Formulation and optimization of enteric coated bilayer tablets of mesalamine by RSM: In vitro – In vivo investigations and roentogenographic study

Parmar, Chintan; Parikh, Kinjal; Mundada, Piyush K; Bhavsar, Dhaval; Sawant, Krutika

doi:10.1016/j.jddst.2018.01.008

Cited by 17 publications

(3 citation statements)

References 30 publications

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“…The rabbit was placed in a prone position for the imaging process. The X-ray images were taken at the time interval of 1, 2, 3,4,5,7, and 8 h. (Parmar, Parikh, Mundada, Bhavsar, & Sawant, 2018;Singh & Pathak, 2015).…”

Section: In Vivo Roentgenographic Studymentioning

confidence: 99%

Preparation, Optimization, and Evaluation of Pellets Containing Mesalamine With Natural Gums For Colon Drug Delivery System

PATHAN¹,

Siddiqui²

2022

Fabad Journal of Pharmaceutical Sciences

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The purpose of the present work was to formulate colon-targeted mesalamine pellets containing gums of Moringa oleifera Lam. (MOG) and Cyamopsis tetragonolobus Taub. (CTG). Formulation of single stimuli mediated release is also difficult to target colon due to variation in the physiological condition, so in present work, pHdependent and enzyme degradation mechanisms are being used to release of drug at the colonic site. Extrusion and spheronization techniques were used for the preparation of pellets. For formulation optimization, factorial design study 32 was used for the selection of the optimized batch. It was found that high ratio of solvent 80:20 and 10% and 7.5% concentration of MOG and CTG respectively produce optimized pellets showed good physical properties and release for F8M and F8C and after coating it showed in vitro release at the colonic condition and in vivo roentgenographic images for targeting. As to say as advantages, spheronization and extrusion method was proved to have economized, whereas natural gums used to control release which added advantage as being as inert and biocompatible. This further formulation scope at industrial scales to reduce side effects of synthetic polymer and make it more biocompatible with the body.

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Section: In Vivo Roentgenographic Studymentioning

confidence: 99%

Preparation, Optimization, and Evaluation of Pellets Containing Mesalamine With Natural Gums For Colon Drug Delivery System

PATHAN¹,

Siddiqui²

2022

Fabad Journal of Pharmaceutical Sciences

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“…Finally, the plug ejects and permits the formulation delivery to the colon, where the drug release is further controlled up to 24 hours by the pH-responsive coat. Parmar et al [29] formulated an enteric coated bilayer (immediate and sustained release layers) tablets of mesalamine using HPMC K4M and HPMC K15M polymers for the sustained release layer. The optimized formulation was coated for different times (20, 40 and 60 min) using Eudragit S-100.…”

Section: Main Text Time Dependent and Ph Responsive Approachesmentioning

confidence: 99%

Recent advances in mesalamine colonic delivery systems

Bayan

2020

Futur J Pharm Sci

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Background: Increased attention has been focused on the continuous development and improvement of mesalamine colonic specific delivery systems, for the effective treatment of inflammatory bowel diseases; thus enhancing therapeutic efficacy and reducing potential side effects. Mesalamine is a class IV drug, according to the Biopharmaceutics Classification System, used usually to treat inflammation associated with colon related diseases such as Crohn's disease and ulcerative colitis. Main text An ideal colon targeting system aims to deliver a therapeutic agent, selectively and effectively, to the colon. This system should ideally retain the drug release in the upper GI tract (stomach and small intestine); while trigger the drug release in the colon. Several approaches have been used to fabricate formulations to achieve a colon specific delivery of mesalamine such as; time dependent, pH responsive, enzymatic/microbial responsive and ultrasound mediated approaches. This overview outlines the recent advances in mesalamine-colon delivery approaches for the potential treatment of ulcerative colitis and Crohn' disease. Conclusion: A combined pH-time dependent delivery system can improve mesalamine colonic drug delivery via employing carriers capable of retarding mesalamine release in the stomach and delivering it at predetermined time points after entering the intestine. The existence of specific enzymes, produced by various anaerobic bacteria present in the colon advocates the advantage of designing enzyme sensitive systems and combining it with pHtime dependent system to improve mesalamine colonic delivery. The use of ultrasound has shown promises to effectively treat inflammatory bowel diseases.

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“…The blood was immediately centrifuged using cooling centrifuge (C-24, Remi Equipment's Pvt. Ltd., Mumbai, India) at 4000 rpm for 10 min at 4° [ 20] . The serum was separated and stored at -72° until analysis by high performance liquid chromatography (HPLC) method.…”

Section: Study Protocolmentioning

confidence: 99%

Design and Optimization of Controlled Release Felbamate Tablets by D-optimal Mixture Design: In vitro-in vivo Evaluation

Parikh¹,

Mundada²,

Sawant³

2019

pharmaceutical-sciences

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For long-term treatment, conventional drug formulations are required to be administered in multiple doses, which have several disadvantages [1]. Design of controlled release (CR) formulations that release drug over an extended period of time is desirable in chronic disease conditions. CR formulations offer many advantages such as low dose, reduced or no fluctuation of drug concentration in the blood, minimal side effects, improved patient compliance and cost effectiveness [2,3]. Matrix technologies have proven to be popular among oral controlled drug delivery technologies because of their ease of manufacturing and simplicity of formulation, high degree of reproducibility, stability of the excipients and dosage form, and ease of technology transfer during scale-up and process validation [4]. Hydrophilic matrix systems are widely used for providing CR from solid oral dosage forms. Hydroxypropyl methylcellulose (HPMC), a semisynthetic polymer derived from cellulose, shows minimal interaction problems when used in basic, acidic or other electrolytic systems due to its nonionic nature. HPMC is enzyme resistant, chemically stable over a wide pH range, has consistently high quality and regulatory approval, making it an excellent carrier material for a matrix system [5]. In matrix tablets prepared with HPMC, the polymer quickly hydrates to form a gelatinous layer when it comes in contact with water. As the outer gel layer fully hydrates and dissolves, a newer inner layer forms gel like structure to retard the water influx and control drug diffusion [6]. Hence, in the current investigation, HPMC was used to prepare CR hydrophilic matrix tablets.

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Formulation and optimization of enteric coated bilayer tablets of mesalamine by RSM: In vitro – In vivo investigations and roentogenographic study

Cited by 17 publications

References 30 publications

Preparation, Optimization, and Evaluation of Pellets Containing Mesalamine With Natural Gums For Colon Drug Delivery System

Preparation, Optimization, and Evaluation of Pellets Containing Mesalamine With Natural Gums For Colon Drug Delivery System

Recent advances in mesalamine colonic delivery systems

Design and Optimization of Controlled Release Felbamate Tablets by D-optimal Mixture Design: In vitro-in vivo Evaluation

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