Sci Rep: 研究人员发现一种新的简易检测方法可提高药物的缓释效果

2020-12-01 MedSci原创 MedSci原创

药物的溶解速度对人体对药物的吸收有着很大的影响,药物溶解太慢或太快时,都会给人带来不便,比如药效发挥速度慢或者导致人体产生不良反应。

药物的溶解速度对人体对药物的吸收有着很大的影响,药物溶解太慢或太快时,都会给人带来不便,比如药效发挥速度慢或者导致人体产生不良反应。

像音叉一样弯曲的玻璃用来测量缓释药物的溶解过程。

例如含阿片类药物羟考酮的氧康定本应能缓解12小时的疼痛。而在一些病人中,它的溶解速度要快得多,因此这些患者便需要频繁地服用,并最终上瘾。

但是评估一种药物在体内溶解情况是非常困难的。药物溶出度必须在尽可能接近人体的实验室条件下进行测量。

在《科学报告》上发表的一篇论文中,加州大学河滨分校的研究人员描述了一种测量药物溶出度的简单、廉价的方法,这将有助于制药公司开发出更好、更一致的缓释药物产品。

DOI: 10.1038/s41598-020-76089-z

影响药物在体内溶解的因素很多,包括胃肠液的pH值和化学成分、胃肠道收缩引起的液体流体力学、患者性别和新陈代谢。例如,OxyContin的制造者注意到,在高脂肪饮食中服用该药可以使患者血液中羟考酮的含量增加25%。

制药公司通常把药物放在一个充满液体的容器里,模拟胃肠道的内容物,然后搅拌液体以重现胃肠道的动力学。每隔一段时间取少量的液体样本,用紫外-可见光谱法或高效液相色谱法测量药物浓度(应随时间增加)。这项测试的数据被用来构建药物在体内的预期行为模型。

常用的测试方法都有或多或少的缺点。例如,引起设备堵塞、流动受阻和气泡,所有这些都会影响药物的溶解。此外,测量过程费时费力,往往无法生产,而且设备昂贵。现有的方法也只提供在取样点采集的溶解“快照”,提供的信息有限。

研究人员采取了截然不同的方法。他们没有测量液体中药物浓度的增加,而是测量了固体颗粒溶解时下降的质量。

他们用模拟的胃肠内容物填充试管,并将非处方缓释药物颗粒导入试管后观察到频率的短暂变化。

在绘制图表时,他们用共振频率峰值与时间作为对比,以了解此时药物颗粒的浮浮力质量。

其中一名研究人员Grover说:“当颗粒溶解时,我们通过振动管来回振荡颗粒,这样可以在整个溶解过程中监测其重量,并获得单个颗粒的溶解曲线。”。

研究小组测试了三种不同的质子泵抑制剂:奥美拉唑、兰索拉唑和埃索美拉唑。尽管它们在体内具有相似的预期作用,但它们的颗粒大小和溶解机制却截然不同。

“我们还发现同一种药物和其仿制药的溶出行为不同。这些单颗粒溶解行为的差异可能导致患者药物吸收率的不同。

研究人员说,这种技术改良了现有测试方法的许多缺点,不仅不需要额外的分析仪器,并且适用于快速溶解和缓慢溶解的配方。通过给出单个颗粒的溶解曲线,可以捕捉到颗粒溶解行为的变化,这是其他方法无法做到的。

Grover说,这项技术比传统的方法更便宜、更容易操作,这使制药公司能够在更广泛的条件下进行更多的试验。

参考资料:

https://medicalxpress.com/news/2020-11-simple-method-aims-time-release-drugs.html

原始出处:

Heran C. Bhakta et al, Measuring dissolution profiles of single controlled-release drug pellets, Scientific Reports (2020).

 

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    2020-12-10 ms8000000663123873

    是不是真心实用?

