Samprasit Wipada, Akkaramongkolporn Prasert, Ngawhirunpat Tanasait, Rojanarata Theerasak, Opanasopit Praneet
Pharmaceutical Development of Green Innovations Group (PDGIG), Faculty of Pharmacy, Silpakorn University , Nakhon Pathom , Thailand.
Drug Dev Ind Pharm. 2015 Jun;41(6):1006-16. doi: 10.3109/03639045.2014.922573. Epub 2014 May 28.
The bitter taste of drug is masked by the exchange of ionized drugs with counter ions of ion exchange resin, forming "resinate". Cyclodextrin reduces the unpleasant taste and enhances the drug solubility by encapsulating drug molecules into its central cavity.
Oral disintegrating tablets (ODTs) using the combination of ion exchange resin and cyclodextrin was developed, to mask the bitter taste and enhance drug dissolution.
Meloxicam (MX) was selected as a model drug. Formulations containing various forms of MX (free drug, MX-loaded resin or resinate, complexes of MX and 2-hydroxypropyl-β-cyclodextrin (HPβCD) or MX/HPβCD complexes, and a mixture of resinate and MX/HPβCD complexes) were made by direct compression. The ODTs were evaluated for weight variation, thickness, diameter, hardness, friability, disintegration time, wetting time, MX content, MX release, degree of bitter taste and stability.
The tablet hardness was ∼3 kg/in(2), and the friability was <1%. Tablets formulated with resinate and the mixture of resinate and MX/HPβCD complexes disintegrated rapidly within 60 s, which is the acceptable limit for ODTs. These results were corresponded to the in vivo disintegration and wetting times. However, only tablets containing the mixture of resinate and MX/HPβCD complexes provided complete MX dissolution and successfully masked the bitter taste. In addition, this tablet was stable at least 6 months.
The combination of ion exchange resin and cyclodextrin could be used in ODTs to mask the bitter taste and enhance the dissolution of drugs that are weakly soluble in water.
通过离子化药物与离子交换树脂的抗衡离子交换形成“树脂酸盐”，从而掩盖药物的苦味。环糊精通过将药物分子包裹在其中心腔内来降低不良味道并提高药物溶解度。
开发使用离子交换树脂和环糊精组合的口腔崩解片（ODT），以掩盖苦味并提高药物溶出度。
选择美洛昔康（MX）作为模型药物。通过直接压片制备含有各种形式MX（游离药物、负载MX的树脂或树脂酸盐、MX与2-羟丙基-β-环糊精（HPβCD）的复合物或MX/HPβCD复合物，以及树脂酸盐和MX/HPβCD复合物的混合物）的制剂。对ODT进行重量差异、厚度、直径、硬度、脆碎度、崩解时间、润湿时间、MX含量、MX释放、苦味程度和稳定性评估。
片剂硬度约为3 kg/in(2)，脆碎度<1%。用树脂酸盐以及树脂酸盐和MX/HPβCD复合物的混合物制备的片剂在60秒内迅速崩解，这是ODT的可接受限度。这些结果与体内崩解和润湿时间相符。然而，只有含有树脂酸盐和MX/HPβCD复合物混合物的片剂能使MX完全溶解并成功掩盖苦味。此外，该片剂至少稳定6个月。
离子交换树脂和环糊精的组合可用于ODT中，以掩盖苦味并提高水中难溶性药物的溶出度。
