Pharmacy and Pharmaceutical Sciences Commons^™

High-Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis And Method Of Generating The Same, Chang-Guo Zhan, Hoon Cho, Hsin-Hsiung Tai

Pharmaceutical Sciences Faculty Patents

A novel computational method and generation of mutant butyrylcholinesterase for cocaine hydrolysis is provided. The method includes molecular modeling a possible BChE mutant and conducting molecular dynamics simulations and hybrid quantum mechanical/molecular mechanical calculations thereby providing a screening method of possible BChE mutants by predicting which mutant will lead to a more stable transition state for a rate determining step. Site-directed mutagenesis, protein expression, and protein activity is conducted for mutants determined computationally as being good candidates for possible BChE mutants, i.e., ones predicted to have higher catalytic efficiency as compared with wild-type BChE. In addition, mutants A199S/A328W/Y332G, A199S/F227A/A328W/Y332G, A199S/S287G/A328W/Y332G, …

Compositions And Methods For Selectively Targeting Cancer Cells Using A Thiaminase Compound, Jeffrey A. Moscow, Shuqian Liu, Younsoo Bae

Pharmaceutical Sciences Faculty Patents

Compositions and methods of treating cancer using a thiaminase compound are described. The presently-disclosed subject matter includes a method of treating cancer by administering a thiaminase compound and a thiamine-dependent enzyme inhibitor.

High-Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis And Method Of Generating The Same, Chang-Guo Zhan, Hoon Cho, Hsin-Hsiung Tai

Pharmaceutical Sciences Faculty Patents

A novel computational method and generation of mutant butyrylcholinesterase for cocaine hydrolysis is provided. The method includes molecular modeling a possible BChE mutant and conducting molecular dynamics simulations and hybrid quantum mechanical/molecular mechanical calculations thereby providing a screening method of possible BChE mutants by predicting which mutant will lead to a more stable transition state for a rate determining step. Site-directed mutagenesis, protein expression, and protein activity is conducted for mutants determined computationally as being good candidates for possible BChE mutants, i.e., ones predicted to have higher catalytic efficiency as compared with wild-type BChE. In addition, mutants A199S/A328W/Y332G, A199S/F227A/A328W/Y332G, A199S/S287G/A328W/Y332G, …

High-Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis And Method Of Generating The Same, Chang-Guo Zhan, Hoon Cho, Hsin-Hsiung Tai

Pharmaceutical Sciences Faculty Patents

A novel computational method and generation of mutant butyrylcholinesterase for cocaine hydrolysis is provided. The method includes molecular modeling a possible BChE mutant and conducting molecular dynamics simulations and hybrid quantum mechanical/molecular mechanical calculations thereby providing a screening method of possible BChE mutants by predicting which mutant will lead to a more stable transition state for a rate determining step. Site-directed mutagenesis, protein expression, and protein activity is conducted for mutants determined computationally as being good candidates for possible BChE mutants, i.e., ones predicted to have higher catalytic efficiency as compared with wild-type BChE. In addition, mutants A199S/A328W/Y332G, A199S/F227A/A328W/Y332G, A199S/S287G/A328W/Y332G, …

Berry Preparations And Extracts, Russell J. Mumper, Jin Dai, Vincent S. Gallicchio

Pharmaceutical Sciences Faculty Patents

A method for deriving compositions having antioxidant and anti-inflammatory activity from berries is provided. The method results in a berry extract compositions having stable anthocyanin content. In one aspect, the method comprises exposing a berry to a solvent composition having a pH of from about 1 to about 4.5, and recovering a berry extract having a stabilized anthocyanin content. The berry may be a blackberry. A cryoprotectant may be added, to further stabilize the anthocyanin content. Compositions comprising the berry extract of the present invention, formulated for oral and/or topical administration, are provided also, including nutritional supplements, capsules, enteric-coated capsules, …

High-Activity Mutants Of Butyrylcholinesterase For Cocaine Hydrolysis And Method Of Generating The Same, Chang-Guo Zhan, Hoon Cho, Hsin-Hsiung Tai

Pharmaceutical Sciences Faculty Patents

A novel computational method and generation of mutant butyrylcholinesterase for cocaine hydrolysis is provided. The method includes molecular modeling a possible BChE mutant and conducting molecular dynamics simulations and hybrid quantum mechanical/molecular mechanical calculations thereby providing a screening method of possible BChE mutants by predicting which mutant will lead to a more stable transition state for a rate determining step. Site-directed mutagenesis, protein expression, and protein activity is conducted for mutants determined computationally as being good candidates for possible BChE mutants, i.e., ones predicted to have higher catalytic efficiency as compared with wild-type BChE. In addition, mutants A199S/A328W/Y332G, A199S/F227A/A328W/Y332G, A199S/S287G/A328W/Y332G, …

