Twin-Screw Melt Granulation with Mannitol: High-Drug-Loaded Immediate-Release Tablets of Caffeine

IF 5.1 4区医学 Q2 PHARMACOLOGY & PHARMACY

AAPS PharmSciTech Pub Date : 2026-06-12 DOI:10.1208/s12249-026-03464-w

Elzbieta Maria Buczkowska, Kirils Kukuls, Zoltán Márk Horváth, Alīna Jaroslava Frolova, Līga Pētersone, Suha Dadou, Valentyn Mohylyuk

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Abstract

High drug-loaded immediate-release formulations can be produced using a solvent-free and continuous melt-granulation method with a twin-screw extruder. Known and widely used high-molecular-weight and hydrophobic melt-binders result in weak tablets and negatively influence the disintegration and dissolution of tablets. Thus, this work aimed to probe mannitol as a melt-binder at a concentration of 30 wt.% and to investigate the effect of twin-screw melt granulation processing temperature and screw speed on the preparation of high drug-loaded immediate-release caffeine tablets with superior mechanical properties. A two-level design of experiment with three center points was used for the screening of the effect of barrel temperature and screw speed on granules and tablets properties. Model drug caffeine was mixed with mannitol (Parteck® M100), while a Pharma 11 extruder with helix feed screw elements and without a nozzle was used for twin-screw melt granulation. Processing conditions were found to significantly influence the solid state of ingredients and the quality of granules. Mannitol, as a melt-binder at a concentration of 30 wt.% at given processing conditions, was proven as an efficient melt-binder for high drug-loaded immediate-release tablets with superior mechanical properties.

Graphical Abstract

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甘露醇双螺杆熔融造粒：高负荷咖啡因速释片

采用双螺杆挤出机无溶剂连续熔融造粒法制备高载药速释制剂。已知和广泛使用的高分子量和疏水熔融结合剂导致片剂弱，并对片剂的崩解和溶出产生负面影响。因此，本研究旨在探讨甘露醇在30 wt.%的浓度下作为熔体粘合剂，并考察双螺杆熔体造粒工艺温度和螺杆速度对制备高负荷、高机械性能的咖啡因速释片的影响。采用三中心点双水平实验设计，筛选筒体温度和螺杆转速对颗粒和片剂性能的影响。模型药物咖啡因与甘露醇（Parteck®M100）混合，同时使用带有螺旋进料螺杆元件且不带喷嘴的Pharma 11挤出机进行双螺杆熔融造粒。研究发现，加工条件对原料的固体状态和颗粒质量有显著影响。甘露醇作为一种熔体粘合剂，在一定的工艺条件下，浓度为30wt .%，被证明是一种高效的熔体粘合剂，用于高载药速释片，具有优异的机械性能。此图像的替代文本可能是使用AI生成的。

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来源期刊

AAPS PharmSciTech 医学-药学

CiteScore

6.80

自引率

3.00%

发文量

264

审稿时长

2.4 months

期刊介绍： AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.