27 results about "Loxoprofen" patented technology

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.

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.

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 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 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.

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 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 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.

To provide a topical pharmaceutical composition containing diclofenac in which crystal precipitation is suppressed. [Solution] A topical pharmaceutical composition comprising (A) one or more selected from the group consisting of loxoprofen, its salts and hydrates thereof, (B) one or more selected from the group consisting of diclofenac, its salts and hydrates thereof, and (C) a lower alcohol, wherein the content of the lower alcohol of (C) is 35% by mass or more and 60% by mass or less based on the total mass of the topical pharmaceutical composition, and the pH of the topical pharmaceutical composition is 5.0 to 7.5.

To provide a new oral pharmaceutical composition that has a low risk of occurrence of small intestine ulcer, contains loxoprofen, and is used as an agent for antipyresis, analgesia or common cold treatment.SOLUTION: An oral pharmaceutical composition contains loxoprofen or a salt thereof, licorice, and magnesium oxide.SELECTED DRAWING: None

The present invention addresses the problem of providing a patch that has excellent skin permeability and good adhesiveness. [Solution] A patch provided with a support and an adhesive layer laminated on the support, the adhesive layer containing loxoprofen sodium hydrate, hydrated silica, polyisobutylene, glycerol ester of hydrogenated rosin, a styrene-isoprene-styrene block copolymer, and phosphoric acid. Based on the total mass of the adhesive layer, the content of the silicon dioxide hydrate is preferably 0.3%-1% by mass, the content of the polyisobutene is preferably 5%-15% by mass, the content of the glycerol ester of the hydrogenated rosin is preferably 10%-20% by mass, the content of the styrene-isoprene-styrene block copolymer is preferably 17%-27.5% by mass, and the content of the phosphoric acid is preferably 0.1%-1.5% by mass.

The invention relates to a loxoprofen sodium patch and a preparation method thereof. The loxoprofen sodium patch comprises a backing layer, a drug-containing matrix layer and a stripping layer, the stripping layer is in contact with the drug-containing substrate layer, and the backing layer covers the drug-containing substrate layer; the drug-containing matrix layer comprises loxoprofen sodium, a penetration enhancer and an acrylate pressure-sensitive adhesive, and the tail end of the acrylate pressure-sensitive adhesive only contains a carboxyl group. The loxoprofen sodium patch is stable in performance, simple in component and excellent in adhesion performance, and has a good transdermal release effect.

To provide a new oral pharmaceutical composition that has a reduced risk of gastric mucosal injury, contains loxoprofen, and is used as antipyretics, analgesics or common cold therapeutic agents.SOLUTION: An oral pharmaceutical composition contains loxoprofen or a salt thereof, and Japanese valerian.SELECTED DRAWING: None

Provided is a method for producing a solid preparation containing (A) at least one selected from the group consisting of loxoprofen, salts thereof, and hydrates thereof and (B) at least one selected from the group consisting of tranexamic acid and salts thereof, the method comprising: a wet granulation step in which a granulation is obtained by supplying water to a raw material powder containing components (A) and (B), wherein, when the addition rate of the water supplied in the wet granulation step is set to X, the plastic limit water addition rate of the raw material powder is set to PL, and the granulation index represented by X / PL is set to Ig, X is adjusted so as to satisfy 0.20 ≤ Ig ≤ 0.99.

The present invention provides a pharmaceutical composition for external use, which contains (a) one or more substances selected from loxoprofen, salts thereof, and hydrates thereof, (b) one or more substances selected from diclofenac, salts thereof, and hydrates thereof, and (d) a lower alcohol, the content of the (d) lower alcohol being 35-60% by mass (inclusive) relative to the mass of the entire pharmaceutical composition for external use. The pH of the external pharmaceutical composition is 5.0 to 7.5. The invention also provides an external pharmaceutical composition. The composition contains (a) one or more substances selected from the group consisting of loxoprofen, salts thereof, and hydrates thereof, (b) one or more substances selected from the group consisting of diclofenac, salts thereof, and hydrates thereof, (c) has a hydrocarbon chain structure and a polyoxyethylene polymerization structure, and has a ratio (P / C) of the average number of moles P of the polyoxyethylene chain added to the number of carbons C of the carbon chain of 1.2 or more. And (d) a lower alcohol, the content of the lower alcohol (d) being less than 35 mass%, and the pH being 6.0-8.0.

