25 results about "Effective drug concentration" patented technology

The invention discloses an application of harmine or a pharmaceutical salt thereof in preparation of an antiviral drug. The drug micromolecule harmine hydrochloride screened from a natural product library can significantly inhibit cracking and replication of KSHV, the application of harmine in KSHV virus resistance is reported for the first time, the effective drug concentration is low, high biosafety is achieved, and a new solution is provided for KSHV treatment.

The invention discloses a decellularized amniotic membrane matrix composite scaffold, a preparation method thereof and application of the decellularized amniotic membrane matrix composite scaffold in orbital bone defect repair, and relates to the technical field of biomedical engineering and biomedical materials. In order to solve the limitation of an existing orbit implant material, methacrylic anhydride (MA) is grafted to HAM, methacrylate HAMMA hydrogel is synthesized, and then the decellularized amnion matrix composite scaffold (HAMMA / HAP / BMP-2) is prepared by combining a simulated body fluid biomimetic mineralization method with 3D printing and ultraviolet curing. The composite scaffold material prepared by the invention can regulate the release of BMP-2 and maintain the effective drug concentration of a bone defect area so as to regulate the immune microenvironment of an early bone defect repair area, collect osteoblasts and accelerate the repair of bone defects.

The present invention relates to a sustained-release injectable composition containing dutasteride. Compared with the conventional Avodart (registered trademark) taken once a day, even if the dosage of dutasteride is the same as or less than that of Avodart, it is possible to show a sustained release effect of dutasteride for 3 months or more, and a long-term drug-taking effect can be shown by a single injection. In addition, it can show a therapeutic effect on benign prostatic hyperplasia, prostate cancer, and hair loss continuously for 3 months or more. The microparticles contained in the sustained-release injectable composition have a constant average diameter, can regulate the release of the drug, and maintain a constant effective drug concentration, and can reduce the foreign body sensation and pain when administered to patients as an injection.

The invention discloses an anti-tumor pharmaceutical composition with a synergistic effect and application thereof, the composition is composed of cis-platinum and atorvastatin, and the molar ratio of the cis-platinum to the atorvastatin is 1: 1.5; the invention provides a different drug concentration ratio scheme for treating cancer cells, inhibiting proliferation and activation of cancer cells and inducing apoptosis of the cancer cells by drug combination at low drug concentration, and compared with a traditional scheme, the scheme weakens drug resistance of the cells, and has the advantages of lower concentration, safer and more effective drug concentration ratio and higher safety. The toxic reaction of an organism caused by high-concentration drugs is weakened.

This invention discloses a compound traditional Chinese medicine powder inhaler for respiratory tract infections and its preparation method, relating to the field of pharmaceutical formulation technology. The compound traditional Chinese medicine powder inhaler for respiratory tract infections is composed of polysaccharide composite gel microspheres, forsythia, scutellaria, honeysuckle, and isatis root. The polysaccharide composite gel microspheres are composed of seaweed sulfated polysaccharide, lentinan, calcium chloride, and curcumin. Seaweed sulfated polysaccharide, lentinan, curcumin, and calcium chloride cross-link to form a three-dimensional network spherical structure, improving the particle morphology and flowability of the micropowder. Furthermore, due to its good hygroscopic and moisturizing properties, it competitively reduces the moisture absorption of the micropowder, preventing aggregation and further improving flowability. In addition, the gel microspheres have excellent adhesion, adhering to the infection site after entering the respiratory tract, reducing expulsion losses due to respiration, maintaining an effective drug concentration at the infection site, and improving therapeutic efficacy.

The invention relates to the technical field of vascular therapy, in particular to a nano-drug and a preparation method thereof.The nano-drug comprises a nano-carrier, a therapeutic drug and cross-linked protein are loaded on the nano-carrier, the cross-linked protein is at least partially loaded on the surface of the nano-carrier, and the cross-linked protein is at least one of silk fibroin, sericin and silk fibroin peptide; the therapeutic drug is at least partially loaded in the nano-carrier. On one hand, cross-linked protein on the surface of the nano-carrier is promoted to be cross-linked with protein in a blood vessel by initiating the photosensitive cross-linking agent, and the nano-carrier is anchored in the blood vessel, so that the risk that nano-drug particles are eluted from the blood vessel wall is greatly reduced; on the other hand, cross-linking of cross-linked protein on the surface of the nano-carrier can be promoted by initiating the photosensitive cross-linking agent, so that the surface of the nano-carrier is gelatinized, the slow release speed of the nano-drug anchored in the blood vessel is more lasting, and further effective drug concentration can be maintained for a long time, restenosis of the blood vessel is inhibited, and the treatment effect is improved.

