49 results about "Loxoprofen" patented technology

The invention discloses a sustained-release pill as well as a preparation method and application thereof, and belongs to the technical field of medicines. The sustained-release pill comprises a pill core and a coating layer coated outside the pill core, the pellet core is prepared from the following raw materials in parts by mass: 8 to 14 parts of loxoprofen sodium, 30 to 60 parts of a filling agent, 3 to 10 parts of an adhesive, 2 to 10 parts of a disintegrating agent, 0.1 to 2 parts of a penetration enhancer, 0.05 to 0.2 part of a pH regulator, 0.1 to 0.5 part of a surfactant and 0 to 20 parts of an auxiliary agent; the coating layer is prepared from an aqueous dispersion liquid containing acrylic resin; the coating layer is prepared from an aqueous dispersion liquid containing acrylic resin. Aiming at the drug characteristics of loxoprofen sodium, the loxoprofen sodium sustained-release tablet is composed of specific auxiliary materials, the drug composition is optimized, the drug release rate is accurately controlled, the bioavailability and stability of the drug are effectively improved, and the loxoprofen sodium sustained-release tablet has a good application prospect in preparation of antipyretic and analgesic drugs.

The invention provides a loxoprofen sodium double-release capsule micro-tablet and a preparation method of the loxoprofen sodium double-release capsule micro-tablet. Through the synergistic effect of the quick-release micro-tablet and the sustained-release micro-tablet, the quick-release micro-tablet can realize quick release and absorption, and the sustained-release micro-tablet can maintain relatively stable blood concentration for a long time. The administration frequency is reduced, the coordination of the postprandial administration requirement and the dietary habit is ensured, and the occurrence of gastrointestinal tract adverse reactions is reduced. The preparation provided by the invention conforms to the dosage form design of the hour pharmacology, can quickly take effect through administration twice every day, can maintain the blood concentration in the high-incidence time period of night diseases, avoids the disadvantage of taking medicine after meal when the night diseases attack, guarantees the sleep quality, and improves the overall treatment effect. The micro tablet is small in size and easy to swallow, and the medication compliance of patients with dysphagia is obviously improved. Through dosage form design and improvement, unmet clinical requirements are expected to be met by virtue of obvious advantages of the traditional Chinese medicine composition.

The invention relates to a dressing for promoting healing of diabetic wounds. Chitosan is dissolved in a hydrochloric acid solution at room temperature to obtain a chitosan solution; the preparation method comprises the following steps: dissolving loxoprofen in ethanol activated by 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide / N-hydroxysuccinimide, dropwise adding into a chitosan solution, adding ethanol while stirring at a high speed by using a magnetic rod to form a transparent solution, and stirring at a low speed in the dark; air-drying the solution in a drying oven to form a solid film, and thoroughly washing the solid film in ethanol to obtain a chitosan-loxoprofen conjugate; the preparation method comprises the following steps: adding chitosan-loxoprofen into a phosphate buffer solution to form a chitosan-loxoprofen solution; dissolving genipin in a phosphate buffer solution to obtain a genipin solution, stirring and mixing the chitosan-loxoprofen solution and the genipin solution at a high speed, cross-linking, and freezing in a refrigerator to obtain the chitosan-loxoprofen / genipin sponge bracket. The dressing disclosed by the invention can effectively relieve chronic inflammation, remarkably improve skin tissue regeneration and stimulate angiogenesis.

The invention discloses a green synthesis process of non-steroidal loxoprofen sodium, and relates to the field of loxoprofen sodium synthesis. A water / organic two-phase free radical bromination and functionalized Pd-Ru / NH2-ZIF-8 catalysis one-step hydrogenation degreasing-tert-butyl ester removal path is adopted. The catalyst is modified by a thiol ligand and cooperates with a chiral inducer to construct a Pd-Ru bimetallic active site, so that the product purity and the product yield are effectively improved, and the catalyst can be repeatedly used. The method is environment-friendly and efficient in process and suitable for industrial application.

