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具有协同抗氧化活性的Trisamo提取物直接压片的处方开发

Formulation Development of Directly Compressible Tablets Incorporating Trisamo Extract With Synergistic Antioxidant Activity.

作者信息

Suksaeree Jirapornchai, Wunnakup Thaniya, Chankana Natawat, Charoenchai Laksana, Monton Chaowalit

机构信息

Department of Pharmaceutical Chemistry, College of Pharmacy, Rangsit University, Pathum Thani 12000, Thailand.

Drug and Herbal Product Research and Development Center, College of Pharmacy, Rangsit University, Pathum Thani 12000, Thailand.

出版信息

Int J Food Sci. 2024 Oct 9;2024:8920060. doi: 10.1155/2024/8920060. eCollection 2024.

DOI:10.1155/2024/8920060
PMID:39421547
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11483649/
Abstract

This work investigates the synergistic antioxidant activity of the compositions of Trisamo (TSM) herbal formula containing the dried fruits of , , and . An augmented simplex lattice design was utilized to investigate the synergistic antioxidant activity, finding an equal mass ratio among the three herbal drugs to exhibit optimal synergistic antioxidant activity, with a combination index of less than 0.8. The optimal TSM extract was used to prepare directly compressible tablets employing a Box-Behnken design response surface methodology, optimizing compressional force (500, 1000, and 1500 psi), sodium starch glycolate (0%, 2%, and 4%), and magnesium stearate (0.5%, 1.0%, and 1.5%). Optimal parameters were a compressional force of 1000 psi, 2% sodium starch glycolate, and 0.5% magnesium stearate. The TSM extract tablet had a weight of 600.06 mg, a diameter of 12.78 mm, a thickness of 4.12 mm, a hardness of 6.85 kP, a friability of 0.30%, and a disintegration time of 1.81 min. Computer model predictions were verified with a low percentage error (≤ 10.00%). After 6 h, phenolic compounds were dissolved to an extent of approximately 40%-80%, including gallic acid (57.11%), corilagin (38.64%), chebulagic acid (58.49%), and chebulinic acid (81.44%). Stability data revealed that the phenolic compounds were retained for 3 months compared to the initial time point, with gallic acid at 81.43% and 100.27%, corilagin at 94.81% and 87.85%, chebulagic acid at 92.22% and 69.83%, and chebulinic acid at 107.00% and 85.54% at 30°C/75% RH and 45°C/75% RH, respectively. The summation of these four compounds did not change significantly when stored under either set of conditions. In summary, mixture design and response surface design were successfully utilized in the optimization of TSM extract tablets with synergistic antioxidant activity.

摘要

本研究考察了含有诃子、毛诃子和余甘子干燥果实的Trisamo(TSM)草药配方组合物的协同抗氧化活性。采用增强单纯形格子设计来研究协同抗氧化活性,发现三种草药之间质量比相等时表现出最佳的协同抗氧化活性,组合指数小于0.8。采用Box-Behnken设计响应面法,使用最佳的TSM提取物制备直接压片,优化压片力(500、1000和1500 psi)、淀粉乙醇酸钠(0%、2%和4%)和硬脂酸镁(0.5%、1.0%和1.5%)。最佳参数为压片力1000 psi、淀粉乙醇酸钠2%和硬脂酸镁0.5%。TSM提取物片剂重量为600.06 mg,直径为12.78 mm,厚度为4.12 mm,硬度为6.85 kP,脆碎度为0.30%,崩解时间为1.81 min。计算机模型预测结果得到验证,误差百分比很低(≤10.00%)。6小时后,酚类化合物溶解程度约为40%-80%,包括没食子酸(57.11%)、柯里拉京(38.64%)、诃子鞣酸(58.49%)和诃子次酸(81.44%)。稳定性数据显示,与初始时间点相比,酚类化合物在3个月内保持稳定,在30°C/75%RH和45°C/75%RH条件下,没食子酸分别为81.43%和100.27%,柯里拉京分别为94.81%和87.85%,诃子鞣酸分别为92.22%和69.83%,诃子次酸分别为107.00%和85.54%。在这两种条件下储存时,这四种化合物的总量没有显著变化。总之,混合设计和响应面设计成功用于优化具有协同抗氧化活性的TSM提取物片剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/5e6e7f71f11c/IJFS2024-8920060.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/03a4a58f8209/IJFS2024-8920060.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/3f71cb9e8f53/IJFS2024-8920060.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/296f331a7b36/IJFS2024-8920060.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/b2af3787c792/IJFS2024-8920060.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/260111eda264/IJFS2024-8920060.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/946e3b3586f3/IJFS2024-8920060.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/5e6e7f71f11c/IJFS2024-8920060.007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/03a4a58f8209/IJFS2024-8920060.001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/3f71cb9e8f53/IJFS2024-8920060.002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/296f331a7b36/IJFS2024-8920060.003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/b2af3787c792/IJFS2024-8920060.004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/260111eda264/IJFS2024-8920060.005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/946e3b3586f3/IJFS2024-8920060.006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/dd2a/11483649/5e6e7f71f11c/IJFS2024-8920060.007.jpg

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