Controlled release floating multiparticulates of metoprolol succinate by hot melt extrusion

Malode, Vilas N.; Paradkar, Anant; Devarajan, Padma V.

doi:10.1016/j.ijpharm.2015.06.045

Cited by 15 publications

(8 citation statements)

References 47 publications

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“…allowing to cool to room temperature (Bhalekar et al, 2009). There have been similar investigations reported in the literature on lipid crystallization behavior (Malode et al, 2015; Windbergs et al, 2009).…”

Section: Resultssupporting

confidence: 85%

Effect of formulation and process variables on lipid based sustained release tablets via continuous twin screw granulation: A comparative study

Kallakunta

Tiwari

Sarabu

et al. 2018

European Journal of Pharmaceutical Sciences

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The current study's aim is to prepare lipid based sustained release tablets via a twin-screw granulation technique and compare those dosage forms with conventional techniques, namely wet granulation and direct compression. The granules were successfully manufactured in a single-step, continuous twin-screw granulation process with a low proportion of binder (Klucel™ EF, HPC SSL) using Compritol® 888 ATO, Precirol® ATO 5 and Geleol™ as sustained release agents. The granules prepared showed good flow characteristics and compaction properties. DSC and XRD studies were conducted to characterize the granules prepared via a twin-screw granulation method and the results demonstrated the crystalline nature of lipids within the granules. FTIR data indicated that there were no interactions with the formulation components investigated. The formulations developed by all three methods were compressed into tablets with a mechanical strength of 14-16 KP. The tablets formulated were characterized for physicochemical properties, in vitro drug release studies, water uptake and erosion studies. These results showed that the drug was not completely released after 24 h for tablets developed by the wet granulation process using all three lipids. The tablets prepared by the direct compression method demonstrated a burst release within 8 to 10 h from Precirol ATO 5® and Geleol™ formulations compared to Compritol® 888 ATO. However, tablets prepared using twin-screw granulation exhibited sustained release of the drug over 24 h and the water uptake and erosion results were in accordance with dissolution data. Stability data for 45 days at accelerated conditions (40 °C/75% RH) showed similar release profiles with ƒ2 values above 50 for all of the twin screw granulation formulations, indicating the suitability of the process for formulating sustained release tablets. These findings of a single-step, continuous twin-screw granulation process are novel and demonstrate new opportunities for development of sustained release tablets.

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Section: Resultssupporting

confidence: 85%

Effect of formulation and process variables on lipid based sustained release tablets via continuous twin screw granulation: A comparative study

Kallakunta

Tiwari

Sarabu

et al. 2018

European Journal of Pharmaceutical Sciences

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“…The structure of the pellets allowed immediate flotation in0.1 N HClduring12-24 hour periods and also theophylline delivery in prolonged fashion (Vo et al, 2015). Malode et al(2015), designed multiple-unit floating delivery system containing metoprolol succinate as model drug incombination withthree different polymers (Eudragit RS PO, polyethylene oxide -PEO WSR 303 and HPMC K100M) and sodium bicarbonate as in situ gas generator. Units based solelyon Eudragit RS PO did not float, even though sodium bicarbonate was present.…”

Section: Targeted Oral Dosage Formsmentioning

confidence: 99%

“…Introducing HPMC in the system in amounts of 15% maintained the short floating lag time but also significantly increased the total floating time up to 12h while delivering the API in continuous manner by zero order kinetics. The optimal formulation was unaffected by storage conditions with regard to floating properties and drug delivery (Malode et al, 2015).…”

Section: Targeted Oral Dosage Formsmentioning

confidence: 99%

Hot-melt extrusion and prilling as contemporary and promising techniques in the solvent free production of solid oral dosage forms, based on solid dispersions

Aleksovski¹,

Vervaet²,

Dreu³

2016

Maced. Pharm. Bull.

