右布洛芬肠溶薄膜片：设计、表征和人体志愿者药代动力学分析。

IF 2.6 4区医学 Q2 PHARMACOLOGY & PHARMACY

Pharmaceutical Development and Technology Pub Date : 2024-10-01 Epub Date: 2024-09-04 DOI:10.1080/10837450.2024.2398537

Anas M Hanif, Abdul Rehman, Rabia Bushra, Nousheen Aslam, Shazia Alam, Hamdy M Dawaba, Aya M Dawaba, Ossama M Sayed

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引用次数: 0

摘要

研究目的本研究旨在为胃刺激剂右布洛芬开发一种稳定且可扩展的肠道薄膜包衣片剂：利用超崩解直接压片法（氯丙维酮），在最佳核心批次上涂覆 Opadry 白色密封涂层，并在肠道内涂覆含颜料（滑石粉）的 Eudragit®L100，显示重量增加了 12%；使用特定 pH 缓冲液和扫描电镜评估释放和完整性，稳定性测试确认在 40 °C 和 75% 相对湿度条件下的保质期为 6 个月：结果：优化后的制剂在磷酸盐缓冲液中 60 分钟内实现了 99.87% 的释放，在酸性条件下 120 分钟内保持了完整性，与 Innovifen 相比，生物利用度更高（相对生物利用度≈121%），Cmax 也更高（18.35 µg/ml 而 Innovifen 为 11.1 µg/ml）：这些结果凸显了该制剂通过延迟肠道技术和快速肠道释放提高患者安全性和疗效的潜力。

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Dexibuprofen enteric film-coated tablets: design, characterization and pharmacokinetic analysis in human volunteers.

Objective: This study aimed to develop a stable and scalable enteric film-coated tablet for the gastric irritant dexibuprofen.

Methods: Utilizing direct compression with super-disintegration (crospovidone), the optimal core batches were coated with Opadry white seal coat and enterically coated with Eudragit^®L100 with pigment (Talc), demonstrating a 12% weight increase; release and integrity were assessed using specific pH buffers and SEM, with stability testing confirming a six-month shelf life at 40 °C and 75% RH.

Results: The optimized formulation achieved 99.87% release in phosphate buffer within 60 min, maintained integrity for 120 min in acidic conditions, and exhibited superior bioavailability compared to Innovifen with relative bioavailability ≈of 121% and elevated C_max (18.35 µg/ml compared to 11.1 µg/ml).

Conclusion: These results highlight the potential of this formulation to enhance patient safety and efficacy through delayed enteric technology and fast intestinal release.

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来源期刊

Pharmaceutical Development and Technology 医学-药学

CiteScore

5.90

自引率

2.90%

发文量

审稿时长

1 months

期刊介绍： Pharmaceutical Development & Technology publishes research on the design, development, manufacture, and evaluation of conventional and novel drug delivery systems, emphasizing practical solutions and applications to theoretical and research-based problems. The journal aims to publish significant, innovative and original research to advance the frontiers of pharmaceutical development and technology. Through original articles, reviews (where prior discussion with the EIC is encouraged), short reports, book reviews and technical notes, Pharmaceutical Development & Technology covers aspects such as: -Preformulation and pharmaceutical formulation studies -Pharmaceutical materials selection and characterization -Pharmaceutical process development, engineering, scale-up and industrialisation, and process validation -QbD in the form a risk assessment and DoE driven approaches -Design of dosage forms and drug delivery systems -Emerging pharmaceutical formulation and drug delivery technologies with a focus on personalised therapies -Drug delivery systems research and quality improvement -Pharmaceutical regulatory affairs This journal will not consider for publication manuscripts focusing purely on clinical evaluations, botanicals, or animal models.