The present invention discloses a crystal form, a preparation method and an application of a 4′-substituted nucleoside compound I having the following structure, including salts, prodrugs, and compositions thereof. Animal pharmacokinetic studies demonstrated that the effective drug concentrations of Compound Ia and Compound Ig in HIV target cells, peripheral blood mononuclear cells (PBMC), were effective in inhibiting HIV replication after 7 and 5 days, respectively. Therefore, Compound I can be used as a long-acting drug for preventing and treating AIDS. R is selected from ethynyl, azide, and cyano groups, X is selected from hydrogen and fluorine, and B is selected from B1 and B2.

The invention discloses an oral care composition for preventing and treating periodontitis, the oral care composition comprises a compound shown in a formula (I) and oral auxiliary materials, by controlling the concentration or dosage of a component (a) in the oral care composition, the oral care composition can generate the effective drug concentration in the range of 1.35-13mM in the oral cavity after being applied to the oral cavity, and the oral care composition can be used for preventing and treating periodontitis. According to the invention, porphyromonas gingivalis can be more effectively inhibited, and meanwhile, a beneficial bacterium lactobacillus reuteri and the total amount of flora in oral cavities of healthy people are not substantially influenced, so that the oral flora microenvironment and flora imbalance can be effectively improved, and oral related diseases can be further avoided or prevented.

Disclosed are an epsilon-poly-L-lysine-based drug conjugate, an intermediate thereof, and an application thereof. The present invention provides an epsilon-poly-L-lysine derivative-drug conjugate that has a controllable group coupling number and controllable group coupling sites and that is represented by formula (I). The drug conjugate of the present invention has one or more among the effect advantages of low renal clearance rate, low liver and spleen clearance rate, long plasma half-life, rapid accumulation of effective drug concentration in lesions, and a better therapeutic effect.

The invention discloses an injectable photo-crosslinking hydrogel loaded with pseudolaric acid as well as a preparation method and application thereof. The preparation method comprises the following steps: 1) respectively dissolving Gelma and HAMA in sterile PBS (Phosphate Buffer Solution) according to the dosage required by a final system; 2) mixing the two solutions, and adding a photoinitiator LAP pre-dissolved in the sterile PBS at 60 DEG C; 3) dissolving golden larch bark acetic acid in dimethyl sulfoxide to prepare a medicine solution with the concentration of 1.0 mg / mL, and then adding the medicine solution into the precursor solution under the condition of continuous stirring; and 4) carrying out 405 nm illumination crosslinking on the obtained precursor solution to form the hydrogel. The hydrogel three-dimensional network can continuously and controllably release pseudolaric acid, maintains a long-acting effective drug concentration at an infected part, shows a strong inhibition effect on a candida albicans standard strain and a clinical drug-resistant strain, and has a good application prospect in a model for treating candida vaginitis and fungal skin wound infection. And all the components show a remarkable'anti-infection-repair promoting 'integrated treatment effect.

The invention provides an anus suppository for treating prostatitis and a preparation method thereof, and relates to the technical field of pharmaceutical preparations. The anus suppository for treating prostatitis comprises an outer-layer sleeve and suppository contents, wherein the suppository contents comprise a heat-clearing and inflammation-diminishing layer, a warming, dredging and blood-activating layer and a qi-tonifying and kidney-tonifying layer which are sequentially distributed from outside to an inner core, and at least part of the suppository contents are wrapped by the outer-layer sleeve. The outer-layer sleeve prevents a large amount of medicine from being discharged after being released in a short time by delaying initial dissolution of a suppository matrix, and can contain dissolved suppository contents so as to prevent the dissolved suppository contents from flowing out of a body due to rectum peristalsis, so that the effective action time of the medicine is prolonged, and the curative effect of the suppository is improved. The medicine effect of the suppository content is fully exerted, and the use experience of a patient is improved; the medicine components permeate outwards at a controllable speed through the permeation part, the local effective medicine concentration of the rectum is maintained, the suppository matrix is gradually dissolved under the action of body temperature, and the traditional Chinese medicine composition is continuously released.

