Eslicarbazepine acetate: a new promising antiepileptic agent
Eslicarbazepine acetate is a third generation, single enantiomer [(S)-(-)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide] member of the commonly prescribed first-line antiepileptic drugs (AEDs), formerly known as BIA 2-093, is a novel central nervous system (CNS)-active compound with anticonvulsant activity. It is a prodrug which is activated to eslicarbazepine (S-licarbazepine), an active metabolite of oxcarbazepine. Eslicarbazepine acetate is used as an adjunctive therapy in adult patients with partial onset seizures. It behaves as a voltage-gated sodium channel (VGSC) blocker and is currently marketed for the treatment of epilepsy. Eslicarbazepine acetate shares with carbamazepine and oxcarbazepine the dibenzazepine nucleus bearing the 5-carboxamide substitute, but is structurally different at the 10,11-position. This molecular variation results in differences in metabolism, preventing the formation of toxic epoxide metabolites such as carbamazepine-10,11 epoxide. This drug is considered as an adjunct to carbamazepine and oxcarbazepine.
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Formulation and evaluation of the oral dispersible tablets of anti-malarial drugs
Optimization of formulation. Physical and In-vitro evaluation of optimized formulation for the release characteristics. Increase the chemical properties like dissolution study. Oral dispersible tablets have received ever-increasing demand during the last decade, and the field has become a rapidly growing area in the pharmaceutical industry. Upon introduction into the mouth, these tablets dissolve or disintegrate in the mouth in the presence of additional water for easy administration of active pharmaceutical ingredients. Optimized formula using polymer coating method exhibited 90% drug release at 15 minutes for model drug but dihydroartemisinin the release was found to be 79% at 15 minutes.
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Healing effect of phenytoin and honey on excisional wound in experimental albino Rats
Phenytoin stimulates connective tissue growth, while honey has been used in treating various wounds and ulcers. This study evaluates 2% phenytoin ointment and honey on excisional wound healing process in experimental albino rats in comparison to 5% Betadine ointment. Method: Wistar albino rats were divided into four groups (n=6). Excisional round full thickness skin wounds of diameter 15 mm were created on back of anaesthetized animals. Medications were applied topically twice daily up to 20 days. Group A – untreated (control), Group B – 5% betadine ointment, Group C - 2% phenytoin oinment and Group D received honey. Wound healing was measured on Days 0, 4, 8, 12, 16 and 20. Number of days taken for complete epithelisation of wound was noted. Statistical analysis was done using ANOVA followed by Tukey-Kramer test and p<0.05 was considered significant. Result: 5% Betadine, 2% phenytoin ointment and honey hastens healing and reduces time taken for complete epithelisation of excisional wound when compared to negative control (p<0.05). 2% phenytoin and honey were superior to 5% betadine. Conclusion: Both 2% phenytoin oinment and honey may be considered for wound healing but their role in healing of infected wound needs to be explored further.
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Antileishmanial activity of Mangifera indica leaf extracts on the in vitro growth of Leishmania donovani promastigotes
Mangifera indica L. (Anacardiaceae), commonly known as Mango, is a large evergreen tree indigenous to Asia and found throughout the Indian subcontinent. In the present study, the in vitro antileishmanial activity of petroleum ether, chloroform and methanol extracts from M. indica leaf was evaluated against Leishmania donovani (strain AG 83) promastigotes by in vitro promastigote cell toxicity assay by using MTT [3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyltetrazolium bromide]. Here, all the test extracts markedly inhibited the growth of L. donovani promastigotes in vitro in a dose dependent manner. The methanol extract was found to be the most active followed by the chloroform and petroleum ether extracts respectively. Therefore, from the present study it can be inferred that M. indica leaf extracts exhibited remarkable antileishmanial activity against Leishmania donovani promastigotes in vitro.
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Encapsulation of olanzapine into Waxes/fat microspheres: Preparation, Characterization and Release kinetics
The objective of the present study was to minimise the unwanted side effects of olanzapine (OZ) drug by kinetic control of drug release by entrapping OZ into gastro resistant, biodegradable waxes such as beeswax (BW), cetostearyl alcohol (CSA), spermaceti ( SP) and fat cetyl alcohol ( CA) microspheres using meltable emulsified dispersion cooling induced solidification technique utilizing a wetting agent. Solid, discrete, reproducible free flowing microspheres were obtained. The yield of the microspheres was up to 94.0%. Microspheres had smooth surfaces, with free flowing and good packing properties, indicating that the obtained angle of repose, % Carr’s index and tapped density values were well within the limit. More than 97.0% of the isolated spherical microspheres were in the particle size range of 312-330 µm as confirmed by scanning electron microscopy (SEM) photographs. The drug loaded in microspheres was found to be stable and compatible with waxes as confirmed by DSC and FTIR studies. The release of drug was controlled for more than 8 h. Intestinal drug release from microspheres was studied and compared with the release behaviour of commercially available formulation Olanex®. The release kinetics followed different transport mechanisms. The drug release performance was greatly affected by the materials used in microsphere preparations, which allows absorption in the intestinal tract.
