30 results about "Adapalene" patented technology

The invention discloses an adapalene external preparation and a preparation method thereof, and relates to the technical field of adapalene preparation preparation. The adapalene gel comprises the following raw materials in percentage by mass: 4.5-7.5% of adapalene, 3.5-8% of a gel base material, 2-4.5% of cellulose, 0.5-2% of a penetration enhancer, 18-25% of a water-retaining agent, 2-5% of a surfactant, a pH value regulator and the balance of water, the dosage of the pH value regulator is based on the standard that the pH value of the adapalene external preparation is regulated to 7-7.5; the gel base material comprises poloxamer or carbomer, and further comprises sa-hao seed gum, and the use amount of the sa-hao seed gum accounts for 25-35% of the total mass of the gel base material. According to the adapalene external preparation provided by the invention, the irritation of adapalene to the skin is basically eliminated by utilizing the effects of the gel base material consisting of poloxamer or carbomer and sa-hao seed gum and the surfactant; the adhesive has good cohesiveness and water-retaining property, can keep the affected part moist after being smeared, promotes medicine absorption, and avoids being wiped off or automatically falling off; the stability is improved, and the medicine slow release time is indirectly prolonged.

The invention discloses a novel application of adapalene and vinca in preparation of a medicine for treating acute myelogenous leukemia by combination, and finds that the adapalene and the vinca have a synergistic inhibition effect on proliferation of an acute myelogenous leukemia cell line, namely the adapalene and the vinca have a remarkable synergistic effect by combination for the first time, so that the application of the adapalene and the vinca in preparation of the medicine for treating the acute myelogenous leukemia is realized; the invention provides an effective drug combination strategy for treatment of acute myelogenous leukemia, and has good clinical application prospects and important transformation significance in the technical field of development of drugs for treating acute myelogenous leukemia.

The invention relates to a pharmaceutical composition, which is prepared from adapalene, benzoyl peroxide, a traditional Chinese medicine extract, an acrylamide and acryloyl dimethyl sodium taurate copolymer, a mixture of isohexadecane and polysorbate 80, docusate sodium, EDTA (Ethylene Diamine Tetraacetic Acid) disodium, glycerol, poloxamer 124, propylene glycol and water, the traditional Chinese medicine extract comprises moutan bark, salvia miltiorrhiza, radix rehmanniae recen, radix sophorae flavescentis, coptis chinensis, rheum officinale, scutellaria baicalensis, menthol and borneol. According to the pharmaceutical composition disclosed by the invention, the synergistic antibacterial and anti-keratosis curative effects of adapalene and benzoyl peroxide can be maintained, and meanwhile, the occurrence rate of local skin dryness, erythema, desquamation, burning heat sensation and contact dermatitis can be remarkably reduced.

The present invention discloses a combined drug for treating acne, which contains bletilla stilbene components and patchouli essential oil for simultaneous or separate administration. By combining bletilla stilbene components and patchouli essential oil in a specific ratio, the present invention significantly inhibits Propionibacterium acnes and acne inflammation, thereby playing a role in treating acne. Moreover, the effect is better than that of either bletilla stilbene components or patchouli essential oil used alone, and is more effective than adapalene gel commonly used at present, showing a synergistic effect and having practical popularization and application value.

The invention discloses an adapalene gel preparation method, which comprises: 1) preparing a carbomer phase: mixing a first solution and a second solution to obtain a mixed solution, and adding carbomer into the mixed solution, the first solution being obtained by mixing edetate disodium and water, the second solution being obtained by mixing edetate disodium and water, and the first solution being obtained by mixing edetate disodium and water; the second solution is obtained by mixing phenoxyethanol, methylparaben and propylene glycol; 2) preparation of adapalene phase: adding water into poloxamer to obtain a solution, and then adding adapalene into the solution; and 3) total mixing: mixing the adapalene phase and the carbomer phase while stirring to obtain a gel precursor, and then degassing, filling and sealing the gel precursor.