The invention provides a sustained-release and quick-release coated tablet and a preparation method thereof, and belongs to the technical field of biological medicines. The outer layer of the core-coated tablet is the quick-release layer, the inner layer of the core-coated tablet utilizes the coating to prolong release, and the core-coated tablet is used as the slow-release layer to realize double-phase release of drugs, so that time-sharing release and outer-layer quick release after single administration are realized, drug peak concentration and effective drug concentration can be reached in a short time after administration, and the inner layer is slowly released by virtue of the coating material; the sustained-release rate is not influenced by the pH value of the intestinal tract, the force of peristalsis and extrusion of gastrointestinal tracts can be borne, the problem that the sudden release rate of the medicine is large in deviation is avoided, and the sustained-release preparation is safer and more effective.

The present invention relates to microparticles containing tilzepatide or a pharmaceutically acceptable salt thereof, and a biocompatible polymer, a method for producing the same, and a pharmaceutical composition containing the same. The microgranulocytes containing tilzepatide according to the present invention exhibit stable drug release over a long period, maintaining effective drug concentrations in the blood over a long period. This extends the drug administration cycle, improves patient adaptation to medication, and reduces side effects caused by rapid initial drug release.

The utility model relates to a joint space occupying device which comprises a space occupying assembly and a supply device, and the supply device is arranged in the space occupying assembly in a sealed mode. The supply device comprises a liquid storage container and supply equipment; the liquid storage container is provided with a first liquid conveying opening, the occupying assembly is provided with a second liquid conveying opening, the first liquid conveying opening is communicated with the second liquid conveying opening through a liquid conveying pipe, and the supply equipment drives liquid in the liquid storage container to be discharged out of the occupying assembly through the liquid conveying pipe. Before installation is completed, the liquid storage container is filled with antibiotic medicine, after the occupied assembly is integrally installed in place, when medical staff need to give antibiotics to a patient, the medical staff only needs to control the supply equipment, the supply equipment drives liquid in the liquid storage container to flow out of the first infusion opening, and the liquid is discharged out of the occupied assembly from the second infusion opening through the infusion tube; the joint spacer can release antibiotics, the local effective drug concentration of a joint cavity part is maintained, drugs can be supplied according to actual needs, and the joint spacer has the advantage of being high in use flexibility.

The invention discloses an anti-hair loss composition containing a cacumen biotae extract as well as a preparation method and application of the anti-hair loss composition, and belongs to the field of daily chemical products. The anti-hair loss composition comprises the following components: a cacumen biotae extract, acetyl tetrapeptide-3, a poloxamer solution, a carbomer swelling solution, an emulsifier, a surfactant, a penetration enhancer and a humectant. The anti-hair-loss composition is prepared by the following steps: S1, dispersing a cacumen biotae extract, an emulsifier and a surfactant to obtain an active matter oil phase; s2, mixing the poloxamer solution and the carbomer swelling solution with a penetration enhancer and a humectant, adding the active matter oil phase, and dispersing to form an emulsion; and S3, after the emulsion is cooled, adding a pH regulator, then adding acetyl tetrapeptide-3, and defoaming, thereby obtaining the product. The anti-alopecia composition provided by the invention can form gel when in use, and is continuously and slowly released, so that hair follicles are exposed to an effective drug concentration for a long time, and the effect of the anti-alopecia composition is improved.

