Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

A sildenafil citrate taste-masking preparation

A sildenafil citrate and preparation technology, applied in the field of medicine, can solve problems such as difficult to achieve taste masking, affect the taste of preparations, limit clinical adaptability and tolerance, etc.

Active Publication Date: 2015-05-27
SHENZHEN NEPTUNUS PHARMA RES INST CO LTD
View PDF6 Cites 9 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, it was found in the study that the preparations made according to the published prescription and preparation method of sildenafil citrate orally disintegrating tablets or sublingual tablets cannot completely cover the bad taste of the main sildenafil citrate , although a wide variety of sweeteners and flavoring agents are added to the prescription, the bitter taste of the main drug is more or less reflected in the oral administration, which greatly affects the mouthfeel of the preparation and limits the clinical adaptability and tolerance
This is because sildenafil citrate has an extremely bitter taste, and the specification is relatively large (140.5mg / tablet containing sildenafil citrate), through conventional dilution of excipients, flavoring agents and other taste-masking methods, Difficult to achieve complete, good taste masking

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A sildenafil citrate taste-masking preparation
  • A sildenafil citrate taste-masking preparation
  • A sildenafil citrate taste-masking preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] [Example 1] Sildenafil citrate melt dispersion-co-grind taste-masking preparation and preparation method thereof

[0024] prescription:

[0025]

[0026]

[0027] *Equivalent to sildenafil free base 100mg, which has the same meaning as "preparation specification: 0.1g". The same below.

[0028] Preparation:

[0029] Weigh the prescribed amount of sildenafil citrate and mix it with HPC evenly, place it in a twin-screw extruder, the throughput is 1kg / h, and the temperature is gradually increased from 20°C to 180°C during the passage, and finally in the Extrude from a discharge nozzle with a diameter of 2 mm, and the resulting molten dispersion filaments are cut and broken into particles with a diameter of about 1 mm. The above-mentioned granules are mixed with glyceryl behenate, the mixture is ground in an impact mill, and then passed through a 20-mesh sieve to obtain ground granules; the above-mentioned ground granules are mixed with xylitol and croscarmellose s...

Embodiment 2

[0030] [Example 2] Sildenafil citrate molten dispersion-co-grind taste-masking preparation and its preparation method

[0031] prescription:

[0032] Element

category

Content (mg / tablet)

Percentage (%)

Sildenafil Citrate

Main drug

35.1

15.0

HPC (Klucel TM ELF)

Thinner / taste masking agent

140.6

60.0

Glyceryl behenate

Taste masking agent

35.1

15.0

Mannitol

fillers / taste masking agents

18.0

7.7

Sodium carboxymethyl starch

disintegrant

2.4

1.0

mint flavor

flavoring agent

0.7

0.3

Magnesium stearate

lubricant

2.4

1.0

total

234.3 mg

100.0

[0033] Preparation:

[0034] Weigh the prescribed amount of sildenafil citrate and mix it with HPC evenly, place it in a twin-screw extruder, the throughput is 1kg / h, and the temperature is gradually increased from 20°C to 170°C during the passage, and finally in t...

Embodiment 3

[0035] [Example 3] Sildenafil citrate melt dispersion-co-grind taste-masking preparation and its preparation method

[0036] prescription:

[0037] Element

category

Content (mg / tablet)

Percentage (%)

Sildenafil Citrate

Main drug

140.5

30.0

HPC (Klucel TM JF)

Thinner / taste masking agent

140.5

30.0

Glyceryl behenate

Taste masking agent

93.7

20.0

Mannitol

fillers / taste masking agents

35.1

7.5

Sorbitol

fillers / taste masking agents

28.1

6.0

Crospovidone

disintegrant

18.7

4.0

lemon zest

flavoring agent

4.7

1.0

Sodium stearyl fumarate

lubricant

7.0

1.5

total

468.3 mg

100.0

[0038] Preparation:

[0039]Weigh the prescribed amount of sildenafil citrate and mix it with HPC evenly, place it in a twin-screw extruder, the throughput is 1kg / h, and the temperature is gradually increased fro...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Diameteraaaaaaaaaa
Diameteraaaaaaaaaa
Login to View More

Abstract

A sildenafil citrate taste-masking preparation and a preparing method thereof are disclosed. The sildenafil citrate taste-masking preparation at least comprises, based on the total weight of tablets, 15-30% of sildenafil citrate, 30-65% of hydroxypropyl cellulose and 15-20% of glyceryl behenate. The preparing method includes: mixing a formula dosage of the sildenafil citrate and a formula dosage of the hydroxypropyl cellulose to prepare melt dispersion, cutting the melt dispersion into particles, grinding the particles together with the glyceryl behenate, fully mixing with other auxiliary materials, and tabletting into tablets for oral administration.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a sildenafil citrate taste-masking preparation and a preparation method thereof. Background technique [0002] Sildenafil citrate is an oral drug for the treatment of erectile dysfunction (ED). It is a selective inhibitor of phosphodiesterase type 5 (PDE5) specific for cyclic guanosine monophosphate (cGMP). Mechanism of Action: The physiological mechanism of penile erection involves the release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation. The activation of guanylate cyclase by NO leads to an increase in the level of cyclic guanosine monophosphate (cGMP), which relaxes the smooth muscle in the cavernous body and fills the blood. Sildenafil is a highly selective phosphodiesterase 5 (PDE5) inhibitor. PDE5 is highly expressed in the corpus cavernosum, while in other tissues (including platelets, blood vessels and visceral smooth muscle, skeletal muscle...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/20A61K31/519A61K47/38A61K47/14A61P15/10A61P9/12A61P11/00
Inventor 李宁王志国崔婧王丽丽杨经安刘小柔王菲刘碧秀
Owner SHENZHEN NEPTUNUS PHARMA RES INST CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com