84 results about "In vivo pharmacokinetics" patented technology

The present invention provides sustained release formulations of estradiol metabolites whereby the in vivo pharmacokinetics are manipulated by a method selected from the group consisting of chemical modification, crystal packing formation, particle size or a combination thereof. Such compositions are useful in the long-term treatment of a wide variety of diseases.

The invention belongs to the field of pharmaceutical preparations and provides a Celecoxib nanosuspension and a preparation method thereof. Celecoxib is a novel non-steroidal anti-inflammatory drug, inhibits cyclooxygenase -2(COX-2) is through specificity, has anti-inflammatory and pain-easing effects and is clinically used for treating osteoarthritis and rheumatoid arthritis. However, the Celecoxib has very low solubility and in-vivo bioavailability. In order to increase the dissolution and the bioavailability of the drug, a high-speed shearing combined high-pressure homogenizing method is adopted to prepare the Celecoxib nanosuspension, the particle size and the polydispersion index PI are used as indicators for formulation technology optimization, a laser particle analyzer and a transmission electron microscope are adopted to study the particle size and form of the drug, the dissolution of the drug is evaluated through in-vitro dissolution experiments, and rat in-vivo pharmacokinetic study is conducted. Measurement results prove that the drug particle size of the nanosuspension is 50-500 nm, and the dissolution and the in-vivo bioavailability of the drug are increased obviously.

The present invention provides a set of in vitro and in silico methodologies for predicting in vivo pharmacokinetics and pharmacodynamics of multiple components; the methodologies comprise mathematical models for solving multiple unknowns which are linearly independent and/or interacting with each other. The present invention can be applied to develop phytomedicines which contain multiple active ingredients without prior identification, isolation and purification of these components.

The invention relates to an anti-tumor multi-medicine resistant targeted liposome and a preparation method thereof, in particular to an anti-tumor multi-medicine resistant long circulating targeted liposome. The invention is characterized in that: quercitin and an anti-tumor medicine are jointly coated in the liposome, and simultaneously target tumor tissues to reverse the multi-medicine resistance of tumors, cytotoxicity of anti-tumor medicines on medicine resistant tumors is enhanced, the change of pharmacokinetic properties of the anti-tumor medicines in vivo and the enhancement of toxic and side effects of the anti-tumor medicines in vivo, which are caused by the difference and interaction of the pharmacokinetic properties of different medicines in vivo, are avoided, and the treatmenteffect on medicine resistant tumors is improved.

The invention belongs to the technical field of medicines, relates to a photosensitizer-chemotherapeutic drug 'photosensitizer-chemotherapeutic integration' micromolecule prodrug, and aims to connecta chemotherapeutic drug with a photosensitizer through ester bonds or mono-thioether bonds to achieve efficient co-carrying and synchronous delivery of the chemotherapeutic drug and the photosensitizer. The photosensitizer-chemotherapeutic drug is prepared from paclitaxel as a chemotherapeutic drug and coked phaeophytin a as a photosensitizer, a self-assembled nano medicine delivery system is alsoprepared, and synergetic medicine release, in-vivo pharmacokinetics and anti-tumor effects of the drug are evaluated. The predrug is simple in preparation process, small and uniform in nanoparticle size, beneficial to enrichment of nanoparticles at tumor parts through an EPR (Enhanced Permeability and Retention) effect, super large in drug loading capacity and easy in surface modification, and reticuloendothelial system uptaking can be effectively avoided, in addition, uptaking of tumor cells upon the nanoparticles can be effectively improved; while photodynamic treatment is carried out, selective release of medicines can be synergistically triggered in tumor cells; by adopting the 'photosensitizer-chemotherapeutic integration' micromolecule prodrug self-assembled nano drug delivery system designed by the invention, the synergetic anti-tumor effects of the photosensitizer and the chemotherapeutic drug can be remarkably improved.

The invention discloses an analysis method for determining rheum emodin, aloe-emodin, chrysophanol and emodin monomethyl ether in blood plasma at the same time and application of rheum emodin, aloe-emodin, chrysophanol and emodin monomethyl ether in pharmacokinetics, wherein the analysis method for determining rheum emodin, aloe-emodin, chrysophanol and emodin monomethyl ether in the blood plasma at the same time comprises the following steps: (1) preparing a sample; (2) detecting. The analysis method for determining rheum emodin, aloe-emodin, chrysophanol and emodin monomethyl ether in the blood plasma at the same time has good specificity, high precision degree, high accuracy and wide linear range and can be used for in vivo pharmacokinetic determination of Chinese medicinal compositions.

