148 results about "Drugs stability" patented technology

The invention relates to a layered drug-loading microneedle patch as well as a preparation method and application thereof. The preparation method of the layered drug-loading microneedle patch comprises the following steps: S1, dissolving a drug and a soluble high-molecular polymer in a solvent according to a mass ratio of (2: 1)-(1: 12) to form a needle tip solution, then filling a needle tip cavity of a microneedle mold with the needle tip solution, drying, and removing redundant drug residues on the surface to form a drug-loading needle tip layer; and S2, filling a mold containing the drug-loading needle tip layer with a photocurable polymer, performing ultraviolet curing for 10-30 seconds under the wavelength of 365-405 nm, and then performing demolding to form a substrate layer, thereby obtaining the layered drug-loading microneedle patch. According to the method, one-time filling of the needle tip part is successfully achieved by combining needle tip auxiliary material proportion optimization, meanwhile, the curing process is rapid, the medicine utilization rate and the process stability are remarkably improved, the medicine stability is good, and the method is suitable for industrial production.

The invention relates to the technical field of drug analysis, and discloses an intelligent drug stability analysis and monitoring system, which comprises a drug information acquisition module, a drug stability analysis module, a drug prediction module, a dynamic regulation and control module and an early warning display module, through the arrangement of the drug stability analysis module and the drug prediction module, the drug storage environment is analyzed to obtain the stability condition of the drug, then the remaining validity period of the drug is obtained, and the stability change of the drug is monitored in real time to prolong the remaining validity period of the drug; meanwhile, liquid medicine and solid medicine are subjected to special analysis, the degradation rate constant of the medicine is obtained on the basis of a second improved Arrhenius formula for the solid medicine, and a physical property cross-border line is set, so that the stability of the medicine is improved by analyzing the stability of the medicine and regulating and controlling environmental parameters, and the stability of the medicine is improved. The medicine validity period and storage time are prolonged, and the storage strategy is dynamically adjusted in combination with medicine chemical characteristics.

The present invention relates to a novel pomalidomide derivative that exhibits improved pharmacological effects compared to pomalidomide, and is used to treat brain diseases. The novel pomalidomide derivative developed in the present invention has excellent binding ability to cereblon, is almost non-cytotoxic, has low possibility of teratogenic side effects, and can regulate TNF-α expression, as well as suppress oxidative stress and has excellent in vivo pharmacokinetic stability, and shows excellent effects of improving the decrease in motor ability, which is a symptom of Parkinson's disease, and increasing the expression of tyrosine hydroxylase, which is decreased in Parkinson's disease, and can be used for the prevention or treatment of brain diseases such as Parkinson's disease.

The invention relates to the field of drug stability evaluation, in particular to an anti-generative drug stability evaluation system and method. Comprising a confrontation sample simulation module, a drug stability test module and an intelligent identification module. The system generates an anti-noise, self-adaptive and stable adversarial sample based on a drug molecular structure, and predicts drug stability under different conditions through environmental physical simulation and a digital twinborn model. And the intelligent identification module executes molecular fragment sensitivity analysis, predicts stability under extreme conditions and outputs an evaluation report. The system solves the problems of efficiency, precision and application range in the prior art, realizes qualitative change evaluation through innovative technology combination, provides a scientific basis for drug research and development, transportation and storage, and remarkably improves the drug stability evaluation level.

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses a cyclophosphamide ternary nano-micelle and a preparation method thereof.The cyclophosphamide ternary nano-micelle prepared through the method can be used for treating malignant lymphoma, multiple myeloma, leukemia, breast cancer, ovarian cancer, cervical cancer, prostatic cancer, colon cancer, bronchial cancer, lung cancer and the like. Reasonable preparation steps and a preparation formula are adopted, the use of an organic reagent is reduced, the irritation of cyclophosphamide is reduced and the stability of the micelle is improved by adjusting a freeze-drying technology, and the cyclophosphamide micelle adopts amphiphilic macromolecules as a carrier material, so that the drug loading capacity and the stability of the micelle are obviously improved, and the bioavailability of the micelle is improved. The ternary nano-micelle system has the advantages that the solubility of cyclophosphamide is improved, the in-vivo bioavailability is increased, the preparation method is simple, the micelle performance is stable, and large-scale industrial production is facilitated.

