CN106511317A - 一种掩味克拉霉素颗粒的制备方法 - Google Patents
一种掩味克拉霉素颗粒的制备方法 Download PDFInfo
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Abstract
本发明公开了一种掩味克拉霉素颗粒的制备方法，通过将克拉霉素与饱和脂肪酸进行加热制粒，降低克拉霉素在水中的溶解度来掩盖克拉霉素的苦味，然后筛选合适粒径的颗粒在流化床或无孔包衣锅中使用不溶性或肠溶包衣材料进行包衣，在颗粒达到适宜的包衣增重后即可得到掩味的克拉霉素颗粒，能够掩盖克拉霉素的明显苦味，改善制剂颗粒的口感，且制备过程操作简单，辅料使用较少，便于生产操作的特点，很好地控制了产品质量。
Description
【技术领域】
本发明涉及一种抗生素药物，具体涉及一种掩味克拉霉素颗粒的制备方法。
【背景技术】
克拉霉素为第二代大环内酯类抗生素，抗菌机理是作用于细菌70S系统中的核蛋白体50S亚单位，阻碍细菌蛋白质的合成。克拉霉素对革兰氏阳性菌、多种革兰氏阴性菌有抗菌作用，此外对厌氧菌及其他病原体，如支原体、衣原体以及军团菌仍有较强的抗菌作用。本品的特点是体外抗菌活性并不显著优于红霉素，体内对金黄色葡萄菌、肺炎双球菌、化脓性链球菌、流感嗜血菌的抗菌活性却较红霉素强2-10倍。克拉霉素对粘膜炎莫拉氏菌、多杀巴斯德氏菌、空肠弯曲菌和胎儿弯曲菌、淋病奈瑟氏球菌、沙门氏菌，嗜肺军团菌及厌氧球菌的抗菌作用均较红霉素强，对幽门螺旋杆菌、沙眼衣原体、肺支原体的抗菌作用是本类抗生素中最强的，此外克拉霉素是治疗艾滋病患者分支杆菌感染的首选药物，克拉霉素有非常明显的苦味，普通制剂技术制成的产品患者难以下咽，对于可冲服的固体制剂药品来说，口感的好坏直接决定了患者对医嘱的服从性，因此提出一种掩味克拉霉素颗粒的制备方法。
【发明内容】
本发明的目的就是解决现有技术中的问题，提出一种掩味克拉霉素颗粒的制备方法，通过热熔、包衣、制粒掩盖克拉霉素颗粒剂的苦味，具有操作过程简单，辅料使用较少，便于生产操作的特点，很好地控制了产品质量。
为实现上述目的，本发明提出了一种掩味克拉霉素颗粒的制备方法，包括以下步骤：
(1)加热制粒
克拉霉素与适量的饱和脂肪酸通过加热制粒的方法降低克拉霉素在水中的溶解度来掩盖克拉霉素的苦味，将克拉霉素与硬脂酸按比例混合均匀后通过热熔挤出设备挤出冷却，克拉霉素与饱和脂肪酸的比例范围为1：10到10：1。
(2)筛选分级
热熔挤出设备挤出冷却后粉碎筛分选取20目到120目克拉霉素颗粒。
(3)包衣烘干
在流化床或无孔包衣锅中使用不溶性或肠溶包衣材料对筛分选取的克拉霉素颗粒进行包衣，进一步掩盖克拉霉素的苦味，包衣增重不少于20％。
作为优选，步骤(1)中所述克拉霉素与饱和脂肪酸的比例范围优选1:3到3:1。
作为优选，步骤(1)中所述加热制粒方法有热熔制粒、喷雾冷凝和热熔挤出制粒，优选喷雾冷凝和热熔制粒。
作为优选，步骤(2)中所述克拉霉素颗粒筛分优选范围为40目到80目。
作为优选，步骤(3)中所述包衣材料为乙基纤维素、羟丙甲纤维素邻苯二甲酸酯、羟丙甲纤维素琥珀酸酯、聚醋酸乙烯邻苯二甲酸酯、甲基丙烯酸与乙基丙烯酸共聚物之中的一种或多种。
作为优选，步骤(3)中所述包衣增重优选25％到120％。
作为优选，所述克拉霉素与饱和脂肪酸的质量比例为：克拉霉素30份，饱和脂肪酸50份；所述包衣材料各组分质量比例为：乙基纤维素10份，蓖麻油1.8份，滑石粉12份，羟丙甲纤维素邻苯二甲酸酯5份，85％乙醇溶液300份。
本发明的有益效果：本发明通过将克拉霉素与饱和脂肪酸进行加热制粒后筛选合适粒径的颗粒在流化床或无孔包衣锅中使用不溶性或肠溶包衣材料进行包衣，在颗粒达到适宜的包衣增重后即可得到掩味的克拉霉素颗粒，具有操作过程简单，辅料使用较少，便于生产操作的特点，很好地控制了产品质量。
