CN112137966A - 一种布洛芬颗粒剂及其制备方法 - Google Patents
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Abstract
一种布洛芬颗粒剂及其制备方法，它涉及药物制备领域，本发明的目的是提供一种布洛芬颗粒及其制备方法，该布洛芬颗粒口感好，颗粒崩解快速，溶出度高，生物利用度高，方便临床服用，该制备方法工序简单、质量可控且适于工业化生产。本发明布洛芬颗粒剂由20.0重量％的布洛芬、60.0‑70.0重量％填充剂、4.0‑5.0重量％粘合剂、4.0‑5.0重量％崩解剂、1.0‑2.0重量％助流剂和0.1‑0.5重量％的甜味剂组成。采用本发明的配方和方法制得的颗粒均匀性和稳定性良好，有关物质低、溶出度高，生物利用度高，而且制备工艺方便易行，成本低廉，不需任何特殊设备，适合工业化生产。本发明应用药物制备领域。
Description
技术领域
本发明涉及药物制备领域，具体涉及一种布洛芬颗粒剂及其制备方法。
背景技术
布洛芬，2-甲基-4-(2-甲基丙基)苯乙酸，IUPAC命名为：2-(4-isobutylphenyl)propanoic acid，CAS No.15687-27-1，分子式C13H18O2，分子量206.28。非甾体抗炎药(NSAID)，具有镇痛、抗炎、解热作用，其作用机制是通过对环氧酶的抑制而减少前列腺素的合成，减轻因前列腺素引起的组织充血、肿胀，降低周围神经痛觉的敏感性，产生镇痛、抗炎作用；并通过下丘脑体温调节中心而起解热作用。
申请号为201510049631.7在中国专利申请公开了布洛芬颗粒及其制备方法。该颗粒剂采用蔗糖和拉环酸钠的辅料改善口味，溶出度不高，显示在pH7.2缓冲液30min取样的溶出度在95％以下。
申请号为200510090752.2在中国专利申请公开了一种布洛芬颗粒剂及其制备方法。该颗粒剂采用糊精、羟丙纤维素和环己基氨基磺酸钠的辅料，仅考虑辅料中不含有糖，但未显示解决了溶出度的问题。
发明内容
本发明的目的是提供一种布洛芬颗粒及其制备方法，该布洛芬颗粒口感好，颗粒崩解快速，溶出度高，生物利用度高，方便临床服用，该制备方法工序简单、质量可控且适于工业化生产。
本发明的重点是解决在15min内使布洛芬颗粒在pH7.2的缓冲液中溶出度达到95％以上。本发明考虑布洛芬颗粒剂的溶出是需要颗粒在缓冲液中先崩解然后主药溶出的过程，所以要达到快速溶出的目的，需要提高颗粒的崩解速度和加快布洛芬的溶解速度。为解决这一问题，一方面在处方中加入崩解剂，提高颗粒的崩解速度使颗粒剂在1min内迅速崩解；另一方面在制备工艺中将布洛芬原料进行微粉化处理，提高原料的表面积可以直接加快溶解速度。同时为保障颗粒剂中的原料含量均匀，要将原辅料均匀的混合，选用特定的比例的乳糖和微晶纤维素两者组合的稀释剂，并加入助流剂二氧化硅，共同解决了原辅料混合不均匀的难题。另外，颗粒剂需要良好的颗粒外型，用聚维酮做粘合剂加入可以制备出很好的颗粒外型，同时不影响溶出度。在处方中加入适量的甜味剂，优选为对人体安全的阿司帕坦，适量的加入可以提高患者服用的依从性。
本发明经过研究，开发出具有众多优点的布洛芬颗粒剂：例如颗粒加入到水中，迅速崩散，适合冲服，方便患者服用。颗粒含量均匀，用药剂量可以根据患者的年龄和体重方便地选择使用。
本发明的颗粒剂(尤其是使用优选配方)制备得到的颗粒剂具有以下优点：
(1)颗粒外观均匀，流动性良好，装量准确，含量均一，溶出度高；
(2)颗粒剂的杂质低，稳定性好；
(3)颗粒剂在pH7.2的缓冲液中15min内溶出度达到95％以上；
(4)颗粒剂服用方便，容易确定儿童患者的给药剂量；
(5)生产工艺简便易行，成本低廉。
附图说明
图1为实施例1制备的布洛芬颗粒在pH7.2条件下溶出曲线，其中，A为参照样品，B为未微粉原料制备的样品，C为微粉原料制备的样品。
具体实施方式
本领域的普通技术人员可以理解，上述各实施方式是实现本发明的具体实施例，而在实际应用中，可以在形式上和细节上对其作各种改变，而不偏离本发明的精神和范围。
为使本发明实施例的目的、技术方案和优点更加清楚明白，下面将详细叙述清楚说明本发明所揭示内容的精神，任何所属技术领域技术人员在了解本发明内容的实施例后，当可由本发明内容所教示的技术，加以改变及修饰，其并不脱离本发明内容的精神与范围。
本发明的示意性实施例及其说明用于解释本发明，但并不作为对本发明的限定。
实施例1
| 处方成分 | 用量kg | 作用 |
| 布洛芬 | 20 | 原料 |