The present invention provides a binary or ternary complex. The complex can improve the stability of a drug, and in particular, inhibit the transesterification reaction within drug molecules. The complex can also improve the efficacy formulation performance of the drug, improving the safety and effectiveness of the drug.

The invention relates to a pharmaceutical composition of a compound shown in a formula (I) or a salt thereof, a preparation and a preparation method thereof. Specifically, the invention discloses a pharmaceutical composition taking a compound as shown in a formula (I) or pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition contains a compound as shown in a formula (I) or pharmaceutically acceptable salts thereof and pharmaceutically acceptable auxiliary materials. The pharmaceutical composition provided by the invention has good pharmaceutical stability and safety, and the preparation method is simple and convenient and is suitable for industrial production. # imgabs0 #

The invention discloses an anti-inflammatory and pain-relieving cataplasm capable of improving drug stability and a preparation method thereof, and belongs to the technical field of traditional Chinese medicines. The inflammation diminishing and pain relieving cataplasm is prepared from the following raw material components: methyl salicylate, eucalyptus oil, synthetic menthol, camphor, borneol, thymol, belladonna liquid extract, diphenhydramine hydrochloride, DL-tartaric acid, gelatin, titanium dioxide, PVP, sorbitol, beta-cyclodextrin, dihydroxyaluminum aminoacetate, castor oil, partially neutralized sodium polyacrylate, glycerol and purified water. Through process improvement and inclusion of volatile materials in the formula with beta-cyclodextrin, the prepared inflammation-diminishing and pain-relieving cataplasm has the characteristics of good stability and capability of remarkably improving in-vitro drug release.

The invention relates to the technical field of pharmaceutical preparations, in particular to a solid dispersion-based sustained-release drug composite carrier as well as a preparation method and application thereof. The preparation method comprises the following steps: carrying out synergistic spray drying on double polymers (hydroxypropyl methylcellulose acetate succinate and polyvinylpyrrolidone-vinyl acetate copolymer) to form a solid dispersion; compounding with mesoporous silica and calcium silicate for localization, and spraying ethanol to activate pores; calcium stearate and magnesium stearate are sequentially added for lubrication; prefabricating a sustained-release skeleton master batch; and finally, mixing, rolling and forming. According to the method, through hierarchical structural design, the drug stability, the powder fluidity and the release controllability are remarkably improved, the method is suitable for industrial production of the dihydroergoline mesylate sustained release preparation, and a release curve is smooth and reliable.

The invention belongs to the technical field of pharmaceutical preparations, and relates to a compound I patch composition, a compound I patch and a preparation method thereof. The patch composition comprises the following components in parts by weight: 0.5-12 parts of a pharmaceutical active component, 10-30 parts of a penetration enhancer, 15-56 parts of a crystal inhibitor and 35-57 parts of an acrylic acid pressure-sensitive adhesive, the patch composition also comprises solvent dimethyl sulfoxide and absolute ethyl alcohol, and the residual quantity of the dimethyl sulfoxide is not less than 2.0%; wherein the active pharmaceutical ingredient is a compound I, and the structural formula of the compound I is shown in the specification. According to the patch composition containing the compound I, the medicine stability is high, medicine crystallization and impurity generation are effectively avoided or reduced, and the patch containing the compound I has higher stability and safety; the patch composition containing the compound I has more appropriate drug permeability, so that the patch containing the compound I has higher drug effectiveness.

The invention discloses a gelatinized and / or micronized nucleoside drug and a preparation method thereof, and belongs to the technical field of drugs. The preparation method comprises the following steps: mixing lipoic acid, a nucleoside drug and an esterification catalyst, carrying out a grafting reaction in a reaction solvent to obtain a lipoic acid grafted nucleoside drug, dispersing the lipoic acid grafted nucleoside drug in an organic solvent to obtain a dispersion liquid, dropwise adding the dispersion liquid into hot water, and carrying out ring opening polymerization to obtain the lipoic acid grafted nucleoside drug. The nucleoside drug nanogel, nanoparticle or nanofiber is obtained, and the structure and performance improvement based on the drug itself is realized. The gelated and / or micronized nucleoside medicine prepared by the invention has obviously improved scavenging rates of DPPH free radicals and ABTS free radicals, and the method can improve the oxidation resistance of the nucleoside medicine and has the characteristic of improving the stability and functionality of the medicine.

