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A Potential Alternative Orodispersible Formulation to Prednisolone Sodium Phosphate Orally Disintegrating Tablets

机译:对泼尼松酸钠口腔崩解片剂的潜在替代的替代配方

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摘要

The orally disintegrating tablet (ODT) has shown vast potential as an alternative oral dosage form to conventional tablets wherein they can disintegrate rapidly (≤30 s) upon contact with saliva fluid and should have an acceptable mouthfeel as long as their weight doesn’t exceed 500 mg. However, owing to the bitterness of several active ingredients, there is a need to find a suitable alternative to ODTs that maintains their features and can be taste-masked more simply and inexpensively. Therefore, electrospun nanofibers and solvent-cast oral dispersible films (ODFs) are used in this study as potential OD formulations for prednisolone sodium phosphate (PSP) that is commercially available as ODTs. The encapsulation efficiency (EE%) of the ODFs was higher (≈100%) compared to the nanofibers (≈87%), while the disintegration time was considerably faster for the electrospun nanofibers (≈30 s) than the solvent-cast ODFs (≈700 s). Hence, accelerated release rate of PSP from the nanofibers was obtained, due to their higher surface area and characteristic surface morphology that permitted higher wettability and thus, faster erosion. Taste-assessment study using the electronic-tongue quantified the bitterness threshold of the drug and its aversiveness concentration (2.79 mM). Therefore, a taste-masking strategy would be useful when further formulating PSP as an OD formulation.
机译:口服崩解片剂(ODT)已经显示为常规片剂的替代口服剂型的巨大潜力,其中它们可以在与唾液流体接触时快速(≤30秒)崩解,并且只要其重量不超过,就应该具有可接受的口感500毫克。然而,由于几种活性成分的苦味,需要寻找合适的替代物,其维持其特征,并且可以更简单且廉价地掩盖。因此,在本研究中使用电纺纳米纤维和溶剂浇铸口服可分散膜(ODF)作为磷酸氢钠(PSP)的潜在OD配方,其可商购获得ODTS。与纳米纤维(≈87%)相比,ODF的封装效率(EE%)更高(≈100%),而电纺纳米纤维(≈30s)比溶剂铸造ODF( ≈700秒)。因此,获得了从纳米纤维获得的PSP的加速释放速率,由于其较高的表面积和特征表面形态,允许更高的润湿性,因此更快地侵蚀。使用电子舌剂的味道评估研究量化了药物的苦味阈值及其厌恶浓度(2.79 mm)。因此,当进一步配制PSP作为OD配方时,味道掩蔽策略将是有用的。

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