A new impurity was detected during high performance liquid chromatographic （HPLC） analysis of eslicarbazepine acetate active pharmaceutical ingredient. The structure of unknown impurity was postulated based on liqui...A new impurity was detected during high performance liquid chromatographic （HPLC） analysis of eslicarbazepine acetate active pharmaceutical ingredient. The structure of unknown impurity was postulated based on liquid chromatography mass spectrometry using electrospray ionization and ion trap analyzer （LC/ESI-IT/MS） analysis. Proposed structure of impurity was unambiguously confirmed by synthesis followed by characterization using 1H, 13C nuclear magnetic resonance spectrometry （NMR）, 1H-1H correlation spectro-scopy （COSY） and infrared spectroscopy （IR）. Based on the spectroscopic and spectrometric data, unknown impurity was characterized as 5-carbamoyl-10,11-dihydro-5H-dibenzo[b,f]azepin-10-yl propionate.展开更多
Eslicarbazepine acetate (ESL) is a new, once daily, orally administered, third generation antiepileptic drug which is indicated in the treatment of partial-onset seizures. ESL is known to exert it's anticonvulsant...Eslicarbazepine acetate (ESL) is a new, once daily, orally administered, third generation antiepileptic drug which is indicated in the treatment of partial-onset seizures. ESL is known to exert it's anticonvulsant effect by blocking the voltage-gated sodium channels. Several clinical trials and pharmacological studies have revealed that seizure control was better with ESL monotherapy (1 200 or 1 600 mg once daily) following a switch from other antiepileptic drugs in comparison with pseudo-placebo patients. The studies have indicated the ESL to be well tolerated and produced only mild to moderate emergent adverse events with the therapy. Being a dibenzazepine family member, structure and chemistry of ESL resembles more or less to carbamazepine and oxcarbazepine. ESL differs structurally from carbamazepine and oxcarbazepine at the 10, 11 position of dibenazepine nucleus. This molecular variation results in differences in metabolism and thus helps to prevent the formation of toxic epoxide metabolites. ESL following oral administration is rapidly metabolised to active metabolite namely S-licarbazepine which is responsible for its pharmacological activity. ESL exhibits acceptable pharmacokinetic profile and shows insignificant drug-drug interactions. In phase III clinical program, ESL was found to be efficacious and well tolerated in adult patients with partial onset seizures previously not controlled with treatment with one or two other antiepileptic drugs.展开更多
Objective: To study the main aspects of osteoporotic emergency fracture of the hip in the Umbria Region in the years 2006-2011. Methods: The study was conducted from January 1 of 2006 to December 31 of 2011, and inclu...Objective: To study the main aspects of osteoporotic emergency fracture of the hip in the Umbria Region in the years 2006-2011. Methods: The study was conducted from January 1 of 2006 to December 31 of 2011, and included only patients over 49 years of age. Patients who did not habitually reside in the region were excluded. They were collected in each based on the following data: age, sex, place of residence (urban or rural), time of the year, fractured side, type of trauma, history of fracture contralateral and perioperative mortality. Results: From 2006 to 2011, a progressive increase in the number of femoral fracture admissions in regional hospitals was observed, equal to 4.73% per annum. The incidence went from 6.8 to 8.1 for 1.000 ultra-65th residents. The most affected age groups are those between 75-84 years and 85-94 years. Conclusions: The epidemiology of osteoporotic hip fracture in the Umbria Region follows a pattern similar to that of other Italian regions. The in-hospital mortality of these patients is partly determined by age and number of complications they suffer during admission. The impact of economic resources on patients who break the osteoporotic hip justifies the implementation of programs for the prevention of osteoporosis and fractures.展开更多
文摘A new impurity was detected during high performance liquid chromatographic （HPLC） analysis of eslicarbazepine acetate active pharmaceutical ingredient. The structure of unknown impurity was postulated based on liquid chromatography mass spectrometry using electrospray ionization and ion trap analyzer （LC/ESI-IT/MS） analysis. Proposed structure of impurity was unambiguously confirmed by synthesis followed by characterization using 1H, 13C nuclear magnetic resonance spectrometry （NMR）, 1H-1H correlation spectro-scopy （COSY） and infrared spectroscopy （IR）. Based on the spectroscopic and spectrometric data, unknown impurity was characterized as 5-carbamoyl-10,11-dihydro-5H-dibenzo[b,f]azepin-10-yl propionate.
文摘Eslicarbazepine acetate (ESL) is a new, once daily, orally administered, third generation antiepileptic drug which is indicated in the treatment of partial-onset seizures. ESL is known to exert it's anticonvulsant effect by blocking the voltage-gated sodium channels. Several clinical trials and pharmacological studies have revealed that seizure control was better with ESL monotherapy (1 200 or 1 600 mg once daily) following a switch from other antiepileptic drugs in comparison with pseudo-placebo patients. The studies have indicated the ESL to be well tolerated and produced only mild to moderate emergent adverse events with the therapy. Being a dibenzazepine family member, structure and chemistry of ESL resembles more or less to carbamazepine and oxcarbazepine. ESL differs structurally from carbamazepine and oxcarbazepine at the 10, 11 position of dibenazepine nucleus. This molecular variation results in differences in metabolism and thus helps to prevent the formation of toxic epoxide metabolites. ESL following oral administration is rapidly metabolised to active metabolite namely S-licarbazepine which is responsible for its pharmacological activity. ESL exhibits acceptable pharmacokinetic profile and shows insignificant drug-drug interactions. In phase III clinical program, ESL was found to be efficacious and well tolerated in adult patients with partial onset seizures previously not controlled with treatment with one or two other antiepileptic drugs.
文摘Objective: To study the main aspects of osteoporotic emergency fracture of the hip in the Umbria Region in the years 2006-2011. Methods: The study was conducted from January 1 of 2006 to December 31 of 2011, and included only patients over 49 years of age. Patients who did not habitually reside in the region were excluded. They were collected in each based on the following data: age, sex, place of residence (urban or rural), time of the year, fractured side, type of trauma, history of fracture contralateral and perioperative mortality. Results: From 2006 to 2011, a progressive increase in the number of femoral fracture admissions in regional hospitals was observed, equal to 4.73% per annum. The incidence went from 6.8 to 8.1 for 1.000 ultra-65th residents. The most affected age groups are those between 75-84 years and 85-94 years. Conclusions: The epidemiology of osteoporotic hip fracture in the Umbria Region follows a pattern similar to that of other Italian regions. The in-hospital mortality of these patients is partly determined by age and number of complications they suffer during admission. The impact of economic resources on patients who break the osteoporotic hip justifies the implementation of programs for the prevention of osteoporosis and fractures.
