Preparation and Evaluation of Valnemulin Hydrochloride Taste-Masking Granules

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BACKGROUND: The bitter taste and strong irritation of valnemulin hydrochloride limit its wide clinical application in pigs by oral.

METHOD: In order to improve its palatability and residence time in the body, the valnemulin hydrochloride taste-masking granules with sustained-release were prepared by combining solid dispersion based on fatty acid with wet granulation. The formulation was screened by orthogonal test with content, yield, grain size and angle of repose as evaluation indexes.

RESULT: The results showed that the optimal granules were composed of corn starch, sucrose, citric acid, valnemulin hydrochloride and myristic acid at a ratio of 40: 20: 20: 11: 19. The daily feed intake of pigs in the optimum taste-masking granule groups was similar to that of its self-control, and significantly higher than that in the valnemulin hydrochloride active ingredient group, suggesting that the optimum granules have satisfactory palatability. The prepared granules improved the oral bioavailability of valnemulin hydrochloride by 3.04 folds and extended its mean residence time (MRT) by 2.33 folds.

CONCLUSION: The granules developed in this study could obviously improve the palatability and sustained release of valnemulin hydrochloride. The producing method of granules by combining solid dispersion powder with wet granulation can provide ideas for other drugs with poor palatability and a short half-life.

Medienart:

E-Artikel

Erscheinungsjahr:

2022

Erschienen:

2022

Enthalten in:

Zur Gesamtaufnahme - volume:19

Enthalten in:

Current drug delivery - 19(2022), 3 vom: 03., Seite 337-346

Sprache:

Englisch

Beteiligte Personen:

Liang, Yongjie [VerfasserIn]
Hu, Danlei [VerfasserIn]
Yan, Yuanyuan [VerfasserIn]
Chen, Dongmei [VerfasserIn]
Xie, Shuyu [VerfasserIn]

Links:

Volltext

Themen:

2AHC415BQG
Anti-Bacterial Agents
Diterpenes
Granules
Journal Article
Myristic acid
Palatability
Powders
Solid dispersion
Sustained release
Valnemulin
Valnemulin hydrochloride

Anmerkungen:

Date Completed 12.04.2022

Date Revised 12.04.2022

published: Print

Citation Status MEDLINE

doi:

10.2174/1567201818666210903151658

funding:

Förderinstitution / Projekttitel:

PPN (Katalog-ID):

NLM330200062