Details

Autor(en) / Beteiligte

• Ibrahim, Mohamed
• Naguib, Youssef W.
• Sarhan, Hatem A.
• Abdelkader, Hamdy

Titel

Preformulation-Assisted Design and Characterization of Modified Release Gastroretentive Floating Extrudates Towards Improved Bioavailability and Minimized Side Effects of Baclofen

Ist Teil von

• Journal of pharmaceutical sciences, 2021-03, Vol.110 (3), p.1227-1239

Ort / Verlag

United States: Elsevier Inc

Erscheinungsjahr

2021

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• Baclofen immediate release mode of administration exhibit sharp plasma peaking that results in the emergence of side effects like hypotension. This research employs preformulation studies to design an optimum dosage form for baclofen to enhance therapeutic outcomes. These studies include partition coefficient and ex-vivo permeation studies. Partition coefficient was found to be 1.27 at pH 7.4. Permeation studies confirmed the presence of specialized transport mechanism through the GIT. It was concluded that an ideal formulation of baclofen should provide slow-release of the drug to avoid sharp peaking. Modified-release floating extrudates of baclofen were prepared using Carbopol 934 and HPMC with different gas-forming agents. Different release-retarding materials (Eudragit L100, Eudragit RS100 and Cetyl alcohol) were used as ingredients in the binder solutions. The prepared extrudates were assessed for their drug content, floating ability, friability properties and in vitro release properties. The prepared extrudates recorded buoyance characteristics for 24 h with a floating lag time varying from 0 to 73.34 s. The optimized extrudates manifested extended baclofen release for up to 8 h compared to 0.2 h for marketed baclofen tablets. This approach was found efficient to provide greater bioavailability and minimize hypotension associated with commercial baclofen tablets.