Solid-state plasticization of an acrylic polymer with chlorpheniramine maleate and triethyl citrate

Zhu, Y.; Shah, Navnit; Malick, A. Waseem; Infeld, M. H.; McGinity, James W.

doi:10.1016/s0378-5173(02)00244-2

Cited by 82 publications

(33 citation statements)

References 23 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Homogenous polymer plasticizer blends undergo a second-order like phase transition at this temperature [19], passing from the rubbery to a glassy state with T g decreasing with increasing plasticizer concentrations [20,21]. Throughout the literature several approaches to determine the glass transition temperature of polymers via computer simulations are reported based on the change of various physical properties at T g .…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Molecular dynamics simulations for drug dosage form development: thermal and solubility characteristics for hot-melt extrusion

Maus

Wagner

Kornherr³

et al. 2008

Molecular Simulation

View full text Add to dashboard Cite

Section: Introductionmentioning

confidence: 99%

“…Employing Eudragit ® RS as a thermal polymer which is known to form multiple unit controlled release matrix particles [20,[34][35][36] the purpose in respect of question two was to distinguish a system of low solubility for the drug compound.…”

mentioning

confidence: 99%

Molecular dynamics simulations for drug dosage form development: thermal and solubility characteristics for hot-melt extrusion

Maus

Wagner

Kornherr³

et al. 2008

Molecular Simulation

View full text Add to dashboard Cite

“…The selected plasticizers were widely used to enhance properties of coating film in coating process. [36][37][38] The hydrophilicity of plasticizers could affect the dissolution rate of drug, so plasticizers were screened in accordance with the solubility in water. The hydrophilicity of plasticizers in water is increased in the sequence of castor oil, TEC, and PEG 6000.…”

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

View full text Add to dashboard Cite

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...

show abstract

“…The polymer toughness and flexibility is improved and lower thermal processing temperatures can be employed. (Zhu et al, 2002).…”

Section: Pharmaceutically Used Plasticizersmentioning

confidence: 99%

Pharmaceutically Used Plasticizers

Snejdrova¹,

Dittrich²

2012

Recent Advances in Plasticizers

View full text Add to dashboard Cite

Solid-state plasticization of an acrylic polymer with chlorpheniramine maleate and triethyl citrate

Cited by 82 publications

References 23 publications

Molecular dynamics simulations for drug dosage form development: thermal and solubility characteristics for hot-melt extrusion

Molecular dynamics simulations for drug dosage form development: thermal and solubility characteristics for hot-melt extrusion

Preparation and Evaluation of Sustained-Release Doxazosin Mesylate Pellets

Pharmaceutically Used Plasticizers

Contact Info

Product

Resources

About