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Floating bioadhesive drug delivery system using novel effervescent agents
Belgamwar V,Surana S
Asian Journal of Pharmaceutics , 2009,
Abstract: Oral sustained release gastroretentive dosage forms offer many advantages for drugs having absorption from the upper gastrointestinal tract and improve the bioavailability of medications that are characterized by the narrow absorption window. A new gastroretentive sustained release delivery system using the novel effervescent system was developed with floating, swellable, and bioadhesive properties. Various release retarding polymers like psyllium husk, HPMC K15M, and a swelling agent crosspovidone in different combinations were tried and optimized to get the release profile for 12hours. The formulations were evaluated for physicochemical characteristics, in vitro drug release profile, swelling characteristics, floating capacity, and in vitro bioadhesive property. i0 n vitro drug release followed the Higuchi kinetics and the release mechanism was found to be of a non-Fickian type. The swelling properties were increased with increasing crosspovidone concentration and contributed to the drug release from the tablet matrix. In this study, an attempt has been made to explore novel effervescent agents such as citroglycine and disodium glycine carbonate for achieving the desired floating time.
Topical delivery of flurbiprofen from pluronic lecithin organogel
Pandey M,Belgamwar V,Surana S
Indian Journal of Pharmaceutical Sciences , 2009,
Abstract: The purpose of this research is to formulate and evaluate the suitability of pluronic lecithin organogels containing flurbiprofen for topical application. Four formulations were developed using flurbiprofen, lecithin, Pluronic F127, isopropyl palmitate, water, sorbic acid and potassium sorbate were coded as FL1, FL2, FL3 and FL4. All the formulations carried 30% w/w of lecithin phase and 70% w/w of Pluronic phase. The formulated organogels were evaluated for appearance and feel psychorheologically, in vitro diffusion study, drug content, viscosity and pH. Release of flurbiprofen from all formulations was monitored via dialysis membrane-70 and Wistar rat skin as a semipermeable membrane into phosphate buffer saline (0.2 M, pH 7.4) using Keshary-Chien diffusion cell. The viscosities of different formulations were determined by using Brookfield Viscometer at 25°. An attempt has been made to explore the potential of pluronic lecithin organogels for topical delivery of flurbiprofen.
Formulation design and optimization of taste-masked mouth-dissolving tablets of Tramadol hydrochloride
Patel K,Shete S,Belgamwar V,Tekade A
Asian Journal of Pharmaceutics , 2010,
Abstract: The aim of the present study was to mask the extremely bitter taste of Tramadol HCL, an opioid analgesic, and to formulate a tablet which can rapidly disintegrate in saliva (rapidly disintegrating tablet). The crucial aspect in the formulation of mouth-dissolving tablets is to mask the bitter taste and to minimize the disintegration time. Taste masking was done using sweetening agent and D-mannitol and taste-masked pellets were prepared by extrusion spheronization technique. Prepared pellets were tested for drug content, taste evaluation in oral cavity and molecular property. Pellet shows significant taste masking, confirmed by in vitro taste evaluation; therefore, it was selected for further study. Pellets were evaluated for density, angle of repose, Carr′s index, Hausner′s ratio and sphericity while tablets were evaluated for disintegration and in vitro dissolution. A 3 2 full factorial design and statistical models were applied to optimize the effect of two factors, i.e. superdisintegrant sodium starch glycolate and taste-masking agent (D-mannitol). In this study, response surface methodology was used for designing of the experiment, generation of mathematical models and optimization study. Taste evaluation of pellets in human volunteers revealed considerable taste masking with a degree of bitterness below threshold value (2.0) within 10 s, whereas Tramadol HCl was rated intensely bitter with a score of +4 for 10 s. The size of the pellets varied from 0.895 to 1.423 mm for different batch and found to be a spherical. Disintegration time of different formulations varied from 30 to 60 s. It was observed that the responses, i.e. disintegration time and sphericity were affected by both the factors. The statistical models were validated and can be successfully used to prepare optimized taste-masked mouth-dissolving tablets of Tramadol HCl with adequate disintegration and shape.
Pluronic lecithin organogel
Belgamwar Veena,Pandey Mohit,Chauk Dhiraj,Surana Sanjay
Asian Journal of Pharmaceutics , 2008,
Abstract: The purpose of this review is to give detail insight of pluronic lecithin organogels (PLOs) as a topical and transdermal drug delivery system. Pluronic lecithin organogel is a microemulsion-based gel that has been effectively used by physicians and pharmacists to deliver hydrophilic and lipophilic drugs topically and transdermally across the stratum corneum. It is thermodynamically stable, viscoelastic, and biocompatible gel composed of phospholipids (lecithin), organic solvent, and polar solvent. Various types of therapeutic agents have been easily incorporated in PLO to improve their topical drug delivery. Pluronic lecithin organogel improves the topical administration of drug mainly because of desired drug partitioning, biphasic drug solubility, and the modification of skin barrier system by organogel components. Beside this, it shows low skin irritation, increases patient compliance, reduces side effects, avoids first pass metabolism, and increases efficiency of drug. In addition, PLO has been shown in vivo and in vitro to modulate the release and permeation of drugs applied transdermally. Thus, in future, it has wide range of applications and opportunities to experiment with various drugs in this type of drug delivery system.
Pulsatile drug delivery system
Belgamwar Veena,Gaikwad Madhuri,Patil Ganesh,Surana Sanjay
Asian Journal of Pharmaceutics , 2008,
Abstract: Pulsatile drug delivery system is the most interesting time- and site-specific system. This system is designed for chronopharmacotherapy which is based on circadian rhythm. The principle rationale for the use of pulsatile release is for the drugs where a constant drug release, i.e., a zero-order release is not desired. Pulsatile drug delivery system is defined as the rapid and transient release of certain amount of molecules within a short time period immediately after a predetermined off-release period, i.e., lag time. Various systems like capsular systems, osmotic systems, pulsatile system based on the use of soluble or erodible polymer coating, use of rupturable membranes and pulsatile system based on membrane permeability are summarized in this article. These systems are beneficial for the drugs having chronopharmacological behavior where night time dosing is required and for the drugs having high first-pass effect and having specific site of absorption in gastrointestinal tract.
