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	<title>口服固体制剂 归档 - 实验室自动化应用一致性评价丨香港力扬企业-溶出仪-药物溶出度仪厂家</title>
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	<title>口服固体制剂 归档 - 实验室自动化应用一致性评价丨香港力扬企业-溶出仪-药物溶出度仪厂家</title>
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		<title>[专家专栏 – 药物溶出研究] 缓释制剂释放机理研究 (双氯芬酸钠缓释片)</title>
		<link>https://nikyang.com/drug-discovery/yolanda-diclofenac-sodium-sr-tablet/</link>
		
		<dc:creator><![CDATA[Ng, Queenie]]></dc:creator>
		<pubDate>Tue, 23 Mar 2021 09:26:08 +0000</pubDate>
				<category><![CDATA[专家专栏]]></category>
		<category><![CDATA[药物研发及检测]]></category>
		<category><![CDATA[Sotax]]></category>
		<category><![CDATA[一致性评价]]></category>
		<category><![CDATA[口服固体制剂]]></category>
		<category><![CDATA[流池法]]></category>
		<category><![CDATA[溶出度测试]]></category>
		<category><![CDATA[药物研发]]></category>
		<guid isPermaLink="false">http://www.nikyang.com/?p=10684</guid>

					<description><![CDATA[<p>口服药物进入体内后进行崩解、溶出和吸收是一个动态和连续的过程。在药物研发的过程当中，需要通过体外溶出实验模拟这 [&#8230;]</p>
<p><a rel="nofollow" href="https://nikyang.com/drug-discovery/yolanda-diclofenac-sodium-sr-tablet/">[专家专栏 – 药物溶出研究] 缓释制剂释放机理研究 (双氯芬酸钠缓释片)</a>最先出现在<a rel="nofollow" href="https://nikyang.com">实验室自动化应用一致性评价丨香港力扬企业-溶出仪-药物溶出度仪厂家</a>。</p>
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<p><span style="font-weight: 400;">口服药物进入体内后进行崩解、溶出和吸收是一个动态和连续的过程。在药物研发的过程当中，需要通过体外溶出实验模拟这些体内的生理过程，以反映药物在体内行为的变化。而<a href="https://www.nikyang.com/new-280620/">缓释制剂</a>在口服后，需按要求缓慢地释放药物，进行体内外相关性（IVIVC）研究，才能保证药物在体内的溶出释放可控，但因为缓释制剂的特性，要进行准确的溶出度测定，先进的仪器和方法就至关重要。</span></p>
<p><span style="font-weight: 400;">目前，常规的溶出度测定方法（例如：桨法和篮法等等）在药物溶出研究方面尚有很多不足，而流池法具有特殊的流体动力学及其灵活性，多种制剂都能广泛应用，尤其在缓释制剂的研发上显示出了极大的优势，美国药典收录了流池法作为四法，而中国药典2020版也已经新增了<a href="https://www.nikyang.com/news-140820-1/">流池法</a>溶出度测试法，成为了篮法、桨法等方法以外的最新溶出度测试策略。</span></p>
<p><span style="color: #333399;"><strong>溶出度测定 &#8211; 缓释制剂释放机理研究 (双氯芬酸钠缓释片) </strong></span></p>
<p>Dissolution Technology曾发表一篇文献，研究了使用流池法进行双氯芬酸钠缓释片剂的溶出度筛选方法。文献当中使用了流池法进行实验，比较了流速和不同尺寸的流池以及载样方式对缓释片剂释放度的影响，找出了双氯芬酸钠缓释片最佳的释放条件后，建立了体外释放度测试，平行考察了诺华两个不同产地生产的参比制剂，以及埃及本地生产的仿制药，得到的溶出曲线显示了不同产品的释放结果。</p>
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										<img width="772" height="453" src="/wp-content/uploads/2021/03/20210322-Case-Study-Ref.png" class="attachment-large size-large" alt="" srcset="/wp-content/uploads/2021/03/20210322-Case-Study-Ref.png 772w, /wp-content/uploads/2021/03/20210322-Case-Study-Ref-300x176.png 300w, /wp-content/uploads/2021/03/20210322-Case-Study-Ref-768x451.png 768w" sizes="(max-width: 772px) 100vw, 772px" />											<figcaption class="widget-image-caption wp-caption-text">诺华不同产地生产的参比制剂以及埃及生产的仿制药的溶出度测定结果（Dissolution Technology, 2009）</figcaption>
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<p><span style="font-weight: 400;">从流池法溶出度测试的结果可以看到，参比制剂和仿制药有明显的差异。最下面的两条溶出曲线，是两个参比制剂的体外释放结果，一个是欧洲上市的，一个是埃及本地上市的。虽然它们有一定的区别，但是它们的释放曲线，可以看作是一个零级释放的曲线，证明它们是缓释效果非常好的处方。但是，埃及本地生产的处方的释放行为并没有显示出缓释的释放机理，跟参比有很大的差异，这个释放行为的巨大差异，肯定也会带来体内吸收行为很大的改变。研究也证明了以流池法进行溶出度测定，能很好的判别缓释制剂之间的释放度差异。</span></p>
