Development and in vivo Evaluation of Gastroretentive Floating Microballoons of Acetohydroxamic Acid for Enhanced Oral Bioavailability |Chapter 4 | Pharmaceutical Science: New Insights and Developments Vol. 10

 

The oral route remains the most preferred and patient-friendly mode of drug administration. Microballoons, a non-effervescent gastroretentive system, are hollow microspheres (<200 µm) composed of polymers or proteins that exhibit excellent buoyancy due to their internal cavity. As multiple-unit systems, they ensure uniform drug distribution, minimise dose dumping, and allow controlled drug release by optimising polymer composition. Acetohydroxamic acid, a urease inhibitor structurally similar to urea, effectively inhibits Helicobacter pylori by penetrating bacterial cells and blocking urease activity, making it suitable for stomach-specific delivery. This study involved the formulation of acetohydroxamic acid floating microballoons, the evaluation of gastric retention by X-ray imaging in rabbits, and bioavailability assessment through pharmacokinetic studies. DSC and FTIR confirmed drug–polymer compatibility. The percentage yield was in the range of 60-90 % for all the formulations. It was found to be less than 70% yield with ethyl cellulose and HPMC K4M, and for the optimised formulation, the yield was around 80 %. The entrapment efficiency was in the range of 60-90 % for all the formulations and was found to be 89.6%for optimized formulation. The percentage buoyancywas in the range of 60-90 % for all the formulations and was found to be 85.5% for optimized formulation. Drug content of all the prepared formulations was found to be within the acceptable range of 90.0 -110.0%. This manuscript is important to the scientific community as it provides a comprehensive and well-validated approach to gastroretentive drug delivery using floating microballoons as a non-effervescent, multiparticulate system. The work offers a reproducible formulation strategy for stomach-specific delivery of urease inhibitors, addressing a critical challenge in the management of Helicobacter pylori infections. Overall, the findings contribute valuable translational insights for the development of advanced oral drug delivery systems with improved clinical efficacy.

 

 

Author(s) Details

Munija Pancheddula
Vision College of Pharmaceutical Sciences & Research, Boduppal, Hyderabad, India.

 

Nemuri Mounika
Vision College of Pharmaceutical Sciences & Research, Boduppal, Hyderabad, India.

 

Upparaboina Srilatha
Vision College of Pharmaceutical Sciences & Research, Boduppal, Hyderabad, India.

 

Shayeda
Department of Pharmaceutics, University College of Pharmaceutical Sciences, Kakatiya University, Warangal-506009, India.

 

Please see the book here :- https://doi.org/10.9734/bpi/psnid/v10/7065

 

Preparation and Assessment of Oral Floating Beads of a NSAID Drug, Tramadol Hydrochloride | Chapter 4 | Pharmaceutical Research: Recent Advances and Trends Vol. 9

Rapid GI transit can prevent complete drug release in the absorption zone and reduce the efficacy of the administered dose since most drugs are absorbed in the stomach or the upper part of the small intestine. Floating bead formulations are designed to stay buoyant in gastric fluids, allowing the drug to be released over an extended period in the stomach. Some common methods for preparing floating beads are- 1. Ionotropic Gelation Method 2. Emulsion Gelation Method 3. Spray-Drying Method 4. Freeze-Drying (Lyophilization) Method 5. Coacervation Method. 6. Emulsion Solvent Evaporation Method 7. Solvent Evaporation Method 8. Extrusion Method 9. Melt dispersion method. In this formulation, Floating beads were fabricated using a modified ionotropic gelation technique using various natural and synthetic polymers in different proportions. The drug used was Tramadol Hydrochloride. Here, the Bonferroni method was applied to the dissolution study to check if there was a significant difference or non-significant difference in the release of drugs in formulated formulations. In the formulated batches BT1 to BT11 did not give in vitro release for 12 hours. In the formulated batch, BT 12 (Sodium alginate 6%: Carbopol 940 1.2 %) shows In vitro release for 12 hours (100.26 ± 0.66%). It also gave floating lag time and floating time immediate, and a floating duration of more than 12 hours. In kinetic model fitting it follows Korsemeyers Peppas equation. Also, it was found stable in 6 months of accelerated stability study. From all the formulation and evaluation studies of oral floating beads of Tramadol Hydrochloride, it was concluded that: Among all different polymer ratios Sodium Alginate 6% and CaCl₂ 3% (2:1 ratio) give formulation of beads. The use of acetic acid in CaCl₂ gives floating of beads for 12 hours. Among different polymers Carbopol 940 gives retarded release for 12 hours. The optimized batch was found to be stable for 6 Months in accelerated stability studies. It was concluded that the use of acetic acid in CaCl₂ gives floating of beads for 12 hours. Moreover, among different polymers, Carbopol 940 gives retarded release for 12 hours and the optimized batch was found to be stable for 6 Months in accelerated stability studies.

 

Author (s) Details

Archana Dinkarrao Kajale
Department of Pharmaceutics, P. Wadhwani College of Pharmacy Yavatmal, 445001, India.

 

Chandewar A. V.
Department of Pharmaceutics, P. Wadhwani College of Pharmacy Yavatmal, 445001, India.

 

Please see the book here:- https://doi.org/10.9734/bpi/prrat/v9/3004