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Hot melt extrusion and prilling are gaining importance as solvent free and continuous techniques in the production of solid oral dosage forms with added value, by incorporating active compound in a molten carrier which is further solidified to form solid dispersion. This article reviews these two techniques in terms of understanding process basics, equipment characteristics, required properties of processed materials and application of the processes for development of solid oral dosage forms. Studies revealed that both hot-melt extrusion and prilling are regarded as simple, robust and continuous methods for processing different types of materials and production of solid dosage forms based on solid matrices. However, understanding of their concepts and requirements together with careful material selection is crucial for stable material processing and obtaining stable products of high-quality. Hot-melt extrusion proved to be a suitable method for production of modified release dosage forms, taste masked dosage forms and dosage forms offering improved drug dissolution rate and solubility. Prilling till now has been successfully applied just in the production of multiple unit drug delivery systems for immediate and sustained drug delivery. Further studies on product development and process understanding are required for full implementation of prilling in the pharmaceutical field.

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“…Controlled-release (Almeida et al, 2011;Grassi et al, 2003;Phaechamud, Thongpin, Choncheewa, 2012;Sharma, Amin, 2013;Tran et al, 2011;Verhoeven, Vervaet, Remon, 2006);  Gastro-retentive/floating systems (Malode, Paradkar, Devarajan, 2015);  High drug loading in immediate-release systems (Cai et al, 2013);  Combination of different delivery systems (Dierickx et al, 2012;Dierickx, Remon, Vervaet, 2013);  Obtention of immediate-release systems, with a focus on masking drug flavor (Gryczke et al, 2011;Issa et al, 2012b);  Improvement in dissolution of poorly soluble drugs (Deng et al, 2012;Kalidova, Fischbach, Kleinebudde, 2012 Controlled-release (Aleksovski et al, 2015;Lopes et al, 2006;Tomuta, Leucuta, 2007);  Combination of different delivery systems (Souza, Goebel, Andreazza, 2013);  Colonic release (Vemula, 2015);  Ocular bio-adhesives (Bozdag et al, 2010;Weyenberg et al, 2003;Weyenberg et al, 2006);  Gastro-retentive/floating systems (Goole et al, 2008;Hauptstein et al, 2013;Katakam et al, 2014);  Obtention of immediate-release systems, with a focus on masking drug flavor (Eckert, Pein, Breitkreutz, 2014);…”

mentioning

confidence: 99%

Physical characterization of multiparticulate systems

Issa

Souza

Duque

et al. 2018

Braz. J. Pharm. Sci.

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The search for new pharmaceutical dosage forms and different drug delivery systems already used in therapeutics is a global trend, serving as an opportunity to expand the portfolio for the pharmaceutical industry. In this context, multiparticulate systems, such as pellets, granules, and minitablets, represent an attractive alternative, given the range of possibilities they provide. Among the methods used in the production of these systems, we highlight the process of extrusion-spheronization for pellet manufacture, wet granulation and hot-melt extrusion for the obtention of granules, and direct compression for minitablets. Although highly versatile, depending on the technology chosen, many processes and formulation variables can influence the ensuing stages of manufacture, as well as the final product. Therefore, the characterization of these small units is of fundamental importance for achieving batch homogeneity and optimal product performance. Analyses, including particle size distribution, morphology, density, porosity, mechanical strength and disintegration, are example tests used in this characterization. The objective of this review was to address the most widely used tests for the physical evaluation of multiparticulate systems.

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Controlled release floating multiparticulates of metoprolol succinate by hot melt extrusion

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Cited by 15 publications

References 47 publications

Effect of formulation and process variables on lipid based sustained release tablets via continuous twin screw granulation: A comparative study

Effect of formulation and process variables on lipid based sustained release tablets via continuous twin screw granulation: A comparative study

Hot-melt extrusion and prilling as contemporary and promising techniques in the solvent free production of solid oral dosage forms, based on solid dispersions

Physical characterization of multiparticulate systems

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