Intra and Extra-granular Disintegrant Properties of Modified Underutilised Red Lima Bean Starch in Paracetamol Tablet Formulation

Abstract Red lima bean (Phaseolus lunatus Linn) Family Fabaceae, has been modified by succinylation and annealing, and used as intra- and extra-granular disintegrants at concentrations of 5 and 10 %w/w in paracetamol tablet formulation in comparison with corn starch BP. The starches were characterised using FT-IR spectroscopy, SEM, proximate analysis, physicochemical and functional properties. FT-IR spectrometry revealed characteristic peaks at 1575.53 and 1713.99 cm-1 for the succinylated starch while the annealed showed no significant difference from the native starch. Modifications did not alter the ovoid shape of the native starch but reduced the particle size. Succinylation improved water absorption capacity, solubility and swelling of lima bean starch but annealing reduced the parameters. Tablets with disintegrants of lima bean starches generally had higher crushing strengths and lower friability than tablets with corn starch. Modifications reduced the disintegration time of the tablets when the starches were incorporated intra-granularly, which suggested particle-particle bond interruption and destruction of hydrogen bonds as mechanism of disintegration. Tablets containing 10 %w/w succinylated red lima bean starch incorporated intra-granularly had the highest disintegration efficiency ratio, DER, indicating a great balance between mechanical and disintegration properties. Modified red lima bean starches incorporated intra-granularly into paracetamol tablets led to faster disintegration and could efficiently substitute corn starch as disintegrant.

摘要 红利马豆（*Phaseolus lunatus* Linn，豆科Fabaceae）经琥珀酰化与退火改性后，以5%w/w和10%w/w的浓度作为粒内与粒外崩解剂应用于对乙酰氨基酚片剂处方中，并以英国药典（British Pharmacopoeia，BP）级玉米淀粉作为对照。采用傅里叶变换红外光谱（Fourier Transform Infrared Spectroscopy，FT-IR）法、扫描电子显微镜（Scanning Electron Microscopy，SEM）、常规成分分析、理化性质与功能特性对该淀粉进行了系统表征。FT-IR光谱分析显示，琥珀酰化淀粉在1575.53 cm⁻¹与1713.99 cm⁻¹处出现特征吸收峰；而退火改性淀粉的红外光谱与原淀粉无显著差异。两种改性方式均未改变原淀粉的卵圆形形貌，但均使淀粉粒径有所减小。琥珀酰化改性可提升红利马豆淀粉的吸水能力、溶解度与溶胀度，而退火改性则会降低上述三项参数。以利马豆淀粉为崩解剂的片剂，其压碎强度通常高于以玉米淀粉为崩解剂的片剂，且脆碎度更低。当淀粉以粒内方式添加时，两种改性方式均缩短了片剂的崩解时限，这表明其崩解机制为打断颗粒间结合并破坏氢键。添加10%w/w粒内琥珀酰化红利马豆淀粉的片剂，其崩解效率比（Disintegration Efficiency Ratio，DER）最高，说明其在机械性能与崩解性能间达到了极佳平衡。将改性红利马豆淀粉以粒内方式添加至对乙酰氨基酚片剂中，可实现更快的崩解效果，能够有效替代玉米淀粉作为崩解剂。