The invention discloses a method for determining related substances in a loxoprofen sodium patch in the technical field of drug detection, and aims to solve the technical blank existing in determination of related substances in a loxoprofen sodium patch in the prior art. The method comprises the following steps: respectively weighing a loxoprofen sodium reference substance and an impurity reference substance, and adding a solvent for dilution to prepare a reference substance solution; taking a loxoprofen sodium patch, stripping a protective layer, adding tetrahydrofuran and methanol, shaking to separate the paste from a backing layer, adding water, shaking again, adding a solvent for dilution, uniformly mixing, centrifuging, and taking supernate to obtain a test solution; injecting the prepared reference substance solution and the test solution into a high performance liquid chromatograph for determination to obtain peak areas of the reference substance solution and the test solution; and calculating the content of the related substances in the loxoprofen sodium patch by adopting an HPLC correction factor method according to the peak areas of the reference solution and the test solution. The method is suitable for measuring the content of the related substances in the loxoprofen sodium patch.

The present invention belongs to the technical field of pharmaceutical formulations, specifically relates to a controlled-release tablet of loxoprofen sodium, its preparation method, and use. The controlled-release tablet comprises a drug-containing immediate-release layer, a drug-containing core layer, and a drug-containing sustained-release layer, the drug-containing core layer comprising a plain tablet core, an enteric coating film, and a sealing coating film. The preparation method includes granulating the raw materials for the drug-containing immediate-release layer and the drug-containing sustained-release layer, respectively, wet granulating the raw materials for the plain tablet core and compressing them into tablets, followed by sequentially applying a first sealing coating, a second enteric coating, and a third sealing coating to obtain a drug-containing core, placing the drug-containing core on the drug-containing sustained-release layer granules and pre-compressing them, and then placing the drug-containing immediate-release layer granules on the pre-compressed tablet, compressing them, and coating them to obtain the drug-containing core. The present invention achieves the sustained-release effect of the loxoprofen sodium tablet core by designing the single-layer structure, raw materials, and coating layer components of the dry-coated tablet, thereby achieving 12-hour in vivo efficacy and improving patient compliance.

According to the loxoprofen sodium patch and the preparation method thereof provided by the invention, in the preparation process of the patch, the loxoprofen sodium patch prepared by optimizing the preparation temperature, the coating temperature and an oxygen control mode of vacuumizing and continuously filling nitrogen has the advantages that the increase amplitude of related substances is low under an accelerated test condition; the stability of the patch can be obviously improved, the coating time can be obviously prolonged, and the patch has important significance for increasing the production batch and improving the production capacity.

The present application relates to a kind of preparation compositions containing the preparation method of loxoprofen derivative shown in general formula (I).The composition is a kind of analgesic antipyretic for preventing and treating rheumatoid arthritis, rheumatoid arthritis, osteoarthritis, joint deformity, gout, lumbago, neck shoulder wrist syndrome and periodontitis, cold, acute respiratory inflammation, such as postoperative inflammation of the diseases of the drug composition, its composition is characterized in that the mass percentage of loxoprofen derivative is 0.5%-5.0%w / w;Including physiologically acceptable crystal inhibitor;And at least one pH regulator.The pharmaceutical composition provided by the present application, compared with the preparation of loxoprofen derivative external preparation of the current existing technical means or the method reported in the public literature, solves the problem of active ingredient crystallization of such preparation, and achieves good effect.

1. The name of the design product: plaster packaging box. 2. The use of the design product: for packaging loxoprofen sodium gel plaster. 3. The design points of the design product: the combination of shape, pattern and color. 4. The picture or photo that best indicates the design points: perspective view. 5. The design for which protection is sought contains colors.

To provide a topical skin preparation containing loxoprofen and 60% by mass or more of lower alcohol based on the total amount of the topical skin preparation, with improved storage stability. [Solution] A topical skin preparation containing loxoprofen or a salt thereof, and one or more pH adjusting agents selected from hydrochloric acid or malic acid and their salts, at a concentration of 60% by mass or more based on the total amount of the topical skin preparation.

