Influence of plasticizers on the mechanical properties of pellets containing Eudragit® RS 30 D

Wang, Chen-Chao; Zhang, Guohua; Shah, Navnit; Infeld, M. H.; Malick, A. Waseem; McGinity, James W.

doi:10.1016/s0378-5173(97)00080-x

Cited by 49 publications

(13 citation statements)

References 19 publications

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“…1/2 , respectively. 20,30) The plasticization of Eudragit by ibuprofen is related to their miscibility at 50°C. 2) Therefore, heat-treating of Eudragit RL containing tablets at 50°C showed decreased drug release, which can be related to the plasticizing effect of ibuprofen on Eudragit polymer.…”

Section: Resultsmentioning

confidence: 99%

Thermal Treating of Acrylic Matrices as a Tool for Controlling Drug Release

Hasanzadeh

Ghaffari

Monajjemzadeh

et al. 2009

CHEMICAL & PHARMACEUTICAL BULLETIN

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The purpose of the present study was to investigate the effect of thermal-treating on the release of ibuprofen from the granules prepared using aqueous dispersions of Eudragit. To accomplish this goal, different formulations were prepared using wet granulation method containing two different types of Eudragit aqueous dispersions, RS30D, RL30D and Avicel as filler. Tablets were prepared using direct compression method. The prepared tablets were thermally treated at 50 and 70°C for 24 h. The drug release from tablets was assessed before and after thermal-treating. The results of release study showed that, thermally-treating the tablets at the temperatures higher than glass transition temperature (Tg) of the polymer can decrease the drug release from matrices. For mechanistic evaluation of the effect of thermal-treating, powder X-ray diffraction (XPD), scanning electron microscopy (SEM), differential scanning calorimeter (DSC), Fourier transform infrared (FT-IR) and helium pycnometer have been employed. The SEM graphs showed that the tablets have smoother surface with less porosity after thermal-treating. FT-IR spectra showed no change in the spectrum of thermally-treated tablet compared to control. In DSC graphs, no crystalline change was seen in the heat-treated samples of ibuprofen tablets, but decreased and widened peak size were related to the probable formation of solid solution of ibuprofen in Eudragit matrix. The results of helium pycnometer showed a significant decrease in the total porosity of some heat-treated samples. This study revealed the importance of thermal treating on the drug release from sustained release tablets containing Eudragit polymer.

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Section: Resultsmentioning

confidence: 99%

Thermal Treating of Acrylic Matrices as a Tool for Controlling Drug Release

Hasanzadeh

Ghaffari

Monajjemzadeh

et al. 2009

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…In order to ensure the adhesion of the enteric coating polymer dispersion, the amount of plasticizer (TEC) was adjusted to manufacturer recommended specifications for enteric coatings (Table 1). Because pharmaceutical acrylic polymers are brittle, fragile and exhibit strong adhesiveness [52], the addition of plasticizers and glidants, such as talc (Table 1), ensures the favorable elasticity of the coatings by decreasing polymer tensile strength [52,53], lowering the film forming temperature without adverse mechanical effects [54][55][56][57][58], and facilitating GI transit through mucosal surfaces by avoiding polymer dispersion agglomeration.…”

Section: Discussionmentioning

confidence: 99%

Oral immunization of rhesus macaques with adenoviral HIV vaccines using enteric-coated capsules

Mercier

Nehete

Passeri

et al. 2007

Vaccine

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Targeted delivery of vaccine candidates to the gastrointestinal (GI) tract holds potential for mucosal immunization, particularly against mucosal pathogens like the human immunodeficiency virus (HIV). Among the different strategies for achieving targeted release in the GI tract, namely the small intestine, pH sensitive enteric coating polymers have been shown to protect solid oral dosage forms from the harsh digestive environment of the stomach and dissolve relatively rapidly in the small intestine by taking advantage of the luminal pH gradient. We developed an enteric polymethacrylate formulation for coating hydroxy-propyl-methyl-cellulose (HPMC) capsules containing lyophilized Adenoviral type 5 (Ad5) vectors expressing HIV-1 gag and a string of six highly-conserved HIV-1 envelope peptides representing broadly cross-reactive CD4 + and CD8 + T cell epitopes. Oral immunization of rhesus macaques with these capsules primed antigen-specific mucosal and systemic immune responses and subsequent intranasal delivery of the envelope peptide cocktail using a mutant cholera toxin adjuvant boosted cellular immune responses including, antigen-specific intracellular IFN-γ-producing CD4 + and CD8 + effector memory T cells in the intestine. These results suggest that the combination of oral adenoviral vector priming followed by intranasal protein/peptide boosting may be an effective mucosal HIV vaccination strategy for targeting viral antigens to the GI tract and priming systemic and mucosal immunity.

