美洛昔康-氨基酸盐/离子对复合物,具有更高的溶解度、溶解性和胃安全性。

IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Hamdy Abdelkader, Adel Al Fatease, Zeinab Fathalla, Mai E Shoman, Heba A Abou-Taleb
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引用次数: 0

摘要

氨基酸作为一种潜在的功能性辅料,在优化难溶性药物的生物制药特性方面备受关注。氨基酸种类繁多,具有多种功能基团、天然化合物、生物相容性和低分子量物质。我们对丝氨酸和精氨酸这两种氨基酸与美洛昔康进行了研究。美洛昔康的溶解度极低;作为非甾体抗炎药,胃部不适和溃疡是常见的副作用。通过沉淀和物理混合技术制备了固体分散体。对制备的组合物进行了体外溶解、对接、DSC、傅立叶变换红外光谱、XRD、溶解度和胃溃疡形成研究。对接表明,碱性氨基酸精氨酸与美洛昔康之间形成了离子对/盐。溶解度和溶解速率分别提高了 3000 倍和 12 倍。DSC、傅立叶变换红外光谱和 X 射线衍射证实了这些发现。接受美洛昔康治疗的大鼠表面胃上皮细胞完整性丧失,并出现溃疡。接受美洛昔康:精氨酸治疗的动物组显示出完整的胃黏膜,表面上皮和胃腺组织良好,与未治疗的对照组几乎相似。精氨酸与胍基组在重复给药 10 天后能够保留胃黏膜。这项研究强调了精氨酸作为功能性辅料的作用,它不仅提高了溶解度和溶解速率,还改善了美洛昔康长期存在的胃部副作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Meloxicam-amino acids salts/ion pair complexes with advanced solubility, dissolution, and gastric safety.

Amino acids have attracted attention as a potential functional excipient for optimizing biopharmaceutics characteristics of poorly soluble drugs. The amino acids are a diverse class with many functional groups, natural compounds, biocompatible, and low-molecular-weight substances. Two amino acids serine and arginine were investigated with meloxicam. Meloxicam has extremely low solubility; being NSAIDs, gastric upset, and ulcer are common side effects. Solid dispersions were produced by precipitation and physical mixing techniques. The produced combinations underwent in vitro dissolution, docking, DSC, FTIR, XRD, solubility, and gastric ulcer formation studies. Docking indicated ion pair/salt formation between the basic amino acid arginine and meloxicam. Both solubility and dissolution rates were increased by up to 3000-fold and 12-fold, respectively. DSC, FTIR an XRD supported these findings. Rats treated with meloxicam showed loss of surface gastric epithelium integrity and ulceration. The animal group received meloxicam: arginine showed intact gastric mucosa with the surface epithelium and gastric glands well organized and nearly similar to the untreated control. Arginine with the guanidine group that was capable of preserving gastric mucosa after repeated administration for 10 days. This study highlighted the role of arginine as a functional excipient that did not only improve solubility and dissolution rates but ameliorated the long-standing gastric side effects attributed to meloxicam.

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来源期刊
CiteScore
5.90
自引率
2.90%
发文量
82
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.
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