<p><span style="font-weight: 400;">流池法克服了一些篮法、桨法等传统溶出度测试法的局限性，例如介质饱和、桨旋转时造成的物理影响、容易堵塞等等问题，尤其是对于一些缓释剂和难溶制剂，更灵活的溶出度测试法是必然的手段。同时，流池法溶出度测试的可重复性和可重现性已经在多项文献研究中等到证实，目前除了对于一些传统制剂的应用，很多新型制剂的研究文献当中也都应用了流池法，尤其是<a href="https://www.nikyang.com/benchtop-solutions/sotax/ce-7smart/">SOTAX CE7smart流池法溶出度测定系统</a>，为流池法的实际应用提供了强大的支持，对于药物研发必然有很大的优势。</span></p>
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<p><span style="font-weight: 400;">参考资料：</span></p>
<p><span style="font-weight: 400;">Laila H. Emara et al. (2009). Investigation of the Effect of Different Flow-Through Cell Designs on the Release of Diclofenac Sodium SR Tablets. Dissolution Technology. May 2009.</span></p>
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												<img width="781" height="424" src="/wp-content/uploads/2021/03/Yolanda-Professional-Profile-withQR.jpg" class="attachment-large size-large" alt="药物溶出流池法专家-赵宇Yolanda专家简历" srcset="/wp-content/uploads/2021/03/Yolanda-Professional-Profile-withQR.jpg 781w, /wp-content/uploads/2021/03/Yolanda-Professional-Profile-withQR-300x163.jpg 300w, /wp-content/uploads/2021/03/Yolanda-Professional-Profile-withQR-768x417.jpg 768w" sizes="(max-width: 781px) 100vw, 781px" />														</div>
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		<p><a rel="nofollow" href="https://nikyang.com/drug-discovery/yolanda-diclofenac-sodium-sr-tablet/">[专家专栏 – 药物溶出研究] 缓释制剂释放机理研究 (双氯芬酸钠缓释片)</a>最先出现在<a rel="nofollow" href="https://nikyang.com">实验室自动化应用一致性评价丨香港力扬企业-溶出仪-药物溶出度仪厂家</a>。</p>
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		<title>如何增加口服固体制剂的 BE 成功率？</title>
		<link>https://nikyang.com/news/increase-be-success-rate/</link>
		
		<dc:creator><![CDATA[Miro]]></dc:creator>
		<pubDate>Sun, 28 Jun 2020 04:30:00 +0000</pubDate>
				<category><![CDATA[最新动态]]></category>
		<category><![CDATA[药物研发及检测]]></category>
		<category><![CDATA[BE 生物等效性实验]]></category>
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		<category><![CDATA[口服固体制剂]]></category>
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		<guid isPermaLink="false">http://www.nikyang.com/?p=7618</guid>

					<description><![CDATA[<p>近年来，不少制药机构对于固体制剂的溶出度测试投入了</p>
<p><a rel="nofollow" href="https://nikyang.com/news/increase-be-success-rate/">如何增加口服固体制剂的 BE 成功率？</a>最先出现在<a rel="nofollow" href="https://nikyang.com">实验室自动化应用一致性评价丨香港力扬企业-溶出仪-药物溶出度仪厂家</a>。</p>
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				<p>近年来，不少制药机构对于<span style="color: #0000ff;"><strong>固体制剂的溶出度测试</strong></span>投入了相当大的精力，却碍于其复杂性，以致一直未能通过<span style="color: #0000ff;"><strong>一致性评价</strong></span>并把药物推出市场。</p>					</div>
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				<p>虽然，目前部分产品的溶出测试顺利 “过关”，但仍有不少产品在生物等效性 (BE) 的实验中 “徘徊不前”，意味着药企相关领域存在着难以逾越的困境，特别是定量采购政策的落地，使得不少药企转而投入到附加值更高的 “高端制剂” 上，无疑又增加了药物研发的困难性和复杂性。</p>					</div>
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			<h2 class="elementor-heading-title elementor-size-default">01. 投入资金高</h2>		</div>
