The purpose of this study was to evaluate the stereoselective pharmacokinetics of valnoctamide (V... more The purpose of this study was to evaluate the stereoselective pharmacokinetics of valnoctamide (VCD) in dogs, rats, and mice; which are the most common animal models for pharmacokinetic, pharmacologic, and toxicologic evaluation; and to compare it with previously published human data. Racemic VCD (mixture of four stereoisomers) was administered intravenously to six mongrel dogs and to rats (five rats per time-point), and intraperitoneally to mice (five mice per time-point). Plasma concentrations of the individual stereoisomers were measured by a stereospecific gas chromatography assay. In dogs, (2S,3R)-VCD had a larger clearance (0.33 L/hиkg) and a larger volume of distribution (0.79 L/kg) than its two diastereomers (0.24-0.25 L/hиkg and 0.65 L/kg, respectively). A tendency toward slightly higher clearance and volume of distribution values for (2S,3R)-VCD was observed in rats and mice as well. Consequently, in all three animal species the half-life (t 1 /2) of (2S,3R)-VCD was not different from the t 1 /2 of the other three VCD stereoisomers. The stereoselective pharmacokinetics of VCD as observed in dogs, rats, and mice is in line with the stereoselectivity previously observed in healthy subjects and epileptic patients.
PURPOSE: To provide a lipid polymer compsn. used for bleaching of the discolored teeth or prevent... more PURPOSE: To provide a lipid polymer compsn. used for bleaching of the discolored teeth or prevention of tooth discoloration. CONSTITUTION: This liquid polymer compsn. contains a water-soluble and low- viscosity cellulose polymer and bleaching agent and is prepd. by adding a stabilizing agent to disodium calcium ethylenediaminetetraacetate, etc. The compsn. is useful for removal of the dental plaque or for treatment of periodontal diseases, such as gingivitis in addition bleaching of the teeth and the prevention of the tooth discoloration. COPYRIGHT: (C)1994,JPO
Background: Thermo mechanical ablation (TMA) is a novel platform for fractional ablation and non-... more Background: Thermo mechanical ablation (TMA) is a novel platform for fractional ablation and non-ablation for skin treatment with no pain. Objective: This study aimed to evaluate the effects of TMA pre-treatment to facilitate transdermal drug delivery. Methods: Novoxel’s proprietary Tixel ® TMA system was evaluated in this study by a diffusion cell system using excised porcine ear skin. A 1 cm 2 tip, composed of a matrix of metallic pyramids, applied on freshly excised pig ear skin samples was operated at an ablative temperature of 400 o C for 6ms and 9ms. Verapamil hydrochloride 1% was used as a hydrophilic model drug known to have a poor absorption across mammal skin. Results: The present study has demonstrated that Tixel treatment for 9 or 6 ms increased skin permeability for verapamil along a 24-hour application period, with a highly significant difference relative to non-treatment control (p<0.05). After 24 hours, the cumulative amount of the drug that had penetrated into 9m...
AmyloLipid nanovesicles (ALNs) are new lipid-modified starch complex nanoparticles developed and ... more AmyloLipid nanovesicles (ALNs) are new lipid-modified starch complex nanoparticles developed and presented as nanocarriers of curcumin for targeting the CNS via the intranasal route. Curcumin has been indicated as a promising active agent with a variety of pharmacological activities, including a potential ability to treat brain tumors, traumatic brain injury, and CNS disorders, such as Alzheimer's disease, as it may inhibit amyloid-βprotein (Aβ) aggregation and Aβ-induced inflammation. Although curcumin has a tremendous potential as a therapeutic agent for CNS disorders, its low bioavailability and its rapid total body clearance reduce any chance for therapeutic levels to reach the brain. By using an optimized (2% crosslinked starch) curcumin-loaded ALNs, which was fabricated from a microemulsion as a precursor, an average of 141.5 ± 55.9 ng/g brain levels and 11.9 ± 12.0 ng/ml plasma concentrations were detected, one hour following intranasal administration of 160 μg/kg dose of curcumin. In comparison, 1 h after IV administration of the same dose, no CUR was detected in the brain and the mean plasma level was approximately one half of the level monitored after intranasal ALNs, i.e., 7.25 ± 0.20 ng/ml. It has been clearly demonstrated, therefore, that a well-designed ALN formulation proved itself as a promising carrier for intranasal delivery and brain targeting of curcumin.
The methods used to lighten tooth discolouration while conserving the tooth structure have attrac... more The methods used to lighten tooth discolouration while conserving the tooth structure have attracted much attention in a society which places a high value on esthetics. The purpose of this article is to present a home bleaching agent that uses a film-forming preparation containing carbamide peroxide (CP) which, while degrading, serves as a slow release delivery system of the bleaching agent. The efficacy of the preparation containing 3% CP and 10% CP on reduction of tooth discolouration is evaluated by a Chromameter in a double-blind placebo-controlled study. The effect of the tested bleaching agent on the gingival status, plaque accumulation and pulp sensitivity is also assessed.