The present disclosure belongs to the field of pharmaceutical formulations and particularly relates to a composition with a synergistic therapeutic effect on acne lesions and a preparation method therefor and use thereof. The composition provided by the present disclosure comprises active ingredients adapalene and dapsone, which exhibit a synergistic therapeutic effect on inflammatory acne lesions when used in combination. Compared with corresponding single drugs, the composition can significantly reduce the number of inflammatory lesions; meanwhile, relative to the topical use of adapalene alone, the composition of the present disclosure can mitigate skin irritation reactions caused by adapalene and exhibits good safety.

The invention provides a local external medicine composition for treating acne as well as a preparation method and application of the local external medicine composition. The pharmaceutical composition disclosed by the invention is prepared from ozlafloxacin, adapalene, a solubilizer, a surfactant and a solvent, wherein the solubilizer is an alcohol compound and / or an ester compound, the hydrophilic-lipophilic balance value of the surfactant is 20-30, and the pH value of the pharmaceutical composition is 4s < 10 >. According to the pharmaceutical composition disclosed by the invention, the ozlafloxacin and adapalene can be effectively released, and in a stability experiment, the content of the ozlafloxacin and adapalene can be kept stable, obvious degradation does not occur, and the particle size distribution is not obviously changed.

The invention provides an HPLC (High Performance Liquid Chromatography) detection method of adapalene gel and application thereof, and particularly relates to the technical field of analysis and detection of medicinal components. The HPLC detection method of the adapalene gel is used for simultaneously detecting the contents of adapalene, methylparaben and phenoxyethanol in the adapalene gel; according to the HPLC detection method, a mixed solution of a mobile phase A and a mobile phase B is used as a mobile phase, and a sample solution to be detected is subjected to gradient elution; the initial volume ratio of the mobile phase A to the mobile phase B is (78-82): (22-18); in the gradient elution, the volume ratio of the mobile phase A to the mobile phase B is from (78-82): (22-18) to (28-32): (72-68) and finally returns to (78-82): (22-18). The detection method is simple and can be used for simultaneously determining the contents of adapalene, methylparaben and phenoxyethanol.

A novel HS-GC pretreatment method is developed, a specific and proper amount of imine alkali is introduced to replace ionic alkali (such as NaOH) used in a traditional method, the imine alkali is competitively combined with electron withdrawing groups in triethylamine and chemical raw material medicine structures, the matrix effect is avoided, the accuracy of determination of triethylamine in raw materials is remarkably improved, and the method is suitable for industrial production. Meanwhile, synergistic accurate determination of triethylamine and other residual solvents can be realized, and experimental steps are simplified. The pretreatment method is suitable for detection of residual solvents such as triethylamine in adapalene raw materials, detection objects can be expanded to other chemical raw materials and other alkaline residual solvents, and the pretreatment method has reference significance for detection of the alkaline residual solvents in other chemical raw material medicines.

The invention discloses gel for treating acne. The gel comprises a drug-loaded pellet, a matrix, a humectant, a bacteriostatic agent and a PH regulator, and the drug-loaded pellet comprises a blank pellet core, adapalene and an adhesive. The invention also provides a preparation method of the gel for treating acne, which comprises the following steps: 1) dissolving the adhesive in water, and then adding adapalene according to the prescription dosage to prepare a coating solution; coating, drying and sieving the blank pellet cores to prepare drug-loaded pellets 1-3 with different particle sizes; 2) dissolving the bacteriostatic agent and the humectant in water, adding the matrix, and uniformly stirring to obtain a mixed solution; and 3) respectively taking 1-3 parts of a certain amount of drug-loaded pellets, uniformly mixing, adding the mixed solution prepared in the step 2), stirring and homogenizing, adjusting the pH value to 5-6, adding water, and fully stirring to obtain the adapalene gel. The adapalene gel particles prepared by the invention are uniform in distribution, good in transdermal absorption effect and high in stability.

1. Name of the product in this design: Packaging Box (Adapalene Benzoyl Peroxygel). 2. Purpose of this design: Product 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 features: the front view. 5. The design for which protection is sought includes color. 6. Other situations requiring explanation: The box in the right view is the barcode area.

