Effect of Plasticizer on Release Kinetics of Diclofenac Sodium Pellets Coated with Eudragit RS 30 D

Kibria, Golam; Roni, Monzurul Amin; Absar, Mohammad; Jalil, Reza-ul

doi:10.1208/s12249-008-9163-4

Cited by 33 publications

(12 citation statements)

References 10 publications

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“…Bunun kitozan konsantrasyonundaki artışın viskoziteyi arttırmasından ve etkin madde difüzyonunu zorlaştırmasından kaynaklı olduğu düşünülmektedir. 11,12 Kitozanın molekül ağırlığı; polimer-plastifiyan ve polimer-çözücü arası ilişkileri, filmlerin fizikokimyasal özellikleri ve etkin madde salım profilleri üzerine etki etmektedir. 13,14 HMW kitozanda etkin LF1 LF2 LF3 LF4 LF4 LF4 MF1 MF2 MF3 MF4 MF5 MF6 MF7 HF1 HF2 HF3 HF4 Polimer Konsantrasyonu (a/h) 3 3 3 2 2 2 3 3 2 2 1 2 2 2 2 1 1 Plastifiyan Madde Tipi PEG PEG PEG PEG PEG PEG PEG PEG PEG PEG PEG PEG PEG PEG PEG PEG PEG 200 400 600 200 400 600 400 400 400 400madde salımının MMW kitozana göre daha yavaş olduğu gözlenmiştir (Şekil 2 ve 3).…”

Section: Fi̇lmleri̇n Su Absorblama Ve şİşme Yeteneği̇unclassified

“…[11][12]15 Düşük molekül ağırlıklı kitozanın polimer zincirinin daha kısa olması kitozanın TPP ile etkileşimini azaltmakta ve bu da etkin madde salımının daha hızlı olmasına yol açmaktadır.…”

Section: Fi̇lmleri̇n Su Absorblama Ve şİşme Yeteneği̇unclassified

“…Plastifiyan olarak kullanı-lan PEG konsantrasyon ve molekül ağırlığı filmin hidrofil karakteri üzerine etki ederek etkin madde salımını etkilemektedir. 12 Kullanılan PEG miktarı arttırıldığında, daha poröz yapı oluşmakta ve oluşan porların boyutları artmaktadır. 13 PEG hidrofil bir madde olduğundan sulu ortamda çözünen por oluşturur.…”

Section: Plastifiyan Olarak Kullanılan Peg Konsantrasyonunun Ve Molekunclassified

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Investigation of Parameters Affecting the Release of Hydrophobic Active Substance from Chitosan Films