The invention provides a nanocrystalline composite oral ulcer film agent as well as a preparation method and application thereof. The nanocrystalline composite oral ulcer film agent comprises a waterproof backing layer and a drug-loading adhesion layer coated on the waterproof backing layer, the drug-loaded adhesion layer comprises a macromolecular hydrogen bond compound formed by a weakly acidic polymer and a nonionic proton receptor polymer, and a nanocrystalline drug. Compared with the prior art, the preparation method has the advantages that the polyacrylic acid polymer and the nonionic cellulose polymer interact to form IPC serving as an adhesion layer film-forming material, the nanocrystals are loaded into the adhesion layer film-forming material, the waterproof backing layer is coated with the adhesion layer film-forming material, and the oral ulcer film agent is prepared after drying and cutting. The obtained film agent has good comfort and adhesive power, shows good drug stability and permeation promotion performance, can be used as a carrier of an oral administration route, prolongs the drug action time and improves the curative effect. The preparation method of the film agent is simple and easy for industrial mass production.

The invention discloses a ruthenium complex as well as a preparation method and application thereof, and belongs to the technical field of organic synthesis. The polypyridine ligand and the ruthenium dimer are combined through the substitution reaction, the chelate of the polypyridine ligand and the ruthenium aromatic hydrocarbon is obtained, the synthesis process is simple, the cost is low, and the chelate can be combined with an existing medicine to improve and enhance the medication curative effect. The prepared ruthenium complex can effectively inhibit cancer cell proliferation, and especially shows an excellent anti-proliferation effect on cervical cancer cells. And the liposome can improve the lipophilicity / lipophilicity of the ruthenium medicines and increase the stability of the medicines, and has better anti-tumor activity compared with platinum medicines and unmodified ruthenium medicines.

The invention relates to the technical field of pharmacy, in particular to a saxagliptin oral preparation and a preparation method thereof. The preparation is prepared from the following components in parts by weight: 5 to 15 parts of saxagliptin or salt thereof, 15 to 30 parts of sodium alginate, 10 to 20 parts of chitosan, 10 to 25 parts of polylactic acid-glycolic acid copolymer (PLGA), 5 to 15 parts of polyvinyl alcohol, 3 to 8 parts of N-acetylcysteine, 2 to 6 parts of vitamin E and 1 to 5 parts of sodium lauryl sulfate. According to the present invention, the drug stability is significantly improved, the chitosan and the sodium alginate are subjected to the polyelectrolyte composite reaction to form the stable gel so as to effectively protect the active components of the drug, and the freeze drying treatment ensures the uniform dispersion and the efficient dissolution of the drug, improves the bioavailability, and enables the drug to be rapidly and fully absorbed and utilized; according to the preparation method, the flexibility of the preparation is improved, the preparation can be easily processed into different dosage forms such as tablets and capsules, the requirements of different patients are met, all the components act synergistically, and the medicine performance is jointly improved.

The present invention provides binary or ternary complexes capable of improving the stability of a drug, particularly inhibiting transesterification within a drug molecule. The compound can also improve the pharmacodynamic preparation performance of the medicine and improve the safety and effectiveness of the medicine.

The invention discloses a preparation method of olmacycline tosylate for injection, belongs to the technical field of pharmaceutical preparations, and provides a special preparation and a preparation method of the olmacycline tosylate for injection in order to solve the problems that the olmacycline tosylate for injection is prone to epimerization and oxidative degradation and the room temperature stabilization time is short after redissolution. According to the preparation, omagazines tosylate is used as a main component and matched with glycerol, vitamin C, thioglycerol, sodium acetate and water for injection, and the pH is adjusted to a proper range through hydrochloric acid or sodium hydroxide. According to the method, by means of the synergistic effect of glycerin and vitamin C, glycerin fixes medicine molecules and protects vitamin C, vitamin C removes oxidation inducements, and thioglycerin is matched to assist in inhibiting degradation, so that the medicine stability is greatly improved, the redissolved liquid medicine can be stabilized at 25 DEG C for 72 hours, the total impurities are controlled at a low level, and the clinical actual requirements are met.

