缓控迟释制剂
2016-12-06 21:22:44 0 举报仅支持查看
AI智能生成
缓控迟释制剂是一种特殊设计的药物剂型，其作用是通过控制药物的释放速度和时间来达到治疗效果。这种制剂能够使药物在体内缓慢释放，从而延长药物的作用时间，减少用药次数，提高患者的依从性。缓控迟释制剂广泛应用于各种疾病的治疗，如心血管疾病、糖尿病、哮喘等。常见的缓控迟释制剂有控释片、控释胶囊、缓释注射剂等。通过合理的设计和制备工艺，缓控迟释制剂能够实现药物的平稳释放，减少不良反应的发生，提高治疗效果。总之，缓控迟释制剂为患者提供了更加便捷、安全和有效的药物治疗方式。
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<div>缓释制剂</div><div><br></div>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">是指用药后能在机内内缓慢释放药物，使药物在较长时间内维持有效血药浓度的制剂，药物的释放多数情况下符合一级或</span><span style="font-family:"Times New Roman";mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:en-US;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">Higuchi</span><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">动力学过程</span>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">控释</span><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">制剂</span></p>
<span class="Apple-tab-span" style="white-space:pre"> </span>是指药物按预先设定好的程序缓慢地恒速或接近恒速释放的制剂，一般符合零级动力学过程
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:仿宋_GB2312;
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">优点</span></p>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">减少服药次数，大大提高病人的顺应性</span>
释药徐缓，使血药浓度平稳，避免峰谷现象，有利于降低药物的毒副作用，减少耐药性的发生
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">缓、控释制剂可发挥药物的最佳治疗效果</span>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";<br>mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:<br>minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;<br>mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;<br>mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">某些缓、控释制剂可按要求定时、定位释放，更适合疾病的治疗</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;">缺点</p><div><br></div><p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"></p>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">临床应用中对剂量调节的灵活性较差，如出现副作用，往往不能立刻停止治疗</span>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">缓释制剂往往是基于健康人群的平均动力学参数而设计，当药物在疾病状态的体内动力学特性有所改变时，不能灵活调节给药方案</span>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">制备缓、控释制剂所涉及的设备和工艺费用较常规制剂昂贵</span>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:Arial;
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">设计要求</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">药物的选择</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">适合制成缓、控释制剂的药物</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">半衰期较短、首过作用强、成瘾性药物</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">不宜制成缓、控释制剂的药物</span></p>
<div>剂量大、药效剧烈、溶解吸收很差、剂量需精密调节、<span style="font-size: 13px;">抗菌效果依赖于峰浓度的抗生素药物</span></div><div><br></div>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">生物利用度</span><span style="font-family:"Times New Roman";mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:en-US;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">——</span><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">为普通制剂的</span><span style="font-family:"Times New Roman";mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:en-US;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">80%~120%</span></p>
<div>峰、谷浓度比值——缓、控释制剂稳态时峰浓度与谷浓度之比应小于普通制剂</div><div><br></div>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
Arial;mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">释药机制</span>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:Arial;
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">溶出机制</span></p>
<div>制成溶解度小的盐或酯</div><div><br></div>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">与高分子化合物形成难溶性的盐</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">控制粒子大小</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:Arial;
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">扩散机制</span></p>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">贮库型</span>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">骨架型</span>
<div>溶蚀与扩散相结合</div><div><br></div>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:Arial;
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">渗透压机制</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:Arial;
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">离子交换作用</span></p>
膜控型缓、控释制剂
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">膜控型缓、控释制剂是指将一种或多种包衣材料对颗粒、片剂、小丸等进行包衣处理，以控制药物的释放速率、释放时间或释放部位的制剂</span>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">控释膜通常为一种半透膜或微孔膜，释药机制是膜腔内的渗透压或药物分子在膜层中的扩散行为</span>
口服择时（定时）释药系统
根据人体的生物节律变化特点，按照生理和治疗的需要而定时、定量释药的一种新型给药系统
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:Arial;
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">缓、控释制剂设计原则</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:Arial;
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">设计时需要考虑的影响因素</span></p>
<div>理化因素</div><div><br></div>
<font color="#000000" face="仿宋_GB2312">生物因素</font>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:Arial;
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">缓、控释制剂的辅料</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:Arial;mso-ascii-font-family:Arial;mso-fareast-font-family:
仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:minor-bidi;
color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%"> 缓、控释制剂中药物的释放速度主要通过辅料来控制，即利用一些高分子材料阻滞药物的释放速度</span></p>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">亲水凝胶骨架材料</span><span style="font-family:"Times New Roman";mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:en-US;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">——</span><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">遇水膨胀，形成凝胶屏障控制药物释放</span>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";<br>mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:<br>minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;<br>mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;<br>mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">非溶蚀性骨架材料</span><span style="font-family:"Times New Roman";mso-ascii-font-family:"Times New