The objective is to provide a pharmaceutical composition that suppresses changes in the appearance of loxoprofen or its salts. [Solution] The inventors of this invention conducted extensive research to solve this problem and found that by incorporating noscapine, it is possible to suppress the change in appearance of loxoprofen or its salt over time. In other words, the pharmaceutical composition is characterized by containing (A) loxoprofen or a salt thereof, and (B) noscapine or a salt thereof, wherein component (A) accounts for 9 to 90% by mass of the total mass of the pharmaceutical composition. According to the present invention, a pharmaceutical composition containing loxoprofen or a salt thereof can be provided that exhibits excellent storage stability.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a loxoprofen sodium preparation and a preparation method thereof. The loxoprofen sodium preparation is composed of a loxoprofen sodium tablet and a tablet outer layer coating, the outer layer coating comprises the following raw materials: L-glutamine, carboxylated chitosan and a coloring agent, the L-glutamine accounts for 24-26% of the mass of the outer layer coating, the carboxylated chitosan accounts for 17-30% of the mass of the outer layer coating, and the coloring agent accounts for 1-2% of the mass of the outer layer coating. The preparation method mainly comprises the following steps: firstly, preparing loxoprofen sodium tablets by a wet granulation process, then preparing a coating solution, and finally, carrying out film coating on the tablets by using the coating solution to obtain the loxoprofen sodium preparation. According to the loxoprofen sodium preparation and the preparation method thereof provided by the invention, the process is simple and convenient, the coating is stable, the release is controllable, the prepared preparation is suitable for being taken by various patient groups, and the medication safety and compliance are further improved while the curative effect is guaranteed.

The invention discloses a hot-melt loxoprofen sodium patch and a preparation method thereof. The hot-melt loxoprofen sodium patch comprises a backing layer, an adhesive layer and a protective layer. The adhesive layer comprises, by weight percentage, 5-6% of loxoprofen sodium or a hydrate thereof, 19-26% of a styrene-isoprene-styrene block copolymer, 5-15% of polyisobutylene, 5-15% of hydrogenated rosin glycerol ester, and 40-50% of liquid paraffin. By optimizing the type and amount of the styrene-isoprene-styrene block copolymer and the polyisobutylene, the adhesive force and cohesive force of the loxoprofen sodium patch are simultaneously improved through their combined action, and the long-term stability of the patch can be maintained.

The invention relates to solid compositions and methods of manufacture. The present invention addresses the problem of providing a solid composition which contains at least one component selected from the group consisting of loxoprofen, salts thereof, and hydrates thereof, and another component, and in which changes in properties are suppressed. [Solution] A solid composition containing the following components: (A) at least one substance selected from the group consisting of loxoprofen, salts thereof, and hydrates thereof; (B) fructose; and (C) one or more components selected from the group consisting of: (C-1) vitamin B1 and vitamin C; (C-2) Chinese herbaceous peony, liquorice and valerian; (C-3) bromhexine, ambroxol, tepiperidine, salts thereof, and hydrates thereof; (C-4) clomastine, salts thereof, and hydrates thereof; and (C-5) dextromethorphan, salts thereof, and hydrates thereof.

The present invention addresses the problem of providing a novel technique for suppressing pharyngitis and restoring water swallowing reflex by using loxoprofen and / or a salt thereof. According to the present invention, provided is a pharmaceutical composition having a pharyngitis-inhibiting effect and containing at least one substance selected from the group consisting of loxoprofen, salts thereof, and hydrates thereof.

1. Name of the designed product: packing box (sodium loxoprofen gel plaster). 2. Use of the designed product: for packing products. 3. Design points of the designed product: combination of shape and pattern. 4. Picture or photo best indicating the design points: perspective view.

The solid preparation of the present invention contains: at least one component (A) selected from loxoprofen, salts thereof, and hydrates thereof; and at least one component (B) selected from tranexamic acid and salts thereof. In an X-ray diffraction pattern measured using a Cu-K [alpha] ray, at least three or more diffraction angles (2 [theta]) in five ranges of 7.3 + / -0.1, 11.0 + / -0.1, 19.1 + / -0.1, 22.2 + / -0.1, and 24.8 + / -0.1 do not have peaks.

The invention provides an ophthalmic preparation containing an aryl propionic acid compound. According to the invention, the active metabolite converted from loxoprofen sodium in vivo, namely the compound as shown in the formula I and the salt thereof, is taken as the effective component and is prepared into various ophthalmic preparations for administration by virtue of a preparation means, so that the problem of low bioavailability due to the fact that only part of prodrugs can be converted into the active metabolite when being directly administered is effectively solved. Compared with the compound shown in the formula I, the salt of the compound has high solubility and good stability, and the ophthalmic preparation prepared by taking the compound as an active component has obviously improved stability and can be stored for a long time. The eye drops are small in side effect, safe, reliable in curative effect and suitable for treating inflammation of external eyes and front eyes, xerophthalmia and eye pain after operation; the raw materials are easy to obtain, the cost is low, industrial large-scale production can be realized, and remarkable economic benefits are achieved.

