Horváth Zoltán Márk, Kukuls Kirils, Frolova Alīna Jaroslava, Žogota Marta, Buczkowska Elżbieta Maria, Pētersone Līga, Mohylyuk Valentyn
Leading Research Group, Faculty of Pharmacy, Rīga Stradiņš University, 21 Konsula St., LV-1007 Riga, Latvia.
Pharmaceutics. 2025 May 21;17(5):676. doi: 10.3390/pharmaceutics17050676.
: Effervescent granules containing citric acid and sodium bicarbonate were successfully prepared for the first time via TS-MG using a polyol (sorbitol) as a melt binder. : Processing parameters, specifically granulation temperature and screw speed, were systematically varied to investigate their influence. The granulation efficiency, inversely related to the wt.% of fines, decreased in the following order across the tested conditions (granulation temperature-screw speed; ℃-rpm): 95-6 > 100-5 > 90-5 > 100-7 > 90-7. Granulation temperature had a minimal impact on the bulk and tapped densities of the uncalibrated granules, whereas increased screw speed led to higher densities, associated with a reduced proportion of fines. The tensile strength of the resulting effervescent tablets increased with granulation temperature and was generally higher for tablets derived from granules with higher granulation efficiency. The residence time within the TS-MG barrel decreased with increasing temperature and screw speed. Notably, the greatest effect of granulation temperature on tensile strength occurred between 90 and 95 °C, particularly under longer residence times. The disintegration time of the tablets was shortest for the 90 °C and 5 rpm condition, corresponding to the lowest tensile strength, while tablets across formulations showed consistent homogeneity as indicated by similar pH values post-disintegration. : These findings underscore sorbitol's suitability as a melt binder and highlight the interplay between TS-MG parameters and the physical characteristics of effervescent granules and tablets.
首次通过热熔融制粒法（TS-MG），以多元醇（山梨醇）作为熔融黏合剂，成功制备出了含有柠檬酸和碳酸氢钠的泡腾颗粒。系统地改变了加工参数，特别是制粒温度和螺杆转速，以研究它们的影响。制粒效率与细粉重量百分比呈负相关，在测试条件（制粒温度-螺杆转速；℃-rpm）下，其降低顺序为：95-6＞100-5＞90-5＞100-7＞90-7。制粒温度对未校准颗粒的堆密度和振实密度影响最小，而螺杆转速增加会导致密度升高，同时细粉比例降低。所得泡腾片的抗张强度随制粒温度升高而增加，对于由制粒效率较高的颗粒制成的片剂，其抗张强度通常更高。在TS-MG料筒内的停留时间随温度和螺杆转速的增加而减少。值得注意的是，制粒温度对抗张强度的最大影响发生在90至95℃之间，特别是在较长停留时间下。在90℃和5 rpm条件下，片剂的崩解时间最短，对应着最低的抗张强度，而各配方的片剂在崩解后pH值相似，表明具有一致的均匀性。这些发现强调了山梨醇作为熔融黏合剂的适用性，并突出了TS-MG参数与泡腾颗粒和片剂物理特性之间的相互作用。
