Search

Eslicarbazepine acetate (ESA) a potent sodium channel blocker and an antiepileptic drug were subjected to various stress conditions as recommended by ICH guideline which includes hydrolytic, oxidative, thermal, and photolytic stress. The degradation studies show that ESA degraded in alkaline hydrolytic condition only while it found to be stable in other stressed conditions. A single degradation product emerged in UPLC studies on Waters Acquity BEH 150 x 2.1 mm, 1.7 µm, C18 column using mobile phase A (0.01M potassium dihydrogen orthophosphate and acetonitrile; 90:10 v/v) and mobile phase B (acetonitrile-watermethanol; 75:5:25 v/v) in the ratio of 50:50 (v/v) at RT 1.83 min with 0.2 ml/min flow rate and 2µl injection volume. The obtain degradation product from Eslicarbazepine acetate was isolated and characterized by IR, 1HNMR and UPLC-MS/MS analytical techniques. IR evaluation exhibited peaks at 3475.73 cm-1, 3363.86 cm-1, 1726.29 cm-1 for O-H, COO-H and C=O group, respectively. 1H NMR spectrum showed singlet at 11.865 which indicated the presence of COOH group. UPLC-MS/MS analysis shows molecular ion peak at 255.2 m/z. The recognized peak in the obtained spectrum confirmed the structure of the degradation product as 10-hydroxy-10,11-dihydro-5H-dibenzo[b,f]azepine-5-carboxylic acid which was formed by alkaline hydrolytic degradation. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

The pentacyclic triterpenic acids isolated from the oleo gum resin of various Boswellia species are collectively called as Boswellic acids (BA). The oleo gum resin obtained from Indian variety i.e. Boswellia serrata (Family – Burseraceae) is commonly known as Salai guggal. The resin fraction of Salai guggal is rich in Boswellic acids and its essential oil is composed of a mixture of mono, di and sesquiterpenes while gum fraction chiefly contains pentose and hexose sugars. This oleo-gum resin is quite popular among traditional practitioners of traditional Chinese and Indian Systems of medicine owing to their wide range of useful biological properties such as anti-inflammatory, anti-arthritic, anti-rheumatic, anti-diarrheal, anti-hyperlipidemic, anti-asthmatic, anti-cancer, anti-microbial anti-fungal, anti-complementary and analgesic activity, etc. It has been used as a herbal medicine since the prehistoric time to cure acute and chronic ailments including inflammatory diseases. Phytochemical investigation of this herbal medicine lead to identification of Boswellic acids which are found to be novel, potent, specific anti-inflammatory agents due to non-redox inhibition of 5-lipoxygenase (5-LO) enzyme. However, the other important targets of Boswellic acids also include topoisomerases, angiogenesis, and cytochrome p450 enzymes. This review is a sincere attempt to discuss and present the current status of therapeutic potential, phytochemical as well as pharmacological profile of Boswellic acids primarily obtained from B. serrata . [ABSTRACT FROM AUTHOR]