Pharmacokinetic Parameters Determination and In Vitro–In Vivo Correlation of Ileocolonic-Targeted pH-Responsive Coated Mini-Tablets of Naproxen

Hadi, Mohd Abdul; Rao, N. G. Raghavendra; Rao, A. Srinivasa

doi:10.3797/scipharm.1503-16

Cited by 6 publications

(3 citation statements)

References 11 publications

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“…One-way ANOVA at a confidence interval of 95% was performed on results obtained from experimental work. Differences were statistically significant if p < 0.05 [ 56 ]. Trials were conducted at n = 6, and their mean ± SD was recorded.…”

Section: Methodsmentioning

confidence: 99%

The Development of Eletriptan Hydrobromide Immediate Release Buccal Films Using Central Composite Rotatable Design: An In Vivo and In Vitro Approach

et al. 2022

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The objective is to develop immediate release buccal films of Eletriptan Hydrobromide (EHBR) using hydroxypropyl methylcellulose (HPMC) E5. The buccal films have the ability to disintegrate rapidly and provide both systemic and local effects. The solvent casting method was employed to prepare the films and the central composite rotatable design (CCRD) model was used for film optimization. All the formulated films were characterized for physicochemical evaluation (Fourier transform infrared spectroscopy (FTIR), X-ray Diffraction (XRD), differential scanning calorimetry (DSC), and Scanning electron microscopy (SEM), in in-vitro, ex-vivo, and in-vivo drug release. The fabricated films were transparent, colorless, and evenly distributed. The FTIR spectra showed no chemical interaction between the drug and excipients. In in-vitro analysis, the film has the highest% drug release (102.61 ± 1.13), while a maximum of 92.87 ± 0.87% drug was diffused across the cellulose membrane having a pore size of 0.45 µm. In the ex-vivo study, drug diffusion across the goat mucosa was performed and 80.9% of the drug was released in 30 min. In-vivo results depict a mean half-life (t½) of 4.54 ± 0.18 h and a Cmax of 128 ± 0.87 (ng/mL); Tmax was achieved in 1 h. Furthermore, instability and histopathological studies buccal films were proven to be safe and act as an effective dosage form. In a nutshell, optimized and safe instant release EHBR buccal films were prepared that have the tendency to provide effect effectively.

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Section: Methodsmentioning

confidence: 99%

The Development of Eletriptan Hydrobromide Immediate Release Buccal Films Using Central Composite Rotatable Design: An In Vivo and In Vitro Approach

et al. 2022

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“…This current study evaluated the in vivo pharmacokinetic parameters [19] and compared the satranidazole from multiunit pellets with raw drugs in a randomized, twoway crossover design. The result obtained was to target the satranidazole drug in the colonic region.…”

Section: In Vivo Study 251 In Vivo Drug Availability Studymentioning

confidence: 99%

Satranidazole-loaded chitosan/locust bean gum/xanthan gum polysaccharide composite multiunit pellets for colon targeting: in vitro–in vivo investigation

Mazumder

Mahanti

Majumdar³

et al. 2022

Beni-Suef Univ J Basic Appl Sci

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Background The colon has a significant site to deliver numerous active materials for colonic diseases. Highly biodegradable polymers hold significant promise among the several techniques available to deliver the drug to the colon. This research aimed to prepare chitosan, locust bean gum and xanthan gum polysaccharide composite satranidazole multiunit pellets for colonic release and assesses the bioavailability with pharmacokinetic parameters after administration of satranidazole raw drug compared to multiunit pellets. Satranidazole multiple unit pellets were prepared based on chitosan, locust bean gum and xanthan gum, which were inexpensive and harmless. The bioavailability study was done by crossover design in which satranidazole raw drug and test formulation was administered to six healthy white albino rats. Results The pharmacokinetic analyses were estimated using the deconvolution of the plasma profile. Compared to the satranidazole drug used as a reference, for the pellets, the maximum plasma concentration was lower (35.02 ± 3.91 ng/ml vs. 51.07 ± 1.21 ng/ml for the satranidazole drug), and the time to attain maximum concentration was 2.50 ± 0.55 h for both drugs and test formulation. Colonic drug content was significantly higher than that of free administered drug. Conclusion The results indicate the acquired pharmacokinetic studies and colonic analysis established the reliability of the pharmaceutical technique and the ability to release satranidazole at the colonic site. Graphical Abstract

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“…Recently, Hadi et al (2014Hadi et al ( , 2015Hadi et al ( , 2016) developed a novel pH-responsive coated mini-tablet filled capsule of naproxen for ileocolonic targeted drug delivery. These optimized minitablets were prepared by the direct compression method and were then coated with a 1:2 ratio of Eudragit L100 and Eudragit S100, respectively, with 20% coating level.…”

Section: Mini-tabletsmentioning

confidence: 99%

pH-Responsive carriers for oral drug delivery: challenges and opportunities of current platforms

et al. 2017

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PR China AbstractOral administration is a desirable alternative of parenteral administration due to the convenience and increased compliance to patients, especially for chronic diseases that require frequent administration. The oral drug delivery is a dynamic research field despite the numerous challenges limiting their effective delivery, such as enzyme degradation, hydrolysis and low permeability of intestinal epithelium in the gastrointestinal (GI) tract. pH-Responsive carriers offer excellent potential as oral therapeutic systems due to enhancing the stability of drug delivery in stomach and achieving controlled release in intestines. This review provides a wide perspective on current status of pH-responsive oral drug delivery systems prepared mainly with organic polymers or inorganic materials, including the strategies used to overcome GI barriers, the challenges in their development and future prospects, with focus on technology trends to improve the bioavailability of orally delivered drugs, the mechanisms of drug release from pH-responsive oral formulations, and their application for drug delivery, such as protein and peptide therapeutics, vaccination, inflammatory bowel disease (IBD) and bacterial infections.

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Pharmacokinetic Parameters Determination and In Vitro–In Vivo Correlation of Ileocolonic-Targeted pH-Responsive Coated Mini-Tablets of Naproxen

Cited by 6 publications

References 11 publications

The Development of Eletriptan Hydrobromide Immediate Release Buccal Films Using Central Composite Rotatable Design: An In Vivo and In Vitro Approach

The Development of Eletriptan Hydrobromide Immediate Release Buccal Films Using Central Composite Rotatable Design: An In Vivo and In Vitro Approach

Satranidazole-loaded chitosan/locust bean gum/xanthan gum polysaccharide composite multiunit pellets for colon targeting: in vitro–in vivo investigation

pH-Responsive carriers for oral drug delivery: challenges and opportunities of current platforms

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