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用于治疗高血压的安立生坦专利快速溶解口腔薄膜的设计优化与评估

Design Optimization and Evaluation of Patented Fast-Dissolving Oral Thin Film of Ambrisentan for the Treatment of Hypertension.

作者信息

Kanugo Abhishek

机构信息

SVKM NMIMS School of Pharmacy and Technology Management, Shirpur, Dhule, 425405, India.

Department of Pharmaceutical Quality Assurance, SVKM Institute of Pharmacy, Dhule, 424001, India.

出版信息

Recent Pat Nanotechnol. 2025;19(2):296-309. doi: 10.2174/0118722105298163240823100003.

DOI:10.2174/0118722105298163240823100003
PMID:39563214
Abstract

BACKGROUND

Cardiovascular diseases, including hypertension, are the prominent source of death globally. High blood pressure is responsible for heart failure and also damages the vital organs of the body, which also creates mortality. The activation of the sympathetic nervous system in the primary sunrise period is a highly critical condition, and several persons have lost their tissue due to the unavailability of medicine at this time.

OBJECTIVE

The present research deals with the progress of fast-dissolving oral thin film (OTF) of Ambrisentan for the prevention and cure of hypertension.

METHODS

The OTF was established using the solvent casting method. The compatibility of Ambrisentan with film former HPMC E15 was checked with FTIR and DSC. The optimization was assessed using the design of the experiment using 32 Box-Behnken designs. The independent parameters were filmed former (X1: HPMC E15), plasticizer (X2: PEG 400), and super disintegrant (X3: cross povidone) and dependable parameters were disintegration time (Y1) and dissolution release (Y2).

RESULTS

The optimized batch F7 showed the least disintegration time (9 sec), folding endurance of (99), content uniformity (98.57%), pH (6.4), and dissolved within 5 min. The scanning electron microscopy confirmed the evenness and smoothness of the film with a particle size of 10 μm. Patent related with OTF (Indian- 202321050359), US (11701339).

CONCLUSION

The investigation indicated that fast dissolving oral thin film of Ambrisentan improves the solubility and therapeutic efficacy in the prevention and treatment of cardiovascular complications. The prompt release of Ambrisentan minimizes the mortality associated with heart attack and hypertension.

摘要

背景

包括高血压在内的心血管疾病是全球主要的死亡原因。高血压会导致心力衰竭,还会损害身体的重要器官,进而导致死亡。在清晨时段交感神经系统的激活是一种极其关键的情况,此时有若干人因药物供应不足而失去组织。

目的

本研究探讨用于预防和治疗高血压的安立生坦速溶口腔薄膜(OTF)的进展。

方法

采用溶剂浇铸法制备OTF。通过傅里叶变换红外光谱(FTIR)和差示扫描量热法(DSC)检测安立生坦与成膜材料羟丙甲纤维素E15(HPMC E15)的相容性。使用32个Box-Behnken设计的实验设计进行优化评估。自变量为成膜材料(X1:HPMC E15)、增塑剂(X2:聚乙二醇400,PEG 400)和超级崩解剂(X3:交联聚维酮),因变量为崩解时间(Y1)和溶出度(Y2)。

结果

优化后的批次F7崩解时间最短(9秒),折叠次数为99次,含量均匀度为98.57%,pH值为6.4,在5分钟内溶解。扫描电子显微镜证实薄膜均匀光滑,粒径为10μm。与OTF相关的专利(印度 - 202321050359,美国 - 11701339)。

结论

研究表明,安立生坦速溶口腔薄膜提高了在预防和治疗心血管并发症方面的溶解度和治疗效果。安立生坦的快速释放将与心脏病发作和高血压相关的死亡率降至最低。

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Studies in Solid Solution Formation between Acetaminophen and Povidone and Mouth-dissolving Strip Formulation.对乙酰氨基酚和聚乙烯吡咯烷酮形成固溶体的研究及口溶膜制剂。
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Hydroxypropyl Methylcellulose Orodispersible Film Containing Desloratadine for Geriatric Use: Formulation and Evaluation.羟丙甲纤维素速溶口腔贴片含地氯雷他定用于老年患者:制剂与评价。
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