The Effects of Plasticizers on the Release of Metoprolol Tartrate from Granules Coated with a Polymethacrylate Film

Okarter, T. U.; Singla, Kavita

doi:10.1081/ddc-100100360

Cited by 28 publications

(11 citation statements)

References 11 publications

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“…The increasing concentration of plasticizers in coating solution generally shows decreased drug release profiles. 35,41) In the present study, similar results were obtained and presented in Fig. 6.…”

Section: Effect Of Coating Agents (Eudragit ® Rl/rs) and Coating Levesupporting

confidence: 80%

“…[32][33][34] The plasticizers were classified into three groups, polyols (polyethylene glycols, propylene glycol), organic esters (triacetin, triethyl citrate, tributyl citrate) and fixed oils (castor oil). 35) Among them, PEG 6000, TEC and castor oil, which represent each group, was selected in the present study. The selected plasticizers were widely used to enhance properties of coating film in coating process.…”

Section: Effect Of Coating Agents (Eudragit ® Rl/rs) and Coating Levementioning

confidence: 99%

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Preparation and Evaluation of Sustained-Release Doxazosin Mesylate Pellets

Kim

et al. 2013

CHEMICAL & PHARMACEUTICAL BULLETIN

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Doxazosin mesylate (DXM) sustained release pellets were prepared by an extrusion-spheronization and fluid-bed coating technique. The core pellets containing DXM were prepared by extrusion-spheronization technique, and coated by a fluid-bed coater to control the release of DXM. The factors affecting to properties of pellets, such as diluent content, type and coating level of coating agents and plasticizers were studied in the present study. Polymethacrylate derivatives (Eudragit ® RS PO and RL PO) were used for coating agents, and polyethylene glycol 6000 (PEG 6000), triethyl citrate (TEC) and castor oil were as plasticizers. To evaluate the properties of prepared pellets, the size of prepared pellets was investigated by sieve analysis technique and the morphology of pellets was evaluated by scanning electron microscopy. Through the dissolution test, factors that have an effect on the dissolution of the drug were evaluated. As the content ratio of microcrystalline cellulose (MCC) had increased, the dissolution was proportionally sustained. Eudragit ® RS PO had more marked sustaining effect on the dissolution rate than Eudragit ® RL PO, and the effect was more pronounced with the increased coating level. PEG 6000 was an appropriate plasticizer for DXM pellets, and increasing the content of PEG 6000, was also slightly decreasing the dissolution rate.Key words sustained release; pellet; extrusion-spheronization; fluid-bed coating; doxazosin mesylate Doxazosin mesylate (DXM) is a selective inhibitor of α 1 -adrenergic receptors and has been demonstrated to be effective for the treatment of hypertension and benign prostatic hyperplasia.1-3) DXM lowers the blood pressure of hypertensive patients by blocking postjunctional α 1 -adrenergic receptors, and then systemic vascular resistance decreases. 4)Taking a DXM can cause first-dose side effects like hypotension because of the rapid increase of drug concentration in the blood.5) Therefore the usual therapy of DXM is initially starting with a low dose (1 mg/d) and gradually increased up to the daily maximum recommended dose (16 mg/d).2) In order to overcome the adverse effects of DXM and to improve inconvenience of the regimen, various studies for controlled-release dosage forms of DXM have been conducted. [6][7][8] Application of the controlled release system to DXM could have benefits such as reducing the adverse effects by minimizing the fluctuation of drug concentration in the plasma. DXM could cause a significant reduction in blood pressure after administration of the first dose, so a formulation of sustained release of DXM could avoid this first dose effect. Among several systems for controlled release of the model drug, multi-unit dosage forms such as pellets or beads coated with polymers used as a release retardant has several advantages. The single unit dosage form like tablets has been widely used because of its simple and cost-effective manufacturing operations and ease of administration. 9,10) In comparison with a single unit dosage form, the multi-unit dosag...

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Section: Effect Of Coating Agents (Eudragit ® Rl/rs) and Coating Levesupporting

confidence: 80%

Section: Effect Of Coating Agents (Eudragit ® Rl/rs) and Coating Levementioning

confidence: 99%

Preparation and Evaluation of Sustained-Release Doxazosin Mesylate Pellets

Kim

et al. 2013

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…[2] This results in polymer chains sliding past each other more easily. As a result, the polymer chains can move around at lower temperatures resulting in decrease in Tg of a polymer [2,13,[21][22][23] Example of plasticizer includes, nitrobenzene, β-naphthyl salicylate, carbon disulphide; [2] glycerine, [24][25][26][27] propylene glycol, [24,[26][27][28] triethyl citrate, [24,[27][28][29] triacetine, [24,27,30] polyethylene glycol, [31] etc. Water or moisture content Increase in moisture content leads to increase in free volume due to formation of hydrogen bonds with polymeric chains increasing the distance between polymeric chains.…”

Section: Plasticizermentioning

confidence: 99%

Glass transition temperature: Basics and application in pharmaceutical sector

Jadhav¹,

Gaikwad²,

Nair³

et al. 2009

Asian J Pharm

137

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“…Optimized pharmacokinetic-pharmacodynamic effects of drugs is a prerequisite for a given extended drug release device to achieve favorable biological response. The drug release profile can be programmed to meet specific requirements by optimizing the composition of formulations, processing parameters such as coating level, drug-polymer ratio and type and amount of polymer-plasticizer utilized (FrohoffHülsmann et al, 1999;Okarter and Singla 2000;Shao et al, 2002). The ideal goal for any drug eluting device is to deliver the therapeutic agent of high efficacy at the right time to the desired location with a concentration high enough over a sufficiently long period.…”

Section: Introductionmentioning

confidence: 99%

Mechanism of controlled release kinetics from medical devices

Raval

Parikh

2010

Braz. J. Chem. Eng.

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-Utilization of biodegradable polymers for controlled drug delivery has gained immense attention in the pharmaceutical and medical device industry to administer various drugs, proteins and other biomolecules both systematically and locally to cure several diseases. The efficacy and toxicity of this local therapeutics depends upon drug release kinetics, which will further decide drug deposition, distribution, and retention at the target site. Drug Eluting Stent (DES) presently possesses clinical importance as an alternative to Coronary Artery Bypass Grafting due to the ease of the procedure and comparable safety and efficacy. Many models have been developed to describe the drug delivery from polymeric carriers based on the different mechanisms which control the release phenomenon from DES. Advanced characterization techniques facilitate an understanding of the complexities behind design and related drug release behavior of drug eluting stents, which aids in the development of improved future drug eluting systems. This review discusses different drug release mechanisms, engineering principles, mathematical models and current trends that are proposed for drug-polymer coated medical devices such as cardiovascular stents and different analytical methods currently utilized to probe diverse characteristics of drug eluting devices.

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The Effects of Plasticizers on the Release of Metoprolol Tartrate from Granules Coated with a Polymethacrylate Film

Cited by 28 publications

References 11 publications

Preparation and Evaluation of Sustained-Release Doxazosin Mesylate Pellets

Preparation and Evaluation of Sustained-Release Doxazosin Mesylate Pellets

Glass transition temperature: Basics and application in pharmaceutical sector

Mechanism of controlled release kinetics from medical devices

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