The purpose of this study was to evaluate the stereoselective pharmacokinetics of valnoctamide (V... more The purpose of this study was to evaluate the stereoselective pharmacokinetics of valnoctamide (VCD) in dogs, rats, and mice; which are the most common animal models for pharmacokinetic, pharmacologic, and toxicologic evaluation; and to compare it with previously published human data. Racemic VCD (mixture of four stereoisomers) was administered intravenously to six mongrel dogs and to rats (five rats per time-point), and intraperitoneally to mice (five mice per time-point). Plasma concentrations of the individual stereoisomers were measured by a stereospecific gas chromatography assay. In dogs, (2S,3R)-VCD had a larger clearance (0.33 L/hиkg) and a larger volume of distribution (0.79 L/kg) than its two diastereomers (0.24-0.25 L/hиkg and 0.65 L/kg, respectively). A tendency toward slightly higher clearance and volume of distribution values for (2S,3R)-VCD was observed in rats and mice as well. Consequently, in all three animal species the half-life (t 1 /2) of (2S,3R)-VCD was not different from the t 1 /2 of the other three VCD stereoisomers. The stereoselective pharmacokinetics of VCD as observed in dogs, rats, and mice is in line with the stereoselectivity previously observed in healthy subjects and epileptic patients.
PURPOSE: To provide a lipid polymer compsn. used for bleaching of the discolored teeth or prevent... more PURPOSE: To provide a lipid polymer compsn. used for bleaching of the discolored teeth or prevention of tooth discoloration. CONSTITUTION: This liquid polymer compsn. contains a water-soluble and low- viscosity cellulose polymer and bleaching agent and is prepd. by adding a stabilizing agent to disodium calcium ethylenediaminetetraacetate, etc. The compsn. is useful for removal of the dental plaque or for treatment of periodontal diseases, such as gingivitis in addition bleaching of the teeth and the prevention of the tooth discoloration. COPYRIGHT: (C)1994,JPO
Background: Thermo mechanical ablation (TMA) is a novel platform for fractional ablation and non-... more Background: Thermo mechanical ablation (TMA) is a novel platform for fractional ablation and non-ablation for skin treatment with no pain. Objective: This study aimed to evaluate the effects of TMA pre-treatment to facilitate transdermal drug delivery. Methods: Novoxel’s proprietary Tixel ® TMA system was evaluated in this study by a diffusion cell system using excised porcine ear skin. A 1 cm 2 tip, composed of a matrix of metallic pyramids, applied on freshly excised pig ear skin samples was operated at an ablative temperature of 400 o C for 6ms and 9ms. Verapamil hydrochloride 1% was used as a hydrophilic model drug known to have a poor absorption across mammal skin. Results: The present study has demonstrated that Tixel treatment for 9 or 6 ms increased skin permeability for verapamil along a 24-hour application period, with a highly significant difference relative to non-treatment control (p<0.05). After 24 hours, the cumulative amount of the drug that had penetrated into 9m...
AmyloLipid nanovesicles (ALNs) are new lipid-modified starch complex nanoparticles developed and ... more AmyloLipid nanovesicles (ALNs) are new lipid-modified starch complex nanoparticles developed and presented as nanocarriers of curcumin for targeting the CNS via the intranasal route. Curcumin has been indicated as a promising active agent with a variety of pharmacological activities, including a potential ability to treat brain tumors, traumatic brain injury, and CNS disorders, such as Alzheimer's disease, as it may inhibit amyloid-βprotein (Aβ) aggregation and Aβ-induced inflammation. Although curcumin has a tremendous potential as a therapeutic agent for CNS disorders, its low bioavailability and its rapid total body clearance reduce any chance for therapeutic levels to reach the brain. By using an optimized (2% crosslinked starch) curcumin-loaded ALNs, which was fabricated from a microemulsion as a precursor, an average of 141.5 ± 55.9 ng/g brain levels and 11.9 ± 12.0 ng/ml plasma concentrations were detected, one hour following intranasal administration of 160 μg/kg dose of curcumin. In comparison, 1 h after IV administration of the same dose, no CUR was detected in the brain and the mean plasma level was approximately one half of the level monitored after intranasal ALNs, i.e., 7.25 ± 0.20 ng/ml. It has been clearly demonstrated, therefore, that a well-designed ALN formulation proved itself as a promising carrier for intranasal delivery and brain targeting of curcumin.
The methods used to lighten tooth discolouration while conserving the tooth structure have attrac... more The methods used to lighten tooth discolouration while conserving the tooth structure have attracted much attention in a society which places a high value on esthetics. The purpose of this article is to present a home bleaching agent that uses a film-forming preparation containing carbamide peroxide (CP) which, while degrading, serves as a slow release delivery system of the bleaching agent. The efficacy of the preparation containing 3% CP and 10% CP on reduction of tooth discolouration is evaluated by a Chromameter in a double-blind placebo-controlled study. The effect of the tested bleaching agent on the gingival status, plaque accumulation and pulp sensitivity is also assessed.
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