17 results about "Lurasidone Hydrochloride" patented technology

A lurasidone hydrochloride composition and a preparation method thereof, comprising a lurasidone hydrochloride granular composition and a lubricant. The lurasidone hydrochloride granular composition comprises lurasidone hydrochloride, cross-linked sodium carboxymethyl cellulose, silicon dioxide, pregelatinized starch, a filler, and a binder.

The present disclosure discloses a lurasidone hydrochloride oral film composition, preparation method and use thereof. The present disclosure discloses the lurasidone hydrochloride oral film composition including an active pharmaceutical, a film-forming material, a plasticizer and a flavoring agent, wherein the active pharmaceutical is (3aR,4S,7R,7aS)-2-((1R,2R)-2-[4-(1.2-benzisothiazol3-yl)piperazine-1-methyl]cyclohexylmethyl)hexahydro-4.7-methylene-2H-isoindole-1,3-dione hydrochloride denoted by the following formula I. The lurasidone hydrochloride oral film composition of the present disclosure has a good dissolution rate, a uniform appearance, a good flexibility, and a uniformity content meeting the requirement. Moreover, during the preparation process of the film liquid of the composition, sedimentation of the film will not occur. After the composition is dissolved in the user’s mouth, the user does not have any gritty feeling.

The invention belongs to the field of pharmaceutical analysis, and relates to a method for detecting chlorinated impurities in a lurasidone hydrochloride raw material. Comprising the following steps: dissolving a lurasidone hydrochloride raw material with formic acid and acetonitrile, adding water for dilution, carrying out ultrasonic precipitation, and filtering to obtain a test solution; wherein the volume ratio of the formic acid to the acetonitrile to the water is (0.9-1.1): (8-10): (85-95); and detecting the test solution by adopting high performance liquid chromatography to obtain the content of the chlorinated impurities in the lurasidone hydrochloride raw material. The detection method is accurate and reliable in result, simple and convenient to operate, high in precision and good in precision and linearity, the problem that lurasidone hydrochloride is not easy to dissolve can be effectively solved, and 40 mg / ml of lurasidone hydrochloride can be dissolved to the maximum extent. The detection method provided by the invention provides a vacancy of a chlorinated impurity detection method, and can be applied to production quality control of lurasidone hydrochloride raw material medicines.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a lurasidone hydrochloride oral instant film agent and a preparation method thereof. The oral instant film agent comprises the following components: an active component, a film-forming material, a plasticizer, a flavoring agent and a pigment. Wherein a film-forming material is preferably a combination of hydroxypropyl methylcellulose E15 and xanthan gum, so that the whole film-forming system has relatively high drug loading capacity; neotame is preferably selected as the flavoring agent, so that the mouth feel of the oral instant film is improved, and meanwhile, the film agent is ensured to have good mechanical properties. Moreover, the oral instant film can be rapidly disintegrated and dissolved in the oral cavity, is high in drug release speed, can rapidly take effect, is beneficial to improving the medication compliance of patients, especially children patients and elderly patients, is convenient to take, and solves the problem that the oral instant film cannot be taken in time under the condition of no water.

The invention discloses a method for detecting a lurasidone hydrochloride hydrolysate. The method is a high performance liquid chromatography, and the chromatographic conditions are as follows: octadecylsilane chemically bonded silica is used as a filler; the mobile phase A is phosphate buffer solution-acetonitrile with the pH value of 6.0 to 8.0; a mobile phase B is acetonitrile water; the flow velocity is 0.5 ml to 1.5 ml per minute; the detection wavelength is 200 to 250 nm; the column temperature is 20-35 DEG C; the temperature of a sample injector is 0-10 DEG C; the sample injection volume is 5-20 microliters. The detection method for the lurasidone hydrochloride hydrolysate is high in specificity, good in separation degree and high in recovery rate.

A method for preparing lurasidone hydrochloride by reacting lurasidone free alkali reacts with hydrochloric acid in a mixed solvent of an alcoholic solvent and an alkyl halide solvent.

The present application relates to a lurasidone hydrochloride pharmaceutical composition and a preparation method thereof. The present application discloses a lurasidone hydrochloride pharmaceutical composition, which comprises lurasidone hydrochloride and a stabilizer, wherein the lurasidone hydrochloride is in nanoscale. The prepared lurasidone hydrochloride pharmaceutical composition can improve the solubility and bioavailability of the drug, and reduce the influence of food effect. The preparation method of the present application is simple in operation, low in production cost and easy to realize industrialized scale-up production.

The invention provides a lurasidone orally disintegrating tablet and a preparation method thereof, and relates to the technical field of pharmaceutical preparations. The lurasidone orally disintegrating tablet is prepared from the following components in parts by mass: 15 to 23 parts of lurasidone hydrochloride, 60 to 70 parts of a filling agent, 1.5 to 3.5 parts of an adhesive, 9 to 12 parts of a disintegrating agent, 0.1 to 1 part of a sweetening agent and 0.5 to 2 parts of a lubricating agent, the filling agent comprises mannitol and microcrystalline cellulose; the mass ratio of the mannitol to the microcrystalline cellulose is 1: (1-5). The lurasidone orally disintegrating tablet prepared by the preparation method disclosed by the invention is fast in disintegration, high in dissolution rate and better in stability.

A lurasidone hydrochloride oral soluble film composition, a preparation method therefor and a use thereof are provided. The lurasidone hydrochloride oral soluble film composition contains an active drug, a film-forming material, a plasticizer and a flavoring agent. The active drug is (3aR,4S,7R,7aS)-2-((1R,2R)-2-[4-(1.2-benzisothiazole 3-yl)piperazine-1-methyl]cyclohexylmethyl)hexahydro-4.7-methylene-2H-isoindole-1,3-dione hydrochloride, as shown in Formula I.

