Haddad Razan, Gardouh Ahmed R
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Jadara University, Irbid 21110, Jordan.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, Egypt.
Adv Pharmacol Pharm Sci. 2024 Oct 17;2024:7914860. doi: 10.1155/2024/7914860. eCollection 2024.
Orodispersible tablet (ODT) is a promising avenue for drug delivery, offering a dosage form that can be disintegrated instantaneously in the mouth and released the drug that dissolves or disperses in the saliva without the addition of water. ODT can effectively boost the dissolution rate and consequently the bioavailability of several hydrophobic drugs. Additionally, ODT is very attractive and suitable for specific patients who are unable to swallow the traditional tablet. The basic approach in the fabrication of oral tablets for hydrophobic drugs relies on the utilization of superdisintegrants which allow prompt disintegration of tablets after swallowing. In the present investigation, escitalopram oxalate was chosen as a model drug, which is a hydrophobic, antidepressant, selective serotonin reuptake inhibitor (SSRI) drug. Nine formulas of escitalopram oxalate ODTs were prepared by varying the concentrations of three different superdisintegrants: sodium starch glycolate, croscarmellose sodium, and crospovidone to improve the dissolution and release of escitalopram oxalate. Each was used in three different concentrations (2.5%, 5%, and 7.5%), and all the ODTs were prepared by the direct compression method. The micrometric characterization of the powder blend used in the formulations was investigated such as angle of repose, bulk and tapped densities, compressibility percent (Carr's index), and Hausner ratio. Furthermore, the prepared ODTs were characterized in terms of weight variation, thickness, diameter, hardness, friability, in vitro disintegration, wetting time, water absorption ratio, drug content, in vitro dissolution, and accelerated stability study. The results showed that the formula (ODT9) that contained 7.5% of the superdisintegrant sodium starch glycolate had superior characteristics in almost all the tests, with a dissolution rate of 100% after 6 minutes. Also, it was stable under the accelerated stability conditions.
口腔崩解片（ODT）是一种很有前景的药物递送途径，它提供了一种剂型，无需加水就能在口腔中瞬间崩解，并释放出溶解或分散在唾液中的药物。ODT可以有效提高几种疏水性药物的溶解速率，从而提高其生物利用度。此外，ODT对无法吞咽传统片剂的特定患者非常有吸引力且适用。制备用于疏水性药物的口服片剂的基本方法依赖于使用超级崩解剂，使片剂在吞咽后迅速崩解。在本研究中，选择草酸艾司西酞普兰作为模型药物，它是一种疏水性抗抑郁选择性5-羟色胺再摄取抑制剂（SSRI）药物。通过改变三种不同超级崩解剂（羟丙基淀粉、交联羧甲基纤维素钠和交联聚维酮）的浓度，制备了九种草酸艾司西酞普兰ODT配方，以改善草酸艾司西酞普兰的溶解和释放。每种崩解剂都以三种不同浓度（2.5%、5%和7.5%）使用，所有ODT均采用直接压片法制备。对制剂中使用的粉末混合物进行了微观特性研究，如休止角、堆密度和振实密度、压缩率（卡尔指数）和豪斯纳比。此外，对制备的ODT进行了重量差异、厚度、直径、硬度、脆碎度、体外崩解、润湿时间、吸水率、药物含量、体外溶解和加速稳定性研究等方面的表征。结果表明，含有7.5%超级崩解剂羟丙基淀粉的配方（ODT9）在几乎所有测试中都具有优异的特性，6分钟后的溶解率为100%。此外，它在加速稳定性条件下也很稳定。
