The effect of chemical heterogeneity of HPMC on polymer release from matrix tablets

Viridén, Anna; Wittgren, Bengt; Andersson, Thomas; Larsson, Anette

doi:10.1016/j.ejps.2008.11.003

Cited by 57 publications

(31 citation statements)

References 30 publications

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“…These two steps take place at the whole process of drug release. When water absorption and swelling reach a critical value, the matrices start to dissolve and release the drugs (36). If the water absorption and polymer swelling cooperate very well, ideal drug release kinetics will be obtained.…”

Section: Discussionmentioning

confidence: 99%

Design and Evaluation of Hydrophilic Matrix System Containing Polyethylene Oxides for the Zero-Order Controlled Delivery of Water-Insoluble Drugs

et al. 2016

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Abstract. The aim of this study was to design a polyethylene oxide (PEO) binary hydrophilic matrix controlled system and investigate the most important influence(s) on the in vitro water-insoluble drug release behavior of this controlled system. Direct-compressed PEO binary matrix tablets were obtained from a variety of low viscosity hydrophilic materials as a sustained agent, using anhydrous drugs as a model drug. Water uptake rate, swelling rate, and erosion rate of matrices were investigated for the evaluation of the PEO hydrophilic matrix systems. The effect of the dose, the solubility of water-insoluble drug, and the rheology of polymers on in vitro release were also discussed. Based on the in vitro release kinetics study, three optimized PEO binary matrices were selected for further research. And, these PEO binary matrices had shown the similar release behavior that had been evaluated by the similarity factor f 2 . Further study indicated that they had identical hydration, swelling, and erosion rate. Moreover, rheology study exhibited the similar rheological equation of Herschel-Bulkley and their viscosity was also within the same magnitude. Therefore, viscosity plays the most important role to control drug release compared to other factors in PEO binary matrix system. This research provides fundamental understanding of in vitro drug release of PEO binary hydrophilic matrix tablets and helps pharmaceutical workers to develop a hydrophilic controlled system, which will effectively shorten the process of formulation development by reducing trial-and-error.

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Section: Discussionmentioning

confidence: 99%

Design and Evaluation of Hydrophilic Matrix System Containing Polyethylene Oxides for the Zero-Order Controlled Delivery of Water-Insoluble Drugs

et al. 2016

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“…This was attributed to the heterogeneous nature of the mucous gel producing uneven penetration profiles. Release from HPMC matrices for controlled drug release was found to be sensitive to alterations in the chemical composition and the polymer gel conformation and substantial batch-to-batch variations in release and swelling could be observed for a single type of HPMC [33,34]. The authors suspect that this might be due to aggregate formation in the gel causing transient cross-linking that could perturb diffusion in some places throughout the gel which cannot be predicted.…”

Section: Discussionmentioning

confidence: 83%

Hydroxypropylmethylcellulose gel application delays Der p 1 diffusion in vitro

Diethart

Emberlin²,

Lewis³

2010

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Background: A special hydroxypropylmethylcellulose powder (Nasaleze®) has been used for the alleviation of nasal symptoms of allergic rhinitis since 1994. The efficacy of the product has been recently proven but the mechanism of action was still largely unknown. The aim of the study was to investigate the hypothesis that the gel formed after moisture absorption in the nose might act as mechanical barrier that prevents allergen diffusion towards the nasal epithelium. Methods: The diffusion of Der p 1 through HPMC and agar gels was measured in vitro after 15, 30, 60, 180 and 360 minutes using ELISA. Agar blocks were used to simulate the nasal mucosa. Control samples without gel layer were obtained. Results: The control samples with no applied gel barrier absorbed 72.2 % of the Der p 1 solution after 15 minutes and 100 % after 60 minutes. In comparison, the HPMC and agar gel layers both significantly delayed Der p 1 diffusion. After 15 minutes 0.76 % had diffused through the HPMC gel layer compared to 28.1 % which diffused through the agar layer. After 360 minutes, 14.1 % of the baseline Der p 1 crossed the HPMC gel layer while 100 % had diffused through the agar layer. Conclusions: HPMC gel significantly reduces Der p 1 diffusion in vitro compared to no barrier and an agar gel layer. This is likely to be due to the small mesh size of the polymer network of HPMC and could have important implications for a preventative treatment of allergic rhinitis.

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“…The substituent pattern of HPMC has previously shown to affect the dissolution rate of pure polymer tablets, where the dissolution rate decreased with increased heterogeneity (Viriden et al, 2009a). Polymer tablets of the analysed grade (USP 2208, 100 cps) are normally found to be totally dissolved within 10-30 h dependent on the shear rate applied (Dahl et al, 1990;Körner, 2006;Tajarobi et al, 2009;Viriden et al, 2009a).…”

Section: Resultsmentioning

confidence: 98%

“…Hence, to obtain the desirable gel layer thickness and release rate, both the molecular weight and the degree of substitution must carefully be balanced. However, control of the release rate by a proper selection of grades has not always been achieved, and batch-to-batch variations within grades have been reported (Dahl et al, 1990;Viriden et al, 2009a). This to some extent be explained by the broad specifications for commercial grades, allowing rather large variability in parameters such as the viscosity and the degree of substitution (Pharmacopoeia, 2008;USP29-NF24, 2008).…”

Section: Introductionmentioning

confidence: 96%

“…Another parameter of HPMC that recently was found to be an important characteristic for matrix tablets was the substituent pattern (Viriden et al, 2009a). In that study Viriden et al related the polymer release from pure polymer tablets composed of seven HPMC batches of the same substituent (USP 2208) and viscosity (100 cps) grade, to the chemistry of the HPMC batches.…”

Section: Introductionmentioning

confidence: 98%

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The effect of substitution pattern of HPMC on polymer release from matrix tablets

Viridén

Larsson

Wittgren

2010

International Journal of Pharmaceutics

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The effect of chemical heterogeneity of HPMC on polymer release from matrix tablets

Cited by 57 publications

References 30 publications

Design and Evaluation of Hydrophilic Matrix System Containing Polyethylene Oxides for the Zero-Order Controlled Delivery of Water-Insoluble Drugs

Design and Evaluation of Hydrophilic Matrix System Containing Polyethylene Oxides for the Zero-Order Controlled Delivery of Water-Insoluble Drugs

Hydroxypropylmethylcellulose gel application delays Der p 1 diffusion in vitro

The effect of substitution pattern of HPMC on polymer release from matrix tablets

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