Formulation and in vitro evaluation of size expanding gastro-retentive systems of levofloxacin hemihydrate.
Size increasing (plug-type) levofloxacin hemihydrate (LVF) tablets for eradication of Helicobacter pylori (H. pylori) were prepared using in situ gel forming polymers including: gellan gum, sodium alginate, pectin and xanthan gum. Effect of cross-linkers: calcium and aluminum chloride, on the drug release was also studied. The prepared tablets were evaluated for their physicochemical parameters: weight variation, thickness, friability, hardness, drug content, water uptake and in vitro drug release. The optimized formula was subjected to further studies such as radial swelling test, FT-IR and DSC. Results revealed that LVF release depends not only on the nature of the matrix but also on the type of cross linker used to form this polymeric matrix. The addition of either calcium chloride or aluminum chloride, as cross-linkers, to gellan gum formulations significantly decreased drug release. Other polymers' formulations resulted in increased drug release upon addition of the same cross-linkers. The formula containing xanthan gum without any cross linker showed the most sustained LVF release with an increase in diameter with time, thus acting as a plug-type dosage form. IR spectra and DSC thermograms of LVF, xanthan gum, and a physical mixture of both, indicated that there was no interaction between the drug and the polymer and confirmed the drug stability.
Department of Pharmaceutics, Faculty of Pharmacy and Drug manufacturing, Pharos University in Alexandria, Alexandria, Egypt. Electronic address: sally.elzahaby@yahoo.com.
Sally A
SA
El-Zahaby
Department of Pharmaceutics, Faculty of Pharmacy and Drug manufacturing, Pharos University in Alexandria, Alexandria, Egypt.
Abeer A
AA
Kassem
Department of Pharmaceutics, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt.
Amal H
AH
El-Kamel
D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000493:pharmacokinetics; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003692:Delayed-Action Preparations / Q000737:chemistry / Q000493:pharmacokinetics; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism; D016480:Helicobacter pylori / Q000187:drug effects; D064704:Levofloxacin / Q000737:chemistry* / Q000493:pharmacokinetics; D011135:Polysaccharides, Bacterial / Q000737:chemistry* / Q000493:pharmacokinetics
D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D011135:Polysaccharides, Bacterial; D064704:Levofloxacin; C048288:gellan gum
Cross-linker; Fluoroquinolone; Gastroretentive; Levofloxacin; Plug-type