Design and evaluation of effervescent floating tablets based on hydroxyethyl cellulose and sodium alginate using pentoxifylline as a model drug

Abstract

The aim of this work was to design and evaluate effervescent floating gastro-retentive drug delivery matrix tablets with sustained-release behavior using a binary mixture of hydroxyethyl cellulose and sodium alginate. Pentoxifylline was used as a highly water-soluble, short half-life model drug with a high density. The floating capacity, swelling, and drug release behaviors of drug-loaded matrix tablets were evaluated in 0.1 N HCl (pH 1.2) at 37°C±0.5°C. Release data were analyzed by fitting the power law model of Korsmeyer–Peppas. The effect of different formulation variables was investigated, such as wet granulation, sodium bicarbonate gas-forming agent level, and tablet hardness properties. Statistical analysis was applied by paired sample t-test and one-way analysis of variance depending on the type of data to determine significant effect of different parameters. All prepared tablets through wet granulation showed acceptable physicochemical properties and their drug release profiles followed non-Fickian diffusion. They could float on the surface of dissolution medium and sustain drug release over 24 hours. Tablets prepared with 20% w/w sodium bicarbonate at 50–54 N hardness were promising with respect to their floating lag time, floating duration, swelling ability, and sustained drug release profile.

In-Depth Study into Polymeric Materials in Low-Density Gastroretentive Formulations

“…Natural gums-gellan gum, guar gum, carrageenans and xanthan gum-other polysaccharides, such as alginates and chitosan [55], and natural polymers such as pectin and gelatin [18] are among natural hydrocolloids or gel-forming agents that have the ability to swell in contact with gastric fluid, maintain a relative integrity of shape and have a bulk density less than the gastric content. The most commonly used natural gums (Table S3) are heteroglycans of high molecular weights.…”

“…Likewise, effervescent floating tablets of pentoxifylline were successfully prepared by using sodium bicarbonate as a gas-forming agent and a mixture of HEC and sodium alginate as the polymeric matrix. The tablets could float on the surface of the dissolution medium and sustain drug release over 24 h [55].…”

“…For example, effervescent floating tablets of pentoxifylline were successfully prepared by using sodium bicarbonate as a gas-forming agent and a mixture of HEC and sodium alginate as a polymeric matrix. The tablets could float on the surface of the dissolution medium and sustain drug release over 24 h [55]. Another example is the formulation of losartan-loaded swellable and floatable GRDDS tablets in which the appropriate combination of HEC, sodium carboxymethyl cellulose (NaCMC) and sodium bicarbonate led to tablets able to float for more than 16 h [65].…”

Formulation and Evaluation of Controlled Release Floating Tablets of Cefixime Using Hydrophilic Polymers

“…In the study one tablet was placed in USP type II paddle apparatus. Dissolution basket was filled with 900 ml of 0.1N hydrochloric acid and maintained the temperature at 37 ± 0.5 0 C. Floating lag time is the time taken for the tablet to rise to the surface of dissolution medium and total floating time is the time tablet float comfortably in dissolution medium 18,19 .…”

Applications of synthetic and semisynthetic polymers (Kollidon K25, Kollidon K90 and Hydroksyethylocellulose) as carriers of ketoprofen in solid oral prolonged release dosage forms. The impact of selected non-ionic surfactants (Tween 80 and Rofam 70) on the release kinetic

“…2 Odpowiednia matryca hydrofilowa mogłaby znacząco zmniejszyć to negatywne działanie. [3][4][5] Aby uwalnianie z matrycy było jak najbardziej zbliżone do kinetyki zerowego rzędu, należy w badaniach preformulacyjnych empirycznie określić jakościowy i ilościowy udział składowych matrycy. 6 Celem pracy było zbadanie przydatności polimerów (syntetycznych Kollidonów K25 i K90; półsyntetycznych -hydroksyetylocelulozy) i dwuwodnego wodorofosforanu wapnia (jako nieorganicznego, nierozpuszczalnego wypełniacza) w konstruowaniu matrycowych stałych doustnych postaci leku z ketoprofenem (ang.…”