INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES

1078-1085

Authors: Y. Prashanthi*

A novel approach has used for the development and validates a rapid, simple and an isocratic RP-HPLC method with PDA detector for the estimation of Lenvatinib drug in pharmaceutical drug dosage form. Lenvatinib was separated using YMC C 18, 4.6 X 150 mm, 5 µ analytical column, a Waters HPLC system and a mobile phase consists of water and methanol in the ratio of 30:70 % v/v, delivered at 0.6 ml/min with 20 µl injection volume. The detector wavelength was at 240 nm. The system suitability parameters for Lenvatinib drug such as theoretical plates and tailing factor were found to be 4384.4, 1.6 respectively. Linearity was established for Lenvatinib in the range of 20 – 100 µg/ml concentration levels with a correlation coefficient of (r2 ) 0.999. The repeatability and reproducibility precision values were found to be 0.75 and 0.31 % respectively. The accuracy values were found to be in the range of 98 – 102 %. The limits of detection and quantification values were 0.48 µg/ml and 1.46 µg/ml respectively. The method was validated for specificity, system suitability, precision, accuracy, LOD and LOQ parameters as per the ICH guidelines. This method can be used for the estimation and analysis of Lenvatinib drug in active pharmaceutical ingredients and pharmaceuticals. Keywords: Lenvatinib, Lenvima, High Performance Liquid Chromatography, Photo Diode Array detector, Estimation

1092-1095

Authors: Heba Ibrahim Abd El-Moaty

Aerial parts successive extraction of Taverniera lappacea demonstrated that the 70% methanol was the highest value (5.66%). It was have positive activity on all tested bacteria (Staphylococcus aureus, Streptococcus spp as bacterial gram positive bacteria), (Escherichia coli, Klebsiella pneumonia, Acinetobacter spp. as gram negative bacteria) and on fungal strain (Candida albicans). Investigation of the active extract (70% methanol) by using HPLC analysis revealed the presence of 22 flavonoid compounds at the aerial parts of the plant, with the major compounds; Apignin-6- glucose -8- rhamnose (227.59 mg/100g), luteolin-6- arabinose -8- glucose (103.91 mg/100g) and Kampferol-3,7-dirhamoside (57.776 mg/100g). Key Words: Taverniera lappacea, flavonoids, antimicrobial activity, HPLC.

1102-1109

Authors: Hady Keita*1,2 , Lucía Quevedo Corona2 , Eduardo Ramírez-San Juan2 , Norma Paniagua-Castro2

The murine model of streptozotocin-induced diabetes mellitus has been widely used for many authors. However, there are meaningful discrepancies about the functional alterations reported; especially regarding vascular response. Objective: The objective of the present study was to examine how the prolonged effects of diabetes mellitus induced by administering streptozotocin affects vascular reactivity, lipoperoxidation and endothelial function in aortic rings and if the administration of nicotinamide will partially protect those adverse outcomes. Performing parallel studies could contribute in part to clarify previous controversial results. Methods: Four groups (n= 8 rats per group) were used; control, control + Nicotinamide, streptozotocin or streptozotocin + Nicotinamide. Animals were euthanized after 20 weeks of streptozotocin and/or Nicotinamide administration. Glucose, lipoproteins plasma levels or lipid peroxidation in liver, heart and thoracic aorta were determined. Thoracic aorta was dissected and vascular reactivity to phenylephrine, isoproterenol, sodium nitroprusside or carbachol was determined. Results: Diabetic rats ingested more food and water, and lost more weight than control rats. The lipid peroxidation was higher in heart, liver and aorta in diabetic rats compared to control rats. In diabetic rats, total cholesterol, Low Density Lipoprotein and Triglyceride were higher and High Density Lipoprotein was lower than in control rats. The vasoconstrictor response to phenylephrine in streptozotocin groups was lower than streptozotocin + Nicotinamide and control groups. Diabetic animals showed a lower vasorelaxation response to carbachol and isoproterenol, but there was no significant difference in vascular response to sodium nitroprusside among groups. Conclusions: The prolonged effect of streptozotocin -induced diabetes increases chronically glycemia and alters vasodilator responses via different from the effect of oxidative stress. The partial protection with nicotinamide reduced vasomotor responses, suggesting that the artery is a major cause of the hypertensive status that characterizes the disease. Keywords: Diabetes; endothelial dysfunction, animal model.

