中药液体制剂的剂型设计关键技术:组分的溶解性质与增溶技术应用

Key technologies in dosage form design of Chinese medicinal liquid preparations:application of component solubility and solubilization technology

中药现代液体剂型如口服液,虽与传统汤剂相似,但在其剂型选择与设计方面还有所不足,而制剂前物料的溶解性质是其关键。该课题组在研究中药制剂前物料的基础上,建立了中药制剂前物料性质体系。该文构建了以组分溶解性质为核心的中药口服液体制剂剂型设计策略,指出物料组分的饱和体积V_(i-n)与制剂日服用量V_(d)之间的关系是剂型设计的关键,V_(i-n)≤V_(d)时可设计选择相关液体剂型,当V_(i-n)>V_(d)时则需要对物料组分采用适宜的增溶技术以满足V_(i-n)≤V_(d)。目前可供选择的增溶技术有添加增溶剂/助溶剂等辅料、调节溶液pH、制备药物的制剂中间体和组分协同增溶等;而随着对中药多糖研究的深入,发现其在中药难溶性成分增溶方面显现出巨大的潜力。中药多糖作为新型的增溶辅料具有一定的前景。

Modern liquid forms of Chinese medicine(CM),such as oral liquid,are similar to traditional decoction,but there are deficiencies in the selection and design of the dosage form,and the solubility of the pre-preparation material is critical.The property system for Chinese medicinal materials(CMMs)was established according to the previous research.The present study established the dosage form design strategy of oral liquid preparations of CM with the solubility as the core,and pointed out the relationship between the saturated volume of component(V_(i-n))and daily dosage of preparation(V_(d))was the key to the dosage form design.To be specific,the prescription can be designed into liquid preparation directly when V_(i-n)≤V_(d),while V_(i-n)>V_(d),the suitable solubilization technologies are needed.At present,the available solubilization technologies include the addition of excipients such as solubilizers/cosolvents,pH adjustment of the solution,and synergistic solubilization of intermediates and components for the preparation of pharmaceuticals.As reported,the polysaccharides of CM have shown great potential in the solubilization of insoluble components of CM,and they have certain prospects as a new solubilizing excipient.