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首页> 外文期刊>International Journal of Pharmaceutics >Preparation of enteric coated timed-release press-coated tablets and evaluation of their function by in vitro and in vivo tests for colon targeting.
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Preparation of enteric coated timed-release press-coated tablets and evaluation of their function by in vitro and in vivo tests for colon targeting.

机译：制备肠溶包衣的定时释放压制包衣的片剂，并通过体外和体内结肠靶向测试来评估其功能。

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As a new oral drug delivery system for colon targeting, enteric coated timed-release press-coated tablets (ETP tablets) were developed by coating enteric polymer on timed-release press-coated tablets composed of an outer shell of hydroxypropylcellulose and core tablet containing diltiazem hydrochloride (DIL) as a model drug. The results of the in vitro dissolution tests in JP 1st fluid (pH 1.2) and JP 2nd fluid (pH 6.8) indicated that these tablets showed both acid resistance and timed-release. To clarify whether ETP tablets could have been of use in the gastrointestinal tract, ETP tablets with a layer of phenylpropanolamine hydrochloride (PPA) (a marker of gastric emptying) between the enteric coating layer and outer shell were prepared, and were administered to beagle dogs. The gastric emptying time and lag time after gastric emptying were evaluated by determining the times at which PPA and DIL first appeared in the plasma (TFA(PPA) and TFA(DIL), respectively). TFA(PPA) and TFA(DIL) were about 4 and 7 h, respectively. This value of TFA(PPA) indicated that ETP tablets displayed acid resistance in the stomach as well as in JP Ist fluid. Subtraction of TFA(PPA) from TFA(DIL) gave a value of about 3 h which agreed well with the lag time determined by in vitro dissolution test in JP 2nd fluid. Also, the results seemed to be in accordance with the time at which the tablets reached the colon after gastric emptying. Therefore, ETP tablets seemed to be an effective tool for oral site-specific delivery including targeting of the colon.
机译：作为用于结肠靶向的新型口服药物递送系统，通过将肠溶性聚合物包衣在由羟丙基纤维素的外壳和含有地尔硫卓的核心片剂组成的定时释放压制片剂上，开发了肠溶定时释放的压制片剂（ETP片剂）。盐酸盐（DIL）作为模型药物。在JP 1st液体（pH 1.2）和JP 2nd液体（pH 6.8）中的体外溶出度测试结果表明，这些片剂同时显示出耐酸性和定时释放性。为了澄清ETP片剂是否可以在胃肠道中使用，制备了在肠溶衣层和外壳之间具有一层苯丙醇胺盐酸盐（PPA）（胃排空的标志物）的ETP片剂，并将其施用于比格犬。通过确定血浆中PPA和DIL首次出现的时间（分别为TFA（PPA）和TFA（DIL））来评估胃排空后的胃排空时间和滞后时间。 TFA（PPA）和TFA（DIL）分别约为4小时和7小时。 TFA（PPA）的该值表明ETP片剂在胃以及JP Ist液中均显示出耐酸性。从TFA（DIL）中减去TFA（PPA）得到的值约为3 h，这与通过JP 2nd体外溶出试验确定的滞后时间很好地吻合。而且，结果似乎与胃排空后片剂到达结肠的时间一致。因此，ETP片剂似乎是口服特定位点递送（包括靶向结肠）的有效工具。

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