The studies on the interaction among disintegrants, lubricants, and gliants, as well as the correlation between water uptake behavior and manufacturing parameters of Ibuprofen tablet formulations

• Main Authors: Teng-Yuan Cheng, 鄭登元
• Other Authors: 蔡東榮
• Format: Others
• Language: zh-TW
• Published: 2006
• Online Access: http://ndltd.ncl.edu.tw/handle/69603362223247035729

碩士 === 高雄醫學大學 === 藥學研究所碩士在職專班 === 94 === The disintegrant, lubricant, and glidant are important components in the solid dosage formulation which they make up small percentage compare with other excipients in the formulation. But they have major influences toward the formulation physical properties, dissolution, and gastrointestinal absorption rate when use of drug. In this study, we construct a custom-made liquid uptake experiment apparatus, according to syphonage theory, to measure water uptake properties for four disintegrants (Sodium starch glycolate (Primojel), Croscarmellose sodium (Disolcel), Crospovidine (Kollidon CL), and Partially pregelatinized starch (Starch 1500)) and the effect of different disintegrants, lubricant (Magnesium stearate, Stearic acid and Talc), and glidant (Aerosil A 200V) ratio on water uptake properties of the various mixed powders. The results shown that among the disintegrants, Primojel has best water uptake property and the Kollidon CL has low water uptake but it has the fastest rate to achieve saturation state. Additionally, when mix with magnesium stearate, the water uptake property of all disintegrants come under the strongest suppression. In contract with above results, the powder samples under coexistence of Aerosil A 200V with lubricants, the water uptake of all disintegrants increased. The second part of this study, we are using Ibuprofen as active pharmaceutical ingredient (API) with various lubricants and glidants tablet formulations as model to study the powder properties. Furthermore, we used a high speed tablet machine to produce the Ibuprofen tablet with Advanced Instrumentation Monitor (AIM) to record the compression force, and ejection force during the compression. Except the tablet hardness, thickness, Tensile strength, and disintegrating, The tablet water uptake properties were measured. The results shown, the Ibuprofen tablet water uptake property is different with powder model without API. The Ibuprofen tablet with Stearic acid as lubricant has higher ejection force and a hardness property than with other lubricants but it has lowest water uptake property. Also, the DSC experiment result has confirmed that the Ibuprofen tablet with Stearic acid is significantly differing with use of other lubricant. As for factors effects on tablet formulation water uptake properties include the use of Aerosil A 200V as glidant, powder preparation variation, and tablet compression pressure are observed. In addition, the tablet ejection forces, tablet integrating time, and tablet physical properties are factors that contribute to significant differences of a tablet formulation.