The present application relates to a kind of HPLC-MS / MS detection method of loxoprofen and its active metabolite trans-OH body in human plasma, it includes the following steps: (1) human plasma sample pretreatment;(2) liquid chromatography-mass spectrometry detection, using mobile phase A and mobile phase B as mixed mobile phase is carried out gradient elution, wherein, mobile phase A is acetonitrile, mobile phase B is 0.05% acetic acid aqueous solution;(3) the determination of loxoprofen and its active metabolite trans-OH body concentration in human plasma.The present application uses ACE, Excel 3SuperC18 as chromatographic column, in the process of gradient elution, the time of optimization elution and the proportion of mobile phase, linear range is all 0.200-40.0ng / mL, lower limit of quantification is low, sensitivity is high, reproducibility, accuracy is all better, can be used to evaluate loxoprofen and its active metabolite trans-OH body each dosage form bioequivalence.

This invention provides a method for preparing loxoprofen acid, relating to the field of biomedical technology. The method involves mixing compound 1, 1-(1-pyrrolidine)cyclopentene, and an organic solvent, performing a condensation reaction, and then hydrolyzing the mixture under acidic conditions to obtain loxoprofen acid; wherein X is a halogen, and R includes -CN or -CONH2. This invention uses compound 1 and 1-(1-pyrrolidine)cyclopentene as starting materials, and prepares loxoprofen acid through a condensation reaction followed by hydrolysis under acidic conditions. The product yield is high, the purity is high, and continuous production of loxoprofen acid is possible. The operation is simple, generates little waste, is environmentally friendly, and has low production costs, making it suitable for industrial production. Furthermore, the preparation method provided by this invention concentrates the solvent after the condensation reaction to allow for subsequent hydrolysis, eliminating the need for separation and purification of the intermediate obtained from the condensation reaction, simplifying the operation steps, generating less waste, and being environmentally friendly.

The application discloses a loxoprofen sodium-containing patch composition, which comprises a backing layer, an adhesive layer and a protective layer, and the adhesive layer comprises, in percentage by weight, 5-6% of loxoprofen sodium or a hydrate thereof, 19-26% of a styrene-isoprene-styrene block copolymer, 5-16% of polyisobutylene, 5-16% of hydrogenated rosin glyceride and 40-50% of liquid paraffin. The loxoprofen sodium patch composition provided by the application can simultaneously improve the adhesive force and cohesion of the loxoprofen sodium patch and maintain long-term stability by optimizing the types of the styrene-isoprene-styrene block copolymer, the polyisobutylene and the liquid paraffin.

An object of the present application is to provide a pharmaceutical composition which improves the anti-inflammatory effect of loxoprofen. According to the present application, there is provided a pharmaceutical composition comprising: at least one selected from the group consisting of loxoprofen, salts thereof, and hydrates thereof, and at least one selected from the group consisting of diclofenac, naproxen, salts thereof, and hydrates thereof.

The invention provides a single-dose non-steroidal anti-inflammatory drug eye drop. According to the present invention, the compound represented by the formula I is obtained through splitting, and the research results show that the free acid of the compound represented by the formula I has characteristics of low water solubility, poor physical and chemical stability, easy moisture absorption, stickiness, poor fluidity and the like; therefore, various salt forms of the compound shown in the formula I are further researched, tromethamine salt of the compound shown in the formula I is finally selected as an effective component from multiple aspects of physicochemical properties and safety, and the eye drops are prepared through a preparation means to be directly used for eye drop administration, so that the problem that when a prodrug is directly used, the dosage of the tromethamine salt is reduced is effectively solved. And the loxoprofen active metabolite can be used for enriching the application of the loxoprofen active metabolite in antipyretic, analgesic and anti-inflammatory medicines.

1. Name of the product in this design: Packaging Box (Loxoprofen Sodium Gel Patch). 2. Application of this design: This design is intended for use in pharmaceutical packaging. 3. The key design elements of this product are the combination of shape, pattern, and color. 4. The image or photograph that best illustrates the design's key points: a 3D model. 5. The design for which protection is sought includes color.