Böncü¹,

Özdemir²

2018

Turkiye Klinikleri J Med Sci

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122itinin asetillenmiş türevi olan kitozan, biyoparçalanır ve biyouyumlu, iyi mekanik özellikleri nedeniyle farmasötik alanda çok ilgi gören doğal bir polisakkarit olup; 1 a) Biyoparçalanır özelliğinden dolayı implant olarak uygulandığında çıkarmak için ikinci bir cerrahi işlem gerektirmemesinden, b) Seyreltik asit çözeltisinde çözünerek formüllerin hazırlanması aşa-masında organik solvan kullanımı gerektirmemesinden, 1 Kitozan Filmlerden Hidrofobik Etkin Madde Salımı Üzerine Etki Eden Parametrelerin İncelenmesi Ö ÖZ ZE ET T A Am ma aç ç: : İbuprofen, analjezik ve antipiretik etkili hidrofobik karakterde bir etkin maddedir. Ça-lışmanın amacı, ibuprofen içeren kontrollü salım yapan kitozan filmler hazırlamak ve hazırlanan filmlerdeki kitozan konsantrasyonu ve molekül ağırlığının, plastifiyan olarak kullanılan polietilen glikol (PEG) konsantrasyonu ve molekül ağırlığının ibuprofenin in vitro salımına etkisini incelemektir. G Ge er re eç ç v ve e Y Yö ön nt te em ml le er r: : Bu amaçla çözücü uçurma yöntemiyle elde edilen filmler, tripolifosfat (TPP) çözeltisinde bekletilerek çapraz bağlanmış ve hazırlanan filmlerden etkin madde salımları statik yön-tem kullanılarak pH 7.2 fosfat tamponu içinde incelenmiştir. Filmlerden etkin madde salımları sıfır derece, Higuchi ve Korsmeyer-Peppas kinetiklerine uyumları yönünden değerlendirilmiştir. B Bu ul l--g gu ul la ar r: : Çalışmada sonuç olarak; hazırlanan filmlerde kitozan konsantrasyonu ve molekül ağırlığındaki artışla etkin madde salım hızları yavaşlamıştır. Plastifiyan olarak kullanılan PEG miktarının artışıyla çalışmada kullanılan oranlarda etkin madde salımında belirgin bir fark görülmezken, PEG molekül ağırlığının artmasıyla ise etkin madde salım hızının arttığı tespit edilmiştir. S So on nu uç ç: : Çalışmada kitozan filmlerden ibuprofenin kontrollü salım yapan preparatlarının hazırlanabileceği görülmüştür.A An na ah ht ta ar r K Ke el li im me el le er r: : Kontrollü salım; kitozan film; çözünme hızı; çözücü uçurma yöntemi A AB BS ST TR RA AC CT T O Ob bj je ec ct ti iv ve e: : Ibuprofen is an hydrophobic active ingredient which is used for analgesic and antipyretic purposes. The aim of the study is to prepare chitosan films containing ibuprofen with controlled release and investigate the effect of concentration and molecular weight of chitosan and polyethyleneglycol (PEG) on the in vitro release of ibuprofen. M Ma at te er ri ia al l a an nd d M Me et th ho od ds s: : For this purpose, the films obtained by solvent evaporation method were cross-linked in a tripolyphosphate (TPP) solution and the in vitro release studies were examined using static method in a medium containing pH 7.2 phosphate buffer. Data obtained from in vitro drug release studies were plotted in various kinetic models: zero order, Higuchi and Korsmeyer-Peppas models. R Re es su ul lt ts s: : As a result of this study, it has been found that the ibuprofen release is decreased by the increase of the chitosan concentration and molecular weight. The in vitro release rate of ibuprofen is decreased w...

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Section: Fi̇lmleri̇n Su Absorblama Ve şİşme Yeteneği̇unclassified

Section: Plastifiyan Olarak Kullanılan Peg Konsantrasyonunun Ve Molekunclassified

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Investigation of Parameters Affecting the Release of Hydrophobic Active Substance from Chitosan Films

Böncü¹,

Özdemir²

2018

Turkiye Klinikleri J Med Sci

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“…The PEG 400 increases drug release as increasing the level from 1% to 3%. These drug release increase may be due to as PEG 400 is hydrophilic agent and solubility enhancing agent 9 .…”

Section: Effect Of Plasticizer On Pellets Roundness and Drug Releasementioning

confidence: 99%

Untitled

2015

IJPSR

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Multiparticulate drug delivery system are mainly oral dosage forms consisting of a multiplicity of small discrete units, each exhibiting some amount desired characteristics such as pellets.The purpose of present study was to prepare sustained release robust matrix pellets of Glipizide. The study revealed successful application of factorial design, optimization of extrusion spheronization process, and sustaining release of Glipizide for formulating uniform, spherical Glipizide pellets. Speed and time of spheronization is critical parameter for optimum sphericity. The Optimum speed and time of operating spheronization is 1350 rpm and 15 min. The results of this study showed that combination of HPMC K100M LVCR as hydrophilic matrix polymer and PEG 400 as potential plasticizer is effective and useful for sustaining the Glipizide release to treat diabetes mellitus. The in-vitro studies showed Q16 at approximately 80% cumulative release in case of F4, F5, F6, It indicates that this system can sustain the release upto 24 h which is desirable for sustained release specificity. Although, the hydrophilic matrix polymer optimization is critical for drug release, this study suggests the promising approach for formulation of sustained release robust matrix pellets of Glipizide.

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“…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

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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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Effect of Plasticizer on Release Kinetics of Diclofenac Sodium Pellets Coated with Eudragit RS 30 D

Cited by 33 publications

References 10 publications

Investigation of Parameters Affecting the Release of Hydrophobic Active Substance from Chitosan Films

Investigation of Parameters Affecting the Release of Hydrophobic Active Substance from Chitosan Films

Untitled

Preparation and Evaluation of Sustained-Release Doxazosin Mesylate Pellets

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