Methods And Compositions For Optimizing Blood And Tissue Stability Of Camptothecin And Other Albumin-Binding Therapeutic Compounds, Thomas G. Burke, Daniel C. Carter

Pharmaceutical Sciences Faculty Patents

The present invention provides methods and formulations for optimizing the anti-cancer and anti-HIV activities of a camptothecin drug, including camptothecin and its related analogs including 9-aminocamptothecin and 9-nitrocamptothecin. The invention involves methodologies and formulations that limit human serum albumin-mediated reduction of the anti-cancer and anti-HIV effects of the camptothecins, and the methods and formulations provide combination therapies in which binding of the camptothecin agent to human serum albumin can be modulated by the administration of a competing agent that also binds human serum albumin. Reduced camptothecin drug binding to human serum albumin can result in elevated camptothecin free drug levels …

Methods To Impair Hematologic Cancer Progenitor Cells And Compounds Related Thereto, Craig Jordan

Pharmaceutical Sciences Faculty Patents

Primitive or progenitor hematologic cancer cells have been implicated in the early stages and development of leukemia and malignant lymphoproliferative disorders, including acute myelogenous leukemia (AML), chronic myelogenous leukemia (CML) and chronic lymphoid leukemia (CLL). Interleukin-3 receptor alpha chain (IL-3Rα or CD123) is strongly expressed on progenitor hematologic cancer cells, but is virtually undetectable on normal bone marrow cells. The present invention provides methods of impairing progenitor hematologic cancer (e.g., leukemia and lymphomic) cells by selectively targeting cells expressing CD123. These methods are useful in the detection and treatment of leukemias and malignant lymphoproliferative disorders. Also provided are compounds useful …

Method And System For In Situ Spectroscopic Evaulation Of An Object, Robert A. Lodder

Pharmaceutical Sciences Faculty Patents

A method and system for spectroscopically determining surface and product characteristics is employed for rapid detection of product characteristics and/or the presence or absence of suspected analytes, and the concentration of the analyte. The method and system uses a signal wide band detector that does not require focusing optics in many environments. It can be used for cleaning validation of pharmaceutical products and process equipment.

Method For Enhancing Protective Cellular Responses To Genotoxic Stress In Skin, Elaine L. Jacobson, Myron K. Jacobson

Pharmaceutical Sciences Faculty Patents

The present invention is directed to methods of using pro-NAD agents capable of enhancing the dermal and epidermal skin cell NAD content. These pro-NAD agents may be administered topically, orally, or parenterally to enhance DNA repair and other protective responses to DNA damage. The invention further relates to pharmaceutical compositions comprising pro-NAD agents that effectively elevate intracellular NAD content. Finally, the invention relates to the method of using the pro-NAD agents to treat disorders such as sunburn and other skin deterioration that results from DNA damage in skin cells.

Methods Of Delaying Development Of Cea-Associated Tumors Using Anti-Idiotype Antibody 3h1, Malaya Chatterjee, Kenneth A. Foon, Sunil K. Chatterjee

Pharmaceutical Sciences Faculty Patents

The present invention provides methods of delaying development of CEA-associated tumors using the anti-idiotype antibody 3H1, particularly in high-risk individuals.

Camptothecin Intermediates And Prodrugs And Methods Of Preparation Thereof, Thomas G. Burke, Dennis P. Curran, Wu Du

Pharmaceutical Sciences Faculty Patents

The present invention relates to novel intermediates and prodrugs of camptothecin and related analogs.

Formulations For Sustained-Release Of Topical Anesthetics And Methods Of Making And Using Same, Michael Joseph Jay, G. Thomas Kluemper, Sang Hun Kim

Pharmaceutical Sciences Faculty Patents

The present invention provides, inter alia, formulations useful to ameliorate symptoms associated with mucosal abrasions, specifically those due to dental orthodontic brackets; oral surgery; periodontal surgery or other procedures. For instance, there is a formulation comprising: 65 to 75% microcrystalline wax; 5 to 15% non-ionic polymer; 15 to 25% topical anesthetic; and 1 to 5% surfactant, wherein the ratio of non-ionic polymer to microcrystalline wax is no greater than 0.2. Preferably, for solid topical anesthetics, the particle size is less than the apertures of a 100-mesh screen. However, the topical anesthetic may also be a liquid. Formulations wherein the mixture …