| 乳糖 | 53.75 | 填充剂 |
| 微晶纤维素 | 15 | 填充剂 |
| 二氧化硅 | 1 | 助流剂 |
| 羧甲淀粉钠 | 5 | 崩解剂 |
| 阿司帕坦 | 0.25 | 甜味剂 |
| 聚维酮K30 | 5 | 粘合剂 |
制备方法是按以下步骤进行：
一、气流粉碎：将布洛芬原料置气流粉碎机中进行气流粉碎，得粉碎后原料。
二、过筛：按批处方量称量，将二氧化硅、羧甲淀粉钠、阿司帕坦、微晶纤维素进行预混合，预混合辅料、乳糖和微粉的布洛芬共同过100目筛，备用。
三、混合：将过筛物料置三维运动混合机中混合20分钟。
四、粘合剂(10％重量聚维酮K30)的制备：称取处方量的聚维酮K30，按聚维酮K30:乙醇:纯化水＝10:2:88的比例配制成粘合剂，备用。
五、混合制粒：将混合物料置于湿法混合制粒机中，按物料重量的35％重量加入粘合剂制软材。制备好的软材置于摇摆式颗粒机18目筛网制粒。
六、干燥：高效沸腾干燥机物料温度达到40-50℃，干燥水分控制2％以下。
七、分装：按中间产品含量计算，每包应含布洛芬0.1克或0.2克，装量约0.5克或1克。
本实施例的布洛芬颗粒，采用气流粉碎技术粉碎的原料，选择适合分散混合的乳糖和微晶纤维素作为填充剂，选择二氧化硅作为助流剂，用过筛混合的方式保证原辅料的混合均匀度，选择聚维酮K30作为粘合剂用湿法制粒工艺制备的颗粒，羧甲淀粉钠作为崩解剂保证颗粒在水中达到良好的崩解效果，从而达到15min的溶出度在95％以上，生物等效性试验显示，自制的样品与参照样品达到等效。
本实施例布洛芬颗粒检测结果如下：
累积溶出度检测结果
布洛芬颗粒的空腹生物等效性试验
布洛芬颗粒的餐后生物等效性试验
对比研究未微粉原料和微粉后的原料的样品累积溶出度检测结果，如图1所示，图中显示，其中，A为参照样品，B为未微粉原料制备的样品，C为微粉原料制备的样品，图1显示微粉后的原料可以显著提高溶出度。
Claims (10)
1.一种布洛芬颗粒剂的制备方法，其特征在于它由20.0重量％的布洛芬、60.0-70.0重量％填充剂、4.0-5.0重量％粘合剂、4.0-5.0重量％崩解剂、1.0-2.0重量％助流剂和0.1-0.5重量％的甜味剂组成。
2.根据权利要求1所述的一种布洛芬颗粒剂的制备方法，其特征在于所述的粘合剂为按质量比为聚乙烯吡咯烷酮：乙醇：纯化水＝10：2：88的比例配制成质量体积百分含量为10％的聚乙烯吡咯烷酮溶液。
3.根据权利要求1所述的一种布洛芬颗粒剂的制备方法，其特征在于所述的助流剂为二氧化硅。
4.根据权利要求1所述的一种布洛芬颗粒剂的制备方法，其特征在于所述的崩解剂为羧甲淀粉钠。
5.根据权利要求1所述的一种布洛芬颗粒剂的制备方法，其特征在于所述的甜味剂为阿司帕坦。
6.根据权利要求1所述的一种布洛芬颗粒剂的制备方法，其特征在于所述的填充剂为乳糖和微晶纤维素按照质量比为5～6：1的比例组成。
7.根据权利要求1所述的一种布洛芬颗粒剂的制备方法，其特征在于每单位剂量布洛芬颗粒剂中含有100毫克或200毫克的布洛芬。
8.制备权利要求1所述的一种布洛芬颗粒剂的方法，其特征在于将布洛芬粉碎至平均粒径2～10微米；称取20.0重量％的布洛芬、60.0-70.0重量％填充剂、4.0-5.0重量％粘合剂、4.0-5.0重量％崩解剂、1.0-2.0重量％助流剂、0.1-0.5重量％的甜味剂、60-70重量％的填充剂，按等量递加法将布洛芬、填充剂、崩解剂、助流剂和甜味剂混合均匀，然后加入粘合剂在湿法制粒机中制备软材，过18目筛制粒，将湿颗粒置于沸腾干燥机烘干后，用1号筛去除大颗粒，用5号筛筛去细粉后，测定颗粒主药含量和水分，确定装量，将上述颗粒分装为0.5克或1.0克/每单位剂量的包装，其中含有布洛芬100毫克或200毫克，用铝塑复合膜包装。
9.根据权利要求8所述的一种布洛芬颗粒剂的制备方法，其特征在于所述的高效沸腾干燥机物料温度达到40-50℃，干燥水分控制2％以下。
10.根据权利要求8所述的一种布洛芬颗粒剂的制备方法，其特征在于按物料重量的35％重量加入粘合剂制软材。
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| CN115581673A (zh) * | 2022-10-28 | 2023-01-10 | 浙江康恩贝制药股份有限公司 | 一种布洛芬颗粒及其制备方法 |
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