Investigation of critical polymer properties for polymer release and swelling of HPMC matrix tablets

Viridén, Anna; Wittgren, Bengt; Larsson, Anette

doi:10.1016/j.ejps.2008.10.021

Cited by 103 publications

(56 citation statements)

References 39 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…WSRN 301 has a high molecular weight and viscosity to form very strong gel layers, which would decrease the drug release rate (34,35). On the contrary, if the polymer viscosity is reduced, the strength of the gel layer will become weak and the drug release rate will become fast.…”

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

View full text Add to dashboard Cite

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.

show abstract

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

View full text Add to dashboard Cite

show abstract

“…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: 82%

Hydroxypropylmethylcellulose gel application delays Der p 1 diffusion in vitro

Diethart

Emberlin²,

Lewis³

2010

View full text Add to dashboard Cite

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.

show abstract

“…The observed increase in swelling property of the tablet with time can be attributed to the fact that hydrophilic polymer gradually absorbs water due to which the outermost hydrophilic polymer hydrates and swells and forms a gel barrier at the outer surface. As the gelatinous layer progressively dissolves and/or is dispersed, the hydration swelling release process is repeated towards new exposed surfaces, thus maintaining integrity of the dosage form (26,27).…”

Section: Discussionmentioning

confidence: 99%

Development and Optimization of Gastro-Retentive Controlled-Release Tablet of Calcium-Disodium Edentate and its In Vivo Gamma Scintigraphic Evaluation

et al. 2015

View full text Add to dashboard Cite

ABSTRACT. Medical management of heavy metal toxicity, including radioactive ones, is a cause for concern because of their increased use in energy production, healthcare, and mining. Though chelating agents like EDTA and DTPA in parenteral form are available, no suitable oral formulation is there that can trap ingested heavy metal toxicants in the stomach itself, preventing their systemic absorption. The objective of the present study was to develop and optimize gastro-retentive controlled-release tablets of calcium-disodium edentate (Ca-Na 2 EDTA). Gastro-retentive tablet of Ca-Na 2 EDTA was prepared by direct compression method. Thirteen tablet formulations were designed using HPMC-K4M, sodium chloride, and carbopol-934 along with effervescing agents sodium bicarbonate and citric acid. Tablet swelling ability, in vitro buoyancy, and drug dissolution studies were conducted in 0.1 N HCl at 37±0.5°C. Ca-Na 2 EDTA was radiolabeled with technetium-99m for scintigraphy-based in vivo evaluation. Formula F8 (Ca-Na 2 EDTA 200 mg, carbopol 100 mg, avicel 55 mg, citric acid 30 mg, NaHCO 3 70 mg, NaCl 100 mg, and HPMC 95 mg) was found to be optimum in terms of excellent floating properties and sustained drug release. F8 fitted best for KorsmeyerPeppas equation with an R 2 value of 0.993. Gamma scintigraphy in humans showed mean gastric retention period of 6 h. Stability studies carried out in accordance with ICH guidelines and analyzed at time intervals of 0, 1, 2, 4, and 6 months have indicated insignificant difference in tablet hardness, drug content, total floating duration, or matrix integrity of the optimized formulation. Gastro-retentive, controlled-release tablet of CaNa 2 EDTA was successfully developed using effervescent technique as a potential oral antidote for neutralizing ingested heavy metal toxicity.

show abstract

Investigation of critical polymer properties for polymer release and swelling of HPMC matrix tablets

Cited by 103 publications

References 39 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

Development and Optimization of Gastro-Retentive Controlled-Release Tablet of Calcium-Disodium Edentate and its In Vivo Gamma Scintigraphic Evaluation

Contact Info

Product

Resources

About