Posted by admin on Jul 31, 2015 in |
A new series of s- triazine based chalcones have been synthesized by the temperature controlled reaction. The first substitution occurs at low temperatures (0°C), the second substitution at approximately at room temperature (25-30°C) and the third at elevated temperatures (70-100°C). This property allows substitution of three different neucleophiles onto the same triazine core which provides a vast array of possible triazine...
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Posted by admin on Jul 31, 2015 in |
Currently there has been an increased interest in using iontophoretic technique for the controlled transdermal drug delivery of medicines, especially in the delivery of proteins & peptides through skin membranes. The delivery of ionic drug molecules and peptide/protein molecules through transdermal delivery to attain a systemic therapeutic effect, chemical or physical methods are needed to improve the rate of penetration of therapeutic drug molecule through the main diffusion barrier present in the skin membrane. In that, the iontophoretic technique is one of the most desirable to enhance the transdermal drug delivery of high molecular weight substances like peptide and proteins using a lower current intensity with a short time period for the desired therapeutic effect. This article is an complete overview of the controlled transdermal drug delivery of ions/proteins/peptides by iontophoresis as well as the principles, laws, mechanisms, factors, design considerations, applications, advantages, limitations of transdermal iontophoretic drug delivery...
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Posted by admin on Jul 31, 2015 in |
The oral route is easiest and most convenient route for drug administration. The major problem in oral drug formulations is low and erratic bioavailability, which mainly results from poor water solubility. This may leads to higher inter subject and intra subject variability and therapeutic failure. The improvement of compounds solubility and bioavailability are the greatest challenges in formulations. The self emulsifying drug delivery system (SEDDS) is a novel approach for enhancing the solubility of formulations; by this approach it is also possible to prolong the release of drug via incorporation of polymers in SEDDS composition which appears to be unique and industrially feasible approach. The SEDDS is an isotropic mixture of oils, surfactants, co-surfactants, co-solvents, etc. It can be used for designing the formulations such as tablets, capsules, pellets, etc. The SEDDS will continue to enable novel applications in drug delivery and solve problems associated with the delivery of poorly soluble...
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Posted by admin on Jul 31, 2015 in |
Combination drug therapy has been shown to be beneficial in chronic multifactorial diseases, infectious diseases and in the treatment of comorbid conditions. Some drug combinations have also been developed to improve the bioavailability of the active components by combining with drug metabolizing enzyme inhibitors. Fixed dose combinations (FDC) offer advantages of better efficacy, ease of administration and patient compliance, while combination therapy generally improves efficacy. For the development of FDCs the primary consideration is the approval status of the drugs to be combined to develop an appropriate strategy. Subsequently, the dose strengths of the individual components need to be considered to be able to allow flexibility of dosing. In order to successfully develop FDC products, demonstration of bioequivalence (BE) to the individual free combinations and lack of pharmacokinetic/pharmacodynamic (PK/PD) drug interaction are essential. Therefore, the development of FDCs requires a good understanding of the biopharmaceutical properties, drug pharmacokinetics and their metabolic pathways. The formulation development program involves pilot stage program followed by registration BE studies with a requirement for...
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Posted by admin on Jul 31, 2015 in |
Penicillin antibiotics have been the main-stay armamentarium in the fight against bacterial diseases due to their availability and ease of use. Penicillin resistance has been attributed to modification of penicillin-binding proteins, production of β-lactamases, overexpression of efflux pumps and reduced permeability. In the past 10 years, research was centred on Gram-positive bacteria, particularly Methicillin-Resistant Staphylococcus aureus (MRSA). The key determinant of resistance in MRSA strains is the penicillin-binding protein (PBP2a). Currently, the production of β-lactamases by Gram-negative bacteria has garnered a degree of attention that seems to be rising rapidly. Gram-negative bacteria pose the greatest risk to public health because of the global emergence and spread of metallo-β-lactamases, including Imipenemase (IMP-types), Verona integrin-encoded-metallo-β–lactamases (VIM-types) and New Delhi metallo-β-lactamases (NDM-types). Not only is the increase in resistance of Gram-negative bacteria to beta-lactams faster than in Gram-positive bacteria, but also there are no current and developmental antibiotics active against metallo-β-lactamase-producing Gram-negative bacteria. This review critically examines the current issues in beta-lactamases responsible for penicillins resistance in relation to the current clinically...
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