122 results about "Drug Kinetics" patented technology

An electronic storage medium that comprises at least one radiopharmaceutical identity, SPECT measured values of at least one radiopharmaceutical kinetic parameter of a flow rate across a tissue membrane, for the radiopharmaceutical, and a set of instructions for associating the at least one radiopharmaceutical kinetic parameter with a disease signature.

A pharmaceutical dosage form such as a capsule capable of delivering therapeutic agents into the body in a time-controlled or position-controlled pulsatile release fashion, is composed of a multitude of multicoated particulates (beads, pellets, granules, etc.) made of one or more populations of beads. Each of these beads except an immediate release bead has at least two coated membrane barriers. One of the membrane barriers is composed of an enteric polymer while the second membrane barrier is composed of a mixture of water insoluble polymer and an enteric polymer. The composition and the thickness of the polymeric membrane barriers determine the lag time and duration of drug release from each of the bead populations. Optionally, an organic acid containing intermediate membrane may be applied for further modifying the lag time and / or the duration of drug release. The pulsatile delivery may comprise one or more pulses to provide a plasma concentration-time profile for a therapeutic agent, predicted based on both its pharmaco-kinetic and pharmaco-dynamic considerations and in vitro / in vivo correlations.

The invention relates to an F-1,2,3-triazole ring-polyethylene glycol-metronidazole compound which has the following structural general formula: L is ethyl or polyethylene glycol with the following structure: n is equal to 0, 1, 2 or 3; M is a triazole ring with the following structure: or, N is ethyl or polyethylene glycol with the following structure; n is equal to 0, 1, 2 or 3; and A is 19F or18F. Under a changeless condition that the invention keeps the metronidazole as a targeting base group, the polyethylene glycol is introduced to modify and change the molecular structure of a medicine, and the aims of improving medicine dynamics and pharmacodynamical properties and increasing the curative effect of the medicine are achieved. The triazole ring, a PEG base group, 2- metronidazole and 18 / 19F nuclide are connected by a click method, and a series of novel F-triazole ring-PEG-metronidazole derivatives are designed and synthesized. The nitro imidazole derivatives can quicken removing from normal tissues by lowering fat solubility so as to enhance a target / non-target ratio and is used for the development research of tumours, cardiac muscles or brain anoxia.

The invention discloses a recombined dimerization anti-thrombin III-Fc fusion protein, of which the in vitro biological activity is similar to or higher than that of the serum derived anti-thrombin III, and the in vivo half-life period is prolonged. The fusion protein provided by the invention contains human anti-thrombin III (hAT), a flexible peptide joint (L) containing about 20 or less amino acids, and a human IgG Fc mutant (vFC) which is represented by hAT-L-vFC (Fc). Such Fc mutant excludes cracking property and shows extremely low bad-Fc-induced side effect. Such hAT-L-vFC fusion protein is prolonged in serum half-life period and enhanced in the biological activity, so that the pharmacokinetics effect and the pesticide effect are improved. The invention further discloses a method for efficiently expressing or producing such recombined fusion proteins by adopting the mammalian cells.

The invention relates to a novel broad-spectrum antifungal medicine compound, a broad-spectrum antifungal medicine composition, an application of the compound or the composition in the preparation of a broad-spectrum antifungal medicine, and an application of the compound or the composition in the preparation of a medicine used for treating severe invasive infection (comprising Candida krusei) caused by invasive aspergillosis and / or Fluconazole-resistant Monilia and / or severe infection caused by Scedosporium and fusarium. The novel broad-spectrum antifungal medicine compound and the broad-spectrum antifungal medicine composition have extensive and strong antifungal activity and better dynamic property and safety. For deep mycotic infection, the novel broad-spectrum antifungal medicine compound and the broad-spectrum antifungal medicine composition are better than the original voriconazole in the aspects of the antibiotic activity and the medicine resistance and is better than amphotericin B in the aspects of safety and effectiveness; and compared with the formerly applied voriconazole, Fluconazole, itraconazole and amphotericin B, the novel broad-spectrum antifungal medicine compound and the broad-spectrum antifungal medicine composition have reinforced medicine effect, less adverse reaction and good safety.

A unit dosage form, such as a capsule or the like for delivering drugs into the body in a circadian release fashion, is comprising of one or more populations of propranolol-containing particles (beads, pellets, granules, etc.). Each bead population exhibits a pre-designed rapid or sustained release profile with or without a predetermined lag time of 3 to 5 hours. Such a circadian rhythm release cardiovascular drug delivery system is designed to provide a plasma concentration-time profile, which varies according to physiological need during the day, i.e., mimicking the circadian rhythm and severity / manifestation of a cardiovascular disease, predicted based on pharmaco-kinetic and pharmaco-dynamic considerations and in vitro / in vivo correlations.

The invention discloses a Fc fusion protein of long-acting recombinant human growth hormone. The Fc fusion protein (hGH-L-vFc fusion protein) disclosed herein contains human growth hormone, flexible peptide linker of about 2-20 amino acids, and human IgG Fc mutant. The Fc mutant is not lytic and has tiny side effect of adverse Fc-mediator. The invention further discloses a method for preparing or generating the fusion protein with high expression level. The hGH-L-vFc fusion protein disclosed herein has prolonged serum half-life period and increased biological activity, so as to improve the pharmacokinetics and drug efficacy, and needs few times of injection required in treatment.

A method, signal processor, device, and system for estimating a parametric or functional image 47 mapping a biological process on the basis of a limited or incomplete sequence of biological process images 40 recorded as a function of time, e.g. by a PET or SPECT scanner after injection of a radio tracer. One or more kinetic parameters 43 are first extracted by applying a pharmacokinetic model 42 (compartmental model of the underlying tracer kinetics) to the sequence of biological process images 40. Additional data 41 are used in the model, comprising at least a predetermined kinetic parameter range (e.g. from the literature), and optionally an input function or a blood clearance function. Next, an iterative algorithm 44 is applied to arrive at a modified sequence of images 45, e.g. by inserting an estimated image into the incomplete sequence of images, utilizing the one or more kinetic parameters 43. After a stop criterion has been fulfilled, the resulting image 47 is finally estimated 46 from the modified sequence of images 45. The method can be used e.g. to estimate a hypoxia parameter k3 image in the case of a FMISO data set where only late-time images are available. The method may be implemented as part of existing PET, SPECT, CT, MR or Ultrasound scanner software, and since only a limited amount of late time post injection images are necessary to provide a reliable result, the method helps to increase patient comfort and clinical throughput.

N-(2-oxaadamantan-1-yl)ureas of formula I, where R3 is H, C1-C3 alkyl, cyclohexyl or phenyl; R is -[CH2]n -Y; n is 0-15; in -[CH2]n - 0-n / 3 of the methylene groups are optionally replaced by non adjacent oxygen atoms; and Y is a 3- or 4-substituted phenyl, a 3- or 4-substituted cyclohexyl, a N-substituted piperidin-4-yl, a N-substituted piperidin-3-yl, a di- or tri-fluorosubstituted phenyl, 4-chloro-3-trifluoromethylphenyl, 3-chloro-4-trifluoromethylphenyl, 4-fluoro-3-trifluoromethylphenyl, or 3-fluoro-4-trifluoromethylphenyl; have epoxide hydrolase (sEH) inhibitory activities similar to thoseof their N-(adamantan-1-yl)urea analogs. Thus, compounds I are useful as API for the treatment of sEH mediated diseases. Besides, in general, compounds (I) have higher water solubilities and lower melting points, what make them more promising from the point of view of pharmacokinetics and formulation.

The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.