INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES

682-692

Authors: Ganesh Kumar Bhatt* Amit Upreti, Preeti Kothiyal

Transdermal drug delivery system are topically applied medication which is used to deliver the specific dose of drug direct entry into systemic circulation after passing through the skin barrier, and it avoid first pass effect. Transdermal patches deliver the drug for systemic effect at a predetermined and control rate through diffusion process. Transdermal drug technology specialists are continuing to search for new methods that can effectively and painlessly deliver large molecule in therapeutic quantities to overcome the difficulties associated with oral route, like poor bioavailability, first pass metabolism and sometime responsible for rapid blood level. The present study was carried out to develop transdermal patches of Rivastigmine with different ratio of HPMC (hydroxyl propyl methyl cellulose) and EC (ethyl cellulose) by solvent casting method. Propylene glycol 3% is used as a plasticizer and Span 80 as permeation enhancer. Formulated transdermal patches were evaluated with regard to physicochemical characteristics (thickness, folding endurance etc.) and In-vitro permeation studies were performed using Franz diffusion cell. The data obtained from in- vitro permeation studies was treated by various conventional mathematical models (zero order, first order, Higuchi and Korsmeyer- Peppa’s) to determine the release mechanism from the transdermal patches formulations. Selection of a suitable release model was based on the values of R2 (correlation coefficient), k (release constant) obtained from the curve fitting of release data. It was found that all the formulations follow the first order kinetics. The regression coefficients (R2 ) for the all formulations F1 to F4 of Higuchi plot was found to be almost linear. All prepared four Formulations, F1 showed maximum in vitro drug release. So, in general it was concluded that transdermal formulation prepared with HPMC (1:2) was the formula of choice as it showed better drug release. Keywords: Transdermal patch, Bioavailability, blood circulation.

693-705

Authors: A. B. Wadekar*, D.T.Tayde

Abstract: The present work deals with the study of proton -ligands and metal- ligands stability constant of 5-p-chlorophenylthiocarbamido-1-naphthol and 5-p-tolylthiocarbamido-1-naphthol with Cu (II), Cd(II) and Cr(III) metal ions at 0.1 M ionic strength in 70 % ethanol-water mixture by Irving–Rossotti titration technique. 5-p-chlorophenylthiocarbamido -naphthol and 5-p-tolylthiocarbamido-1-naphthol form 1:1 complexes by interacting with Cu(II), Cd(II) and Cr(III) metal ions were found in present work. The values of proton-ligand stability constant (pK) and metal-ligand stability constants (log k) were evaluate and compared from resultant data. The effect of substituents were also studied from resultant estimated data on pK and log K. Keywords: 5-p-chlorophenylthiocarbamido-1-naphthol, 5-p-Tolylthiocarbamido -1-naphthol, stability constant, pH-metry.

713-727

Authors: Preeti Pokhariya *, G Ganarajan and Preeti Kothiyal

The aim of this research is to prepare and evaluate the Mouth dissolving tablet of Telmisartan introducing the use of newly arising natural excipient as a superdisintegrants .The applied Naturat superdisintegrants(chitosan and gellan gum) has versatile property in the Mouth disintegrating tablets using Telmisartan as model drug. Mouth disintegrating tablets are the useful formulations for pediatrics, geriatric, and physically and mentally disabeled patients resulting in improved patient compliance. Telmisartan is an antihypertensive drug which belongs to the class of Angiotensin Receptor ΙΙ (Type- ATΙ) Antagonist. It is a poorly soluble drug (BCS class-II) and its absorption is dissolution rate limited. The oral bioavailability of Telmisartan is 45%. Hence, in this research an attempt was made to develop Mouth dissolving tablets of Telmisartan formulated with natural disintegrating agent and superdisintegrants(synthetic) combination with superior dissolution properties. The aim is to formulate various batches of mouth dissolving tablets of Telmisartan by using chitosan, gellan gum, microcrystalline cellulose, crospovidone and sodium starch glycolate with different concentrations by direct compression. The tablets were evaluated for the precompression parameters such as bulk density, compressibility, angle of repose etc and post compression parameters like hardness, weight variation, friability, disintegration time and in-vitro dissolution profiles . Among all the 5 formulation F4 is the best formulation because it show the high percentage of drug release in which was found to be 96.13% in 120 min and disintegration time was found to be 20 sec, as well as F4 formulation show the best results in every evaluation aspects. Key words: Telmisartan, chitosan, gellan gum, cross povidone, micro crystalline cellulose, sodium starch glycolate, Mouth dissolving tablets.

738-749

Authors: Narender Boggula*, Ridhika M Patel, Akhil Rapolu, Pramod Kumar Bandari, Krishna Mohan Chinnala

Benzoxazole and its derivatives are important class of bioactive molecules, their importance is due to their versatile application in the field of drugs and pharmaceuticals as well as in chemical systems. It finds use in research as a starting material for the synthesis of larger, usually bioactive structures. A new series of Benzoxazol-2-ylthio-N’-(4-substituted) acetohydrazide derivatives (IV a-k), were obtained by synthesising new schiff’s bases derived from benzoxolyl-2-mercaptoacetohydrazide derivatives by treating with various aryl/hetero aryl aldehydes. Their chemical structures have been confirmed by 1H-NMR, 13C-NMR, FT-IR and Mass spectral data. The synthesised derivatives (IV a-k) were screened for their in-vitro anti bacterial activities by agar diffusion method. Among the synthesized derivatives IVb, IVe, IVk, IVi showed significant antibacterial activity. Key Words: Benzoxazole, heterocyclic compounds, aryl/hetero aryl aldehydes, schiff’s bases, anti bacterial activity.

756-758

Authors: Jasmin Elizabeth Thomas1*, Merin Joseph1, Elizabeth Phoeba Paul1, Apollo James2, T Sivakumar3

Steven Johnson Syndrome (SJS) presents as severe mucosal erosions with widespread erythematous and cutaneous macules all over the body. Majority of the cases are drug induced. NSAIDs, antimicrobials, anti-convulsants causes SJS. Adverse drug reactions are one of the leading causes of hospitalisation. At this point, we present a case of Steven Johnson Syndrome induced by two anti-epileptic drugs i.e. Phenytoin and Phenobarbitone which is rare. Keywords : Phenytoin, Phenobarbitone, Steven Johnson Syndrome.

767-772

Authors: Kirtimaya Mishra*, B. Kiran Kumar , M. Muthu Kumari , B. S. S. Subrahmanyam

A simple UV-Visible Spectrophotometric method was developed for the determination of chlorpheniramine maleate in pure and its pharmaceutical formulations. chlorpheniramine maleate exhibited maximum absorption at 262nm in 0.1N HCl and obeyed linearity in the concentration range of 10-60 μg/ml. The proposed method was statistically validated.All the proposed methods are simple, selective, reproducible, sensitive and accurate with good precision. Some of the methods were proved to be superior to most of the reported methods. All these proposed methods for estimation of selected drugs such as chlorpheniramine maleate were successfully applied either in bulk or pharmaceutical formulations. The proposed methods can be used as alternative methods to the reported ones for the routine determination of selected drugs under the study in bulk and pharmaceutical dosage forms. Keywords: chlorpheniramine maleate, UV-Visible Spectrophotometer, Hydrochloric acid.