A kind of sildenafil citrate oral preparation and preparation method thereof

A technology for sildenafil citrate and oral preparations, which is applied in the field of sildenafil citrate oral preparations and their preparation, can solve the problems of increased toxicity of final metabolites, increased types and dosages of excipients, and increased control risks.

Active Publication Date: 2021-11-23
GUANGZHOU BAIYUNSHAN PHARMA HLDG CO LTD BAIYUNSHAN PHARMA GENERAL FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the one hand, the use of antioxidants and acidogens has led to an increase in the types and dosage of excipients, increasing the risk of control; on the other hand, the toxicity of antioxidants requires attention: BHA has anti-estrogen-like activity and may cause cancer ; and tert-butylmethylphenol may cause calcium metabolism disorders, and the toxicity of its terminal metabolite (BHT-Q) increases significantly
CN103908434 does not mention the impact on impurity B and related control strategies

Method used

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  • A kind of sildenafil citrate oral preparation and preparation method thereof
  • A kind of sildenafil citrate oral preparation and preparation method thereof
  • A kind of sildenafil citrate oral preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0051] This example has prepared a kind of sildenafil citrate oral tablet, and in this tablet, preparation raw material comprises:

[0052] Sildenafil citrate 20g, microcrystalline lactose compound 320g, hydroxyethyl methylcellulose 10g, hydroxyethyl cellulose 20g, carmellose calcium 25g, magnesium stearate 5g, acesulfame potassium 0.5g .

[0053] The preparation method is: wet granulate the compound of sildenafil citrate and microcrystalline lactose and carmellose calcium with 50% ethanol-hydroxyethylmethylcellulose-hydroxyethylcellulose solution, and dry in an oven at 50°C , using a 24-mesh swinging machine to granulate, mix evenly with lubricant magnesium stearate and flavoring agent acesulfame potassium, and press into 1000 tablets.

Embodiment 2

[0055] This example has prepared a kind of sildenafil citrate oral tablet, and in this tablet, preparation raw material comprises:

[0056] Sildenafil citrate 25g, starch 200g, lactose 200g, hydroxymethylcellulose 15g, crospovidone 30g, magnesium stearate 5g, hydroxysugar chloride 1g.

[0057] The preparation method is as follows: sildenafil citrate, starch, lactose, and crospovidone are wet-granulated with 30% ethanol-hydroxyethyl methylcellulose solution, dried in an oven at 60° C., and granulated with an 18-mesh swinging machine. After being uniformly mixed with lubricant magnesium stearate and flavoring agent hydroxysugar chloride, pressed into 1000 tablets.

Embodiment 3

[0059] This example has prepared a kind of sildenafil citrate oral tablet, and in this tablet, preparation raw material comprises:

[0060] Sildenafil citrate 50g, microcrystalline cellulose 285g, calcium hydrogen phosphate 140g, hydroxyethyl cellulose 50g, carboxymethyl starch sodium 18g, magnesium stearate 6g, starch hydrolyzed oligosaccharide 1g.

[0061] The preparation method is: premix sildenafil citrate with hydroxyethyl cellulose and 150g microcrystalline cellulose for 10 minutes, then add the remaining microcrystalline cellulose, calcium hydrogen phosphate, carboxymethyl starch sodium and starch hydrolyzed oligosaccharides Mix for 30 minutes in total, finally add magnesium stearate and mix for 5 minutes, and press into 1000 tablets.

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Abstract

The invention provides an oral preparation of sildenafil citrate and a preparation method thereof. The oral preparation includes sildenafil citrate, a binder and auxiliary materials, wherein the binder includes hydroxyethyl cellulose, hydroxypropyl At least one of cellulose and hydroxyethylmethylcellulose. Compared with the prior art, in the sildenafil citrate oral preparation of the present invention, the binder used has the effect of anti-oxidation concurrently, can significantly reduce the generation of oxidative degradation product impurity B, can reduce impurity B at the same time Accumulation during the shelf life, no need to add additional antioxidants or antioxidant synergists. In addition, the oral preparation of sildenafil citrate provided by the present invention has less auxiliary material consumption, relatively simple prescription composition, and significantly reduced production cost.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an oral preparation of sildenafil citrate and a preparation method thereof. Background technique [0002] Sildenafil citrate is the first type 5 phosphodiesterase (phosphodiesterase 5, PDE-5) inhibitor approved by the U.S. Food and Drug Administration (FDA) in March 1997 , is a prescription drug for the treatment of erectile dysfunction (erectile dysfunction, referred to as ED), originally developed by Pfizer of the United States, with the trade name Viagra, and the dosage form is tablets, and the specifications include 0.1g, 50mg and 25mg. Viagra was first launched in Italy on April 1, 1998. [0003] The chemical structural formula of sildenafil is as follows: [0004] [0005] Studies have shown that sildenafil can enhance the release of NO by inhibiting the decomposition of cyclic guanosine monophosphate PDE-5 in the cavernous body, thereby...

Claims

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Application Information

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Patent Type & AuthorityPatents(China)
IPC IPC(8): A61K9/20A61K9/16A61K9/48A61K31/519A61K47/38A61K47/22A61K47/26A61P15/00
CPCA61K9/1617A61K9/1623A61K9/1652A61K9/2013A61K9/2018A61K9/2054A61K9/4858A61K9/4866A61K31/519A61P15/00
Inventor王玮邓琪李翠芬罗志波王健松
OwnerGUANGZHOU BAIYUNSHAN PHARMA HLDG CO LTD BAIYUNSHAN PHARMA GENERAL FACTORY