Methods Of Treating Eye Conditions With Human Leukocyte Elastase (Hle) Inhibitory Agents, George A. Digenis, Charles Khouri

Pharmaceutical Sciences Faculty Patents

A method of reducing corneal scarring or fibroblast proliferation comprises applying to an area of a subject's eye afflicted with the condition a corneal scar-fibroblast proliferation-reducing amount of a free or polymer-bound HLE inhibitory agent under conditions and for a period of time effective to attain the desired effect. A method of reducing neovascularization of corneal scar tissue comprises applying to an area of a subject's eye afflicted with the condition a neovascularization-inhibitory amount of a free or polymer-bound HLE inhibitory agent under conditions and for a period of time effective to attain the desired effect.

Apparatus And Method For Noninvasive Chemical Analysis, Robert A. Lodder

Pharmaceutical Sciences Faculty Patents

A method and apparatus are provided for magnetohydrodynamic acoustic-resonance, near-IR spectroscopy. The method includes a step of applying to a subject under study a magnetic field having a strength between 2,00-10,000 gauss, near-IR radiation having a wavelength between 800-3,000 nm and an acoustic wave having a frequency between 10 khz -1 Mhz. The method also includes the steps of inducing vibration of ions in the magnetic field and detecting an electric wave generated magnetohydrodynamically by the acoustic wave induced vibration of the ions. Next is the collecting of the electrical, acoustical and near-IR spectra and the analyzing of the collected …

Low Molecular Weight Thiocarbamates As Inhibitors Of Elastase, Uses And Method Of Synthesis, George Digenis, Nikolaos P. Rodis

Pharmaceutical Sciences Faculty Patents

To see this abstract, please download this patent.

Apparatus And Method For Multiple Wavelength Of Tissue, Robert A. Lodder, Lisa A. Cassis

Pharmaceutical Sciences Faculty Patents

An apparatus for analyzing the chemical composition of tissue includes a near infrared light source, a fiber-optic probe, a mechanism for directing the light from the light source onto the tissue and detectors for detecting light reflected by the tissue. The light source transmits an incident beam having a wavelength ranging from 1000 to 2500 nm. A compound parabolic concentrator (CPC) is connected to a distal end of the fiber optic probe to focus or concentrate the wavelengths of light simultaneously and in parallel on a particular spot of tissue. Alternatively, an inverted, substantially conical reflector is positioned to scatter …

Non-Destructive Method For Radiolabelling Biomolecules By Halogenation, Anwar A. Hussain, Lewis W. Dittert

Pharmaceutical Sciences Faculty Patents

A kit and method of non-destructively radiolabelling a biomolecule substrate by halogenation, including the steps of: a) reacting a secondary amine with a chlorinating agent to produce an N-chloro secondary amine, (b) reacting the N-chloro secondary amine with a salt of a radiolabelled halogen to produce a radiolabelled halogenating agent, (c) reacting a solution of the biomolecule substrate with the radiolabelled halogenating agent, and (d) recovering a radiohalogenated biomolecule from the reaction of step (c). The kit and method allow for more complete iodination with a lessening of side reactions such as decomposition of the biomolecule substrate to be labelled.

Apparatus And Method For Noninvasive Chemical Analysis, Robert A. Lodder

Pharmaceutical Sciences Faculty Patents

A method and apparatus are provided for magnetohydrodynamic acoustic-resonance, near-IR spectroscopy. The method includes a step of applying to a subject under study a magnetic field having a strength between 2,00-10,000 gauss, near-IR radiation having a wavelength between 800-3,000 nm and an acoustic wave having a frequency between 10 khz-1 Mhz. The method also includes the steps of inducing vibration of ions in the magnetic field and detecting an electric wave generated magnetohydrodynamically by the acoustic wave induced vibration of the ions. Next is the collecting of the electrical, acoustical and near-IR spectra and the analyzing of the collected spectra. …

Composition Of, Method Of Producing And Method Of Using A Stabilized Formulation For Assaying Peroxide Activity, Hsin-Hsiung Tai

Pharmaceutical Sciences Faculty Patents

A formulation for use in detecting and/or determining peroxidase activity comprises a mixture in solution of tetramethylbenzidine, hydrogen peroxide, a buffering agent and bacitracin as a stabilizing agent. The formulation is used as a peroxidase substrate that is stable in solution for an extended period of time and provides enhanced color sensitivity.