The present invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a loxoprofen sodium controlled-release tablet, and a preparation method and use thereof. The controlled-release tablet includes a drug-containing immediate-release layer, a drug-containing tablet core layer and a drug-containing sustained-release layer. The drug-containing tablet core layer includes a plain tablet core, an enteric coating film and an isolation coating film. The preparation method includes: preparing a granule of a drug-containing immediate-release layer and a granule of drug-containing sustained-release layer respectively from a raw material of the drug-containing immediate-release layer and a raw material of the drug-containing sustained-release layer; subjecting a raw material of a plain tablet core to wet granulation, tableting, and then sequentially coating with a first layer of isolation coating , a second layer of enteric coating, and a third layer of isolation coating to obtain a drug-containing tablet core; and placing the drug-containing tablet core on the granule of the drug-containing sustained-release layer, pre-compressing, and then placing the granule of the drug-containing immediate-release layer on the pre-compressed tablet, tableting, and coating to obtain the tablet. In the present invention, the tablet structure, raw materials, coating and the like components of the core-coated tablet are designed to achieve the effect of sustained-release of the loxoprofen sodium tablet core, so that the tablet can be effective in vivo for 12 h and improve patient compliance.

To provide a topical pharmaceutical composition containing indomethacin, diclofenac sodium, felbinac, salicylic acids, or heparins, wherein irritation to the application site is reduced. [Solution] A topical pharmaceutical composition that contains component (A) and component (B) below, wherein component (A) is one or more selected from the group consisting of components (A-1) to (A-5) below, and which reduces irritation to the application site. Ingredient (A-1): Indomethacin Ingredient (A-2): Diclofenac sodium Ingredient (A-3): Felbinac Ingredients (A-4): Salicylic acids Ingredient (A-5): Heparinoid Ingredient (B): One or more selected from the group consisting of loxoprofen, its salts, and their hydrates.

[Problem] To provide a pharmaceutical composition for external use containing loxoprofen and biphenylacetic acid, in which crystal precipitation is suppressed. [Solution] A pharmaceutical composition for external use, the composition contains (A) one or more substances selected from loxoprofen, salts thereof, and hydrates thereof, (B) one or more substances selected from felbinac, salts thereof, and hydrates thereof, and (C) one or more surfactants having a hydrocarbon chain structure and a polyoxyethylene structure, the ratio of the average number of moles of added polyoxyethylene chains to the number of carbon atoms of the hydrocarbon chain being 2.0 or less. And (D) a lower alcohol, wherein the content of the lower alcohol, the content of the surfactant, and the pH satisfy predetermined conditions.

The invention discloses an alpha-nitrogen modified ibuprofen amide non-steroidal anti-inflammatory drug lead compound and a preparation method thereof. The lead compound of the alpha-nitrogen modified ibuprofen non-steroidal anti-inflammatory drug comprises alpha-azide ibuprofen (or ketoprofen, naproxen, loxoprofen and flurbiprofen) amide, alpha-triazole ibuprofen (or ketoprofen, naproxen, loxoprofen and flurbiprofen) amide, alpha-phosphamide ibuprofen (or ketoprofen, naproxen, loxoprofen and flurbiprofen) amide, alpha-nitrogen modified ibuprofen (or ketoprofen, naproxen, loxoprofen and flurbiprofen) amide and alpha-nitrogen modified ibuprofen (or ketoprofen, naproxen, loxoprofen and flurbiprofen) amide. Animal experiments prove that the alpha-azide ibuprofen amide, the alpha-phosphamide ibuprofen amide and the like show anti-inflammatory and analgesic activity which is remarkably superior to that of ibuprofen, and a novel non-steroidal anti-inflammatory drug capable of replacing the ibuprofen is expected to be developed.

The present invention addresses the problem of providing a bitterness-masked pharmaceutical composition that contains at least one selected from the group consisting of loxoprofen, salts thereof, and hydrates thereof. The present invention provides a pharmaceutical composition comprising: at least one selected from the group consisting of loxoprofen, salts thereof, and hydrates thereof; a sugar alcohol; and a compound including at least one metal selected from the group consisting of alkali metals and alkaline earth metals.