Kakino Yukari, Hishikawa Yoshihiro, Onodera Risako, Tahara Kohei, Takeuchi Hirofumi
Department of Research and Development, Ohkura Pharmaceutical Co., Ltd.
Department of Drug Delivery Technology and Science, Laboratory of Pharmaceutical Engineering, Gifu Pharmaceutical University.
Chem Pharm Bull (Tokyo). 2017;65(11):1035-1044. doi: 10.1248/cpb.c17-00447.
Jellies for oral administration are dosage forms that contain water, as stipulated in the Japanese Pharmacopeia, and heat is generally applied to the jellies during the manufacturing process. Therefore, it is difficult to formulate drugs that may be affected adversely by water and/or heat. To solve this problem, we tried to develop a powder form of gel as a novel dosage form (dry jelly: jelly medicine extemporaneously prepared) that is converted to jelly after addition of water at the time of administration. For this purpose, a basic gel formulation consisting of pectin, glucono-δ-lactone, dibasic calcium phosphate hydrate, and sucrose was investigated to evaluate the critical factors affecting gelation phenomena. The gel form was developed by adjusting the amount of each component of the formulation and of water added. Gelation occurred even with hard water containing metal ions (hardness of approximately 304 mg/L), and no changes in gel hardness occurred. The desired gel hardness could be controlled by adjusting the amount of water. The gel hardness changed over time after the addition of water, but this change did not affect the dissolution behavior of drugs formulated in the dry jelly.
口服果冻是《日本药局方》规定的含有水的剂型，在制造过程中通常会对果冻进行加热。因此，难以配制可能会受到水和/或热不利影响的药物。为了解决这个问题，我们试图开发一种粉末状凝胶作为新型剂型（干果冻：临用前用水制成的果冻状药物），在给药时加水后可转化为果冻。为此，研究了由果胶、葡萄糖酸 -δ-内酯、水合磷酸氢钙和蔗糖组成的基本凝胶配方，以评估影响凝胶化现象的关键因素。通过调整配方中各成分的用量和加入的水量来开发凝胶形式。即使使用含有金属离子的硬水（硬度约为304mg/L）也会发生凝胶化，凝胶硬度没有变化。所需的凝胶硬度可以通过调整水量来控制。加水后凝胶硬度随时间变化，但这种变化不影响干果冻中配制药物的溶解行为。
