80 results about "Plasma drug concentration" patented technology

The invention is directed to oral modified/controlled release drug formulations which provide a rapid initial onset of effect and a prolonged duration of effect. Preferably, the peak concentration is lower than that provided by the reference standard for immediate release formulations of the drug, and the duration of effect falls rapidly at the end of the dosing interval.

The invention belongs to the field sustained/controlled-release preparations, in particular to an oral sustained/controlled-release pellet combination containing ginkgo biloba extract and a preparation method. The oral sustained/controlled-release pellet combination is composed of (A) a core containing a pill; (B) an insulating coating layer; (C) a sustained-release coating layer; (D) and an enteric-coated coating layer. The invention is the traditional Chinese medicine multi-component sustained-release pellet combination which is taken once by 24 hours and the multi-unit sustained-release pellet combined preparation with the different drug release systems, the core containing the pill is prepared by adopting the extrusion pill rolling method, a novel sustained-release multi-layer coating technology and a fluidized bed are utilized for coating the sustained-release pellet, the rapid-release part and the sustained-release part of the coated pellet are mixedly filled into a hard capsule or pressed into a pellet tablet. The sustained-release pellet has stable coating process and good reproducibility, thereby being applicable to the industrial mass production; and the drug quality of the preparation is stable through the long-term storage. The in vitro release test shows that the multiple components of the traditional Chinese medicine can achieve the sustained-release role, the sustained-release preparation can significantly increase the transmembrane absorption and the stability of various effective active ingredients by oral drug administration, the curve of plasma drug concentration in vivo is smooth, and the design purpose of 24-hour sustained-release is achieved.

The invention discloses a time quick-release and slow-release preparation of isosorbide mononitrate. The technical problem for the invention to solve is to provide a time quick-release and slow-release preparation, which is provided with long time of retaining the effective plasma-drug concentration and a low interval of 5-ISMN plasma-drug concentration. Each structure layer of the invention is orderly arranged from the inside to the outside as a parent nuclear of a pill core, a drug layer of a second dosage, an insulating layer, a slow-release coating layer, a drug layer of a first dosage, an expanding layer and a release controlling layer. The weight percentages of each layer are 15 to 40 percent of the parent nuclear of the pill core, 0.3 to 5.7 percent of the drug layer of the second dosage, 0 to 20 percent of the insulating layer, 5 to 40 percent of the slow-release coating layer, 0.7 to 13.4 percent of the drug layer of the first dosage, 5 to 30 percent of the expanding layer and 5 to 40 percent of the release controlling layer. The invention combines the characteristics of a time quick-release and slow-release medication system to avoid the drug resistance as well as accurately meet the clinical requirement of the angina treatment of the patient of the coronary heart disease.

The invention discloses a sinomenine or an enteric-coated controlled-release tablet of hydrochloride thereof. The prepared enteric-coated controlled-release tablet hardly releases the drug in artificial simulated gastric juice, but can slowly and smoothly release the drug in artificial simulated intestinal juice; the sustained release time of the drug can achieve more than 12 hours or even 24 hours; the enteric-coated controlled-release tablet is taken once or twice daily, the plasma drug concentration in vivo is smooth, and the peak-valley phenomenon of the plasma drug concentration is reduced; as the prepared enteric-coated controlled-release tablet hardly releases the drug in stomach, the contacted concentration of the drug with the gastric mucosa is small, the stimulation of the stomach caused by the drug is alleviated. As the prepared enteric-coated controlled-release tablet sustainedly slowly releases the drug in intestinal tract, the times of the drug administration are reduced, and the patient compliance is improved, thereby being applicable to the needs of the clinical development.

The present invention provides a tamsulosin hydrochloride sustained-release capsule. The tamsulosin hydrochloride sustained-release capsule of the present invention can avoid the sudden release of the drug tablets and the performance differences generated from the gastric emptying differences, display minor food effect or do not display food effect, and obtain the stable curve of the plasma drug concentration and longer action time simultaneously, so as to reduce the occurrence of cardiovascular side effects, greatly improve the safety, effectiveness and compliance of the medication for the patients. The tamsulosin hydrochloride sustained-release capsule of the present invention can ensure the sustained and regular release of the main ingredient tamsulosin hydrochloride after the oral administration, and the present invention is characterized by convenient administration, durable function, stable efficacy, fewer side effects and so on.