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				<p>BE (生物等效性) 试验需投入大量资金，不同品种的测试所花费高达几十万到几千万不等，近年来更是成倍翻涨，加上固体制剂的一致性评价难度极高，一旦出现试验失败，便需要另外<span style="color: #0000ff;"><strong>投入更多资金</strong></span>继续测试。</p>					</div>
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			<h2 class="elementor-heading-title elementor-size-default">02. 花费大量精力、时间</h2>		</div>
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				<p>是什么原因导致 BE (生物等效性) 测试进展停滞不前呢？终其原因，在于<strong><span style="color: #0000ff;">没有找到关键的溶出曲线</span>。</strong></p><p>在仿制药研发的过程中，选取合适的测试手段去对比自研处方和参比制剂的异同是仿制药开发中常用的测试手段。由于固体制剂的体外溶出度测试能部分有效地反映药物体内的行为，因此是仿制药在筛选处方和工艺中的有效方法。而能够有效反馈自制处方与参比制剂在溶出中的细微差别，结合体内药动学知识进行分析，才能有效地找到体外那条关键的曲线<strong>。</strong></p>					</div>
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			<h2 class="elementor-heading-title elementor-size-default">流池法</h2>		</div>
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				<h5 style="text-align: center;"><strong>帮助提升口服制剂的 BE 成功率</strong></h5>					</div>
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				<h6 style="text-align: right;"><span style="color: #0000ff;">RLD – 参比制剂</span></h6><h6 style="text-align: right;"><span style="color: #0000ff;">S – 自研药样品</span></h6>					</div>
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				<p>美国药典第 4 法 (USP 4) —— 流池法的应用，为科研人员在仿制药开发的过程提供了更为有利的条件。如上图所述，某 pH 依赖型的 BCSII 类自研产品，在尝试了桨法多个介质条件后，预 BE 仍然失败了。</p><p>在运用流池法后，一次实验过程采用 3 种溶出介质进行测试，发现体外自研样品比参比释放更慢的情况，这与体内药物的释放趋势正好一致。而国外上市的相同仿制样品，显示其参比制剂相似性良好，从而更加说明流池法具有更优的判别结果。</p><p>流池法，以恒定的速率去溶解药品，有效模拟了人体体内药物溶解后被有效吸收的情况，并能表征体内不同消化部位 pH 的变化情况，因而能更真实、准确地反映药物在人体体内的溶出情况。而设备精密的构造让科研人员得到更精准的测试结果，因此可降低体外的溶出度试验与 BE 测试结果不一致的情况。因此，如果以流池法作为筛选处方或工艺的主要手段，可以大幅度减少资金预算、时间及精力。</p>					</div>
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				<h6 style="text-align: center;"><strong>力扬提供 Sotax CE 7smart (USP 4) 流池法溶出仪</strong></h6><h6 style="text-align: center;"><strong>为口服制剂的 BE 成功率再增“砖瓦”！</strong></h6>					</div>
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				<p>Sotax CE 7smart 溶出仪是专为难溶和缓释药物制剂型设计，也支持对固体制剂及多种制剂如微球、脂质体、纳米、软胶囊、栓剂、微丸、缓控释胶囊 / 片剂等的溶出度测试。其满足流池法规定的介质流速、流动、温度等要求，助力科研人员更快捷、精准获取符合人体体内流体动力学模式的溶出曲线；同时，CE 7smart 溶出仪能实现整个溶出过程自动化，避免了传统测试模式所耗费的精力、时间等缺陷，提高固体制剂通过一致性评价检测的成功率。</p>					</div>
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				<p>在过去 2 年里, 力扬成功利用 CE 7smart 流池法溶出仪比对 40 多个 BE 失败的产品, 显示了 85% 以上的有效性，即找到了处方与参比的差异。最理想的一个案例是调整了 2 个实验条件，就找到了 BE 失败批次与参比之间的显着性差异，而原有方法做了几十上百条曲线仍然没有区分。最后客户结合实验现象分析，很快调整了处方后，重试预 BE 成功。</p>					</div>
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				<p>不要让一致性评价检测成为固体制剂溶出度测试的绊脚石。力扬推荐 Sotax CE 7smart (USP 4) 溶出仪，助力提高 BE 成功率！</p>					</div>
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		<p><a rel="nofollow" href="https://nikyang.com/news/increase-be-success-rate/">如何增加口服固体制剂的 BE 成功率？</a>最先出现在<a rel="nofollow" href="https://nikyang.com">实验室自动化应用一致性评价丨香港力扬企业-溶出仪-药物溶出度仪厂家</a>。</p>
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