Time-delayed sustained release pharmaceutical composition comprising dapoxetine for oral administration

A technology of delayed release of dapoxetine, which is applied in the direction of drug combination, medical preparations containing active ingredients, drug delivery, etc. It can solve the problems of inability to exert itself, different half-life in the blood, etc., and achieve the goal of satisfying sexual desire and reducing side effects Effect

Inactive Publication Date: 2013-03-06
NAVIPHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, the Tmax of the premature ejaculation treatment agent and the impotence treatment agent are basically similar, each about 1 hour. Therefore, if they are administered at the same time, the drug effects of premature ejaculation and impotence will take the same time and the patient's sexual desire can be satisfied at the initial stage of taking. The blood half-life of each drug is different, and after a certain period of time after administration, the desired effect after simultaneous use cannot be exerted, so it needs to be improved.

Method used

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  • Time-delayed sustained release pharmaceutical composition comprising dapoxetine for oral administration
  • Time-delayed sustained release pharmaceutical composition comprising dapoxetine for oral administration
  • Time-delayed sustained release pharmaceutical composition comprising dapoxetine for oral administration

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1, manufacturing a pharmaceutical composition (1): bilayer tablet form

[0046] 33.6 g of Dapoxetine HCI was mixed with 89.4 g of lactose hydrate (Supertab 14SD), 80.0 g of microcrystalline cellulose (Avicel Ph200) and 12.0 g of crospovidone (Kolidon CL) before adding 1.0 g Magnesium stearate slip blend creates an immediate release blend. In addition, after mixing 33.6 g of dapoxetine hydrochloride, 24.4 g of lactose hydrate (Supertab 14SD), 75.0 g of hydroxypropyl methylcellulose (Methocel E50), and 35 g of polyvinylpyrrolidone VA64 (Kolidon VA64), 1.0 g was added Magnesium stearate creates an extended release blend. Each layer of each tablet contained 216 mg of the immediate-release mixture and 169 mg of the sustained-release mixture, and each layer contained 30 mg of each tablet, and a total of 60 mg of dapoxetine was manufactured. Then, it was coated with a coating solution prepared by dissolving the white film coating in purified water so that each tabl...

Embodiment 2

[0047] Example 2, Manufacture of Pharmaceutical Composition (2): Dosage Form of Mixed Tablets

[0048] 100.8g dapoxetine hydrochloride was mixed with 148.2g lactose hydrate (Pharmatose200), 300.0g microcrystalline cellulose (Avicel Ph101) and 36.0g croscarmellose sodium (Ac-Di-Sol), and then used The mixed solution prepared by dissolving 12.0 g of povidone (Kolidon K-30) in purified water was mixed to form particles and then dried. Then, 3.0 g of magnesium stearate was added after ingot into granules with a tablet machine to produce immediate-release granules. In addition, after mixing 100.8 g of dapoxetine hydrochloride with 316.2 g of lactose hydrate (Pharmatose 200) and 135.0 g of hydroxypropylmethylcellulose (Methocel E50), it was mixed with 15.0 g of povidone (Kolidon K-30) in The combined solution made by dissolving pure water is mixed to make granules and dried. Then 3.0 g of magnesium stearate was added by grading and mixed to manufacture sustained-release granules...

Embodiment 3

[0049] Embodiment 3, manufacture pharmaceutical composition (3): dosage form of bilayer tablet

[0050] The immediate-release mixture produced in Example 1 and the sustained-release granules produced in Example 2 were compressed with a double-layer tablet press so that each layer contained 216 mg and 169 mg, thereby producing each tablet with each layer Contains 30 mg bilayer tablet containing a total of 60 mg dapoxetine. Then, it was coated with a coating solution prepared by dissolving the white film coating in purified water so that each tablet contained 15 mg of the white film coating.

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Abstract

The present invention relates to a time-delayed sustained release pharmaceutical composition for oral administration, which comprises an immediate release phase and a prolonged sustained release phase, wherein said immediate release phase and prolonged sustained release phase respectively comprise dapoxetine therein as an active ingredient.; The pharmaceutical composition of the present invention comprises dapoxetine, which is an agent for treating premature ejaculation, in both the immediate release phase and the prolonged sustained release phase thereof, to thereby immediately exhibit the effectiveness of the pharmaceutical composition of the present invention in order to enable a patient to achieve sexual satisfaction during the early stage of administration, as well as to reduce side effects by means of the time-delayed sustained release of the prolonged sustained release phase during the early stage of administration and enable a continuous in vivo absorption of dapoxetines, to thereby lengthen the duration of the effectiveness of the pharmaceutical composition of the present invention.; Further, agents for treating erectile dysfunction, such as sildenafil, tadalifil or the like can be added to the immediate release phase so as to allow for a coincidence of the durations of the effectiveness of a premature ejaculation treatment agent and erectile dysfunction treatment agents, even though a half-life difference exists between the two types of treatment agents, thus maximizing patient satisfaction.

Description

technical field [0001] The present invention relates to a delayed-release oral pharmaceutical composition composed of an immediate-release phase and a sustained-release phase, and the immediate-release phase and the slow-release phase respectively contain dapoxetine as an active ingredient. Background technique [0002] Premature ejaculation is one of the most important phenomena leading to sexual dissatisfaction. It is a symptom of persistent or recurrent ejaculation before, during or after sexual intercourse before minimal sexual stimulation. The proportion of American men suffering from this symptom reaches 30~40% %. Traditional premature ejaculation treatment agents are basically non-oral drugs, such as lidocaine and other local anesthetics. These drugs are not only inconvenient to use, but also reduce the sexual desire satisfaction of the other party. Now some oral medicines for the treatment of premature ejaculation have begun to appear on the market, such as impotenc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/138A61K31/519A61K9/20
CPCA61K31/519A61K31/138A61K31/522A61K9/209A61K31/4985A61P15/00A61P43/00A61K9/20
Inventor 李昌珪朴相根
Owner NAVIPHARM CO LTD
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