serum.RESULTS The T.bellirica fruit ethyl acetate extract exhibited superior metal ion chelating and nitric oxide radical scavenging abilities during in vitro antioxidant assays as compared to aqueous extracts.Oral administration of ACF in rats(15 mg/kg)for 21 d produced oxidative stress and adversely affected liver function suggesting liver injury.Treatment with extracts(ethyl acetate and aqueous),EA and silymarin accounted for a significant reduction in the adverse effects of ACF on oxidative stress and liver function markers in serum and hepatic tissue in rats.Histopathological evaluation of the liver indicated that the extracts and EA significantly decreased the degree of liver damage.The in vivo efficacy of EA was higher than T.bellirica fruit extracts.Of these extracts,ethyl acetate extract revealed comparatively better antioxidant and hepatoprotective activity.CONCLUSION Ellagic acid and T.bellirica fruit extracts exhibited considerable hepatoprotective and antioxidant activities in long-term ACF-treated rats.
文摘The objective of the study was to develop film coated tablets of aceclofenac using wet granulation technique. Possible drug-excipient interaction was evaluated by HPLC （high performance liquid chromatography） and FTIR （fourier infrared spectroscopy）. The tablets prepared were assessed for their physicochemical, in vitro dissolution at pH 1.2, 4.5, 6.8 and 7.5 and stability characteristics. Comparison with a commercial aceclofenac product was made in vitro and in vitro studies. There was no interaction between aceclofenac and used excipients. Furthermore, the physicochemical properties of the tablets were satisfactory. The dissolution profile of one of the formulated aceclofenac tablets （D07） was statistically similar （p 〈 0.05） to that of the commercial aceclofenac brand in all the dissolution media. The formulated products ware stable and showed no changes in physical appearance, drug content, or dissolution pattern after storage at 40 ℃/75% RH for 6 months. The results indicate that it is feasible to achieve a stable aceclofenac tablet formulation by using wet granulation technique.
文摘Aceclofenac is a new generational Non-Steroidal Anti-Inflammatory Drug (NSAID), and is considered a better alternative to the popular pain-killer diclofenac, as it overcomes some of the adverse gastrointestinal and cardiac side effects associated with the latter. However, the bioavailability of the drug remains limited due to low aqueous solubility (0.058 μg/mL) and poor dissolution characteristics. Hence, improving its dissolution characteristics is of prime significance in order to establish its optimal therapeutic efficacy. In an effort to tackle this issue, we report the use of novel Soluplus®-based nanocomposites, prepared from emulsion templates, as effective drug loading agent for aceclofenac. Nanoemulsion templates were prepared by high-shear homogenization using a probe sonicator. The emulsions were subsequently lyophilized to obtain free flowing powders. The amorphization of the drug with increasing polymer content was clearly observed from powder X-ray diffractogram, while the drug-polymer interaction was explored by FTIR spectroscopy. The phase purity and homogeneity of the formulation was characterized using Differential Scanning Calorimetry. The dissolution profiles of the formulations were established by an USP paddle apparatus. Phase solubility study was conducted to evaluate the effect of polymer concentration on aqueous solubility of aceclofenac. The values of Gibbs-free energy (ΔG°tr) associated with the aqueous solubility of aceclofenac in the presence of Soluplus was used to optimize the polymer content. The in vitro dissolution rates of aceclofenac from the nanoparticles were significantly higher compared to the pure drug. Thus, Soluplus nanoparticles provide promising formulations for the improvement of the dissolution profiles and thus, the bioavailability, of aceclofenac.
文摘Aim:Non-steroidal anti-inflammatory drugs are the most used analgesics for postoperative pain management.Aceclofenac is a newer phenylacetic acid derivative,and being a predominant cyclooxygenase-2 inhibitor,it has better gastrointestinal tolerability than diclofenac.The aim was to compare the efficacy and safety of aceclofenac and diclofenac in managing postoperative pain using the Face Legs Activity Cry Consolability(FLACC)score and a visual analog scale(VAS)following composite resection for oral cancer.Methods:Seventy-six patients who underwent composite resection for oral cancer at a tertiary care hospital were randomly assigned to receive either injection of aceclofenac 150 mg or diclofenac 75 mg intramuscularly at 0,12,24,36,48,and 60 h postoperatively.The FLACC score was recorded at 2,4,8,12,and 24 h,and the VAS score was recorded at 24,36,48,60,and 72 h.Intravenous tramadol 100 mg was given as a rescue analgesic if the FLACC or VAS score was>3.The patient satisfaction score was recorded at 72 h.Results:There were 61 female and 15 male patients.Mean surgery durations in the aceclofenac and diclofenac groups were 450.00±116.00 and 416.84±130.63 minutes,respectively.Mean FLACC scores between the two groups were not significantly different.Patients receiving diclofenac had significantly lower mean VAS scores(P=0.005)at 72 than at 24 h.There was no significant difference in mean VAS scores between groups.The amount of rescue analgesic required in both groups was similar(P=0.34).At 72 h,31.57%of patients graded their satisfaction as good in the aceclofenac group and 34.21%in the diclofenac group.Nausea and dyspepsia were common adverse effects in both groups.Conclusion:Aceclofenac was as effective as diclofenac in reducing postoperative pain following composite resection for oral cancer.In individuals with a history of gastritis or peptic ulcer,aceclofenac can be an alternative to diclofenac.
