Development and Evaluation of Floating Microspheres of Anticonvulsant Drug by 32 Full Factorial Design.

IF 1.8 Q3 PHARMACOLOGY & PHARMACY
Manish Bhise, Karunakar Shukla, Sourabh Jain, Nitin Bhajipale, Suresh Sudke, Pramod Burakle
{"title":"Development and Evaluation of Floating Microspheres of Anticonvulsant Drug by 3<sup>2</sup> Full Factorial Design.","authors":"Manish Bhise,&nbsp;Karunakar Shukla,&nbsp;Sourabh Jain,&nbsp;Nitin Bhajipale,&nbsp;Suresh Sudke,&nbsp;Pramod Burakle","doi":"10.4274/tjps.galenos.2021.53050","DOIUrl":null,"url":null,"abstract":"<p><strong>Objectives: </strong>Present study was to develop and evaluate gastroretentive microspheres by the solvent evaporation technique.</p><p><strong>Materials and methods: </strong>Gabapentin and HPMC K100 were used to develop the formulations. Gastroretentive microspheres were developed by the solvent evaporation technique from the preliminary batches of gabapentin microspheres batch FMG3 were selected for factorial study.</p><p><strong>Results: </strong>Factorial batches showed the mean particle size of the floating microsphere formulations for gabapentin (FFMG1-FFMG9) was in the range of 185.63 ± 0.13 to 510.04 ± 0.09 μm. The percentage yields of formulations FFMG1 to FFMG9 for gabapentin ranged from 53.5 ± 0.95 to 96.64 ± 0.42. The buoyancy percentage was calculated for the formulations and found that all formulations could float on dissolution medium for 12 h. The drug loading in gabapentin microspheres was found 65.29 ± 0.46 to 84.3 ± 0.44. The swelling study was found to be 756.34 ± 1.48 to 890.46 ± 0.78 for gabapentin. Batch FFMG6 and FFMC2 showed better drug release 99.1% and 99.25% respectively. The optimized formulation FFMG6 for gabapentin showed an n value 0.8474 and R<sup>2</sup> value 0.9965.</p><p><strong>Conclusion: </strong>Optimized formulation obeys Korsmeyer-Peppas release. Scanning electron microscopy images of microspheres were spherical, discrete, and freely flowing. ANOVA for the given formulations showed <i>p</i> value less than 0.0500. The stability study indicated no significant changes in the microspheres. In radiographic images, floating microspheres were retained in the stomach of rabbits for twelve hours.</p>","PeriodicalId":23378,"journal":{"name":"Turkish Journal of Pharmaceutical Sciences","volume":"19 5","pages":"595-602"},"PeriodicalIF":1.8000,"publicationDate":"2022-10-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9634442/pdf/TJPS-19-595.pdf","citationCount":"2","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Turkish Journal of Pharmaceutical Sciences","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.4274/tjps.galenos.2021.53050","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 2

Abstract

Objectives: Present study was to develop and evaluate gastroretentive microspheres by the solvent evaporation technique.

Materials and methods: Gabapentin and HPMC K100 were used to develop the formulations. Gastroretentive microspheres were developed by the solvent evaporation technique from the preliminary batches of gabapentin microspheres batch FMG3 were selected for factorial study.

Results: Factorial batches showed the mean particle size of the floating microsphere formulations for gabapentin (FFMG1-FFMG9) was in the range of 185.63 ± 0.13 to 510.04 ± 0.09 μm. The percentage yields of formulations FFMG1 to FFMG9 for gabapentin ranged from 53.5 ± 0.95 to 96.64 ± 0.42. The buoyancy percentage was calculated for the formulations and found that all formulations could float on dissolution medium for 12 h. The drug loading in gabapentin microspheres was found 65.29 ± 0.46 to 84.3 ± 0.44. The swelling study was found to be 756.34 ± 1.48 to 890.46 ± 0.78 for gabapentin. Batch FFMG6 and FFMC2 showed better drug release 99.1% and 99.25% respectively. The optimized formulation FFMG6 for gabapentin showed an n value 0.8474 and R2 value 0.9965.

Conclusion: Optimized formulation obeys Korsmeyer-Peppas release. Scanning electron microscopy images of microspheres were spherical, discrete, and freely flowing. ANOVA for the given formulations showed p value less than 0.0500. The stability study indicated no significant changes in the microspheres. In radiographic images, floating microspheres were retained in the stomach of rabbits for twelve hours.

32全因子设计抗惊厥药物漂浮微球的研制与评价。
目的:利用溶剂蒸发技术制备胃保留微球并对其进行评价。材料与方法:以加巴喷丁、HPMC K100配制。以加巴喷丁微球为原料,采用溶剂蒸发法制备胃保留微球,选择FMG3批次进行析因研究。结果:阶乘批析结果表明,加巴喷丁漂浮微球制剂(ffmg1 ~ ffmg9)的平均粒径范围为185.63±0.13 ~ 510.04±0.09 μm;复方FFMG1 ~ FFMG9对加巴喷丁的收率范围为53.5±0.95 ~ 96.64±0.42。计算了各制剂的浮力百分比,发现各制剂均可在溶出介质上漂浮12 h。加巴喷丁微球的载药量为65.29±0.46 ~ 84.3±0.44。加巴喷丁的肿胀研究结果为756.34±1.48 ~ 890.46±0.78。批次FFMG6和FFMC2的释药效果较好,分别为99.1%和99.25%。加巴喷丁最佳处方FFMG6的n值为0.8474,R2为0.9965。结论:优化后的配方符合Korsmeyer-Peppas释放规律。微球扫描电镜图像呈球形,离散,自由流动。对给定配方的方差分析显示p值小于0.0500。稳定性研究表明微球无明显变化。在x线摄影图像中,漂浮的微球在兔子的胃中保留了12小时。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 求助全文
来源期刊
CiteScore
3.60
自引率
5.90%
发文量
79
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信