The invention discloses a kinesio tape with massage particles and a preparation method thereof, and relates to the technical field of kinesio tapes, the kinesio tape sequentially comprises a tape layer, an adhesive layer, a particle adhesion layer and an isolation layer from top to bottom, and the side, opposite to the isolation layer, of the particle adhesion layer is provided with a plurality of massage particles. According to the kinesio patch with the massage particles and the preparation method of the kinesio patch, through the arrangement of the massage particles, hyaluronic acid between cells can be decomposed, medicine permeability is improved, and medicine contained in the patch layer can be better absorbed by skin; meanwhile, drug release can be delayed, so that the drug action time is prolonged, and the local effective drug concentration is maintained; a basis is provided for cell attachment and proliferation, and repair and regeneration of damaged muscle tissues are facilitated; the massage particles have the effects of resisting bacteria and promoting wound healing, can prevent skin infection possibly occurring in the use process of the patch, and are beneficial to recovery of muscle injury; the sticking effect of the patch is improved, and meanwhile, the irritation to the skin can be reduced.

The invention provides an anus suppository for treating sphincter relaxation and a preparation method of the anus suppository, and relates to the technical field of pharmaceutical preparations. The anus suppository for treating sphincter relaxation comprises an outer-layer sleeve, a suppository matrix and a traditional Chinese medicine composition, the outer-layer sleeve is an oval tube with an opening, the outer-layer sleeve comprises a sealing part and a permeating part, the sealing part is located at the end, away from the opening, of the outer-layer sleeve, and at least part of the suppository matrix is wrapped by the outer-layer sleeve. The sealing part prevents a large amount of medicine from being discharged after being released in a short time by delaying initial dissolution of a suppository matrix, and can contain dissolved suppository contents so as to prevent the dissolved suppository contents from flowing out of a body due to rectum peristalsis, so that the effective action time of the medicine is prolonged, and the curative effect of the medicine is improved. The medicine effect of the suppository content is fully exerted, and the use experience of a patient is improved; the medicine components permeate outwards at a controllable speed through the permeation part, the local effective medicine concentration of the rectum is maintained, the suppository matrix is gradually dissolved under the action of body temperature, and the traditional Chinese medicine composition is continuously released.

This invention relates to the field of pharmaceutical chemistry, specifically to a Devimistat derivative with mitochondrial targeting function, its preparation method, and its application in antitumor drugs. This derivative covalently couples the mitochondrial-attractant 3-aminopropyl(triphenyl)phosphine bromide (TPP) group to the antitumor active molecule Devimistat, utilizing the affinity of the TPP cation for the mitochondrial transmembrane potential to drive the drug's specific accumulation in the mitochondrial matrix. While retaining the original drug's interference with the tricarboxylic acid cycle and inhibition of PDH and KGDH complex activity, this derivative significantly increases the effective drug concentration within tumor cells, thus solving the problem of limited efficacy of Devimistat due to its lack of targeting.

This application provides a soluble microneedle patch for treating nail fungal infections. The microneedles in the patch comprise: 0.1-7% of a drug component by weight, with the remainder being a matrix component. The matrix component comprises macromolecules with polar bonds having an average molecular weight of 0.05-30,000, macromolecules with polar bonds having an average molecular weight of 100,000-900,000, and macromolecules with polar bonds having an average molecular weight of 1,000,000-2,600,000. The drug component and microneedles work together to allow the drug to penetrate the nail plate directly to the deep connective tissue of the nail bed, killing the fungus. The patch exhibits high effective drug concentration, strong transdermal ability, significant therapeutic effect, no irritation, and no toxic side effects. Furthermore, the microneedles demonstrate excellent short-term rapid treatment and long-term sustained-release therapeutic effects.

This invention belongs to the field of veterinary drug formulation technology, specifically relating to the preparation and application of a novel uterine injection for dairy cows. The uterine injection is obtained by dissolving poloxamer and other drugs in a solvent. It remains in a solution state at low temperatures, facilitating drug administration. In the uterine environment, it forms a gel in situ. This gel state prolongs the drug's retention time within the uterus, avoiding the rapid loss associated with traditional solutions. Simultaneously, it achieves sustained drug release, increases the local effective drug concentration, and enhances the bactericidal and anti-inflammatory effects. The gel structure provided by this invention is stable, exhibits good sustained-release effect, and demonstrates excellent biocompatibility, showing promising application prospects.