The present invention relates to a composition of aliphatic emulsion preparation for malignant thoracicoabdominal hydrops and its preparation method. It is made up by adopting pure natural anticancer medicine elemene and at least one polysaccharide selected from ginseng polysaccharide, astragalus polysaccharide, acanthopanax polysaccharide and lyceum polysaccharide as raw material. Said invention can obviously raise solubility of medicine, increase stability of medicine, effectively remove and kill cancer cells and raise immunity of body.

This invention arrests the hydrophilic silicone macrochains into semi-interpenetrating polymer network via in situ photo-gelation assisted 3D microextrusion printing technique. The printed hybrid hydrogel has shown microporous morphology with tunable diffusion behaviour. The flow behaviour of the hydrogel has been tested showing high elastic modulus, low tan δ, high gel strength, and delayed network rupturing behaviour. The uniaxial compression test showed the almost zero permanent set which could promote it as an elastomer mimetic soft biomaterial. Moreover, the drug loading into the hydrogel has been performed which showed hydrophilic silicone dependent non-Fickian anomalous transport. The encapsulated drug stability inside hydrogel matrices also showed no deterioration of the pristine drug molecules even after one month storage. This could be the first hydrodrophilic silicone based soft biomaterial will serve as an excellent controlled drug delivery device.

The invention belongs to the technical field of medicine manufacturing, and particularly relates to a compound preparation containing faropenem sodium as well as a preparation method and application of the compound preparation. According to the invention, the production prescription is optimized, the stability of the medicine can be effectively improved, the unpleasant smell of the medicine is covered, and the medication compliance of children is obviously improved. The epigallocatechin-aluminum complex can serve as a free radical scavenger in a preparation system, oxygen free radicals are effectively captured and neutralized, and the influence of oxidative stress on the medicine is reduced; moreover, the existence of aluminum ions not only enhances the stability of EGCG, but also reduces the drug degradation reaction under the catalysis of the ions through chelation with trace metal ions (such as iron, copper and the like) in the preparation. In addition, aluminum ions can also directly form a stable complex with faropenem sodium, so that the chemical stability of the faropenem sodium is further improved.

The present invention discloses a method for evaluating the stability of antibody-drug conjugates, which includes using orthogonal experimental grouping to investigate the use of antioxidants, the participation of oxygen, and the incubation pH value, simulating the time of ADC drugs in the systemic circulation, investigating the changes in the appearance after long-term plasma incubation under different incubation conditions, and searching for specific metabolites. By comparing the peak intensities of specific metabolites, the incubation effect is evaluated. Only the system conditions that can detect specific predicted metabolites are considered to be the environments that normally produce metabolism. The intensity level of specific metabolites can be used to evaluate the quality of the incubation system conditions; the present invention for evaluating the stability of ADC drugs can effectively solve the problem of how to better extend the blood system incubation time, filling the blank of the stability evaluation system for this new type of drug, antibody-drug conjugates.