The invention belongs to the field of medicine preparations, and particularly relates to polysialic acid lipid grafted derivatives, a preparing method thereof and applications of the derivatives, particularly applications for preparation and modification of microparticle preparations. Sialic acid units in the polysialic acid are connected through alpha-2,8-glucosidic bonds, and lipid segments and hydroxy in the sialic acid units are connected through ester bonds. A structural formula is shown in the description, wherein SA is a sialic acid unit, x is the number of the lipid segments grafted in the polysialic acid molecule, m is the number of the sialic acid units in the polysialic acid molecule, the m is not more than 100 and not less than 1, the x is not more than 30 and not less than 1, x/m is 5-30%, R-CO- is derived from R-COOH, and the R-COOH is a lipid compound containing carboxyl. Immunogenicity of microparticle preparations prepared or modified by the compounds is extremely low and the microparticle preparations have excellent in-vivo pharmacokinetic properties.

The invention relates to preparation of a carbon nanotube doped fenbufen molecularly imprinted polymer sustained-release material and specifically relates to a fenbufen sustained-release molecularly imprinted polymer material which is prepared by utilizing ionic liquid 1-butyl-3-methylimidazole tetrafluoroborate and a deep-eutectic solvent as a binary pore-foaming agent and doping single-wall carbon nanotubes. The fenbufen sustained-release molecularly imprinted polymer material is prepared from raw materials by mass: 0.67 to 0.76% of fenbufen, 0.03 to 0.06% of single-wall carbon nanotube, 2.41 to 2.75% of 4-vinyl pyridine, 18.16 to 20.69% of ethylene glycol dimethacrylate, 18.37 to 48.39% of deep-eutectic solvent, 30.06 to 57.08% of 1-butyl-3-methylimidazole tetrafluoroborate and 0.25 to 0.29% of azodiisobutyronitrile. The fenbufen sustained-release molecularly imprinted polymer material disclosed by the invention has a good sustained-release effect; in-vivo pharmacokinetics show that compared with 1.5h peak time and 46.1% bioavailability of an imprinted polymer without carbon nanotubes, peak time of blood drug concentration in a rat body can reach 4 hours and bioavailability can be 140% compared with commodity medicine, and performance is stable. The preparation of the carbon nanotube doped fenbufen molecularly imprinted polymer sustained-release material disclosed by the invention lays a foundation for a molecularly imprinted technology to be applied to a medicine transfer system.

The patent of the invention relates to a polymeric micelle capable of realizing synchronous administration of sorafenib and curcumin and a preparation method of the polymeric micelle, and belongs to the field of novel medicine preparations in health and medicines. The PCL-PEG-PCL (polycaprolactone -polyethylene glycol-polycaprolactone) is taken as a carrier material, the polymeric micelle capable of synchronously releasing sorafenib and curcumin is prepared according to a filming rehydration method, the solubility and the bioavailability of sorafenib and curcumin are improved, and the purposes of synergetic administration of medicines and enhancement of treatment effects are fulfilled. The patent concretely investigates the optimal polymer carrier material, the carrier material, the medicine dosage ratio, the rehydration temperature, time and volume of the filming rehydration method, the in vitro dissolution and the studies on in vivo pharmacokinetics of mice, the finally prepared polymeric micelle can realize synchronous administration of sorafenib and curcumin, the long-circulation effect is obvious, and the polymeric micelle has broad research significances and commercial popularization prospect.

The invention belongs to the technical field of medicines, and particularly relates to a preparation method of a content of a soft nintedanib ethanesulfonate capsule. The content is prepared from nintedanib ethanesulfonate, wherein the grain size distribution range of the nintedanib ethanesulfonate is D90 from 40 mu m to 80 mu m. By studying the stability of a suspension system of the content of the soft nintedanib ethanesulfonate capsule and determining in-vivo pharmacokinetic parameters of wistar rats, the influence of the grain size of the nintedanib esylate as a raw material on the physical stability and bioavailability of the soft nintedanib ethanesulfonate capsule is discovered to be great, and the soft nintedanib ethanesulfonate capsule is ultimately discovered to have good physicalstability and be similar to pharmacokinetic behaviors of reference preparations in terms of absorption when the grain size of the nintedanib ethanesulfonate material is 40 mu m to 80 mu m, and moreover, since the grain size control range of the raw material is broadened, the production cost and the technological requirements are reduced. The invention further provides the preparation method of the content, the process of which is reasonable.