1128-1138

Authors: Waheed M. Salem

Cilostazol is a drug used to treat the symptoms of intermittent claudicating, which is basically leg pain caused by walking. Thermogravimetry/derivative thermogravimetry and differential thermal analysis are useful techniques that have been successfully applied in the pharmaceutical industry to study the thermal degradation and kinetic parameters; activation energy (Ea), frequency factor (A), and reaction order (n), as regarding the physicochemical properties of drugs and excipient molecules, such as polymorphism, stability, purity, formulation compatibility, among others. The kinetic parameters were evaluated by isothermal and non-isothermal conditions including Ozawa’s conventional method, Ozawa–Flynn–Wall and Friedman isoconversional methods. The kinetic parameters were determined using the thermogravimetric curves of the decomposition process. The results of TG analysis revealed that the main thermal degradation for the Cilostazol occurs during two temperature ranges of 175–300 and 300–600 °C. The TG/DTA analysis of Cilostazol indicates that this drug melts (at about 160 °C) before it decompose. The results showed that as the heating rate was increased, decomposition temperatures of the compounds were increased. Also, the kinetic parameters such as activation energy values obtained were 162.2 and 163.12 kJ mol-1 for the isothermal and non-isothermal conditions, respectively. Finally, the values of ΔS # , ΔH # , and ΔG # of the decomposition reaction were calculated. Key words: Thermal decomposition, Cilostazol, isothermal

1147-1162

Authors: D.M. Ravichand

The elderly patients suffering from knee related problems should know the importance of usage of nutrient supplements and also selfcare activities which are inexpensive and at the same time are useful in overcoming the problems, especially pain. The study was aimed for determining the efficacy and safety of one such supplement namely Nutricharge BJ for regaining the knee joint health in the elderly population. The study was designed as a single centre, randomized, double blind, placebo controlled trial to evaluate the efficacy and safety. The study subjects had undergone physical findings on examination of the knee, Short-Form McGill Pain Questionnaire-2 (SF-MPQ-2), Pain Visual Analog Scale, Western Ontario and McMaster Universities Osteoarthritis Index (WOMAC) and pain scale and self-assessment questionnaire both before and after a treatment period for assessing the safety and efficacy of Nutricharge BJ. It was observed that a reduction of 57.5% in SF-MPQ2 pain scores occurred in the Nutricharge BJ Group and was highly statistically significant. TheWOMAC scores in the Nutricharge BJ group, when compared to placebo Group were found to be 73.7%. It was found that the difference in reduction in WOMAC pain scores between the two groups over a period of the 90-days was highly significant (P<0.0001).The Pain Scale function scores before and after the period of follow-up showed significant reduction in pain (87.3%) between the two groups.In pain visual analogue scale and patient assessment questionnaire, a reduction of 53.6% and 54.1% was observed respectively in Nutricharge BJ group and was significant. The Nutricharge BJ supplement significantly aids in improving the physical function, activity and above all the quality of life in the elderly population. It was observed that there was no adverse drug reactions were reported during the study period and thus showing the product-Nutricharge BJ is safe for human consumption. Keywords:Knee Joint, WOMAC™, Nutrition Supplement, BUA

1172-1181

Authors: K. Rekha Rani

The objective of the presentreserach work was to formulate bioadhesive microspheres of Voriconazole using different polymers Eudragit RS 100, Ethyl Celulose, Sodium alginate were formulated to deliver Voriconazole via oral route.Increase in the polymer concentration led to increase in % Yield, % Drug entrapment efficiency, Particle size. The invitro drug release decreased with increase in the polymer.Analysis of drug release mechanism showed that the drug release from the formulations followed diffusion and the best fit model was found to be Korsmeyer-Peppas.FT-IR studies were carried out to find out the possible interaction between the selected drugs and polymer. FT-IR studies revealed that there was no interaction between the selected drugs and polymer. Among the different batches, Formulation F6 was selected as the ideal formulations, after considering their mean particle size, free flowing nature, better drug loading capacity, and in vitro drug release. The % drug release microspheres was found to be 97.65%. Keywords: Voriconozole,Microspheres

1186-1190

Authors: Gh. Hassan Bhat1 , Mushtaq Ahmed Parray* 2 , Ghulam Mohammad Jan3

Boswellia in the family Burseraceae, particularly Boswellia sacra (syn: B. carteri, B. thurifera, B. bhaw-dajiana), B. frereana and B. serrata (Indian frankincense.). Frankincense resin is edible and is used in traditional medicines in Africa and Asia for digestion and healthy skin. For internal consumption, it is recommended that frankincense be translucent, with no black or brown impurities. Exposure to 11-keto-β-boswellic acid (KBA), a lead boswellic acid in the novel solubilized frankincense extract Boswelan, is increased when taken with food. Keywords: Burseraceae, resin, traditional medicines, translucent, boswellic acid