This application belongs to the field of biomedicine, specifically relating to a method for preparing an antitumor composition for pets, aiming to solve the technical problems of low bioavailability, poor stability, and poor drug administration compliance of poorly soluble active ingredients in antitumor drugs for pets. The method includes: a raw material pretreatment step, in which curcumin, resveratrol, quercetin, green tea polyphenols, and astragalus polysaccharides are pulverized and sieved separately; an organic phase preparation step, in which egg yolk lecithin and solid lipids are dissolved in an ethanol-acetone mixed solvent, and curcumin and resveratrol are added and dissolved by stirring in a water bath; an aqueous phase preparation step, in which poloxamer F68 is dissolved in purified water and dissolved in a water bath; a high-pressure homogenization step, in which a nanoemulsion containing a solid lipid core is prepared; a moderately polar component encapsulation step, in which quercetin and green tea polyphenols are ultrasonically dispersed and then added dropwise to the nanoemulsion; a freeze-drying step, in which a nano-lyophilized powder is obtained; and an outer hydrophilic component coating step, in which astragalus polysaccharides are sprayed or adsorbed onto the surface of the freeze-dried powder. The composition obtained by this method is a core-shell multilayer nanoparticle with a core consisting of curcumin and resveratrol encapsulated by solid lipids, a middle shell adsorbing quercetin and green tea polyphenols, and an outer shell coated with astragalus polysaccharides. This application utilizes the above-mentioned layered encapsulation technology to achieve stable co-encapsulation of multiple antitumor active ingredients, improve the bioavailability of poorly soluble components, optimize drug stability, and enhance antitumor effects through multi-target synergistic effects. Simultaneously, it endows the composition with immunomodulatory functions and sustained-release properties. The composition can be formulated into a nano-lyophilized powder form, making it easy to add to pet food or formulate into a paste for administration, improving pet drug compliance. Figure 2 is a schematic diagram of the three-layer core-shell nanoparticle structure of the composition of this invention.

The invention relates to process development of a preparation prescription of a coronavirus 3CL protease inhibitor compound Iscartrevir and a preparation method of the coronavirus 3CL protease inhibitor compound Iscartrevir. By strictly screening and optimizing the formula, the preparation with a specific prescription ratio is obtained. According to the preparation, the medicine stability is improved, through the overall synergistic effect of the dry granulation step, in the preparation process of the medicine components, the flowing property of totally mixed materials is good, and the sticking problem is further solved. Meanwhile, the preparation is simple in production process, short in production period, energy-saving, efficient, low in cost and suitable for industrial mass production.

The present application relates to the microRNA drug technical field, specifically to the application of hsa-let-7f-5p in the preparation of a drug for treating muscle steatosis, and discloses that hsa-let-7f-5p can inhibit muscle fat infiltration by inhibiting fibroblast / adipogenic progenitor cell adipogenic differentiation, and hsa-let-7f-5p can be used as a microRNA drug in the treatment of diseases such as muscle fat infiltration and muscle steatosis, and diseases related to fat infiltration, for example, muscle atrophy, muscle injury, obesity, diabetes, etc. The relevant nucleic acid fragments are wrapped in liposomes, so that the drug stability and drug efficiency can be improved. The technical scheme can solve the technical problem that there is no drug capable of effectively inhibiting muscle steatosis and treating muscle injury in the prior art, and has an ideal application and promotion prospect in the fields of sports medicine and rehabilitation treatment.

The invention belongs to the technical field of medicine dosage forms, and particularly relates to a conjugated estrogen-progestational hormone double-layer tablet and a preparation method thereof. The preparation method comprises the following steps: performing powder mixing on conjugated estrogen and a first medicine auxiliary material to obtain conjugated estrogen powder; carrying out wet granulation on progestational hormone and a second medicine auxiliary material to obtain progestational hormone granules; and tabletting the conjugated estrogen powder and the progestational hormone particles by using a double-layer tablet press to obtain the conjugated estrogen-progestational hormone double-layer tablet. The conjugated estrogen-progestational hormone double-layer tablet prepared by the invention can simultaneously meet the slow release of conjugated estrogen and the quick release of progestational hormone, so that the medicine taking frequency is reduced, and the compliance of a patient is improved; and meanwhile, the stability of a drug bound with estrogen and the bioavailability of progestational hormone are improved.

The invention discloses a transdermal drug delivery patch with a five-layer structure and application thereof, and belongs to the technical field of pharmaceutical preparations. The patch comprises a backing film, a donepezil hydrochloride-containing reservoir layer, a controlled release film, an organic alkali-containing adhesion layer and a release film. The release rate of the donepezil hydrochloride is controlled through the controlled release film, the donepezil hydrochloride is isolated from organic alkali, the drug stability is improved, the drug release rate is regulated and controlled, the donepezil hydrochloride passes through the controlled release film and then is subjected to an in-situ reaction with the organic alkali in the adhesion layer, and the donepezil hydrochloride is converted into donepezil free alkali for transdermal delivery. According to the patch, the drug stability is improved, the preparation process is simple, the local safety is high, and the transdermal permeability of donepezil can be remarkably improved.

