International Journal of Pharmaceutical Sciences and Drug Research

224-228

Authors: Nilesh Jain1*, Brahma P Gupta1, Navneet Thakur1, Ruchi Jain1, Jitendra Banweer1, Deepak Kumar Jain2, Surendra Jain1

The term “phyto” means plant while “some” means cell-like. Phytosomes are little cell like structure. This is advanced forms of herbal formulations which contains the bioactive phytoconsituents of herb extract surrounds and bound by a lipid. Most of the bioactive constituents of phytomedicines are water-soluble compounds like flavonoids, glycosides; terpenoids in which flavonoids are a major class of bioactive compounds possesses broad therapeutic activities. Because of water soluble herbal extract and lipophilic outer layer phytosomes shows better absorption and as a result produce better bioavailability and actions than the conventional herbal extracts containing dosage form. They are produced by a patented process whereby the standardized plant extract or its constituents are bound to phospholipids, mainly phosphatidylcholine, producing a lipid compatible molecular complex. This phyto-phospholipid complex (phytosome) resembles a little cell. Phytosomes exhibit better pharmacokinetic and pharmacodynamic profile than conventional herbal extracts. Phytosome technology has been effectively used to enhance the bioavailability of many popular herbal extracts including milk thistle, ginkgo biloba, grape seed, green tea, hawthorn, ginseng etc and can be developed for various therapeutic uses or dietary supplements.

236-246

Authors: Saurabh Srivastava1*, Garima Mishra2

Formulation development is the most emerging and upcoming face of pharmaceutical technology in the current era. It is contemporarily capturing the market leaps and bounds with recent trends and developments with its innovative techniques. The day-to-day advancements in the research have provided an edge to this brilliant branch of pharmaceutical sector for not only uplifting the pharmacy profession but also to conquer the diseased state for nurturing the health and humanity. The fluid-bed technology or air-suspension process is the potential tool to develop newer trends and implications in the sector of formulation development with maximum therapeutic efficacy. The technology is used for granulation/agglomeration, layering and coating of a wide range of particle size. In addition; the technique can be used for the drying process as well. The three patterns of the fluid-bed processes could be characterized by the position/location of the spray nozzle i.e. top spray, bottom spray or tangential spray. This article reviews the three techniques with some innovative fluid bed pelletizing technologies like CPS™, MicroPx™, ProCell™ and discusses their applications, advantages and limitations. These advanced pelletizing technologies are recentely added to complement the actual capabilities of standard fluid bed processing for development of various dosage forms of “Multiple Unit Particulate Systems” (MUPS) with better therapeutic efficacy and economic benefits.

254-260

Authors: Sinosh Skariyachan*, Rao Shruthi Krishnan, Usha B Biradar

E2F3 encodes a transcription factor important for cell cycle regulation and DNA replication. It plays a significant role in the development of various types of human cancer. Genomics and proteomics features of the tumor marker have a pronounced significance in the pharmainformatics studies. The crystal structure of E2F3 is not available in any structural database; hence a 3D structure is very essential for structural studies and discovery of potential inhibitors against tumour proteins. In this study we modelled a 3D structure of E2F3 by X-ray crystal structure of Bovine Bc1 with Azoxystrobin of Bos taurus (PDB ID: 1SQB, Chain B) used as the template. Our study found that E2F3 predominantly consists of α helix. The RMSD value of modelled protein was found to be 0.5 Ao and steriochemical validation shows 86. 1% residues are in allowed region of Ramachandran plot. Further validation was done by various empirical force fields. Overall quality factor of the model identified to be 57.36 and error values of individual residues are negligible. The modeled protein was submitted to Protein Model Database and can be downloaded with PMDID 0076554.With the help of docking studies the best ligand against E2F3 was found to be Vinblastine, an antitumor alkaloid isolated from Vinca rosea, with binding energy -4558.33.The ligand interacts with the modeled protein at residues Glu-432, Asp-433, Tyr-434, Leu-435 and 436.The other best inhibitors identified from our study were Oncovin, Navelbine, Taxol and Taxotere. The investigation concluded that these drugs could be used as the potential inhibitors against E2F3 tumor marker in prostate and breast cancer.

265-268

Authors: Vilas A. Arsul*, R. O. Ganjiwale, P. G. Yeole

Literature survey revealed that phyllanthin and hypophyllanthin from Phyllanthus niruri, wedenolactone from Eclipta alba, and kutkin from Picrorhiza kurroa are responsible for hepatoprotective activity, and phenolic and flavonoids are responsible for antioxidant activity. A selected polyherbal formulation composed of 7 herbal extract mixtures such as Phyllanthus niruri, Eclipta alba, Cichorium intybus, Boerhaavia diffusa, Embelia ribes, Berberis aristata and Picrorhiza kurroa. The phytochemical evaluation was carried out by estimation of total phenolic content and total flavonoids. The antioxidant activity was compared with ascorbic acid (ASC) and Rutin as standard. The hepatoprotective activity in carbon tetrachloride induced hepatotoxicity were studied. Assessment of liver function was made by estimating the activities of SGOT, SGPT, ALP, Cholesterol, Bilirubin and Total protein. From the study it is seen that formulation exhibit significant activity.