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“…These solubility parameters can be predicted using group contributions derived from the structures of the two materials. 38 Accordingly the overall value of solubility parameters (δt) for ibuprofen and Eudragit RS PO were calculated based on the group contributions of their structural components; these values were found equal to 19 40 Wang et al 41 for Eudragit RS PO. Therefore a good miscibility between these two components is predicted, as the difference (1.81 (J/cm…”

Section: Theoretical Assessment Of the Miscibility Of Ibuprofeneudragmentioning

confidence: 99%

An Investigation into the Relationship between Predicted Drug Miscibility and Product Stability for Hot Melt Extruded Systems: Ibuprofen Dispersions in Eudragit RS PO

Albarahmieh

Craig

2015

MOJBB

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This study explores the relationship between theoretical and experimental prediction of hot melt extrudate miscibility and subsequent performance on storage using a relevant model system. More specifically, an investigation was conducted into the miscibility and separation of ibuprofen within hot melt extruded matrices of Eudragit RS PO intended for transdermal delivery. Theoretical miscibility was assessed via melting point depression and solubility parameter calculation, while experimental values were obtained using thermal, imaging and spectroscopic analysis. The addition of ibuprofen was found to assist processing in terms of reducing torque via plasticization effects. The incorporation of ibuprofen in the polymeric matrices was assessed as a function of time, both in the dry state and on exposure to ambient relative humidity. A good correlation was found between the theoretical and practical estimates of solubility, with high drug loadings (30-35% w/w) achieved which remained stable over a month at low humidity storage, despite the low Tg of the systems. The stability was reduced for systems stored at 60% RH/25°C despite the water uptake being relatively low, indicating a marked dependence of miscibility on water content. Fragility calculations were also performed on the mixed systems, indicating high strength and stability. Overall, the study has demonstrated that ibuprofen incorporation in Eudragit RS PO may be estimated both theoretically and practically, with stable systems noted when stored under dry conditions. Keywords: extrusion, solid dispersion, amorphous, solubility, polymeric drug delivery system, physical characterization, mathematical model, physical stability MOJ Bioequivalence & Bioavailability Research ArticleOpen Access An investigation into the relationship between predicted drug miscibility and product stability for hot melt extruded systems: ibuprofen dispersions in Eudragit RS PO 29Copyright: ©2015 Albarahmieh et al. Citation: Albarahmieh E, Sheng Q, Craig DQM. An investigation into the relationship between predicted drug miscibility and product stability for hot melt extruded systems: ibuprofen dispersions in Eudragit RS PO. MOJ Bioequiv Availab. 2015;1(2):28-37. DOI: 10.15406/mojbb.2015.01.00008 stability of the product, particularly in terms of miscibility. These two considerations may be mutually dependent as the drug may plasticize the polymer matrix, thereby aiding processing, but by the same token the robust conditions used may lead to an inflated incorporation ratio, resulting in later phase separation. 30 Furthermore, characterisation of drug solubility within a Transdermal drug delivery system (TDDS) is crucial for performance prediction, since flux is a function of activity, which may in turn be determined by equilibrium solubility within the matrix. 31,32 Overall, therefore, effective prediction and characterisation of incorporation and associated stability is essential for effective product development.Our hypothesis is that theoretical and practical approaches wi...

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Influence of plasticizers on the mechanical properties of pellets containing Eudragit® RS 30 D

Cited by 49 publications

References 19 publications

Thermal Treating of Acrylic Matrices as a Tool for Controlling Drug Release

Thermal Treating of Acrylic Matrices as a Tool for Controlling Drug Release

Oral immunization of rhesus macaques with adenoviral HIV vaccines using enteric-coated capsules

An Investigation into the Relationship between Predicted Drug Miscibility and Product Stability for Hot Melt Extruded Systems: Ibuprofen Dispersions in Eudragit RS PO

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