Detection Method For Liquids Using Near Infrared Spectra, Leonard J. Galante, Robert A. Lodder

Pharmaceutical Sciences Faculty Patents

A method for detecting the presence or absence of microorganisms in a liquid test sample is provided without need for withdrawing an aliquot or destroying the sample. The method comprises taking near-infrared spectra of the sample and comparing it visually or mathematically to the spectra of a standard, which may be the values of the spectra known to the operator or may be a standard sample that is provided and run side-by-side.

Method And Apparatus For Detecting Microorganisms Within A Liquid Product In A Sealed Vial, Robert A. Lodder

Pharmaceutical Sciences Faculty Patents

An apparatus and method are provided for the noninvasive and nondestructive detection of microorganisms within a liquid product contained within a sealed vial. The apparatus includes a near-IR light source that produces both incident and reference beams having a wavelength between 800 and 2500 nm and, more preferably, 1100 and 1360 nm. The apparatus also includes an integrating sphere having incident and reference beam ports and a sample window opposite the incident beam port. A detector is mounted in the integrating sphere substantially adjacent the sample window. A substantially U-shaped mirror is provided to hold the vial. The U-shaped mirror …

Biodegradable, Low Biological Toxicity Radiographic Contrast Medium And Method Of X-Ray Imaging, Michael J. Jay, Yun Ryo

Pharmaceutical Sciences Faculty Patents

A biodegradable, low biological toxicity, particulate radiographic contrast medium comprises biodegradable polymeric spheres of average molecular weight average diameter about 10-1,000 nm or about 0.01-1.0 micron carrying in at least radiographic contrasting amount of a radiographically opaque element.

A method of obtaining a tomographic image of the body portion of a subject comprises administering to the subject a radiographically-detectable amount of the biodegradable, low-toxicity radiographic medium of claim 1; allowing for the spheres to be taken-up by the body portion; and X-raying an area comprising the body portion.

A method of improving the contrast of a tomographic image of a …

Porous Microspheres For Drug Delivery And Methods For Making Same, Patrick P. Deluca, Motoko Kanke, Toyomi Sato, Hans G. Schroeder

Pharmaceutical Sciences Faculty Patents

Controlled release drug delivery systems comprised of spherical microporous polymeric network of interconnecting channels containing pore incorporated drugs or other agents wherein the drugs or agents are confined within the pore channel are described. Also disclosed are processing parameters in connection with the novel method of the invention for obtaining drug delivery systems especially suited for parenteral as well as oral administration.

Method Of Administering Narcotic Antagonists And Analgesics And Novel Dosage Forms Containing Same, Anwar A. Hussain

Pharmaceutical Sciences Faculty Patents

The invention provides a novel method of administering narcotic antagonists, narcotic analgesics and related compounds, and novel dosage forms containing those compounds which are adapted for nasal administration. The nasal dosage forms disclosed include solutions, suspensions, gels and ointments. Especially preferred compounds which can be advantageously administered in accordance with the invention include naloxone, naltrexone, nalbuphine, levorphanol, buprenorphine, butorphanol, Δ⁹-tetrahydrocannabinol (THC), cannabidiol (CBD) and levonantradol.

Novel Method Of Administering Β-Blockers And Novel Dosage Forms Containing Same, Anwar A. Hussain

Pharmaceutical Sciences Faculty Patents

The invention provides a novel method of administering selected known adrenergic β-receptor blocking agents, such as dichloroisoproterenol, pronethalol, sotalol and alprenolol, which are of use in the treatment of angina pectoris, arrhythmias, hypertension and other cardiac conditions, and migraine. The invention further provides novel dosage forms of those β-blockers which are adapted for nasal administration and which include solutions, suspensions, gels and ointments.

Method Of Administering Natural Female Sex Horomones, Anwar A. Hussain, Shinichiro Hirai, Rima Bawarshi

Pharmaceutical Sciences Faculty Patents

The invention relates to a novel method of administering the natural female sex hormones, 17 β- estradiol and progesterone, to achieve enhanced bioavailability thereof. The invention further relates to novel dosage forms of 17 β- estradiol and/or progesterone which are adapted for nasal administration, such as solutions, suspensions, gels and ointments. The dosage forms containing a combination of 17 β-estradiol and progesterone are particularly useful as contraceptives, while the dosage forms containing only one of the hormonal components find utility in the treatment of conditions such as menopause, menstrual disorders, etc., which are known to respond to administration of a …