The present application belongs to the field of pharmaceutical preparations, and particularly relates to a sustained-release analgesic pharmaceutical composition, a method for preparing same, and use thereof. The pharmaceutical composition of the present application comprises a drug, a delivery carrier, and a release regulator. The drug is selected from at least one of a local anesthetic and a non-steroidal anti-inflammatory drug. The release regulator is selected from a phospholipid compound. The delivery carrier is selected from a saccharide and an esterified form thereof. According to the present application, the coaction of the phospholipid compound and the delivery carrier can increase the plasma drug concentration upon the initial release in vivo, reduce the time to peak, enhance the analgesic effect in the early stage after a surgery, and ensure the long-term release of the drug, thus effectively relieving the postoperative pain, reducing the administration frequency, and promoting skin wound healing. The use of a specific solubilizer provides good stability for the drug and prevents precipitation. The composition can be administered through the wound, making it easy to use.

The invention discloses an external clindamycin phosphate solution, which is prepared from the following raw materials in parts by weight: 0.6 to 1.2 parts of clindamycin phosphate, 0.1 to 0.2 part of resveratrol, 0.02 to 0.04 part of glutathione, 0.1 to 0.2 part of xanthan gum, 0.3 to 0.6 part of poloxamer, 25 to 32 parts of glycerol and the balance of water according to the weight of 100 parts. The traditional Chinese medicine composition can be stored for a long time, is good in medicine stability, and can well relieve side effects such as dry skin, sensitive irritation and skin rash.

The invention provides a preparation method of a magnesium acetyltaurate nano eye medicine. The preparation method comprises the following steps: S1, preparing magnesium acetyltaurate pure medicine nano particles; s2, preparing cell membrane vesicles with high expression of transferrin; s3, sufficiently mixing the magnesium acetyltaurate nanoparticles and the cell membrane vesicles with high expression of transferrin, and performing ultrasonic treatment to obtain the magnesium acetyltaurate nano eye medicine. The magnesium acetyltaurate nano eye drops loaded on the cell membrane vesicles capable of highly expressing transferrin, prepared by the invention, have relatively high drug concentration and have long-time drug stability.

According to the invention, a polymer prodrug is designed and prepared, and a dasatinib (DAS) and triphenylphosphine-adriamycin (TPP-DOX, TD) co-loaded nano-micelle is constructed; the preparation method has the advantages that 1) the optimal preparation process of the polymer micelle is determined by a single factor investigation method, namely the optimal nano-micelle is prepared by using a dialysis method and taking DMF (Dimethyl Formamide) as a solvent according to the mass ratio of a prodrug material to a carried drug being 15: 1, and the preparation method is simple and clear and is easy to industrialize; 2) the particle size is small and uniform, so that the nanoparticles can be enriched at a tumor part through an EPR effect; 3) the amphiphilic micromolecule prodrug improves the water solubility of DAS, improves the drug stability, has high drug loading capacity, and avoids adverse reactions possibly caused by carriers and auxiliary materials; and 4) the polymer nano-micelle co-loaded with the DAS and the TPP-DOX has good MMP-2 sensitive responsiveness, enhances the drug targeting delivery capability, has good blood compatibility and safety, improves the drug curative effect, reduces the toxic and side effects, and has a good tumor MDR reversing effect.

The invention provides thalidomide and magnesium acetyltaurate nano eye medicine as well as a preparation method and application thereof. The preparation method comprises the following steps: S1, preparing thalidomide and magnesium acetyltaurate co-assembled nano particles; s2, preparing BHK21 cell membrane vesicles with high expression of transferrin; s3, the thalidomide and magnesium acetyltaurate co-assembled nanoparticles and the BHK21 cell membrane vesicles with high expression of transferrin are fully mixed and then subjected to ultrasonic treatment, and the thalidomide and magnesium acetyltaurate nano eye medicine is obtained. The thalidomide and magnesium acetyltaurate nano eye medicine has relatively high medicine concentration and has long-time medicine stability.