Preparation of ebastine dispersible tablets by hot-melt dispersion

XU Chengzhi; ZHAO Zhiliang; DU Shuangyou; FENG Qianjian; ZHANG Chong

doi:10.3969/j.issn.1006-0111.2017.05.007

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Objective To prepare ebastine dispersible tablets by hot-melt dispersion method using hypromellose as a carrier. Methods Ebastine was heated to melt and dispersed in hot solution of hypromellose. The mixture was adsorbed by mannitol and then used to prepare dispersible tablets. The characteristics of hot-melt dispersion were analyzed by the methods of differential scanning calorimetry and X-ray powder diffraction. A comparison of dissolution curves between self-made dispersible tablets and original ebastine tablets was performed. Results The analysis of X-ray diffraction and differential scanning calorimetry showed that the ebastine in solid matrix remained the main crystalline characteristics. The dissolution of ebastine hot-melt dispersion was 95.07% in 15 min in vitro, which was significantly higher than that of micronized ebastine raw material. Moreover, the accumulative dissolution of ebastine dispersible tablets in 30 min was about 30% higher than the original drug. Conclusion The method of hot-melt dispersion using hypromellose as a carrier improved the ebastine dissolution significantly.

Preparation of ebastine dispersible tablets by hot-melt dispersion

Hangzhou Aoyipollen Pharmaceutical Co., Ltd, Hangzhou 310018, China

Received Date: 2016-06-13

Rev Recd Date: 2016-11-15

Key words:

ebastine /
dissolution /
hypromellose

Abstract: Objective To prepare ebastine dispersible tablets by hot-melt dispersion method using hypromellose as a carrier. Methods Ebastine was heated to melt and dispersed in hot solution of hypromellose. The mixture was adsorbed by mannitol and then used to prepare dispersible tablets. The characteristics of hot-melt dispersion were analyzed by the methods of differential scanning calorimetry and X-ray powder diffraction. A comparison of dissolution curves between self-made dispersible tablets and original ebastine tablets was performed. Results The analysis of X-ray diffraction and differential scanning calorimetry showed that the ebastine in solid matrix remained the main crystalline characteristics. The dissolution of ebastine hot-melt dispersion was 95.07% in 15 min in vitro, which was significantly higher than that of micronized ebastine raw material. Moreover, the accumulative dissolution of ebastine dispersible tablets in 30 min was about 30% higher than the original drug. Conclusion The method of hot-melt dispersion using hypromellose as a carrier improved the ebastine dissolution significantly.

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Reference (6)

[1]	西班牙艾美罗医用药物工业有限公司.依巴斯汀片说明书［Z］.2014年版.
[2]	日医工株式会社.依巴斯汀口腔崩解片［P］.特开2008-143853.2006-06-26.
[3]	魏振平,胡会国,毛世瑞,等.西沙比利HPMC固体分散体的制备及对药物体外释放促进作用［J］.中国药剂学杂志,2004,2(6):129-133.
[4]	Tsunashima D, Yamashita K, Ogawara K, et al. Preparation of extended release solid dispersion formulations of tacrolimus using ethylcellulose and hydroxypropylmethylcellulose by solvent evaporation method ［J］. J Pharm Pharmacol,2016,68(3):316-323.
[5]	Jung HJ, Ahn HI, Park JY, et al. Improved oral absorption of tacrolimus by a solid dispersion with hypromellose and sodium lauryl sulfate［J］. Int J Biol Macromol,2016,83(2):282-287.
[6]	Vo CL, Park C, Lee BJ. Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs［J］. Eur J Pharm Biopharm,2013,85(3):799-813.

[1]	西班牙艾美罗医用药物工业有限公司.依巴斯汀片说明书［Z］.2014年版.
[2]	日医工株式会社.依巴斯汀口腔崩解片［P］.特开2008-143853.2006-06-26.
[3]	魏振平,胡会国,毛世瑞,等.西沙比利HPMC固体分散体的制备及对药物体外释放促进作用［J］.中国药剂学杂志,2004,2(6):129-133.
[4]	Tsunashima D, Yamashita K, Ogawara K, et al. Preparation of extended release solid dispersion formulations of tacrolimus using ethylcellulose and hydroxypropylmethylcellulose by solvent evaporation method ［J］. J Pharm Pharmacol,2016,68(3):316-323.
[5]	Jung HJ, Ahn HI, Park JY, et al. Improved oral absorption of tacrolimus by a solid dispersion with hypromellose and sodium lauryl sulfate［J］. Int J Biol Macromol,2016,83(2):282-287.
[6]	Vo CL, Park C, Lee BJ. Current trends and future perspectives of solid dispersions containing poorly water-soluble drugs［J］. Eur J Pharm Biopharm,2013,85(3):799-813.

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Preparation of ebastine dispersible tablets by hot-melt dispersion

doi: 10.3969/j.issn.1006-0111.2017.05.007

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