稻草秸秆综纤维素对阿司匹林片崩解性能的影响

doi:10.11949/0438-1157.20190466

摘要/Abstract

摘要：

以稻草秸秆为原料，经过SO₃微热爆预处理、木质素降解、漂白等工序制备出了稻草秸秆综纤维素，并将其用作片剂崩解剂进行了性能评价。参照《中国药典》(2015版)中的有关规定，检测了稻草秸秆综纤维素的各项指标；以阿司匹林为模型药物，以市售微晶纤维素为对照，测定了稻草秸秆综纤维素的崩解性能。结果表明，稻草秸秆综纤维素质量符合《中国药典》(2015版)中的相关规定，且崩解性明显优于市售微晶纤维素，可用作片剂崩解剂。在稻草秸秆综纤维素用量为3％~5%时即可达到微晶纤维素用量为15%~20%的崩解效果，这一效果的呈现与稻草秸秆综纤维素的形态结构以及含有半纤维素组分有着密切联系。

关键词: 生物质, 稻草秸秆, 综纤维素, 降解, 崩解剂, 药物

Abstract:

Rice straw holocellulose, prepared from biomass rice straw by SO₃ micro-thermal explore, degradation of lignin and bleaching, was used as tablet disintegrating agent. The performance was evaluated by using it as a tablet disintegrating agent. According to the relevant standards of Chinese Pharmacopoeia (2015 Edition), several characters of rice straw holocellulose, such as surface morphology, specific surface area, pH etc., were detected. Taking aspirin as model drug, the disintegration performance of rice straw holocellulose was determined and compared with commercial microcrystalline cellulose. The results showed that the quality of rice straw holocellulose was in accordance with the relevant regulations of Chinese Pharmacopoeia, and the disintegration of rice straw holocellulose was obviously superior to that of commercial microcrystalline cellulose. The same disintegration effect with 15%—20% microcrystalline cellulose can be attained by using only 3%—5% rice straw holocellulose. This result should be closely owed to the structure and semicellulose of rice straw holocellulose.

Key words: biomass, rice straw, holocellulose, degradation, disintegrant, pharmaceuticals

中图分类号:

TB 32

李双凤, 王淮, 陈家丽, 姚日生, 朱慧霞, 马晓静. 稻草秸秆综纤维素对阿司匹林片崩解性能的影响[J]. 化工学报, 2019, 70(11): 4420-4427.

Shuangfeng LI, Huai WANG, Jiali CHEN, Risheng YAO, Huixia ZHU, Xiaojing MA. Effect of rice straw holocellulose on disintegration of aspirin tablets[J]. CIESC Journal, 2019, 70(11): 4420-4427.

图/表 12

图1 稻草秸秆综纤维素制备工艺流程图

Fig.1 Flowchart of straw cellulose preparation

图2 市售微晶纤维素（a）和稻草秸秆综纤维素（b）的外貌特征

Fig.2 Physical characteristics of microcrystalline cellulose (a) and rice straw holocellulose (b)

表1 稻草秸秆综纤维素化学组分含量

Table 1 Content of rice straw holocellulose/%

样品	纤维素含量	半纤维素含量	木质素含量
原稻草秸秆	38.24	21.56	16.4
市售微晶纤维素	96.55	1.76	0.48
稻草秸秆综纤维素	69.59	27.26	0.67

图3 稻草秸秆综纤维素(a)和市售微晶纤维素(b)的电镜扫描图

Fig.3 Scanning electron microscopy of rice straw holocellulose (a) and microcrystalline cellulose (b)

表2 稻草秸秆综纤维素物理性能分析

Table 2 Physical performance analysis of rice straw holocellulose

性能	市售微晶纤维素	稻草秸秆综纤维素
溶胀体积比（h ₂/h ₁±SD）	1.6 ± 0.15	2.14 ± 0.17
结晶度	65.63%	75.84%
休止角	38.9°	50.7°
堆密度	0.442 g/cm³	0.191 g/cm³

表3 纤维素的药典要求及考察结果

Table 3 Requirements of pharmacopoeia for cellulose and results of investigation

检验项目	中国药典标准粉状纤维素	中国药典标准微晶纤维素	自制稻草秸秆综纤维素
酸碱度	pH 5.0~7.5	pH 5.0~7.5	pH=5.6
水中溶解物	≤1.5%	≤0.2%	0.19%
醚中溶解物	≤0.15%	≤0.05%	0.14%
炽灼残渣	≤0.3%	≤0.1%	0.21%
干燥失重	≤6.5%	≤7%	5.17%
重金属	≤百万分之十	≤百万分之十	合格
聚合度	≥440	≤350	749
氯化物	无要求	≤0.03%	<0.03%
淀粉	无要求	遇碘不显蓝色	遇碘不显蓝色
电导率	无要求	电导率之差不得过75 μS/cm	71 μS/cm

表4 实验处方

Table 4 Experimental prescription

崩解剂含量/%		药品含量/%
崩解剂含量/%		阿司匹林	乳糖	甘露醇	酒石酸	滑石粉	10%淀粉浆
	1	16.7	64.6	14.7	1	2	适量
	2	16.7	63.6	14.7	1	2	适量
	3	16.7	62.6	14.7	1	2	适量
	5	16.7	60.6	14.7	1	2	适量
	10	16.7	55.6	14.7	1	2	适量
	15	16.7	50.6	14.7	1	2	适量
	20	16.7	45.6	14.7	1	2	适量

图4 崩解剂添加量对片剂脆碎度的影响

Fig.4 Effect of amount of disintegrant on tablet friability

图5 崩解剂添加量对片剂硬度的影响

Fig.5 Effect of disintegrant addition on tablet hardness

图6 崩解剂添加量对片剂崩解时间的影响

Fig.6 Effect of amount of disintegrant on disintegration time of tablets

图7 微晶纤维素为崩解剂片剂的崩解过程

Fig.7 Disintegration process of microcrystalline cellulose as disintegrating agent tablet

图8 稻草粉状综纤维素为崩解剂片剂的崩解过程

Fig.8 Disintegration process of rice straw powdered holocellulose as disintegrant tablet

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