【具体实施方式】
本发明提出一种掩味克拉霉素颗粒的制备方法，包括以下步骤：
(1)加热制粒
克拉霉素与适量的饱和脂肪酸通过加热制粒的方法降低克拉霉素在水中的溶解度来掩盖克拉霉素的苦味，将克拉霉素与硬脂酸按比例混合均匀后通过热熔挤出设备挤出冷却，克拉霉素与饱和脂肪酸的比例范围为1：10到10：1。
(2)筛选分级
热熔挤出设备挤出冷却后粉碎筛分选取20目到120目克拉霉素颗粒。
(3)包衣烘干
在流化床或无孔包衣锅中使用不溶性或肠溶包衣材料对筛分选取的克拉霉素颗粒进行包衣，进一步掩盖克拉霉素的苦味，包衣增重不少于20％。
步骤(1)中所述克拉霉素与饱和脂肪酸的比例范围优选1:3到3:1；所述加热制粒方法有热熔制粒、喷雾冷凝和热熔挤出制粒，优选喷雾冷凝和热熔制粒。步骤(2)中所述克拉霉素颗粒筛分优选范围为40目到80目。步骤(3)中所述包衣材料为乙基纤维素、羟丙甲纤维素邻苯二甲酸酯、羟丙甲纤维素琥珀酸酯、聚醋酸乙烯邻苯二甲酸酯、甲基丙烯酸与乙基丙烯酸共聚物之中的一种或多种；所述包衣增重优选25％到120％。
本发明的具体实施例为：
克拉霉素与饱和脂肪酸的质量比例为：克拉霉素30份，饱和脂肪酸50份；所述包衣材料各组分质量比例为：乙基纤维素10份，蓖麻油1.8份，滑石粉12份，羟丙甲纤维素邻苯二甲酸酯5份，85％乙醇溶液300份。
将克拉霉素与硬脂酸按比例混合均匀后通过热熔挤出设备挤出冷却后粉碎筛分选取30到100目颗粒待用；将乙基纤维素、羟丙甲纤维素邻苯二甲酸酯和蓖麻油溶解在300克85％的乙醇水溶液中然后将超细滑石粉在溶液中分散均匀得乙基纤维素乙醇溶液待用，将克拉霉素未包衣颗粒投入流化床中使用配制好的乙基纤维素乙醇溶液进行底喷包衣。
上述实施例是对本发明的说明，不是对本发明的限定，任何对本发明简单变换后的方案均属于本发明的保护范围。
Claims (7)
1.一种掩味克拉霉素颗粒的制备方法，其特征在于包括以下步骤：
(1)加热制粒
克拉霉素与适量的饱和脂肪酸通过加热制粒的方法降低克拉霉素在水中的溶解度来掩盖克拉霉素的苦味，将克拉霉素与硬脂酸按比例混合均匀后通过热熔挤出设备挤出冷却，克拉霉素与饱和脂肪酸的比例范围为1：10到10：1。
(2)筛选分级
热熔挤出设备挤出冷却后粉碎筛分选取20目到120目克拉霉素颗粒。
(3)包衣烘干
在流化床或无孔包衣锅中使用不溶性或肠溶包衣材料对筛分选取的克拉霉素颗粒进行包衣，进一步掩盖克拉霉素的苦味，包衣增重不少于20％。
2.如权利要求1所述的一种掩味克拉霉素颗粒的制备方法，其特征在于：步骤(1)中所述克拉霉素与饱和脂肪酸的比例范围优选1:3到3:1。
3.如权利要求1所述的一种掩味克拉霉素颗粒的制备方法，其特征在于：步骤(1)中所述加热制粒方法有热熔制粒、喷雾冷凝和热熔挤出制粒，优选喷雾冷凝和热熔制粒。
4.如权利要求1所述的一种掩味克拉霉素颗粒的制备方法，其特征在于：步骤(2)中所述克拉霉素颗粒筛分优选范围为40目到80目。
5.如权利要求1所述的一种掩味克拉霉素颗粒的制备方法，其特征在于：步骤(3)中所述包衣材料为乙基纤维素、羟丙甲纤维素邻苯二甲酸酯、羟丙甲纤维素琥珀酸酯、聚醋酸乙烯邻苯二甲酸酯、甲基丙烯酸与乙基丙烯酸共聚物之中的一种或多种。
6.如权利要求1所述的一种掩味克拉霉素颗粒的制备方法，其特征在于：步骤(3)中所述包衣增重优选25％到120％。
7.如权利要求1所述的一种掩味克拉霉素颗粒的制备方法，其特征在于：所述克拉霉素与饱和脂肪酸的质量比例为：克拉霉素30份，饱和脂肪酸50份；所述包衣材料各组分质量比例为：乙基纤维素10份，蓖麻油1.8份，滑石粉12份，羟丙甲纤维素邻苯二甲酸酯5份，85％乙醇溶液300份。
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