1196-1202

Authors: Vinay Sharma* 1 , Jyoti Saxena2 ,

Lipases catalyze hydrolysis of fat/lipid into their components. Microbial lipases are preferred than the animal and plant lipases because of their stability, specificity and unique properties. Microbial lipases are excreted by a variety of bacteria, fungi and yeasts. Lipases are used in various industries (pharmaceutical, food, detergent, oil, paper etc). At present the demand of industries for lipases are very higher, therefore we have to increase the production of enzyme form indigenous microbial strains in order to fulfill the various applications in industries. Normally microbial strain produces little amount of lipases to meet the cellular requirements but for the industrial purposes, the amount of lipases can be enhanced by the optimization technique. Different parameters (carbon sources, nitrogen sources, pH, temperature and incubation period) can be optimized in order to increase productivity of lipase. Lipase production is normally stimulated in presence of lipidic carbon sources (oil) into the culture media, which indicates the inducible nature of microbial lipases. By keeping the above points in mind, the present review is focused on optimization of culture medium constituents and growth conditions for increased growth of lipolytic fungi and productivity of extracellular lipase. Keywords: Lipases, microbial strains, optimization technique, lipolytic fungi, pH, temperature, carbon source

1210-1222

Authors: Marwa A.Omran

Voltammetric behavior of dantrolene sodium (Dan) was comparatively investigated in Britton Robinson (BR) buffer as electrolyte at pencil graphite (PGE) and glassy carbon (GCE) electrodes, cyclic voltammetry (CV) gave one reversible cathodic anodic peak at -0.302, -0.249 V at PGE and -0.257, -0.178 V at GCE respectively and another irreversible cathodic one at -0.748 at PGE and -0.694 V at GCE. Differential pulse (DPV) and square wave (SWV) voltammetry were investigated for the reversible cathodic peak and gave at PGE, linearity range from 0.395-2.955 and 0.395-1.9 µg/mL with correlation coefficient 0.999 for both, LOD 0.09 and 0.052µg/mL, LOQ 0.273 and 0.158 µg/mL, respectively and at GCE, linearity range from 0.974- 2.44 and 0.199- 2.96 µg/mL with correlation coefficient 0.999 for both, LOD 0.167 and 0.095 µg/mL, LOQ 0.507 and 0.289 µg/mL, respectively. The proposed procedures were successfully applied to the determination of Dan with good recovery in pharmaceutical dosage form, human mother milk and urine directly without any pretreatment at both electrodes. The techniques were validated and revealed good accuracy and reproducible results. Keywords: Dantrolene Sodium, Biological fluids, pencil graphite electrode, glassy carbon electrode, Pharmaceuticals, Voltammetry.

1237-1250

Authors: Vinod Varmaan1, 2, Yuawa Rani1 and VasudevaRao Avupati

The predominance of multifactorial diseases has become an epidemic in the tropical and sub-tropical areas all over the world. According to the reports of the World Health Organization (WHO), around 250 million people are currently living with diabetes and this number is expected to be more than 366 million by 2030. Although, there are a number of naturally occurring and synthetic agents (glitazones) that activate PPARγ, the identity of the true natural ligand of this receptor is still unknown; this may be the reason for their lethal side effects. In silico virtual screening has presently become an integral part of contemporary drug research. A variety of computational tools are being developed and refined to effectively employ fast screening methods to yield potent hits. In recent past, an explosive growth in the successful applications employing a wide range of methods, such as molecular docking, pharmacophore modelling, etc. Efforts are also being made to employ the drug likeliness of a given compound. Hence in the present investigation, it was hypothesized worthwhile to discover a new prototype of molecule to facilitate our search for novel PPARγ agonists by using computer aided molecular docking studies. In conclusion, we could identify the potential ligands 4, 16 and 22 with predicted PPPAγ ligand binding domain agonistic activity equal to 0.1 μg/mL. Keywords: Diabetes mellitus (DM), PPARγ, In silico, Virtual screening