    0

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  4. [GetPortalCommentsPageByObjectIdResponse(id=1907627, encodeId=772b190e627db, content=<a href='/topic/show?id=379fe3364c9' target=_blank style='color:#2F92EE;'>#研究人员#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=62, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=73364, encryptionId=379fe3364c9, topicName=研究人员)], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=db5b227, createdName=gostraight, createdTime=Wed Jul 07 08:09:47 CST 2021, time=2021-07-07, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=906735, encodeId=b377906e3528, content=是不是真心实用?, beContent=null, objectType=article, channel=null, level=null, likeNumber=86, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://img.medsci.cn/20201126/e63111794ca84000a00f7117dcdfb179/74951f6b6dec4250ab4b91a00c0b23bb.jpg, createdBy=fa935420470, createdName=ms8000000663123873, createdTime=Thu Dec 10 16:20:00 CST 2020, time=2020-12-10, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1457120, encodeId=9eb5145e12031, content=<a href='/topic/show?id=b7e86254347' target=_blank style='color:#2F92EE;'>#检测方法#</a>, beContent=null, objectType=article, channel=null, level=null, likeNumber=42, replyNumber=0, topicName=null, topicId=null, topicList=[TopicDto(id=62543, encryptionId=b7e86254347, topicName=检测方法)], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=8fe35841975, createdName=gracezdd, createdTime=Thu Dec 03 08:09:47 CST 2020, time=2020-12-03, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=904196, encodeId=e9be904196cc, content=这项技术比传统的方法更便宜、更容易操作,这就是最大的优势。, beContent=null, objectType=article, channel=null, level=null, likeNumber=81, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://img.medsci.cn/20200901/629d1ce7d6f64d17a642c37c90dea72c/202f9333a3ea4b23a9b07ede3364e86b.jpg, createdBy=1a335163906, createdName=Sunny orchard, createdTime=Wed Dec 02 10:45:34 CST 2020, time=2020-12-02, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=904127, encodeId=b40890412e92, content=这种技术改良了现有测试方法的许多缺点,不仅不需要额外的分析仪器,并且适用于快速溶解和缓慢溶解的配方, beContent=null, objectType=article, channel=null, level=null, likeNumber=91, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=https://img.medsci.cn/20210325/2d9c955949df4b349a439f1a6773499e/b39f4845e869489d95bc545c79cf60fa.jpg, createdBy=303f5433779, createdName=Oranhyg, createdTime=Wed Dec 02 08:28:22 CST 2020, time=2020-12-02, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=1047230, encodeId=1647104e2309f, content=疗效只是效果的众多方面之一,还要看对患者的获益,包括生活质量等因素共同决定效果的, beContent=null, objectType=article, channel=null, level=null, likeNumber=48, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=f0620, createdName=CHANGE, createdTime=Tue Dec 01 20:09:47 CST 2020, time=2020-12-01, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=903982, encodeId=2c5c9039824b, content=好文章, beContent=null, objectType=article, channel=null, level=null, likeNumber=87, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=f55d5440378, createdName=ms8000000493516655, createdTime=Tue Dec 01 19:37:45 CST 2020, time=2020-12-01, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=903976, encodeId=0cf99039e663, content=真不错, beContent=null, objectType=article, channel=null, level=null, likeNumber=69, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=null, createdBy=d0725440373, createdName=ms1000000133673730, createdTime=Tue Dec 01 19:20:04 CST 2020, time=2020-12-01, status=1, ipAttribution=), GetPortalCommentsPageByObjectIdResponse(id=903967, encodeId=853e90396e9e, content=有意义, beContent=null, objectType=article, channel=null, level=null, likeNumber=25, replyNumber=0, topicName=null, topicId=null, topicList=[], attachment=null, authenticateStatus=null, createdAvatar=, createdBy=f0d45220203, createdName=1477a9cbm52暂无昵称, createdTime=Tue Dec 01 18:38:52 CST 2020, time=2020-12-01, status=1, ipAttribution=)]
    2020-12-02 Sunny orchard

    这项技术比传统的方法更便宜、更容易操作,这就是最大的优势。

    0

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    2020-12-02 Oranhyg

    这种技术改良了现有测试方法的许多缺点,不仅不需要额外的分析仪器,并且适用于快速溶解和缓慢溶解的配方

    0

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    2020-12-01 CHANGE

    疗效只是效果的众多方面之一,还要看对患者的获益,包括生活质量等因素共同决定效果的

    0

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    2020-12-01 ms8000000493516655

    好文章

    0

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    2020-12-01 ms1000000133673730

    真不错

    0

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    2020-12-01 1477a9cbm52暂无昵称

    有意义

    0

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