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

Message Board

Respected readers, authors and reviewers, you can add comments to this page on any questions about the contribution, review, editing and publication of this journal. We will give you an answer as soon as possible. Thank you for your support!

Name

E-mail

Phone

Title

Content

Verification Code

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.

HTML

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.

Message Board

Preparation of ebastine dispersible tablets by hot-melt dispersion

doi: 10.3969/j.issn.1006-0111.2017.05.007

Abstract

References

Proportional views

通讯作者: 陈斌, [email protected]

Article Metrics

Related

Proportional views