Methods for isothermal titration calorimetry analysis of the binding affinity of protease inhibitors to plasma proteins. A method that can quantitatively calculate free drug concentrations of protease inhibitors in human plasma, as well as a method to calculate therapeutic amounts and dosage regimens. Furthermore, the present invention provides a method that can calculate the effect of plasma proteins on the antiviral activity (EC50 values) of protease inhibitors from their binding affinities to plasma proteins. The present invention provides as well a method that can evaluate the in vivo anti-HIV efficacy of PIs in human plasma.

The invention creatively discloses a drug penetration dynamic evaluation method based on a three-dimensional cell model. The method comprises the steps that (1) a three-dimensional somatic cell model and a "penetration dynamics" mathematic model are established, the penetration behavior of an antitumor drug in somatic cells and an accumulation process in all layers of cells are described semi-quantitatively, and fitting is performed to obtain corresponding dynamic parameters; (2) drug concentrations in all layers of cells at different time points after the drug is given according to different concentrations can be subjected to backward prediction based on the obtained dynamic parameters, and the prediction result is highly consistent with an experience result; (3) biological factors influencing characteristic dynamic parameters are analyzed, the penetration behavior of the drug in tumor tissue is speculated according to a plasma drug concentration time course, and the speculation result is highly consistent with an experiment result; and (4) the model and the evaluation method are applied to a second-phase clinical drug INNO-206, and reasons for superiority of the clinical effect of the drug to that of doxorubicin are expounded from the aspect of in-tumor penetration, so that the universality of the method is further verified.

The novel positively charged pro-drugs of oxicams and related compounds in the general formula (1) 'Structure 1' were designed and synthesized. The positively charged amino groups of these pro-drugs not only largely increases the solubility of the drugs, but also bonds to the negative charge on the phosphate head group of membranes and pushes the pro-drug into the cytosol. The results suggest that the pro-drugs diffuses through human skin approximately 100 times faster than do oxicams and related compounds. It takes 1-2 hours for oxicams and related compounds to reach the peak plasma level when they are taken orally, but these prodrugs only took about approximately 50 minutes to reach the peak plasma level when they are taken transdermally. In plasma, more than 90% of these pro-drugs can change back to the parent drugs in a few minutes. The prodrugs can be used medicinally in treating any oxicams-treatable conditions in humans or animals. Second, the prodrugs can be administered not only orally, but also transdermally for any kind of medical treatments and avoid most of the side effects of oxicams. Controlled transdermal administration systems of the prodrugs enable oxicams and related compounds to reach constantly optimal therapeutic blood levels to increase effectiveness and reduce the side effects of oxicams and related compounds. Another great benefit of the transdermal administration of these pro-drugs is that administering medication, especially to children, will be much easier.

The invention relates to a quantitative analysis method of the plasma-drug concentration of a novel compound WSJ-557 in SD rat plasma. The method comprises the following steps of (1) adding methanol and internal standard working fluid into the SD rat plasma after the WSJ-557 intragastric administration; after the vortex, adding ethyl acetate for liquid-liquid extraction; then, performing vortex and centrifugation; taking liquid supernatant; (2) using octadecyl silane bonded silica gel as filling agents for chromatographic column treatment at the column temperature being 40 DEG C, wherein an ultra-high performance liquid chromatography system uses a general binary high-pressure pump and a sample feeding device; using a mixed solution of methanol-ammonium acetate water solution as a flowingphase; performing gradient elution; (3) using an ESI ion source as an ion source and a multi-reaction monitoring mode (MRM) for positive ion detection. The quantitative analysis ions are respectivelyWSJ-557:m/z316.1 to 260.0, m/z237.0 to 194.0; the collision energy is 15eV. The quantitative analysis method has the advantages that the specificity is high; the sensitivity is high; the sampling quantity of samples is small; the pretreatment is simple and fast; the analysis period is short and the like. The method is particularly applicable to the plasma-drug concentration determination and pharmacokinetic study of WSJ-557 in SD rat plasma.