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Sustained release drug delivery system
Now a days as very few drugs are coming out of research and development and already existing drugs are suffering the problem of resistance due to their irrational use specifically in case of drugs like antibiotics. Hence, change in the operation is a suitable and optimized way to make the some drug more effective by slight alteration in the drug delivery. Sustained Release is also providing promising way to decrease the side effect of drug by preventing the fluctuation of the therapeutic concentration of the drug in the body. This article contains the basic information regarding sustained-release formulation and also the different types of the same.
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Formulation and evaluation of fast dissolving tablets of metoprolol tartrate by direct compression technique
The present investigation was undertaken with a view to develop a fast dissolving tablet of Metoprolol Tartrate which offers a new range of product having desired characteristics and intended benefits prepared by direct compression methodusing different concentrations of superdisintegrant. In the present work Fast dissolving tablets of metoprolol tartrate were prepared by direct compression super disintegrants such as sodium starch glycolate, croscarmellose sodium and crospovidone. All the tablets of metoprolol tartrate were subjected to weight variation, hardness, friability, in vitro dispersion, drug polymer interaction, drug content uniformity, and in vitro drug release The drug release from tablets of metoprolol tartrate prepared by direct compression was found to be 97.20% of D1 drug release within 10 minute. It is concluded that Metoprolol Tartrate fast dissolving tablets could be prepared using superdisintegrant with improved bioavailability and rapid onset of action.
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Influence of storage condition on the shelf life of amoxicillin tablets
Quality of pharmaceutical is of vital importance for patient safety. The loss of potency may influence the efficacy and safety of pharmaceuticals. This study determines the influence of storage conditions on the shelf life and potency of selected antibiotics. A significant statistical difference was observed across the potency data selected antibiotics brands. The data point out that maximum reduction in shelf life was observed at room temperature as compared with cool temperature. These results authenticated that improper storage conditions resulted in failure to meet product characteristic and specification during shelf life. Optimum storage conditions and procedures ensure that the potency and integrity of medicinal products are maintained throughout their shelf life.
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Formulation and evaluation of captopril Transdermal Patches
The present study comprises of an investigation of captopril a potent ACE inhibitors used orally to treat hypertension, as a feasible candidate for transdermal drug delivery. The present research work was undertaking to formulate a Transdermal drug delivery system of captopril, to investigate the effect of different penetration enhancers, and to study the in vitro permeation characteristics of the drug through the excised rat skin. In the present study, Transdermal patches of captopril were formulated using EC, PVA, PVP, PEG6000. All the formulation were used in combinations and penetration enhancers like DMSO, DMF, PG used in each groups. The effect of penetration enhancer in permeation through rat skin, revealed that DMF showed better result. In vitro skin permeation studies indicated that PVA: PEG6000 matrix type film may be fabricated in to effective system and DMF showed better result. The penetration enhancer DMF demonstrated the highest flux of 0.102 mg/cm2/hr and followed by PG 0.073 mg/cm2/hr from CE2 AND DE2 respectively.
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Pharmacological evaluation of Symplocos Racemosa bark extracts on experimentally induced ulceritis in rat model
Peptic ulcer disease (PUD) is chronic and appalling. Now-a-days it is the most prevalent disease affecting the world’s population. PUD is the main reason for morbidity and mortality in 50% of world’s working population. The pathophysiology of peptic ulcer disease is best viewed as an imbalance between mucosal defense factors (bicarbonate, mucin, prostaglandin, nitric oxide, and other peptides and growth factors) and injurious factors (acid and pepsin)3. Review of Literature suggests that the presence of tannins, flavonoids, Alkaloids, saponins, terpenoids, and steroids is responsible for antiulcerogenic activity. Preliminary Phytochemical investigation of aqueous and ethanolic extracts from bark powder of symplocos racemosa (SR) reveals the presence of tannins, carbohydrates, proteins, alkaloids and steroids .Hence the present study aims at pharmacological evaluation of anti ulcer activity of SR (symplocaceae) in experimentally induced (pylorus ligation and Aspirin-induced) ulcers in rat models. LD50 was found to be 2000mg/kg body weight, so, the therapeutic doses 250mg/kg and 500mg/kg were selected for both the extracts (alcoholic and ethanolic). Considering the parameters like pH , gastric volume, free acidity, total acidity and ulcer index (percentage protection) we concluded that aqueous extract 500mg/body weight was equipotent to the standard (lansoprazole-8mg/kg body weight). The same results was reflected by statistical analysis (one way ANOVA p<0.05) and histopathological study.
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