A series of N-hydroxyformamide tumor necrosis factorconverting enzyme (TACE)/matrix metalloprotease (MMP) inhibitors were evaluated for their potential to induce human cytochrome P450 3A (CYP3A). Two in vitro assays were used: 1) a cell-based reporter gene assay for activation of the pregnane X receptor (PXR), and 2) a primary “sandwich” culture of human hepatocytes. Approximately 50 TACE/MMP i...

Floating microspheres have emerged as a potential candidate for gastroretentive drug delivery system. For developing a desired intragastric floatation system employing these microspheres, it is necessary to select an appropriate balance between buoyancy and drug releasing rate. These properties mainly depend on the polymers used in the formulation of the microspheres. Hence it is necessory to s...

Objective: Chlorzoxazone (CLZ) is centrally acting skeletal muscle relaxant. It is insoluble in water, so employed for the formation of solid dispersions (SD) as a means to enhance the dissolution rate, and carrier selected was polyethylene glycol 6000 (PEG 6000). Methods: The SDs were prepared by different methods and characterized by in vitro drug release, drug content, fourier transform infr...

Nine compounds, 3-hydroxy-4,5-dimethoxyphenyl-beta-D-glucopyranoside (1), beta-D-fructfuranosyl-alpha-D-(6-vanilloyl)-glucopyranoside (2), beta-D-fructfuranosyl-alpha-D-(6-syringyl)-glucopyranoside (3), 3-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-2-[4-(3-hydroxy-1-(E)-propenyl)-2-methoxyphenoxy]propyl-beta-D-glucopyranoside (4), 3-hydroxy-1-(4-hydroxy-3-methoxyphenyl)-2-[4-(3-hydroxy-1-(E)-propenyl...

ME T H Y L N P R O P Y L ETHER is an isomer of di-ethyl ether and possesses the formula CHs-O(CHI)J-CHJ. The physical properties of the two drugs are similar, and the vapour pressure curve of methyl-n-propyl ether is such that it may be used in the Oxford Vaporizer No. 1 without any alteration in the calibration of the instrument (see Figure). Methyl-n-propyl ether has a very unpleasant pungent...

An attempt was made to formulate Buccal patches of Isoxsuprine hydrochloride, a potent and long acting vasodilator and uterine suppressant , by using Hydroxyl propyl methyl cellulose(HPMC), Polyvinyl pyrolidone K-30 (PVP K-30) and Hydroxyl ethyl cellulose (HEC). Twelve batches of buccal patches were prepared by solvent casting technique in which the best formulation was found out. The polymers ...

Objective: Buccal drug delivery is the most suited route for local as well systemic of drugs. Cilnidipine an L/N type dihydropyridine 4th generation calcium channel blocker (CCB), which decreases hypertension by blocking N-type to attenuate vascular sympathetic neurotransmission. It has high first-pass metabolism leading low bioavailability. Hence present research work was undertaken formulate ...

The main objective of the current study was to formulate poorly water soluble drug Spirinolactone by using solid dispersion technique in order to achieve a better dissolution rate which would further help in enhancing oral bioavailability. Solid dispersions were prepared using two methods; solvent method and fusion method. Solid dispersion was prepared by using polymers, such as Hydroxy propyly...

The phenol of 1-(3-(1H-imidazol-1-yl)propyl)-3-(4-hydroxy-3-methoxyphenyl)thiourea was selectively carbon-11 labelled to generate [11C]PBD150 in 7.3% yield from [11C]methyl triflate (non-decay corrected; radiochemical purity ≥95%, specific activity = 5.7 Ci/µmol, n=5). Evaluation of [11C]PBD150 by small animal PET imaging (mouse and rat) determined it does not permeate the blood brain barrier, ...