The present disclosure belongs to the field of pharmaceutical formulations, and particularly relates to a compound composition of adapalene and dapsone for topical dermal use, a preparation method therefor, and use thereof. The composition of the present disclosure has at least one of the following excellent characteristics: high solubility of drug active ingredients in a carrier, small particle size of drug particles, stable particle size, good skin absorption, high in-vitro release efficiency, small particle size of composition oil drops, good stability, good therapeutic effect, small skin irritation, and good placement stability. The composition of the present disclosure can be directly used as a formulation, or can be further prepared into formulations of different dosage forms after other carriers are added.

The disclosure provides a topical gel formulation comprising 1-1.5 wt. % clindamycin phosphate, 2.5-3.5 wt. % benzoyl peroxide, and 0.1-0.2 wt. % adapalene, in combination with a gelling agent, a polyhydric alcohol, and water, useful in treating inflammatory skin conditions, including acne, together with methods of making and using the same.

The invention discloses a preparation method of adapalene gel with high stability, and belongs to the technical field of medicine preparation. The deep eutectic solvent (DES) is used as a drug carrier (menthol, thymol and octanol), compared with a traditional organic solvent, the property is milder, photocatalytic degradation of adapalene can be reduced, and therefore the chemical stability of drugs is kept. According to the adapalene gel obtained by the invention, particularly the gel prepared from menthol, thymol and octanol according to the molar ratio of 1: 1: 0.1 is stable in performance and has a wide application prospect.

The invention relates to the technical field of adapalene production, and discloses an adapalene raw material preparation method which comprises the following steps: (1) adding a basic salt reagent into an alcohol solvent, and stirring until the basic salt reagent is dissolved; (2) adding 6-bromo-2-naphthoic acid into the alkaline alcohol solution in the step (1) under the protection of nitrogen, and uniformly stirring to obtain a mixed suspension; (3) stirring and heating the mixed turbid liquid in the step (2) under a nitrogen protection condition, and stirring and cooling to 10-30 DEG C; and (4) carrying out suction filtration, pulping and suction filtration on the mixed suspension cooled to 10-30 DEG C in the step (3), collecting a filter cake, and carrying out forced air drying to obtain the 6-bromo-2-sodium naphthoate. The invention provides a preparation process of 6-substituted-2-sodium naphthoate, which is simple, low in cost and suitable for industrialization, and is applied to synthesis of adapalene.

1. Name of the designed product: packaging box (adapalene gel). 2. Use of the designed product: packaging for storage, transportation and sale of products. 3. Design points of the designed product: combination of shape and pattern. 4. Picture or photo best indicating the design points: perspective view. 5. The claimed design contains color.

The invention relates to a microbial limit test method of adapalene benzoyl peroxide gel, and belongs to the technical field of microbial limit test. The method comprises the following steps: (1) preparation of a test solution: taking adapalene benzoyl peroxide gel, adding the adapalene benzoyl peroxide gel into normal saline to completely dissolve, adding 9.6-10.4% of a sterile calcium chloride solution, uniformly mixing, standing, taking supernate, and diluting to obtain the test solution; (2) taking a plurality of test solutions, grouping, respectively putting into different sterile plates, pouring into a culture medium, culturing after cooling, and calculating the total number of microorganisms by adopting a combined counting mode after the culture is finished; and (3) taking the supernate, inoculating the supernate into a sterile plate containing a culture medium, performing enrichment culture, performing streak inoculation into an agar culture medium after enrichment culture is finished, performing selective culture, counting typical bacterial colonies after selective culture is finished, and judging whether corresponding control bacteria grow or not. According to the method disclosed by the invention, the bacteriostatic activity of adapalene benzoyl peroxide gel is eliminated, and a microbial limit test method meeting the requirements of pharmacopeia is obtained.

