Evaluation of the drug solubility and rush ageing on drug release performance of various model drugs from the modified release polyethylene oxide matrix tablets

Abstract

Hydrophilic matrix systems are currently some of the most widely used drug delivery systems for controlled-release oral dosage forms. Amongst a variety of polymers, polyethylene oxide (PEO) is considered an important material used in pharmaceutical formulations. As PEO is sensitive to thermal oxidation, it is susceptible to free radical oxidative attack. The aim of this study was to investigate the stability of PEO based formulations containing different model drugs with different water solubility, namely propranolol HCl, theophylline and zonisamide. Both polyox matrices 750 and 303 grade were used as model carriers for the manufacture of tablets stored at 40 °C. The results of the present study suggest that the drug release from the matrix was affected by the length of storage conditions, solubility of drugs and the molecular weight of the polymers. Generally, increased drug release rates were prevalent in soluble drug formulations (propranolol) when stored at the elevated temperature (40 °C). In contrast, it was not observed with semi soluble (theophylline) and poorly soluble (zonisamide) drugs especially when formulated with PEO 303 polymer. This indicates that the main parameters controlling the drug release from fresh polyox matrices are the solubility of the drug in the dissolution medium and the molecular weight of the polymer. DSC traces indicated that that there was a big difference in the enthalpy and melting points of fresh and aged PEO samples containing propranolol, whereas the melting point of the aged polyox samples containing theophylline and zonisamide was unaffected. Graphical abstractᅟ Electronic supplementary materialThe online version of this article (doi:10.1007/s13346-016-0344-5) contains supplementary material, which is available to authorized users.

Electrospun 5-chloro-8-hydroxyquinoline-Loaded Cellulose Acetate/Polyethylene Glycol Antifungal Membranes Against Esca

“…The incorporation of 5-Cl8Q in the polymer matrix is expected to impart antifungal activity to the obtained membranes. Moreover, PEG and PEO have been reported as solubilizing agents for poorly water-soluble drugs [25] and will lead to the more rapid release of the biologically active compound.…”

Discriminative Dissolution Method Using the Open-Loop Configuration of the USP IV Apparatus to Compare Dissolution Profiles of Metoprolol Tartrate Immediate-Release Tablets: Use of Kinetic Parameters

“…Similar to the ANOVA-based method, dissolution efficiency (DE) is not considered a method of choice to establish similarity between dissolution profiles according to the FDA and EMA guidelines, but it can be used on highly variable dissolution profiles as long as it is statistically valid and satisfactorily justified [ 1 ]. Although the DE is mainly used to compare drug release [ 54 ], this method was proposed in 1975 to establish similarity mainly for immediate-release dosage forms [ 55 ]. Meanwhile, the median dissolution time (MDT) and median residence time (MRT) are more applicable to controlled release systems [ 56 ], and for this reason, they were not included in the analysis.…”

Artikel Review: Pengaruh Perlakuan Pada Pati Sebagai Superdisintegran Terhadap Waktu Hancur Fast Disintegrating Tablet

“…Konjugasi pati dengan suatu asam amino endogenik seperti leucine dan glycine, derivatisisasi dengan polysuccinimide, konjugasi pati jagung-Neusilin UFL2 memungkinkan dapat meningkatkan disintegrasi tablet dengan waktu hancur kurang dari 60 detik dapat dilihat pada Tabel 3. Waktu hancur yang lebih cepat ini disebabkan karena leucine mengandung amina (NH2) dan memiliki luas permukaan yang besar yang dapat meningkatkan penyerapan air dan pembengkakan pada permukaan pati [53], penambahan bahan bersifat polar dari polysuccinimide memfasilitasi hidrofilitas [54], glycine memiliki sifat pembasahan yang sangat baik [55], Neusilin UFL2 dapat meningkatkan kualitas tablet (sifat alir, disintegrasi, kelarutan) [56], sehingga granula pati menunjukan adanya rongga yang menyebabkan pembengkakan dan penyerapan meningkat karna porositas yang tinggi [48].…”