The invention relates to the technical field of biomedicines and relates to a hypoxia responsive liposome preparation, and preparation and applications thereof. In particular, the invention relates to hypoxia responsive liposome-AQ4N-dihydroporphin e6 and preparation and application thereof, and especially, application thereof in enhancement of killing cells in tumor hypoxia zones in photodynamics therapy. The liposome preparation is composed of a liposome, AQ4N and dihydroporphin e6, has uniform particle size and is excellent in dispersion in water. The particle size of the liposome preparation is mainly about 100 nm in water. The liposome preparation can carry photosensitive molecules and dimethyldiguanide and is an ideal medicine carrier, and also has excellent in-vivo pharmacokinetics behavior. A test proves that the liposome-AQ4N-dihydroporphin e6 preparation is very-highly enriched at tumor parts, so that after the photodynamics therapy, the preparation can cause a more serious hypoxia status in the tumor zone, thereby improving the killing effect on the hypoxia cells of the AQ4N and obtaining excellent synergistic therapy effects on tumor.

The invention provides a method for quantitatively detecting naringin, aurantiamarin, neohesperidin, baicalin and wogonoside in a blood plasma sample by adopting liquid chromatography tandem mass spectrometry, and the method comprises the following steps: (1) preparaing a sample; (2) detecting. The analysis method provided by the invention has good specificity, high precision degree, high accuracy and wide linear range and can be used for in vivo pharmacokinetic determination of Chinese medicinal compositions.

The invention relates to ethylenediamine compounds of which the structural formula is as shown in a formula (I), pharmaceutically acceptable salts, a preparation method thereof and application of the ethylenediamine compounds in preparing medicines for treating infectious diseases caused by tubercle bacillus and particularly infectious diseases caused by multidrug resistant tubercle bacillus. The compounds of which the structural formula is shown in the (I) have good in vitro tubercle bacillus resistant activity and good in vivo pharmacokinetics property.

The invention relates to a 4-pyridine substituted phthalazinone compound, a preparation method, a pharmaceutical composition and an application thereof, the structure of the 4-pyridine substituted phthalazinone compound is shown as a formula I, the compound of the formula I has improved pharmaceutical physicochemical properties and in-vivo pharmacokinetic properties, oral bioavailability is high,druggability is good, The compound is a non-nucleoside small-molecule HBV virus inhibitor which is novel in structure and can be orally taken.

The present invention provides a 1,2,4-triazolone derivative represented by Formula (1A) having an antagonistic activity on the arginine-vasopressin 1b receptor or a pharmaceutically acceptable salt thereof and provides a pharmaceutical composition comprising the compound or the salt as an active ingredient, in particular, a therapeutic or preventive agent exhibiting favorable pharmacokinetics in a disease such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, or alopecia.

The invention provides a preparation method and application of a tegaserod water-soluble organic acid salt. Specifically, the invention provides a water-soluble organic acid salt of a compound as shown in a structural general formula (I). The organic salt can be used as a PI3K/Akt/mTOR and JAK-STAT3 signal channel inhibitor and an immunomodulator for use of developing drugs for treating tumors and inflammations. In the tegaserod organic acid salt provided by the invention, the solubility of the tegaserod D-pyroglutamate in water is greater than 600 mg/mL, and is improved by more than 3000 times compared with that of maleate. Therefore, obvious advantages are generated in the aspects of in-vivo pharmacokinetic behaviors of medicines, development of new dosage forms of the medicines and the like, and the compound can be used for improvement of a preparation process and development of the new dosage forms and has practicability. In the study of antitumor activity in mice, the tegaserod D-pyroglutamate has obvious inhibitory activity on prostatic cancer and melanoma, and the growth inhibitory activity on melanoma B16F10 reaches 50.6%.