[Problem] To provide a pharmaceutical composition for external use, which comprises indomethacin, diclofenac sodium, biphenylacetic acid, a salicylic acid, or a heparin, and which alleviates irritation to a site to which the pharmaceutical composition is applied. [Solution] A pharmaceutical composition for external use, which is a composition that mitigates irritation to an application site, and which contains: one or more components (A) selected from the group consisting of the following components (A-1)-(A-5), and (B) one or more components (B) selected from the group consisting of the following components (A-1)-(A-5), the component (B) being one or more selected from the group consisting of the following components (A-1)-(A-5); component (A-1): indomethacin component (A-2): diclofenac sodium component (A-3): biphenylacetic acid component (A-4): salicylic acid component (A-5): heparin analogue component (B): one or more substances selected from the group consisting of loxoprofen, salts thereof, and hydrates thereof.

To provide a topical pharmaceutical composition containing loxoprofen and felbinac, wherein crystal precipitation is suppressed. [Solution] (A) One or more selected from the group consisting of loxoprofen, its salts and hydrates thereof, (B) One or more selected from the group consisting of felbinac, its salts and hydrates thereof, (C) One or more surfactants having a hydrocarbon chain structure and a polyoxyethylene structure, wherein the ratio of the average number of added moles of the polyoxyethylene chain to the number of carbon atoms of the hydrocarbon chain is 2.0 or less, and (D) Lower alcohol. An external pharmaceutical composition containing a lower alcohol, a surfactant, and a pH that meets predetermined conditions.

The invention discloses a loxoprofen sodium patch and a particle size control method of a special raw material medicine of the loxoprofen sodium patch, and aims to solve the problems that in the prior art, the dispersibility of raw material medicines in a matrix is poor, and the in-vitro permeation rate difference of patches among batches is large. The method comprises the following steps: screening raw material medicines; pre-treating the screened crude product of the raw material medicine; carrying out crushing treatment on the pretreated raw material medicines by adopting a low-temperature jet mill; carrying out grading treatment on the crushed raw material medicines by adopting an airflow grader according to a preset condition; putting the graded raw material medicines into a constant-temperature and constant-humidity box, and carrying out crystal form stabilizing treatment; carrying out particle size detection on the raw material medicine subjected to crystal form stabilization treatment, and carrying out post-treatment on the raw material medicine of which the particle size detection reaches a preset standard, so as to obtain the special raw material medicine for the loxoprofen sodium patch. The loxoprofen sodium patch preparation method is suitable for loxoprofen sodium patch preparation, and the effects that the particle size distribution of the raw material medicine is narrow, the patch matrix is adapted, and the dispersion uniformity of the medicine in the matrix is guaranteed can be achieved.

To provide a solid composition containing at least one selected from the group consisting of loxoprofen, a salt thereof and a hydrate thereof, and other components, and having suppressed property change.SOLUTION: (A) at least one member selected from the group consisting of loxoprofen and salts and hydrates thereof, (B) fructose, and (C) one or more members selected from the group consisting of (C- 1) vitamin B1 and vitamin C, (C- 2) peony root, licorice, and valerian, (C- 3) bromhexine, ambroxol, tipepidine and salts and hydrates thereof, (C- 4) clemastine and salts and hydrates thereof, and (C- 5) dextromethorphan and salts and hydrates thereof; A solid composition comprising: SELECTED DRAWING: None