The invention discloses adapalene benzoyl peroxide gel. The adapalene benzoyl peroxide gel is prepared from adapalene, benzoyl peroxide, 3%-7% of diethylene glycol monoethyl ether, 0.1%-0.3% of caprylic / capric polyethylene glycol glyceride and other pharmaceutically acceptable auxiliary materials. Through synergistic combination of the specific solvent and the surfactant, the problem that benzoyl peroxide is difficult to uniformly disperse only by conventional stirring in the prior art is successfully solved. According to the preparation method, the gel which is uniform in medicine dispersion, fine and smooth in texture and free of gravel feeling can be obtained only through conventional stirring, and complex processes such as high shearing, ultrasonic or spray drying and the like with safety risks do not need to be relied on. The process is simple, the cost is low, the production safety is high, and the obtained product has excellent stability and transdermal absorption performance.

The disclosure provides a topical gel formulation comprising 1-1.5 wt. % clindamycin phosphate, 2.5-3.5 wt. % benzoyl peroxide, and 0.1-0.2 wt. % adapalene, in combination with a gelling agent, a polyhydric alcohol, and water, useful in treating inflammatory skin conditions, including acne, together with methods of making and using the same.

The invention discloses a preparation method of adapalene key intermediate 1-(5-bromo-2-methoxyphenyl) adamantane. According to the preparation method, p-bromophenol and 1-adamantanol are subjected to a Friedel-Crafts reaction and methylation reaction to obtain the adapalene key intermediate 1-(5-bromo-2-methoxyphenyl) adamantane. The preparation method provided by the invention has the advantages of cheap and easily available raw materials, avoidance of high-base-toxicity reagents, simplicity and safety in operation, high yield, low cost, high product purity, high yield and the like, is very environment-friendly and is suitable for industrial amplification.

The invention belongs to the technical field of analysis and detection, and discloses an adapalene gel in-vitro release detection method which comprises the following steps: in an adapalene gel in-vitro release process, an adopted receiving medium is a mixed solution of a PBS buffer solution containing 0.5-2% of lauryl sodium sulfate and isopropanol; and the filter membrane is a PTFE (Polytetrafluoroethylene) filter membrane soaked by a receiving medium. And the detection method has the advantages of convenience, high efficiency, good linearity, strong specificity and high accuracy.

Methods for enhanced dermal delivery of adapalene esters to treat skin conditions including acne, rosacea, and photoaging are described. The invention is based on the discovery that applying lipophilic adapalene esters to non-disinfected skin and / or with preserved natural microflora results in significantly enhanced penetration and therapeutic and non-therapeutic efficacy compared to conventional protocols involving preliminary skin disinfection. The methods avoid antimicrobial pretreatments, preserve beneficial skin microorganisms, and achieve high absorption and penetration of the adapalene ester while maintaining safety and reducing treatment complexity.

The invention discloses an optimized adapalene gel preparation method, which comprises: 1) preparing an edetate disodium solution: adding edetate disodium powder into purified water, and stirring to form a uniform edetate disodium solution; the method comprises the following steps: 1) preparing an edetate disodium solution, 2) preparing a carbomer phase: scattering carbomer into the edetate disodium solution in a small amount and multiple times under a stirring condition, 3) preparing an adapalene solution: mixing adapalene, propylene glycol and glycerol, and stirring until adapalene is completely dissolved in propylene glycol and glycerol to form a uniform adapalene solution; and 4) preparation of adapalene gel: under a stirring condition, fully mixing the adapalene solution with a carbomer phase, and adjusting the pH value of the gel with sodium hydroxide to obtain the adapalene gel.

The invention discloses a temperature-sensitive controlled-release acne-removing skin care product and a preparation method thereof, and belongs to the field of cosmetic preparations. According to the skin care product, mesoporous silica with ordered nano pore channels is used as a carrier, and high-activity and high-irritation acne removal components such as retinol, adapalene or salicylic acid are loaded in the pore channels of the mesoporous silica; and then, under the low-temperature condition of less than or equal to 10 DEG C, poloxamer F127 is utilized to perform self-assembly packaging on the surfaces of the drug-loaded particles and the inlets of the pore channels, and a temperature-sensitive gating layer is formed. The structure is kept closed at normal temperature, so that the long-term storage stability of the active ingredients is ensured; when the composition is smeared on skin, the gating layer is subjected to phase change shrinkage, and the pore channels are intelligently opened, so that the slow and controllable release of active ingredients is realized, and the 2-hour burst release rate is 1t; 5%. The product provided by the invention has excellent storage stability and intelligent slow-release function, and effectively solves the industrial problems of poor stability of acne-removing active components, high skin irritation caused by high burst release rate of traditional dosage forms and the like.

