Development of gastroretentive drug delivery system for cefuroxime axetil:<i>In vitro</i>and<i>in vivo</i>evaluation in human volunteers

Bomma, Ramesh; Veerabrahma, Kishan

doi:10.3109/10837450.2012.660698

Cited by 18 publications

(10 citation statements)

References 14 publications

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“…Much more linearity of the IVIVC curve (r=0.996; p<0.001) was observed for the optimized gastroretentive formulation than for the marketed formulation (r=0.698; p<0.01). The results confirmed the prevalence of IVIVC in the prepared gastroretentive formulation, as drug release was able to maintain a linear pace with the in vitro dissolution construing the in vivo drug absorption (16). The latter curve, however, exhibited significantly improved fitting with quadratic model demonstrating the prevalence of nonlinearity (r=0.894; p<0.01).…”

Section: Characterization Of the Floating-bioadhesive Tabletssupporting

confidence: 67%

“…The conventional immediate release (IR) formulation available in the market shows inability to accomplish desired drug release profile owing to poor retentivity in the stomach for extended periods of time. Although literature reports have demonstrated the utility of diverse GR floating formulations of cefuroxime axetil, yet, these systems are not considered to be highly satisfactory for attaining the desired retentivity in the gastric absorption window owing to floatation characteristics only (13)(14)(15)(16)(17)(18). Thus, attempts were made to develop the GR tablets employing dual approach of floatation and bioadhesion for maintaining drug absorption and plasma concentration of the drug for prolonged periods of time and improving the therapeutic efficacy of cefuroxime axetil.…”

Section: Introductionmentioning

confidence: 99%

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QbD-Oriented Development and Characterization of Effervescent Floating-Bioadhesive Tablets of Cefuroxime Axetil

et al. 2015

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ABSTRACT. The objective of the present studies was systematic development of floating-bioadhesive gastroretentive tablets of cefuroxime axetil employing rational blend of hydrophilic polymers for attaining controlled release drug delivery. As per the QbD-based approach, the patient-centric target product profile and quality attributes of tablet were earmarked, and preliminary studies were conducted for screening the suitability of type of polymers, polymer ratio, granulation technique, and granulation time for formulation of tablets. A face-centered cubic design (FCCD) was employed for optimization of the critical material attributes, i.e., concentration of release controlling polymers, PEO 303 and HPMC K100 LV CR, and evaluating in vitro buoyancy, drug release, and ex vivo mucoadhesion strength. The optimized formulation was embarked upon through numerical optimization, which yield excellent floatation characteristic with drug release control (i.e., T 60% >6 h) and bioadhesion strength. Drug-excipient compatibility studies through FTIR and P-XRD revealed the absence of any interaction between the drug and polymers. In vivo evaluation of the gastroretentive characteristics through X-ray imaging and in vivo pharmacokinetic studies in rabbits revealed significant extension in the rate of drug absorption (i.e., T max , K a , and MRT) from the optimized tablet formulation as compared to the marketed formulation. Successful establishment of various levels of in vitro/in vivo correlations (IVIVC) substantiated high degree of prognostic ability of in vitro dissolution conditions in predicting the in vivo performance. In a nutshell, the studies demonstrate successful development of the once-a-day gastroretentive formulations of cefuroxime axetil with controlled drug release profile and improved compliance.

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Section: Characterization Of the Floating-bioadhesive Tabletssupporting

confidence: 67%

Section: Introductionmentioning

confidence: 99%

QbD-Oriented Development and Characterization of Effervescent Floating-Bioadhesive Tablets of Cefuroxime Axetil

et al. 2015

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“…In vivo study confirms burst effect at 4 h in indicating the optimization of the dosage form. Bomma and Veerabrahma [12] investigated the cefuroxime axetil sustained-release floating tablets using polymers like HPMC K4M and polymer combination of HPMC K4M and polyox WSR 303 by effervescent technique. All the formulations could sustain drug release for 12 h. Yang et al [13] proposed asymmetric triple layer tablet for the triple drug treatment (tetracycline, metronidazole, and bismuth salt) of Helicobacter using HPMC and poly (ethylene oxide) as the major rate-controlling polymeric excipients.…”

