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Preparation of Citric Acid-Locust Bean Gum (CA-LBG) for the Disintegrating Agent of Tablet Dosage Forms
Journal of Pharmaceutical Innovation ( IF 2.6 ) Pub Date : 2021-10-11 , DOI: 10.1007/s12247-021-09591-0
Wuryanto Hadinugroho 1, 2 , Suwaldi Martodihardjo 2 , Achmad Fudholi 2 , Sugeng Riyanto 2
Affiliation  

Purpose

Analyze the effect of HCl concentration 0.24 mol as a synthesis catalyst on the viscosity of CA-LBG and determine the effect of the application of CA-LBG as a disintegrating agent on the physical quality of tablets.

Methods

Citric acid-locust bean gum (CA-LBG) was synthesized from citric acid (CA) and locust bean gum (LBG) using hydrochloric acid (HCl) and ultraviolet irradiation (UV 254 nm, 100 min). The CA-LBG was analyzed by Fourier transform infrared spectroscopy (FTIR), nuclear magnetic resonance (NMR), scanning electron microscopy (SEM), esterification efficiency, solubility, and viscosity. The tablet formulation used CA-LBG with a concentration variation of 0.5%, 1%, 2%, 4%, 8%, and 12%. Preparation of tablets by direct compression uses a spray dray lactose (SDL) as a filler with a tablet weight of 200 mg.

Results

Synthesis conditions using 0.24 mol HCl to produce CA-LBG 9.48 cP. The presence of CA-LBG as a disintegrating agent has variation effects to thickness, break force, tensile strength, and friability according to the concentration used. In the formulation process, increasing the concentration of CA-LBG in the tablet mass decreased the flow rate and increased compressibility.

Conclusion

The increase in the concentration of CA-LBG in tablets accelerated the disintegration of tablets without the influence of other tablet parameters. The CA-LBG disintegration activity through repulsion between CA-LBG deformations on the tablet when wetted with disintegration medium. The repulsion force occurs due to the character of CA-LBG which has low solubility and low viscosity.

Graphical Abstract



中文翻译:

用于片剂剂型崩解剂的柠檬酸-刺槐豆胶(CA-LBG)的制备

目的

分析盐酸浓度0.24 mol作为合成催化剂对CA-LBG黏度的影响,并确定应用CA-LBG作为崩解剂对片剂物理质量的影响。

方法

柠檬酸-刺槐豆胶 (CA-LBG) 由柠檬酸 (CA) 和刺槐豆胶 (LBG) 使用盐酸 (HCl) 和紫外线照射 (UV 254 nm, 100 min) 合成。CA-LBG 通过傅里叶变换红外光谱 (FTIR)、核磁共振 (NMR)、扫描电子显微镜 (SEM)、酯化效率、溶解度和粘度进行分析。片剂配方使用 CA-LBG,浓度变化为 0.5%、1%、2%、4%、8% 和 12%。通过直接压片制备片剂使用喷雾干燥乳糖 (SDL) 作为填充剂,片重为 200 毫克。

结果

使用 0.24 mol HCl 产生 CA-LBG 9.48 cP 的合成条件。根据使用的浓度,CA-LBG 作为崩解剂的存在对厚度、断裂力、拉伸强度和脆性有不同的影响。在制剂过程中,增加片剂质量中 CA-LBG 的浓度会降低流速并增加可压性。

结论

片剂中CA-LBG浓度的增加加速了片剂的崩解,而不受其他片剂参数的影响。当用崩解介质润湿时,CA-LBG 崩解活性通过片剂上 CA-LBG 变形之间的排斥力实现。由于CA-LBG具有低溶解性和低粘度的特性,产生排斥力。

图形概要

更新日期:2021-10-12
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