The invention provides a riboflavin gastric-floating tablet and a preparation method thereof. The riboflavin gastric-floating tablet prepared by the method comprises the following raw materials in percentage by weight: 1%-5% of riboflavin, 10%-50% of hydroxypropyl methyl cellulose, 5%-25% of ethylcellulose, 2%-40% of hexadecanol, 5%-40% of lactose, 1%-10% of sodium bicarbonate, 1%-10% of light pharmaceutical calcium carbonate and 1%-10% of magnesium stearate. The riboflavin gastric-floating tablet is low in toxic and side effects of medication, has the functions of prolonging the action time of medicines, and maintaining stable plasma drug concentration; and the bioavailability of the medicine is improved.

The invention provides a compound simvastatin niacin sustained-release capsule and a preparation method thereof. In the compound sustained-release capsule preparation, each capsule comprises 200 to 500 mg of niacin and 20 mg of simvastatin. The compound sustained-release capsule is prepared by the following steps: preparing blank pills, preparing niacin sustained-release pills; preparing simvastatin sustained-release pills, and preparing capsules. The product is suitable for treating primary hypercholesterolemia and mixed dyslipidemia; according to the characteristics, the niacin part is used as the sustained-release part and the simvastatin is used as the immediate-release part to produce the compound preparation, so that all the components exert synergism in the body, exert the efficacy to the largest extent, reduce the toxic and side effects of the drug, reduce the fluctuation of the plasma drug concentration in the body and reduce the drug taking times of the patient; the efficacy on relieving hypercholesterolemia of the product is obviously superior to that of any single prescription preparation.

The invention provides a piribedil sustained-release tablet and a preparation method thereof. The piribedil sustained-release tablet comprises the following raw material components in percent by weight: 10-80% of piribedil, 1-70% of framework material, 10-80% of filler, 0.1-5% of lubricating agent and an appropriate amount of adhesive. The piribedil sustained-release tablet provided by the invention has the advantages that releasing rate of piribedil is increased, drug stability is improved, the defects that a drug therapeutic effect is reduced owning to fluctuation of plasma drug concentration is overcome, stable plasma drug concentration is maintained for a long time, motion complication caused by a dopamine receptor stimulated by fluctuation of drug concentration is avoided, the requirement of a continuous activated dopamine receptor is met, compliance of a patient is improved and a clinical effect of the piribedil sustained-release tablet is guaranteed.

The invention belongs to the technical field of ticagrelor and in particular relates to a ticagrelor slow-release preparation as well as preparation and application thereof. The ticagrelor slow-release preparation provided by the invention comprises at least one rapid release layer and at least one slow release layer, wherein each of the rapid release layer and the slow release layer contains theticagrelor; the mass ratio of the content of the ticagrelor in the rapid release layer to the content of the ticagrelor in the slow release layer is 1 to (3 to 7); the ticagrelor slow-release preparation is used as a medicine for anti-platelet treatment; on one hand, the preparation has reasonable plasma drug peak concentration; on the other hand, the residual ticagrelor is slowly released and stable plasma drug concentration is maintained; the anti-platelet treatment effect is good and the bleeding tendency is reduced; the preparation is orally taken once each day and has good patient compliance and high utilization safety; the preparation method of the ticagrelor slow-release preparation has the advantages of simple technology, relatively low cost and good practicability.