The invention discloses adapalene gel and a preparation method thereof. The adapalene gel is prepared from the following components in percentage by mass: 0.1 percent of adapalene, 0.8 to 1.4 percent of carbomer, 4 to 5 percent of propylene glycol, 0.1 to 0.3 percent of poloxamer, 0.05 to 0.15 percent of edetate disodium, 0.10 to 0.15 percent of methylparaben, 0.15 to 0.35 percent of phenoxyethanol and the balance of purified water. The adapalene gel is low in irritation, the preparation method is simple in process step, high in operability, uniform in dispersion and not prone to agglomeration, and the irritation of the adapalene gel can be improved.

The invention relates to the field of chemical synthesis of medicines, and provides a preparation method of adapalene, which comprises the following steps: reacting 6-halo-2-methyl naphthoate with metal zinc to prepare an organic zinc reagent; in a system containing a cuprous reagent, 2-(1-adamantyl)-4-halogenated anisole and the organic zinc reagent prepared in the first step are subjected to a coupling reaction, and adapalene is obtained after hydrolysis. The method simplifies the process route, reduces the production cost, solves the problem of high impurity control difficulty in the traditional method, and is suitable for industrial production.

The invention relates to adapalene gel and a preparation method thereof, and relates to the technical field of medicines, the adapalene gel comprises adapalene, a humectant, a bacteriostatic agent, a gel matrix, a metal chelating agent, a surfactant, a pH regulator and purified water; the preparation method comprises the following steps: adding the metal chelating agent and part of purified water into a dissolving tank, stirring and dissolving the humectant and the bacteriostatic agent, and slowly adding into the dissolving tank to obtain a mixed solution I; adding the gel matrix into the dissolving tank in a shearing state to obtain a mixed solution II; carrying out ultrasonic treatment on adapalene, a surfactant and part of purified water under the action of an ultrasonic instrument until the raw materials are uniformly dispersed, and adding into the mixed solution II to obtain a mixed solution III; stirring and shearing the mixed solution III. According to the preparation method, the gel matrix is added into the mixed solution I in a shearing state, the gel matrix can be completely swelled within 10 minutes, no obvious block mass exists, and the production efficiency is high; the ultrasonic pre-dispersion of adapalene is increased, so that the agglomeration condition of the raw materials is remarkably improved, and the content uniformity of the preparation is improved.

The disclosure provides a topical gel formulation comprising 1-1.5 wt. % clindamycin phosphate, 2.5-3.5 wt. % benzoyl peroxide, and 0.1-0.2 wt. % adapalene, in combination with a gelling agent, a polyhydric alcohol, and water, useful in treating inflammatory skin conditions, including acne, together with methods of making and using the same.

The invention belongs to the technical field of chemical synthesis, and in particular relates to an N-(1, 3-dioxo-2-aryl octahydrocyclopenta [c] pyrrole-4-yl) benzamide derivative and a synthesis method of the N-(1, 3-dioxo-2-aryl octahydrocyclopenta [c] pyrrole-4-yl) benzamide derivative. The invention successfully develops a [3 + 2] cycloaddition reaction of a photocatalytic cyclopropanamide compound and an N-substituted maleimide derivative, the N-(1, 3-dioxo-2-aryl octahydrocyclopenta [c] pyrrole-4-yl) benzamide derivative can be prepared according to the synthetic method disclosed by the invention, the yield can reach 34-92%, and the preparation method is simple and easy to operate. A convenient, mild-condition and efficient synthesis path is provided for constructing the functional five-membered carbocyclic compound, and a reaction system shows excellent functional group compatibility and substrate universality. Besides, through successful derivatization with complex drug molecules such as febuxostat and adapalene, the application potential of the synthesis method is highlighted, and the compound is expected to be widely applied to drug development and research.

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