Solubility Enhancement of Raloxifene Using Inclusion Complexes and Cogrinding Method
Payal H. Patil,Veena S. Belgamwar,Pratibha R. Patil,Sanjay J. Surana
Journal of Pharmaceutics , 2013, DOI: 10.1155/2013/527380
Abstract: The objective of the present work was to enhance the solubility and dissolution of practically water-insoluble drug raloxifene HCl (RLX), for the same two approaches that were used. In the first approach, drug was kneaded with hydroxypropyl-β-cyclodextrin (HPβCD), and in the second one drug was cogrinded with modified guar gum (MGG). The drug-cyclodextrin complex and drug-MGG cogrind mixtures were characterized by differential scanning calorimetry, X-ray diffraction studies, scanning electron microscopy, and Fourier transform infrared spectroscopy. The solubility and dissolution study reveals that solubility and dissolution rate of RLX remarkably increased in both methods. It was concluded that the prepared inclusion complex showed a remarkable increase in solubility and dissolution of poorly water-soluble drug raloxifene. In the cogrinding mixture, a natural modified gum is used as a surfactant and enhances the solubility and dissolution of RLX without requiring addition of organic solvent or high temperature for its preparation; thus, process is less cumbersome and cost effective. But when both methods were compared; HPβCD complexation method showed significant enhancement of drug solubility. 1. Introduction Solubility of a drug is an important property that mainly influences the extent of oral bioavailability. Enhancement of oral bioavailability of poorly water soluble drugs is the most challenging aspect of drug development [1]. Most of the new chemical entities suffer from low bioavailability due to their low aqueous solubility and dissolution. Therefore, it is very important to find appropriate formulation approaches to improve aqueous solubility and bioavailability of poorly aqueous soluble drugs [2]. Raloxifene (marketed as Evista by Eli Lilly and Company) is an oral second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It is 2-(4-hydroxyphenyl)-3-({4-[2-(piperidin-1-yl) ethoxy] phenyl} carbonyl)-1-benzothiophen-6-ol that has estrogenic actions on bone and antiestrogenic actions on the uterus and breast. It belongs to class II drug according to biopharmaceutical classification system (BCS), that is, low solubility and high permeability. But raloxifene has very less bioavailability, only 2%, and it would be advantageous to increase the solubility of such molecule. Raloxifene is available in salt form as raloxifene HCl [3]. The drug is poorly absorbed from the gastrointestinal (GI) tract therefore; it is important to enhance aqueous solubility and dissolution rate which may lead to
Nonsmooth Optimization Algorithms in Some Problems of Fracture Dynamics  [PDF]
V. V. Zozulya
Intelligent Information Management (IIM) , 2010, DOI: 10.4236/iim.2010.211073
Abstract: Mathematical statement of elastodynamic contact problem for cracked body with considering unilateral restrictions and friction of the crack faces is done in classical and weak forms. Different variational formulations of unilateral contact problems with friction based on boundary variational principle are considered. Nonsmooth optimization algorithms of Udzawa’s type for solution of unilateral contact problem with friction have been developed. Convergence of the proposed algorithms has been studied numerically.
Precessing Ball Solitons as Self-Organizing Systems during a Phase Transition in a Ferromagnet  [PDF]
V. V. Nietz
Applied Mathematics (AM) , 2013, DOI: 10.4236/am.2013.410A3010
Abstract:

Precessing ball solitons (PBS) in a ferromagnet during the first order phase transition is induced by a magnetic field directed along the axis of anisotropy, while the action of the periodic field perpendicular to the main magnetic field has been analyzed. Under these conditions, the characteristics of arising equilibrium PBS are uniquely determined by the frequency of the periodic field, but the solitons with other frequencies are impossible. For such structure, the entropy increase connected with dissipation is compensated by the decrease of the entropy due to the external periodic field. It is shown that the equilibrium PBS are essentially the “self-organizing systems” that can arise spotaneously in a metastable state of ferromagnet.

Movement of Self-Organizing Solitons in Ferromagnet  [PDF]
V. V. Nietz
Applied Mathematics (AM) , 2015, DOI: 10.4236/am.2015.610155
Abstract: Precessing ball solitons (PBS) in a ferromagnet during the first order phase transition induced by a magnetic field directed along the axis of anisotropy, while the additional action of high-frequency field perpendicular to the main magnetic field, are analyzed. It is shown that the spatial motion of solitons, associated with thermal fluctuations in the crystal, does not destroy the equilibrium of self-organized PBS.
Lα Line of Dark Positronium as a Nongravitational Detection of DM  [PDF]
V. Burdyuzha, V. Charugin
Journal of Modern Physics (JMP) , 2015, DOI: 10.4236/jmp.2015.613187
Abstract: An attempt to predict the new atomic dark matter lines is done on the example of a dark lepton atom-positronium. Its Layman-alpha line with the energy near 3 GeV may be observable if the appropriate conditions are realized. For this we have studied a γ-ray excess in the center of our galaxy. In principle, this excess may be produced by the Lα line of a dark positronium in the medium with Compton scattering. The possibility of observations of an annihilation line (E~300 TeV) of dark positronium is also predicted. Other proposals to observe the atomic dark matter are shortly described. Besides, Hα line (1.3μ) of usual positronum must be observable in the direction on the center of our galaxy.
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