Roman";<br>mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:<br>minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:en-US;<br>mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;<br>mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">——</span><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";<br>mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:<br>minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;<br>mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;<br>mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">不溶于水或水溶性极小的高分子聚合物</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";<br>mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:<br>minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;<br>mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;<br>mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">生物溶蚀性骨架材料</span><span style="font-family:"Times New Roman";mso-ascii-font-family:"Times New Roman";<br>mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:<br>minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:en-US;<br>mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;<br>mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">——</span><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";<br>mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:<br>minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;<br>mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;<br>mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">本身不溶解，胃肠液环境下可逐渐溶蚀</span></p>
<div>缓释包衣材料</div><div><br></div>
<div>不溶性材料——不溶于水的高分子聚合物，无毒，具有良好的成膜性能和机械性能，溶解能力不受胃肠液pH影响</div><div><br></div>
<div>肠溶性材料——胃中不溶，小肠偏碱性环境下能溶解的高分子材料</div><div><br></div>
增稠剂
<div>水溶性高分子材料，溶于水后，其溶液黏度随浓度增大而增加，黏度增加可减慢药物的扩散速率，延缓药物吸收</div><div><br></div>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:Arial;
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">缓</span><span style="font-family:仿宋_GB2312;mso-ascii-font-family:Arial;mso-fareast-font-family:
仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:minor-bidi;
color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">控释制剂简介</span></p>
骨架型缓释制剂
骨架制剂是指药物和一种或多种骨架材料通过压制、融合等技术手段制成的片状、粒状或其它形式的制剂
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">亲水性凝胶骨架片</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">蜡质类骨架片</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">不溶性骨架片</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">骨架型小丸</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:Arial;
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">质量评价</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:Arial;
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">体外</span><span style="font-family:仿宋_GB2312;mso-ascii-font-family:Arial;mso-fareast-font-family:
仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:minor-bidi;
color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">评价</span></p>
<div>释放度试验方法</div><div><br></div>
<font color="#000000" face="仿宋_GB2312">取样点设计</font>
<div>实验结果分析</div><div><br></div>
<div>体内评价</div><div><br></div>
生物利用度
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">是指剂型中的药物吸收进入人体血液循环的速度和程度</span>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:<br>"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;<br>mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:<br>12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:<br>text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">生物等效性</span>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">是指一种药物的不同制剂在相同实验条件下，给以相同剂量，其吸收速度和程度没有明显差异</span>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">口服定位释药系统</span>
是指口服后能将药物选择性地输送到胃肠道某一特定部位，以速释或缓释、控制释放药物的剂型
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:仿宋_GB2312;
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">口服定位释药系统的目的</span></p>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">改善药物在胃肠道的吸收，避免其在胃肠生理环境下失活</span>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">治疗胃肠道局部疾病，提高疗效，减少剂量，降低全身性副作用</span>
改善缓释、控释制剂因受胃肠道运动的影响而造成的药物吸收不完全、个体差异大等现象
姓名：谭畅
班级：制药升14级
学号：2016520461
择时与定位释药机制
<div>胃定位释药系统——主要通过延长胃内的滞留时间来实现</div><div><br></div>
胃内滞留片是指一类能滞留于胃液中，延长药物在消化道内的释放时间，改善药物吸收，有利于提高药物生物利用度的片剂
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; text-indent: 0in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";
mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:
minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;
mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;
mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">目的</span></p>
<p style="margin-top: 4.32pt; margin-bottom: 0pt; margin-left: 0.5in; direction: ltr; unicode-bidi: embed; vertical-align: baseline;"><span style="font-family:仿宋_GB2312;mso-ascii-font-family:"Times New Roman";<br>mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;mso-bidi-theme-font:<br>minor-bidi;color:black;mso-color-index:3;mso-font-kerning:12.0pt;language:zh-CN;<br>mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:text2;<br>mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">促进弱酸性药物和十二指肠段有主动转运药物的吸收</span></p>
<div>提高在肠道环境不稳定的药物在胃部的吸收</div><div><br></div>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">提高治疗胃部和十二指肠部位疾病的疗效</span>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">延长胃肠道滞留时间，药物得到充分的吸收</span>
<div>途径</div><div><br></div>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">胃内漂浮滞留</span>
胃壁黏附滞留
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">磁导向定位技术</span>
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">膨胀滞留</span>
口服结肠定位给药系统
<span style="font-family:仿宋_GB2312;mso-ascii-font-family:
"Times New Roman";mso-fareast-font-family:仿宋_GB2312;mso-bidi-font-family:+mn-cs;
mso-bidi-theme-font:minor-bidi;color:black;mso-color-index:3;mso-font-kerning:
12.0pt;language:zh-CN;mso-style-textfill-type:solid;mso-style-textfill-fill-themecolor:
text2;mso-style-textfill-fill-color:black;mso-style-textfill-fill-alpha:100.0%">是指用适当方法，使药物避免在胃、十二指肠、空肠和回肠前端释放，运送到人体回盲部后释放而发挥局部或全身治疗作用的一种给药系统，是一种定位在结肠释药的制剂</span>
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