1264-1270

Authors: Mamillapalli Vani*1, AbdulRahaman2 , Avula Prameela Rani 3

The present study has been conducted to evaluate the antiasthmatic potential from the inflorescence extracts of Gomphrena serrata. to validate its traditional use. The antiasthmatic activity of hydroalcoholic and acetone extracts was studied by two models histamine and acetyl choline induced bronchospasm in guinea pigs and histamine and acetyl choline induced contraction on isolated guinea pig ileum. The preconvulsive time at a dose of 400mg/Kg in guinea pigs and inhibition of contractions on guinea pig ileum at a concentration of 0.5mg were investigated and compared with the control groups. Phytochemical studies revealed the presence of flavonoids, phenolics, steroids, triterpenoids. The extracts have significantly reduced the bronchospasm induced by histamine and acetylcholine, as well as the contractions of ileum. Therefore the present study concludes that the hydroalcoholic and acetone extracts of Gomphrena serrata exhibited antiasthmatic activity which may be due to phytochemical substances probably causing suppression of antibody production or inhibition of antigen induced histamine and acetylcholine. Key words: Gomphrena serrata, asthma, bronchospasm, histamine, acetylcholine

1276-1282

Authors: Kanika Nayak*, Manoj Kumar Mishra, Garima Verma

Convenience of administration and patient compliance are gaining significant importance in the design of dosage forms. Glibenclamide is an orally administered antihyperglycemic agent, used in the management of non-insulindependant (type-2) diabetes mellitus. Difficulty in swallowing (dysphagia) is common among all age groups, especially in elderly and pediatrics. Persons suffering from dysphagia may get choked when they consume liquid formulations, thus to alleviate such problem liquid formulation of high viscosity were prepared. Formulation of oral soft gel (batches of Glibenclamide) were prepared by using hydrophilic polymer guar gum at concentration ranging from 0.3-0.5% w/v and pectin at two different concentrations (0.2% and 0.3% w/v). The batch with 0.5% w/v guar gum and 0.2%w/v pectin not only showed 85% drug release after 1h. The prepared batches were evaluated for appearance, viscosity, pH, drug content, syneresis and in vitro drug release. The optimized batch showed substantial stability when subjected to short term stability study (0-8°C and at room temperature). The problem of dose measurement by patients was outweighed as oral medicated gels are to be packed in unit dose container. Keywords: Diabetes mellitus, Jelly, Dysphagia, Glibenclamide.

1291-1296

Authors: Diana Laila Ramatillah

Introduction: Chronic Kidney Disease (CKD) is a condition of reducing renal function in excreting metabolism residual. Dietary habit, using of drugs in a long time, losing of body fluid, infection, a complication of disease and family history are the factors of end-stage renal disease (ESRD), while ESRD becomes one of the largest public health problems in the world. Objective : To evaluate the complication of disease and risk of death in chronic kidney disease (CKD) non-hemodialysis patients. Method : literature review about studies that reported the risk of death from CKD. The accumulated risk is calculated using the ratio of confidence for the method of random effects meta-analysis of the data medium quality and high quality. Results : Atherosclerosis is increased in CKD patients. It is known from Zahran, M.et.al study whereas they did research about risk factor of atherosclerosis by measuring Carotid Intima-Media Thickness (CIMT) for all subjects. Besides that, CKD changes the metabolism of vitamin D which is one of the most important factors in the pathogenesis of secondary hyperparathyroidism and chronic kidney disease-mineral bone disorder (CKD_MBD). Chronic kidney disease patients also cannot produce Erythropoietin Stimulating Agent (ESA) like normal patients, so it causes anemia. Diabetes mellitus, hypokalemia, and hyperkalemia also found in CKD patients.There are some complications of chronic kidney disease: cardiovascular disease, deficiency vitamin D, diabetes mellitus type II, hypokalemia, hyperkalemia, and anemia. Conclusion : These complications will be a risk of death factors on CKD patients if the patients are not handled well. Keywords: Chronic Kidney Disease, Risk of Death, Complications , Non-Hemodialysis, Anemia, Diabetes Mellitus

1309-1314

Authors: Palak1 , Kriti Soni2 , and Kanchan Kohli

Broccoli contains sulforaphane, an isothiocyanate which is formed by the action of myrosinase enzyme on glucoraphanin. This sulforaphane has anticancer properties and can also help in treating many diseases like kidney disorders, skin diseases etc. The present paper highlights the development of UV and TLC method, which will be used in further research. The paper highlights the development of UV method in three media namelyDistilled water, phosphate buffer 7.4 and HCl buffer 2.3. This paper also highlights the Development of TLC method for the identification of sulforaphane in Broccoli extract. Key words: Broccoli, sulforaphane and glucoraphanin