Section: Introductionmentioning

confidence: 99%

Application of Design of Experiment for Polyox and Xanthan Gum Coated Floating Pulsatile Delivery of Sumatriptan Succinate in Migraine Treatment

Jagdale¹,

Pawar²

2014

BioMed Research International

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Migraine follows circadian rhythm in which headache is more painful at the awakening time. This needs administration of dosage form at night time to release drug after lag period when pain gets worse. Sumatriptan succinate is a drug of choice for migraine. Sumatriptan succinate has bitter taste, low oral bioavailability, and shorter half-life. Present work deals with application of design of experiment for polyox and xanthan gum in development of press coated floating pulsatile tablet. Floating pulsatile concept was applied to increase gastric residence of the dosage form. Burst release was achieved through immediate release tablet using crospovidone as superdisintegrant (10%). Pulse lag time was achieved using swellable polymer polyox WSR 205 and xanthan gum. 32 experimental design was applied. Optimized formulation was evaluated for physical characteristics and in-vitro and in-vivo study. From results, it can be concluded that optimized batch F8 containing polyox WSR205 (72.72%) and xanthan gum (27.27%) of total weight of polymer has shown floating lag time of 55 ± 2 sec, drug content of 100.35 ± 0.4%, hardness of 6 ± 0.1 Kg/cm2, and 98.69 ± 2% drug release in pulse manner with lag time of 7 ± 0.1 h. Optimized batch showed prolong gastric residence which was confirmed by in-vivo X-ray study.

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“…The drug content in each formulation was determined by triturating 20 tablets in a mortar and powder equivalent to 100 mg of cefuroxime axetil was added in 100 mL of simulated gastric fluid (SGF) without enzyme, followed by shaking for 30 min. The sample was filtered, suitably diluted and analyzed by the UV-visible spectroscopy (Patel & Patel, 2006;Bomma & Veerabrahma, 2012) (UV-1800, Shimadzu, Tokyo, Japan).…”

Section: Characterization Of Granules and Minitabletsmentioning

confidence: 99%

Design and characterization of cefuroxime axetil biphasic floating minitablets

et al. 2014

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Biphasic floating minitablets of cefuroxime axetil were prepared by melt granulation technique using two different grades of gelucire namely 50/13 and 43/01 to maintain constant plasma drug concentration. Loading dose of cefuroxime axetil was formulated as immediate release (IR) minitablets by using hydrophilic grade of gelucire 50/13. Maintenance dose was formulated as floating sustained release (SR) minitablets by using hydrophobic grade of gelucire 43/01. The prepared IR and SR granules were subjected to micromeritic studies and scanning electron microscopy. Fourier transform infrared spectroscopy (FT-IR) study revealed that drug and selected carriers were compatible. In vitro dissolution study of optimized IR minitablets showed more than 85% of loading dose dissolved within 30 min. Optimized SR minitablets showed zero lag time with floating duration more than 12 h. The drug release from SR minitablets was linear with square root of time with non-Fickian diffusion-controlled release. The optimized batch of minitablets was filled into 0 size hard gelatin capsule. In vitro dissolution study for capsule showed an immediate burst release followed by SR up to 12 h. There is no significant change in dissolution data after storage at 40 C and 75% RH for three months. Microbiological assay of dissolution samples of optimized minitablets filled in capsules showed proportionate increase in inhibition of growth against Escherichia coli up to 12 h samples. In vivo bioavailability study in albino rabbits showed three times improvement in oral bioavailability.

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Development of gastroretentive drug delivery system for cefuroxime axetil:In vitroandin vivoevaluation in human volunteers

Cited by 18 publications

References 14 publications

QbD-Oriented Development and Characterization of Effervescent Floating-Bioadhesive Tablets of Cefuroxime Axetil

QbD-Oriented Development and Characterization of Effervescent Floating-Bioadhesive Tablets of Cefuroxime Axetil

Application of Design of Experiment for Polyox and Xanthan Gum Coated Floating Pulsatile Delivery of Sumatriptan Succinate in Migraine Treatment

Design and characterization of cefuroxime axetil biphasic floating minitablets

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