Formulation and evaluation of sustained release bioadhesive tablets of ofloxacin using 3²factorial design

Abstract

Background:Oral sustained release gastroretentive dosage forms offer many advantages for drugs having absorption from upper gastrointestinal tract and improve the bioavailability of medications that are characterized by narrow absorption window. The aim of current study was to design sustained release bioadhesive gastroretentive dosage form of ofloxacin.Materials and Methods:A 32 full factorial design was employed to systematically study the drug release profile and bioadhesive strength. Carbopol 934P and HPMC K100M were selected as the independent variables. Compatibility between drug and polymer was tested by fourier transform infrared (FTIR) and X-ray diffraction (XRD) techniques. Tablets were prepared by direct compression and were evaluated for tablet characteristics, swelling study, adhesion strength, percent drug released, radiographic imaging study and stability study. The optimized formulation was then compared with marketed formulation (Oflin OD®).Results:Tablets prepared showed good tablet characteristics, optimum swelling property, and good adhesion strength with high detachment force. Most of the formulations including the optimized formulation followed Higuchi kinetics and the drug release mechanism was found to be anomalous. Radiographic image proved that tablet remains intact in its structural integrity and shape in stomach up to 24 h. The short-term accelerated stability testing was carried out for the optimized formulation, and results revealed that drug content, in-vitro dissolution and all other parameters were within acceptable limits.Conclusion:Thus, the prepared bioadhesive gastroretentive ofloxacin tablet may prove to be a potential candidate which increases the bioavailability of ofloxacin for any intragastric condition.

In Vitro in Vivo Studies on Floating Microspheres for Gastroretentive Drug Delivery System: A Review

“…Radiology or X-ray is another alternative technique where a radio-opaque material with the GRDDS is included. This technique has been noted in the evaluation of gastroretentivity, the rate of disintegration of DFs, and their esophageal transit [81]. To diagnose and monitor the GIT, gastroscopy is another commonly used technique.…”

Gastro-retentive oral drug delivery systems: a promising approach for narrow absorption window drugs

“…Among these drugs with NAW is L-DOPA [24], furosemide [25], baclofen [26], riboflavin [27] and para-aminobenzoic acid [28,29]. The prepared formulations could effectively sustain the release of such drugs but the major drawbacks in these formulations these drugs have NAW; therefore prolonging the drug release cannot be sufficient to improve drug bioavailability as these drugs cannot be absorbed after passing the desired part of the absorption [30,31]. In general, drugs which display NAW difficult to be formulated as immediate release DDS or oral controlled release drug delivery system (CRDDS) because of the preparation of these drugs in the form of immediate release dosage forms require frequent use of a dosage form which did not improve patient compliance in addition to side effects related to the rapid release of those drugs, while sustain drug release could prolong the release time which in such cases shows no benefits because only the drug absorbed in a definite segment along the GIT [32].…”

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“…Gangurde HH et al, reported that the detachment force was increased with the increase in polymer concentration after evaluating the sustained release GRDDS tablets of ofloxacin. This could be due to the availability of more adhesive sites and polymer chains for interpenetration with mucin, resulting consequently in the increase of bioadhesive strength 26 . Recently Kar K et al, also demonstrated the similar results and concluded that hydrophilic polymers are the good candidate for preparation of bioadhesive tablet 27 .…”