The invention relates to a slow release long-acting rasagiline transdermal patch with high bioavailability and a preparation method thereof. The patch is characterized in that effective amount of rasagiline and a substrate are contained, wherein the concentration of rasagiline is in the range of 0.1 mg/cm2 - 2 mg/cm2, every patch contains 1 mg - 10 mg of rasagiline, and the substrate contains one or more than two kinds of the following substances: acrylic polymers containing no carboxylic group and silicone polymers with silanol groups capped by alkyls. The time of maximum plasma drug concentration of the patch is prolonged to be 5 times or more that of oral tablets, and the bioavailability of the patch is 130 percent or more of that of oral tablets. The patch in the invention can be applied to effectively inhibit monoamine oxidase B (MAOB) for at least 3 days, in addition, the preparation method is simple and suitable for industrial production.

The invention discloses a lithium carbonate sustained release tablet. The sustained release tablet is prepared from lithium carbonate, a sustained-release material and other ingredients. The sustained-release material is a hydrophilic gel skeleton material or an erodible matrix material, wherein the other ingredients comprise an adhesive, a pore-foaming agent, a surfactant, a lubricant, a flow aid, filler, a disintegrant and a wetting agent. The lithium carbonate sustained release tablet has the advantages that administration times are reduced, the peak and valley phenomenon of plasma-drug concentration is avoided or reduced, a stable and lasting effective plasma-drug concentration is provided and the safety and the effectiveness of a drug are improved.

The invention relates to a special sustained-release preparation of natural antibiotics curcurbitacin, in particular to a membrane controlled or/and matrix release oral preparation with the composition as follows: curcurbitacin 5 to 20%, water insoluble medical macromolecular material 30 to 65%, water soluble medical macromolecular material 5 to 25%, and conventional auxiliary material 15 to 45%. The special sustained-release preparation of natural antibiotics curcurbitacin has the advantages of retarding the release of curcurbitacin from drug preparation, reducing the peak and peak valley for drug absorption, facilitating stable plasma drug concentration, and especially facilitating the disease treatment when the sustained release is combined with rapid release since the rapid release part can be rapidly released to produce the plasma drug concentration required for treatment as soon as possible, while the sustained release part can subsequently provide stable plasma drug concentration and reduce the fluctuation of plasma drug concentration.

An isosorbide dinitrate sustained-release preparation is a tablet which consists of isosorbide dinitrate, sustained-release materials and other pharmaceutical excipients, wherein, the sustained-release materials are selected from hypromellose (E4M) and carmellose sodium. As the drug is released in digestive tract according to the procedure after the oral administration, the effective plasma drug concentration in human body can be maintained stably and sustainedly, therefore the invention has the advantages of good healing efficacy, long drug effect, less side effects, small number of the times of the administration of the patients, convenient usage and so on; the invention not only has the function of treating and alleviating angina symptoms, but also has the special advantages of preventing sudden onset and protecting the daily lives of the patients and safely passing through the incidence peak of the diseases, therefore, the invention provides reliable means and great convenience for the treatment of the patients and the self-prevention of sudden onset; the price of the drug is cheap, which is conductive to the administration of ordinary patients.

The invention discloses a solvent of artesunate for intramuscular injection, and particularly relates to a solvent of artesunate for intramuscular injection, which has a slow release function and is used by animals. The solvent is prepared from the following components in percentage by volume: 20% of 1,2-propanediol, 15% of ethanolamine, 15% of polyvinylpyrrolidone-K15, and the balance of sterilewater for injection. The solvent can realize high solubility and safety of artesunate well, has the advantage of slow release at the same time, can maintain effective plasma drug concentration of a drug for a long time in an organism, and reduces the times of drug administration; and compared with oral administration and intravenous injection, the intramuscular injection is easier to operate in veterinary clinical practice.

