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Dapoxetine tablets and preparation method thereof

The technology of a lubricant and a filler is applied in the field of pharmaceutical preparations for treating premature ejaculation in men, which can solve problems such as affecting blood coagulation function, and achieve the effects of high bioavailability, small side effects and convenient taking.

Active Publication Date: 2015-05-06
JIANGSU TIANZHAO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In 2005, the FDA rejected the applications of Johnson & Johnson, ALZA and other companies, and did not approve the marketing of Dapoxetine. This drug must have significant side effects, but the pharmaceutical company did not disclose it for commercial interests. This drug is functionally Antidepressants also have the effect of suppressing blood pressure. In addition to common adverse reactions, such as dry mouth, loss of appetite, nausea, insomnia, and fatigue at the beginning of medication, there are also reports of stroke, heart attack, and hypotension. It may affect blood coagulation function, so it is contraindicated for patients with active peptic ulcer and bleeding

Method used

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  • Dapoxetine tablets and preparation method thereof
  • Dapoxetine tablets and preparation method thereof
  • Dapoxetine tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Dapoxetine tablet and preparation method of the present embodiment, its each composition is:

[0025]

[0026] The steps are:

[0027] 1. Micronize 30g of dapoxetine and 55g of mannitol together, and control the particle size to 0.5-5um;

[0028] 2. Dry and mix 10g of croscarmellose sodium and 2g of sodium lauryl sulfate through a 100-mesh sieve for 5 minutes;

[0029] 3. The fine powder obtained in the previous step and 1 / 2 of the disintegrating agent are made into a soft material with an aqueous ethanol solution, and granulated with a 20-mesh sieve;

[0030] 4. Dry the prepared granules at 50°C and sieve with 18 meshes;

[0031] 5. First add the remaining 1 / 2 of the disintegrating agent and 2g of orange flavor to the dry granules and mix for 5 minutes, then add 1g of talc powder and mix for 5 minutes until the intermediate is tested and then control the tableting pressure to form a chewable tablet. .

Embodiment 2

[0033] Dapoxetine tablet and preparation method of the present embodiment, its each composition is:

[0034]

[0035] The steps are:

[0036] 1. Micronize 60g of dapoxetine and 116g of sucrose together, and control the particle size to 1-5um;

[0037] 2. Dry and mix 18g sodium carboxymethyl starch and 1g sodium lauryl sulfate through an 80-mesh sieve for 5 minutes;

[0038] 3. The fine powder obtained in the previous step and 1 / 2 of the disintegrating agent are made into a soft material with an aqueous ethanol solution, and granulated with a 20-mesh sieve;

[0039] 4. Dry the prepared granules at 60°C, and sieve with 18 meshes;

[0040] 5. Add the remaining 1 / 2 of the disintegrating agent and 3g of mint flavor to the dry granules and mix for 10 minutes, then add 2g of magnesium stearate and mix for 5 minutes until the intermediate is tested and then control the tablet pressure to form a chewable tablet, that is have to.

Embodiment 3

[0042] Dapoxetine tablet and preparation method of the present embodiment, its each composition is: prescription

[0043]

[0044]

[0045] The steps are:

[0046] 1. Micronize 33.6g of dapoxetine hydrochloride and 55g of lactose together, and control the particle size to 1-10um;

[0047] 2. Dry and mix 8g of croscarmellose sodium and 2g of sodium lauryl sulfate through an 80-mesh sieve for 5 minutes;

[0048] 3. The fine powder obtained in the previous step and 2 / 3 of the disintegrating agent are made into a soft material with an aqueous ethanol solution, and granulated with a 20-mesh sieve;

[0049] 4. Dry the prepared granules at 60°C, and sieve with 18 meshes;

[0050] 5. Add the remaining 1 / 3 of the disintegrating agent and 0.8g of aspartame to the dry granules and mix for 5 minutes, then add 0.6g of magnesium stearate and mix for 5 minutes until the intermediate is qualified and then control the tableting pressure to form a Ordinary tablets, that is.

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Abstract

The invention relates to dapoxetine tablets and a preparation method thereof. The dapoxetine tablets comprise the following components in percentage by weight: 10 to 50 percent of dapoxetine, 30 to 80 percent of a filling agent, 3 to 20 percent of a disintegrant, 0.5 to 1 percent of a lubricant and 0.2 to 2.5 percent of a flavoring agent. The preparation method comprises the following steps: micronizing the dapoxetine and the filling agent and controlling the particle size to be 0.5-20 [mu]m; preparing the fine powder obtained in the previous step and a part of the disintegrant into a soft material by ethanol water and pelletizing by a 24-mesh sieve; drying the obtained fine particles at the temperature of 50 to 70 DEG C and straightening by a 20-mesh sieve; sequentially adding the rest disintegrant, the flavoring agent and the lubricant into the dried particles, carrying out blending for two times, and until intermediates are qualified by detection, and carrying out tabletting, so that the dapoxetine tablets are obtained, wherein blending is carried out for one time before the lubricant is added and then is carried out again after the lubricant is added. The dapoxetine tablets are coated or uncoated conventional tablets, chewable tablets and orally disintegrating tablets, are used for treating male prospermia, high in drug adsorption speed and bioavailability, and convenient to take and have small side effects.

Description

technical field [0001] The invention relates to a pharmaceutical preparation for treating premature ejaculation in men, specifically a tablet, including coated or uncoated ordinary tablets, chewable tablets and orally disintegrating tablets. Background technique [0002] Dapoxetine, the chemical structure is: (S)-N,N-dimethyl-3-(naphthyl-1-oxyl)-phenylalanine [0003] [0004] It is a selective serotonin reuptake inhibitor with a short half-life, used for the treatment of premature ejaculation in men, developed by companies such as Johnson & Johnson, and marketed in a few countries in Europe. The drug is absorbed quickly and can quickly reach the effective blood concentration. The peak time is 1.4 to 2.0 hours. The peak blood concentration of a single dose of dapoxetine 30 and 60 mg is 297 and 498 ng / mL respectively, which is dose-related. The volume of distribution It is 21L / kg, widely distributed in tissues, the drug concentration in nerve tissue is close to that in bl...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20A61K31/138A61K47/20A61P15/08
Inventor 孙大正沈玉红陈凤刘丽玲辛晓娜
Owner JIANGSU TIANZHAO PHARMA
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