<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%">药物应用类型</span></p>
<div>小分子化合物、单克隆抗体、药物载体制剂等</div><div><br></div>
<div>靶向制剂的体内作用机制和分类</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;"><font color="#000000" face="仿宋_GB2312">靶向制剂的分类</font></p><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%">一级靶向制剂</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%">以特定器官和组织为靶标输送药物的制剂</span></p>
<div>二级靶向制剂</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%">以特定细胞为靶标输送药物的制剂</span></p>
<div>三级靶向制剂</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%">以细胞内特定部位或细胞器为靶标输送药物的制剂</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%">靶向制剂的作用机制</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%">最理想化的作用机制</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%">最理想化的,所谓智能型药物载体</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%">的概念是:载体能够自动完成检测、识别、释放药物的过程,攻击体内疾病目标,达到精确制导、药到病除的效果</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";
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%">常见的作用机制</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%">被动靶向制剂</span>
是指由于载体的粒径、表面性质等特殊性使药物在体内特定靶点或部位富集的制剂
主动靶向制剂
是指药物载体能对靶组织产生分子特异性相互作用的制剂
<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%">物理化学靶向制剂</span>
<span class="Apple-tab-span" style="white-space:pre"> </span>是指通过设计特定的载体材料和结构,使其能够响应于某些物理或化学条件而释放药物的制剂
<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%">靶向药物输送系统</span>
如果一个药物并不具有分子靶向特性,但却能依靠其制剂材料及结构的设计实现分子的靶向效果,即能够选择性地将药物定位或富集在靶组织、靶器官、靶细胞或细胞内结构的药物载体系统,称为靶向制剂,或靶向载体,或靶向药物输送系统
<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%">生物导弹</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%">近二十年来,靶向药物相继上市,都属于能够较特异性地作用于肿瘤细胞的靶向制剂,即所谓的“生物导弹”,把肿瘤的药物治疗带入了“分子靶向药物”时代</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: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%">特点</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%">具有特异性的肿瘤杀伤效果</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%">可避免药物作用于其它组织可能造成的毒副作用</span>
靶向药物输送系统
<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%">如果一个药物并不具有分子靶向特性,但却能依靠其制剂材料及结构的设计实现分子的靶向效果,即能够选择性地将药物定位或富集在靶组织、靶器官、靶细胞或细胞内结构的药物载体系统,称为靶向制剂,或靶向载体,或靶向药物输送系统</span>
<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%">靶向制剂的结构及分类</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%">药物大分子共价结合物</span>
<span class="Apple-tab-span" style="white-space:pre"> </span>将药物以及各种功能分子通过化学反应与高分子载体(或蛋白)共价结合的化合物
<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%">颗粒型靶向载体系统</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%">药物与载体及各种功能分子以非共价作用自组装形成的载体结构</span>
前药
<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%">通过化学反应将药物活性基团改构或衍生形成的一种新的惰性结构,其本身不具有药理活性,在体内特定的靶组织中经化学反应或酶降解,再生为活性药物而发挥治疗作用</span>