The application discloses a preparation method of lurasidone hydrochloride and belongs to the technical field of chemical synthesis. The method comprises the following steps: A: reacting (3aR,7aR)-4'-(benzo[d]isothiazol-3-yl) octahydrospiro[isoindol-2,1'-piperazine]-2-X ammonium with ronexiamine, toluene and potassium carbonate to generate an intermediate product shown in formula III (3aR,4R,7S,7aS)-2-((1R,2R)-2-(4-(benzo[d]isothiazol-3-yl)piperazine-1-methyl)cyclohexyl)methyl)-3a,4,7,7a-tetrahydro-1H-4,7-methylisoindol-1,3(2H)-dione; B: reacting the intermediate product shown in formula III with hydrogen and a catalyst Y to generate lurasidone, and reacting lurasidone with hydrochloric acid to generate lurasidone hydrochloride. The application avoids the use of a phase transfer catalyst, overcomes the defects of low separation yield, poor selectivity, low yield and high cost, and has great implementation value and social and economic benefits due to the following advantages: raw materials are easy to obtain, operation is simple, reaction conditions are mild, and waste is less.

Provided are a lurasidone hydrochloride orally dissolving film composition, a preparation method and application thereof. The lurasidone hydrochloride orally dissolving film composition comprises an active drug, a film forming material, a plasticizer and a flavoring agent, and the active drug is (3aR,4S,7R,7aS)-2-((1R,2R)-2-[4-(1.2-benzisothiazole 3-yl)piperazine-1-methyl]cyclohexylmethyl)hexahydro-4.7-methylen-2H-isoindole-1,3-dione hydrochloride salt as shown in formula I. The obtained lurasidone hydrochloride orally dissolving film composition has a good dissolution rate, does not have a sand feeling after dissolving in the oral cavity, has a uniform appearance, good flexibility, and does not have sedimentation during the preparation of the film liquid, and the content uniformity meets the requirements.

The invention discloses a lurasidone hydrochloride sublingual or buccal membrane as well as a preparation method and application thereof. The lurasidone hydrochloride sublingual or buccal membrane agent comprises lurasidone hydrochloride with the particle size of less than or equal to 10 microns, a membrane forming material, a plasticizer and a flavoring agent, the film forming material comprises one or more of polyoxyethylene, polyvinyl alcohol, hydroxypropyl methyl cellulose, hydroxy propyl cellulose, sodium carboxymethyl cellulose, methyl cellulose, ethyl cellulose and copovidone; the lurasidone hydrochloride with the particle size of less than or equal to 10 microns is prepared by a homogenizing method. The film agent is absorbed through a near-end mucous membrane, the problems of first-pass metabolism and gastrointestinal tracts are avoided, and the film agent is rapidly absorbed to take effect. The preparation is high in dissolution rate, uniform and stable in medicine content and capable of being dissolved in the oral cavity without drinking water, and the compliance of a patient is improved. The lurasidone hydrochloride raw material prepared by the preparation method of the film agent has a particle size of less than 10 [mu] m, is simple in production process, is environment-friendly and safe, and is convenient for commercial production and application.

1. Name of the product of this design: Packaging kit (lurasidone hydrochloride orally disintegrating film). 2. Purpose of this design product: used for product packaging. 3. The key design point of this design product lies in the combination of shape and pattern. 4. The image or photograph that best illustrates the key design features: 3D image of Kit 1. 5. Kit Description: Kit 1 is the packaging box; Kit 2 is the packaging bag.

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a lurasidone hydrochloride-containing pharmaceutical composition and a preparation method thereof, the pharmaceutical composition further comprises a film-forming material and a plasticizer, and the film-forming material comprises polyvinyl alcohol. The pharmaceutical composition and the lurasidone hydrochloride oral instant film prepared from the pharmaceutical composition provided by the invention have in-vivo bioavailability equivalent to that of commercially available tablets, can be quickly disintegrated in the oral cavity without water, have good taste and bring convenience to clinical use. In addition, the device also has good stability and is convenient for production management. In addition, the lurasidone hydrochloride oral instant film provided by the invention is high in drug loading capacity, thin in thickness, small in tablet weight, excellent in mechanical property, convenient to produce and transport, beneficial to improving the specification of the film agent and good in social benefit.

Provided are a lurasidone hydrochloride oral soluble film composition, a preparation method therefor and a use thereof. The lurasidone hydrochloride oral soluble film composition contains an active drug, a film-forming material, a plasticizer and a flavoring agent. The active drug is (3aR,4S,7R,7aS)-2-((1R,2R)-2-[4-(1.2-benzisothiazole 3-yl)piperazine-1-methyl]cyclohexylmethyl)hexahydro-4.7-methylene-2H-isoindole-1,3-dione hydrochloride, as shown in Formula I. The obtained lurasidone hydrochloride oral soluble film composition has a good dissolution rate, has no gravelly feeling in the oral cavity after dissolution, has a uniform appearance and good flexibility, and does not precipitate during the preparation of the film liquid; content uniformity thereof meets requirements.

A lurasidone hydrochloride formulation, comprising lurasidone hydrochloride and a carrier, wherein the carrier comprises: Soluplus, and at least one of HPMCAS HG and HPMCAS HF. The formulation can increase the dissolution rate and solubility of lurasidone hydrochloride and ensure increased dissolution of lurasidone hydrochloride in the small intestine, such that the bioavailability and in-vivo absorption of lurasidone hydrochloride is improved, reducing excessive medication restrictions, avoiding reduced or even ineffective therapeutic effects caused by improper medication, and thus ensuring normal exertion of the efficacy of the drug. Moreover, the lurasidone hydrochloride formulation can also weaken or eliminate the food effect, thereby facilitating greater flexibility and compliance in patient medication.