Journal of Pharmaceutical Technology, Research and Management
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Synthesis and Pharmacological Evaluation of Some Novel Imidazole Derivatives for Their Potential Anti-hypertensive Activity
Get PDFBenzimidazole, which is a heterocyclic nucleus, plays an important role in various medicines. A number of therapeutic agents such as H1 antihistaminic agent clemizole, a potent opioid analgesic etonitazene, nonnucleoside antiviral compound enviroxime, for promotion of excretion of uric acid irtemazole, non sedating antihistaminic agent astemizole, anti ulcer drugs omeprazole and pentoprazole, antihelmintic thiabendazole, antinematodal nocodazole etc. are based on benzimidazole heterocyclic nucleus. The synthesis of various benzimidazole derivatives by the reaction of ortho phenylene diamine I with various organic acids to yield 2-substituted benzimidazole derivatives II which on further treatment with nitric acid and sulphuric acid yielded 5-nitro-2-substituted benzimdazoles III. Coupling of this compound with halogenated beta picoline V yielded the title compounds. The structures of synthesized compounds were elucidated mainly by spectral evidence. All the compounds were screened for their anti-hypertensive activity. The compounds exhibited moderate to signiicant activities
Development and Validation of Static HS-GC Method for the Determination and Quantification of Residual Solvents of Bromhexine Hydrochloride (BHX)
Get PDFThe determination of residual solvents in drug substances is the mandatory requirement by various health authorities in the world. There are no analytical methods available in the literature that can simultaneously separate and quantitate residual solvents in bromhexine hydrochloride (BHX) active pharmaceutical ingredient (API). This paper describes the development and validation of a simple, efficient, accurate, and robust static headspace gas chromatography method for the determination of residual solvents, namely methanol, ethanol, ethyl acetate, monochlorobenzene, and benzene, in BHXAPI. This new method has been demonstrated to be accurate, linear, precise, reproducible, specific, and robust for its intended purpose. The method gives very good sensitivities viz. detection limits for benzene is 0.4 ppm, ethyl acetate 2 ppm and for others solvents 5 ppm and precision (below 9.0 % RSD) for all solvents. The results of this evaluation strongly indicate that this method can be readily used to determine residual solvents in BHX.
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An Ethanol-Based Proliposome Technology for Enhanced Delivery and Improved “Respirability” of Antiasthma Aerosols Generated Using a Micropump Vibrating-Mesh Nebulizer
Get PDFSalbutamol sulphate liposomes were generated using ethanolbased proliposomes followed by nebulization using an Aeroneb Pro vibrating-mesh nebulizer. The droplet size, output and fine particle fraction (FPF) of the drug incorporated in liposome formulation were compared to those of a conventional drug solution. Aerosol output was determined gravimetrically and drug output was analyzed by using high performance liquid chromatography. The potential of aerosol deposition in deep lung was evaluated using inertial impaction and laser diffraction. The effect of formulation surface tension on the aerosol performance was studied. Output and FPF were improved using liposomes compared to the conventional solution, for instance, FPF values were 57.85% and 45.81% respectively. The volume median diameter as measured by laser diffraction was respectively 3.44 μm and 3.22 μm; however, the higher FPF of the liposome formulation is justified by the lower polydispersity of its aerosol. The improved aerosol performance using liposomes was attributed to the reduction of surface tension caused by the presence of phospholipid. This is the first study that demons trates the ability of liposomes to improve the nebulized drug output and FPF
Advances in Magnetofection & − Magnetically Guided Nucleic Acid Delievery:a Review
Get PDFDuring the last decade, nanomagnetic methods for delivering and targeting nucleic acids have been developed which are often referred to as magnetofection. Nucleic acids carry the building plans of living systems. As such, they can be exploited to make cells produce a desired protein, or to shut down the expression of endogenous genes or even to repair defective genes. Hence, nucleic acids are unique substances for research and therapy. To exploit their potential, they need to be delivered into cells which can be a challenging task in many respects. Magnetofection provides a novel tool for high throughput gene screening in vitro and can help to overcome fundamental limitations to gene therapy in vivo. Magnetofection is nucleic acid delivery to cells, supported and site-specifically guided by the attractive forces of magnetic fields acting on nucleic acid shuttles (vectors) which are associated with magnetic nanoparticles. In a magnetofection procedure, self-assembling complexes of enhancers like cationic lipids with plasmid DNA or small interfering RNA (siRNA) are associated with magnetic nanoparticles and are then concentrated at the surface of cultured cells by applying a permanent inhomogeneous magnetic field