This utility model relates to the field of capsule technology and discloses a double-layer capsule for intestinal targeted drug delivery, comprising: an outer layer and an inner layer, the inner layer being disposed inside the outer layer, and a connecting sealing layer disposed on the outside of the inner layer. The outer layer has an outer thickness of 0.1–0.5 mm. The inner layer employs microporous membrane controlled-release technology, has a thickness of 0.5–2 mm, and includes a microporous membrane layer made of ethyl cellulose. The microporous membrane layer has micropores with a diameter of 0.1–10 micrometers on its outer surface. The connecting sealing layer is disposed between the outer and inner layers. The outer layer includes a hydroxypropyl methylcellulose phthalate shell, and the inner cavity of the inner layer has an inner liner layer, the inner cavity of which has an inner plate. This double-layer capsule for intestinal targeted drug delivery can achieve continuous drug release in the intestine, ensuring that an effective drug concentration is maintained in the intestine, thereby acting more effectively on the intestinal lesion site and improving the therapeutic effect on intestinal diseases.

The application discloses application of dehydropeimine or a pharmaceutical salt thereof in preparation of an antiviral medicine. The small-molecule dehydropeimine hydrochloride screened from a natural product library can significantly inhibit KSHV lytic replication, and the application of dehydropeimine in KSHV antiviral treatment is reported for the first time. The effective drug concentration is low, and the dehydropeimine has high biological safety. The application provides a new solution for KSHV treatment.

The present invention relates to a sustained-release injectable composition containing dutasteride, which can produce a sustained dutasteride release effect for more than 3 months even when the dosage of dutasteride administered is the same or lower than that of conventional once-daily Avodart®, thereby enabling a sustained drug administration effect for a long period of time with a single injection. In addition, it can continuously provide therapeutic effects for benign prostatic hyperplasia, prostate cancer, and hair loss for more than 3 months, and the microparticles included in the sustained-release injectable composition have a constant average diameter, so the release of the drug can be controlled to maintain a constant effective drug concentration, and the foreign body sensation and pain when administered to a patient as an injection can be reduced.

The application discloses a bone marrow cavity targeted drug release microsphere and belongs to the technical field of medical devices. The drug release microsphere is spherical in structure and contains drugs, and can be implanted into the inside of a bone marrow cavity. The spherical structure is suitable for the microenvironment of the bone marrow cavity, and after implantation, the drug release microsphere is freely distributed, does not press and does not damage tissues, fully contacts with bone marrow fluid, guarantees the global uniform dispersion of drugs, locally releases drugs for a long time, maintains the effective drug concentration in the bone marrow cavity, has remarkable treatment effect, and rarely enters the whole body circulation, greatly reduces the side effects of drugs on the whole body, is minimally invasively implanted, is simple to operate, has small trauma, is fast in postoperative recovery, reduces the treatment cost and physical burden of patients, is preferably made of a degradable medical biocompatible material, has no immune rejection, can be synchronously degraded and has no residue, does not need secondary surgery, and is high in clinical safety. The drug release microsphere can be flexibly designed in specification, drug type and loading mode, is wide in clinical adaptability, can be used alone or in combination with other devices, and is rich in application scenarios.

The invention belongs to the technical field of traditional Chinese medicines, and particularly relates to a traditional Chinese medicine composition and liposome for dispelling effects of alcohol and protecting liver as well as a preparation method and application thereof. The traditional Chinese medicine composition for dispelling the effects of alcohol and protecting the liver is prepared from the following raw materials in parts by mass: 1-100 parts of semen hoveniae, 1-100 parts of flos puerariae and 1-100 parts of radix puerariae. The hovenia dulcis thunb, the flower of kudzuvine and the root of kudzu vine are used as raw materials, and the hovenia dulcis thunb, the flower of kudzuvine and the root of kudzu vine are in synergistic interaction, so that the hovenia dulcis thunb, the flower of kudzuvine and the root of kudzu vine have the effects of dispelling effects of alcohol and protecting liver, have definite effects of improving liver functions and liver pathology on liver injury caused by ethanol, and are Furthermore, compared with common oral dosage forms, lipidosome, paste and patch prepared from the traditional Chinese medicine composition can bypass the first-pass effect of the liver, reduce decomposition of the medicine in the metabolic process, improve the effective medicine concentration and further improve the effects of dispelling the effects of alcohol and protecting the liver.