Formulation and in vitro and in vivo evaluation of film-coated montelukast sodium tablets using Opadry® yellow 20A82938 on an industrial scale

Abstract

Purpose:The aim of this study was to formulate stable film-coated montelukast sodium (MS) tablets using Opadry® yellow 20A82938 (Montikast® tablets) and to evaluate their in vitro and in vivo release profile.Methods:MS core tablets were manufactured using a direct compression method. Opadry yellow 20A82938 aqueous coating dispersion was used as the film-coating material. Dissolution of the film-coated tablets was tested in 900 mL of 0.5% sodium lauryl sulfate solution and the bioequivalence of the tablets was tested by comparing them with a reference formulation – Singulair® tablets. In vitro–in vivo correlation was evaluated. The stability of the obtained film-coated tablets was evaluated according to International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use guidelines.Results:The efficiency of the film coating was determined by subjecting the coated tablets to gastric pH and drug release was analyzed using high-performance liquid chromatography. The coated tablets had no obvious defects. MS release met the study criterion of not less than 80% dissolved after 30 minutes in 0.5% sodium lauryl sulfate solution. Statistical comparison of the main pharmacokinetic parameters clearly indicated no significant difference between test and reference in any of the calculated pharmacokinetic parameters. Level A correlation between in vitro drug release and in vivo absorption was found to be satisfactory.Conclusion:These findings suggest that aqueous film coating with Opadry yellow 20A82938 is an easy, reproducible, and economical approach for preparing stable MS film-coated tablets without affecting the drug-release characteristics.

Novel montelukast sodium-loaded clear oral solution prepared with hydroxypropyl-β-cyclodextrin as a solubilizer and stabilizer: enhanced stability and bioequivalence to commercial granules in rats

“…5. In FDA regulation on montelukast sodium-loaded commercial oral products, 0.5 % (w/v) sodium lauryl sulphate in water must be used as a dissolution medium [9,40]. The drug from the oral solution and commercial granules was rapidly dissolved in this medium at the initial times.…”

“…The montelukast sodium-loaded commercial granule (Singulair Ò ) and oral solution at the montelukast base dose of 2 mg/kg was orally administered. After administration, 0.2 ml of blood was withdrawn from the cannulated right femoral artery of the rat at the predetermined timepoints [37,39,40]. The blood sample was centrifuged at 14,0009g at 4°C for 3 min using a 5415C centrifuge (Eppendorf, Hauppauge, NY, USA) and plasma was separated from the blood.…”

Generalized in vitro-in vivo relationship (IVIVR) model based on artificial neural networks

“…Further, in order to demonstrate the real application of the system, a new dataset was introduced, including data from the recent study published by Zaid et al concerning the in vitro-in vivo characteristics of montelukast,44 which is a completely unknown structure in the system. Prediction of its behavior is presented in Figure 6.…”

In Vitro-In Vivo Correlation (IVIVC): From Current Achievements Towards the Future

“…Successful IVIVC using the basket apparatus was established for metoprolol ER, metoprolol immediate release (IR), ibuprofen ER capsules, and novel once-daily ketoprofen ER formulations (35)(36)(37)(38). Examples of drugs with IVIVC developed based on the paddle apparatus are griseofulvin fast disintegrating tablets, diltiazem MR, alprazolam controlled-release tablet, carbamazepine IR, diclofenac osmotic pump tablets, and montelucast IR tablets (39)(40)(41)(42)(43)(44).…”