The novel positively charged pro-drugs of arylanthranilic acids in the general formula (1) 'Structure 1' were designed and synthesized. The compounds of the general formula (1) 'Structure 1' indicated above can be prepared from mefenamic acid, meclofenamic acid, flufenamic acid, niflumic acid, flunixin, and related compounds, by reaction with suitable alcohols, thiols, or amines and coupling reagents, such as N, N'-Dicyclohexylcarbodiimide, N, N'-Diisopropylcarbodiimide, O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate, O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate, Benzotriazol-1-yl-oxy-tris (dimethylamino)phosphonium hexafluorophosphate, et al. The positively charged amino groups of these pro-drugs not only largely increases the solubility of the drugs, but also bonds to the negative charge on the phosphate head group of membranes and pushes the pro-drug into the cytosol. The results suggest that the pro-drugs diffuses through human skin ~200 times faster than does mefenamic acid, meclofenamic acid, flufenamic acid, niflumic acid, flunixin, and related compounds. It takes 2-4 hours for mefenamic acid, meclofenamic acid, flufenamic acid, niflumic acid, flunixin, and related compounds to reach the peak plasma level when they are taken orally, but these prodrugs only took about ~50 minutes to reach the peak plasma level when they are taken transdermally. In plasma, more than 90% of these pro-drugs can change back to the parent drugs in a few minutes. The prodrugs can be used medicinally in treating any NSAIAs-treatable conditions in humans or animals. The prodrugs can be administered not only orally, but also transdermally for any kind of medical treatments and thus avoid most of the side effects of NSAIAs, most notably GI disturbances such as dyspepsia, gastroduodenal bleeding, gastric ulcerations, and gastritis.

The invention discloses an uncaria slow-release pill preparation and a preparation method thereof. The uncaria slow-release pill preparation is prepared from 10-40 parts by weight of uncarine or rhomotoxine and 50-90 parts by weight of substrates, wherein the substrates comprise 40-60 parts by weight of hydrophilic substrates and 10-30 parts by weight of hydrophobic substrates. In the invention, the uncaria slow-release pill preparation is slowly released by a slow-release technique so that the fluctuation of plasma drug concentration can be effectively reduced, the phenomenon of 'peak valley' generated from frequent administration of the common preparation can be avoided, the utilization rate of the drug is improved, and medical expenses can be reduced; the uncaria slow-release pill preparation reduces the direct stimulation of the drug to gastrointestinal tracts to reduce the generation of side effects of the drugs and be easier for patients to tolerate, is beneficial to long-term treatment and is more beneficial to the treatment of hypertension. In addition, the process is simplified so that the uncaria slow-release pill preparation process is easy to operate, the uncaria slow-release pill preparation is easy to carry and take, the problems existing in the prior art are solved and the purpose of the invention is achieved.

The invention provides an ELISA (Enzyme-linked Immunosorbent Assay) kit for detecting methotrexate and application thereof. The kit is prepared from the following reagents: a methotrexate coated 96-pore microporous plate, a methotrexate monoclonal antibody, an antibody diluting solution, an HRP (Hypothalamic Regulatory Peptide)-labeled goat anti-mouse secondary antibody, a methotrexate standard product, a washing liquid concentrated solution, a sample diluting solution, a TMB (Tetramethylbenzidine) color-developing solution and a stopping solution. The stable, rapid and simple methotrexate detection kit is obtained through improving the combination of all reagents and improvement on parameters of the reagents; when the ELISA kit is applied, the standard deviation value of the kit is relatively small. The ELISA kit can be used for detecting the plasma drug concentration of patients who utilize the methotrexate with a large dosage and detecting the plasma drug concentration of patients who utilize the methotrexate with a small dosage.

The invention discloses a lurasidone hydrochloride nano mixed suspension solution for durable intramuscular injection and a preparation method of the nano mixed suspension solution. The raw materialsof the nano mixed suspension solution comprise 0.1-0.5 wt.% of lurasidone hydrochloride and 0.1-0.3 wt.% of a stabilizer, and a solvent is water for injection. Through high-speed dispersion, in combination with a wet-method medium grinding method, the lurasidone hydrochloride is prepared into the nano mixed suspension solution for intramuscular injection, the first-pass effect is avoided, and thesolubility and dissolution rate of the medicine after muscle injection are improved. After muscle injection, the effect can be achieved continuously for 3-7 days, the drug administration frequency isreduced, fluctuation of the plasma drug concentration is reduced, and the compliance and safety of a patient during medicine taking are improved.