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羟丙基甲基纤维素作为水凝胶基质以及柠檬酸-刺槐豆胶作为控释片的负性基质

Hydroxypropyl Methylcellulose as Hydrogel Matrix and Citric Acid-Locust Bean Gum as Negative Matrix for Controlled Release Tablet.

作者信息

Hadinugroho Wuryanto, Martodihardjo Suwaldi, Fudholi Achmad, Riyanto Sugeng, Prasetyo Jefri

机构信息

Faculty of Pharmacy, Widya Mandala Surabaya Catholic University, Kalisari Selatan No. 1, Pakuwon City, Surabaya 60112, Indonesia.

Faculty of Pharmacy, Gadjah Mada University, Sekip Utara, Yogyakarta 55281, Indonesia.

出版信息

ACS Omega. 2023 Feb 16;8(8):7767-7778. doi: 10.1021/acsomega.2c07432. eCollection 2023 Feb 28.

Abstract

: This study aimed at determining the optimum concentration of hydroxypropyl methylcellulose (HPMC) as hydrogel matrix and citric acid-locust bean gum (CA-LBG) as negative matrix for controlled release tablet formulation. In addition, the study was to determine the effect of CA-LBG and HPMC. CA-LBG accelerates the disintegration of tablets into granules so that the HPMC granule matrix swells immediately and controls drug release. The advantage of this method is that the tablets do not produce large HPMC gel lumps without drug (ghost matrix) but form HPMC gel granules, which can be rapidly degraded after all of the drug is released. The experiment followed the simplex lattice design to obtain the optimum tablet formula with CA-LBG and HPMC concentrations as optimization factors. Tablet production by the wet granulation method and ketoprofen is the model of the active ingredient. The kinetics of ketoprofen release was studied using several models. Based on the coefficients of each polynomial equation that HPMC and CA-LBG increased the value of angle of repose (29.91:27.87), tap index (18.99:18.77), hardness (13.60:13.32), friability (0.41:0.73), and release of ketoprofen (52.48:99.44). Interaction of HPMC and CA-LBG increased the value of angle of repose (3.25), tap index (5.64), and hardness (2.42). Interaction of HPMC and CA-LBG too decreased the friability value (-1.10) and release of ketoprofen (-26.36). The Higuchi, Korsmeyer-Peppas, and Hixson-Crowell model is the kinetics of eight experimental tablet formulas. The optimum concentrations of HPMC and CA-LBG for controlled release tablets are 32.97 and 17.03%, respectively. HPMC, CA-LBG, and a combination of both affect the physical quality of tablet and tablet mass. CA-LBG is a new excipient candidate that can control drug release from tablets by the matrix disintegration mechanism on the tablet.

摘要

本研究旨在确定羟丙基甲基纤维素(HPMC)作为水凝胶基质以及柠檬酸-刺槐豆胶(CA-LBG)作为控释片制剂负性基质的最佳浓度。此外,该研究还旨在确定CA-LBG和HPMC的作用。CA-LBG可加速片剂崩解成颗粒,从而使HPMC颗粒基质立即膨胀并控制药物释放。该方法的优点是片剂不会产生无药物的大HPMC凝胶块(空骨架),而是形成HPMC凝胶颗粒,在所有药物释放后可迅速降解。实验采用单纯形格子设计,以CA-LBG和HPMC浓度作为优化因素来获得最佳片剂配方。通过湿法制粒生产片剂,酮洛芬作为活性成分的模型。使用几种模型研究了酮洛芬的释放动力学。基于每个多项式方程的系数,HPMC和CA-LBG提高了休止角(29.91:27.87)、堆密度(18.99:18.77)、硬度(13.60:13.32)、脆碎度(0.41:0.73)以及酮洛芬的释放量(52.48:99.44)。HPMC和CA-LBG的相互作用提高了休止角(3.25)、堆密度(5.64)和硬度(2.42)。HPMC和CA-LBG的相互作用也降低了脆碎度值(-1.10)和酮洛芬的释放量(-26.36)。Higuchi、Korsmeyer-Peppas和Hixson-Crowell模型是八个实验片剂配方的动力学。控释片的HPMC和CA-LBG最佳浓度分别为32.97%和17.03%。HPMC、CA-LBG及其组合会影响片剂的物理质量和片重。CA-LBG是一种新型辅料候选物,可通过片剂上的基质崩解机制控制药物从片剂中的释放。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b0fe/9979311/d91355296219/ao2c07432_0003.jpg

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