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目的:通过制备黄芩苷固体分散体,提高其溶出度,并考察聚山梨酯-80对其固体分散体溶出度的影响。方法:采用熔融法和溶剂法,制备PEG6000、PVP K30 2种不同载体材料、不同比例的固体分散体。比较原料药、物理混合物、固体分散体中的黄芩苷溶出度,确定最佳载体和最佳比例,然后在此基础上添加聚山梨酯-80,考察其对固体分散体中黄芩苷溶出度的影响。结果:以PVP K30为载体制备的黄芩苷固体分散体,其体外溶出明显高于、快于PEG6000制备的固体分散体;随着PVP固体分散体中聚山梨酯-80用量的增加,黄芩苷的溶出速率加快,溶出度亦进一步提高。结论:以PVP为载体,采用溶剂法制备的药物-载体比例为1:8的固体分散体能显著提高黄芩苷的溶出速率;聚山梨酯-80能进一步促进其溶出。
OBJECTIVE: To improve the dissolution of baicalin solid dispersion and investigate the effect of polysorbate-80 on the dissolution of solid dispersions. Methods: Two kinds of carrier materials of PEG6000 and PVP K30 with different proportions of solid dispersions were prepared by melt method and solvent method. To compare the dissolution of baicalin in bulk drug, physical mixture and solid dispersion, determine the optimal carrier and the optimal ratio, and then add polysorbate-80 on this basis to investigate the dissolution of baicalin in solid dispersion influences. Results: The solid dispersion of baicalin prepared with PVP K30 as carrier had a higher dissolution rate in vitro than the solid dispersion prepared with PEG6000. With the increase of polysorbate-80 in PVP solid dispersion, Dissolution rate to speed up dissolution was also further improved. CONCLUSION: Solid dispersions with solvent-loaded drug-carrier ratio of 1: 8 with PVP as carrier could significantly improve the dissolution rate of baicalin. Polysorbate-80 could further promote its dissolution.