272-274

Authors: Nasir Hussaina*, Pooja Joshib, Amit Bhandarib, Rajaram Dangia, Rehana Khanamb, Ganpat L. Talesaraa

New tetra-dentate Schiff base N’, N”-1, 2-diphenylethane-1, 2-diylidenedibenzohydrazide (1) was synthesized by the condensation of benzil with isonizide. Further ligand (1) was converted into Cu (II) complex with N’, N”-1, 2-diphenylethane-1, 2-diylidenedibenzohydrazide (2) by treatment of (1) with CuCl2.2H2O and in another route Ni (II) complex with N’, N”-1, 2-diphenylethane-1, 2-diylidenedibenzohydrazide (3) was synthesized with reaction of (1) with NiSO4.7H2O. Polarographic studies of Cu (II) and Ni (II) complexes with ligand have been done in alcoholic medium and the stability constant log β values were found for Cu (II) and Ni (II) complexes Ligand and complexes were characterized by IR and 1HNMR, and complexes tested for biological activity.

278-280

Authors: P. Joshi, N. Pareek, D. Upadhyay, R. Khanam, A. Bhandari, RS Chauhan, AK Goswami*

The electrochemical behavior of complex of Cu (II) with 3-hydroxy-3-m-tolyl-1-p-(sulphonamido) phenyltriazene was studied. It was observed that HTSP forms 1:3 complex with Cu (II) in between pH 6.5 to 7.1. It was found that the reduction process of Cu (II) - HTSP complex is two electrons reversible reduction process at D.M.E. The logarithm value of stability constant of 1:3 Cu(II)-3-hydroxy-3-m-tolyl-1-p-(Sulphonamido) phenyltriazene complex has been found to be 11.63. The present paper also reports antifungal activity of hydroxytriazene 3-hydroxy-3-m-tolyl-1-(4-sulphonamidophenyl) triazene, and its Cu (II) complex against Rhizoctonia solani, the fungi causing disease in fennel. The result has been expressed as percentage inhibition (PI) of mycelial growth as well as sclerotium formation at 500 ppm for both ligand as well as complex. The result shows that PI value in complex is 87.03 whereas for ligand 79.63. Thus it is clear that complex is better in activity against the fungi compared to its respective ligand. The result has been interpreted in terms of theory of drug action proposed by Paton.

286-290

Authors: Abou Attia F. M.1, El-Dars F. M. S. E.2, El-Ries M. A.1, Mohamed O. I.2, Mohamed M. S.3*

A kinetic method for the accurate and sensitive determination of telithromycin has been described. The method is based on the oxidation of telithromycin with alkaline KMnO4. At a fixed time of 24 min. the formed magnate ion is spectrophotometrically measured at 610 nm. The concentration of telithromycin is calculated using the calibration equation for the fixed time and initial rate methods. Beer´s law was obeyed from 3.24-12.9µg ml-1 The assays limits of detection were 0.2-0.70µg ml-1 and the R.S.D. (n= 5) was 0.6 %. Recovery was 99.8 and 100.83%. The analytical performance of the, in terms of accuracy and precision, were statistically validated, the results were satisfactory RSD ≤ 2%. The method has been applied successfully to commercial tablet dosage form. Statistical comparison of the result with the reference method showed excellent agreement and proved that no significant difference in the accuracy and precision.

294-301

Authors: Rama Bukka*, Kalyani Prakasam, Chintan D Patel

The aim of the present work was to prepare and evaluate a buccal film for intraoral delivery of Rasagiline. Formulations were prepared using 32 full factorial design to explore the effects of carbopol P 940 and sodium alginate (as independent variables) on mucoadhesive strength and drug release (as dependent variables). In addition to the above, the prepared films were also evaluated for surface pH, percentage moisture absorption (PMA), Percentage moisture loss (PML), folding endurance and content uniformity. The release profile data was subjected to curve fitting analysis to describe the release mechanism from the buccal films. The main effects and the interaction terms were quantitatively evaluated by quadratic model. The Rasagiline release was decreased with increase in both the polymers. Carbopol has more pronounced effect than sodium alginate on the mucoadhesive strength. The objective of the study is to optimize formulation with desirable mucoadhesive strength and drug release. The experimented values are in good agreement with expected values for the optimized formulation which demonstrate the feasibility of the model in the development of buccal film.