Garzón Serra María de Lourdes, Villafuerte Robles Leopoldo
Departamento de Sistemas Biológicos, Universidad Autónoma Metropolitana-Xochimilco, Calzada del Hueso 1100, Col. Villa Quietud, C. P. 04960, Distrito Federal, Mexico.
Int J Pharm. 2003 Jun 4;258(1-2):153-63. doi: 10.1016/s0378-5173(03)00185-6.
The tablet tensile strength (T) of agglomerated mixtures of microcrystalline cellulose-Avicel PH 102 (MC), calcium carbonate (CC) and polyvinylpyrrolidone (Povidone, PVP), lubricated with magnesium stearate (MS), and formed under a compaction pressure (P(c)) ranging up to 618MPa has been determined. The compactibility was defined through: ln(-ln(1-T/T(max)))=Slope x lnP(c)+Intercept. MC/CC mixtures added of an agglutinant, before and after lubrication, show an important positive effect on their tablet tensile strength compared to a lineal relationship. This positive effect becomes smaller with decreasing compaction pressures. By different mixing methods, the higher the mixing efficiency the higher the compactibility, following the order: spray-dried>wet massing>tumble mixing. The compactibility of MC/CC/PVP spray-dried mixtures with calcium carbonate content from 20 to 60% was equal to or greater than that of pure microcrystalline cellulose. After lubrication with 2% MS the compactibility decreased, only the mixture with the maximal tablet tensile strength attained the tensile strength of pure microcrystalline cellulose. The presence of the binder, the lubricant and higher compaction pressures allow the accommodation of higher calcium carbonate proportions in the mixtures, at the maximal tablet tensile strength of the series. The lubricant decreases in a greater extent the compactibility of mixtures with a continuous phase of MC/PVP than that of CC/PVP. This is attributed to the plastic behavior of the MC/PVP continuous phase compared to a calcium carbonate continuous phase able to disrupt the Povidone and the possible lubricant coatings allowing a stronger interparticle interaction.
已测定了微晶纤维素 - 埃维安PH 102(MC)、碳酸钙(CC)和聚乙烯吡咯烷酮(聚维酮,PVP)的团聚混合物的片剂抗张强度(T),这些混合物用硬脂酸镁(MS)润滑,并在高达618MPa的压制压力(P(c))下成型。压实性通过以下公式定义:ln(-ln(1 - T/T(max)))=斜率×lnP(c)+截距。与线性关系相比,添加凝集剂的MC/CC混合物在润滑前后对其片剂抗张强度显示出重要的积极影响。随着压制压力的降低,这种积极影响会变小。通过不同的混合方法,混合效率越高,压实性越高,顺序为:喷雾干燥>湿法制粒>滚筒混合。碳酸钙含量为20%至60%的MC/CC/PVP喷雾干燥混合物的压实性等于或大于纯微晶纤维素的压实性。用2%的MS润滑后,压实性降低,只有具有最大片剂抗张强度的混合物达到了纯微晶纤维素的抗张强度。在该系列的最大片剂抗张强度下,粘合剂、润滑剂的存在以及更高的压制压力使得混合物中能够容纳更高比例的碳酸钙。与CC/PVP连续相的混合物相比,润滑剂在更大程度上降低了以MC/PVP为连续相的混合物的压实性。这归因于与碳酸钙连续相相比,MC/PVP连续相的塑性行为,碳酸钙连续相能够破坏聚维酮和可能的润滑剂涂层,从而允许更强的颗粒间相互作用。