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PDE5 inhibitor and dapoxetine coated chip and preparation method thereof

A technology of dapoxetine and PDE5, which is applied in the field of medicine and achieves the effects of good compliance, improved efficacy and good safety.

Pending Publication Date: 2022-04-15
福建瑞泰来医药科技有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent CN112263581A discloses a double-layer tablet compound preparation for treating PE and ED and its preparation method. The compound preparation is composed of dapoxetine for treating PE and tadalafil for treating ED, and is compressed with a double-layer tablet The machine presses the two active ingredients into the upper and lower layers respectively. Although they are not directly mixed, the upper and lower layers are still in close contact, which does not fundamentally solve the risk of compatibility reactions between the two active ingredients.

Method used

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  • PDE5 inhibitor and dapoxetine coated chip and preparation method thereof
  • PDE5 inhibitor and dapoxetine coated chip and preparation method thereof
  • PDE5 inhibitor and dapoxetine coated chip and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0080] Embodiment 1: Tadalafil dapoxetine pack chip

[0081] ① Preparation of tablet core

[0082] Weigh 560g of dapoxetine hydrochloride, 13g of silicon dioxide, 407g of lactose, and 10g of croscarmellose sodium, place in a hopper mixer, 10 rpm, mix for 15 minutes, add 10g of magnesium stearate, continue Mix for 5 minutes to obtain the tablet core blend material; put the tablet core blend material in the tablet press, and punch the tablet with a 5mm circular flat oblique, so that the tablet weight is about 60mg, and the hardness is 20-40N, that is, Dapoxime Ting tablets and chips. The plain tablet is placed in a coating pan, coated with gastric-soluble hydroxypropyl methylcellulose coating powder, and the weight is increased by about 3%, and the dapoxetine tablet core is obtained.

[0083] ② Preparation of shell material

[0084] Weigh 7g of hydroxypropyl cellulose, 2.8g of sodium lauryl sulfate, place in 175ml of purified water, stir to dissolve, and use it as a binder; w...

Embodiment 2

[0087] Embodiment 2: Tadalafil dapoxetine pack chip

[0088] ① Preparation of tablet core

[0089] Weigh 448g of dapoxetine hydrochloride, 13g of silicon dioxide, 30g of croscarmellose sodium, and 1g of red iron oxide, place them in a material bag for premixing, and pass through a 40-mesh sieve to obtain a premixed material; Place in a hopper mixer, add 498g of lactose, 10 rpm, mix for 15 minutes, add 10g of magnesium stearate, and continue mixing for 5 minutes to obtain the tablet core blend material; put the tablet core blend material into the tablet , with a 5mm round flat oblique punching tablet, so that the tablet weight is about 50mg, the hardness is 20-40N, and the dapoxetine tablet core is obtained.

[0090] ② Preparation of shell materials

[0091] Weigh 7g of hydroxypropyl cellulose, 2.8g of sodium lauryl sulfate, place in 175ml of purified water, stir to dissolve, and use it as a binder; weigh 40g of tadalafil, 715.2g of lactose, and croscarmellose Sodium 36g, hy...

Embodiment 3

[0094] Embodiment 3: Tadalafil dapoxetine pack chip

[0095] ① Preparation of tablet core

[0096] Weigh 224g of dapoxetine hydrochloride, 10g of silicon dioxide, 30g of croscarmellose sodium, and 1g of red iron oxide, place them in a material bag for premixing, and pass through a 40-mesh sieve to obtain a premixed material; Place in a hopper mixer, add 730g of lactose, 10 rpm, mix for 15 minutes, add 5g of magnesium stearate, and continue mixing for 5 minutes to obtain the tablet core blend material; put the tablet core blend material into the tablet , use a 5mm round flat oblique punching tablet, so that the tablet weight is about 50mg, and the hardness is 20-40N, that is, the dapoxetine tablet core is obtained.

[0097] ② Preparation of shell material

[0098]Weigh 7g of hydroxypropyl cellulose, 2.8g of sodium lauryl sulfate, place in 175ml of purified water, stir to dissolve, and use it as a binder; weigh 40g of tadalafil, 715.2g of lactose, and croscarmellose Sodium 36...

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Abstract

The invention relates to the technical field of medicines, in particular to a compound preparation for treating male erectile dysfunction and premature ejaculation and a preparation method thereof. The PDE5 inhibitor and dapoxetine coated tablet comprises a tablet core and a shell layer, the PDE5 inhibitor is arranged in the tablet core, and the dapoxetine is arranged in the shell layer; or dapoxetine is disposed within the tablet core and a PDE5 inhibitor is disposed within the shell layer; the weight ratio of the dapoxetine to the PDE5 inhibitor is (4-70): (2.5-100); according to the dosage form of the core-coated tablet, the PDE5 inhibitor and dapoxetine can be respectively placed in the shell layer and the tablet core, the mode that the tablet core is independently tableted and the shell layer material is prepared into the shell layer is realized, and the problems of compatibility reaction, influence on the drug effect and generation of more impurities caused by direct powder pressing of a common double-layer tablet are avoided.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a compound preparation for treating male erectile dysfunction and premature ejaculation and a preparation method thereof. Background technique [0002] Erectile dysfunction (Erectiledysfunction, ED) refers to the inability to achieve or maintain an erection for a satisfactory sexual life, and is the most common male sexual dysfunction disease. The three most widely used oral drugs for ED treatment are Sildenafil, Vardenafil and Tadalafil. Sildenafil is a phosphodiesterase 5 (phosphodiesterase 5, PDE5) inhibitor developed and produced by Pfizer of the United States, which was launched in the United States under the trade name Viagra in April 1998. Vardenafil is another PDE5 inhibitor jointly developed by Germany's Bayer and GlaxoSmithKline. Its trade name is Levitra. It was first launched in Germany in September 2003 and approved for marketing in China in September 2004. . Tad...

Claims

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Application Information

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IPC IPC(8): A61K9/24A61K9/36A61K31/138A61K45/06A61P15/10
Inventor 高保安褚襄萍王刚许洁刘金丹陈仕魁姚建堤毛昌元
Owner 福建瑞泰来医药科技有限公司
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