Overall mechanism behind matrix sustained release (SR) tablets prepared with hydroxypropyl methylcellulose 2910

Tahara, Koichiro; Yamamoto, Kyosuke; Nishihata, Toshiaki

doi:10.1016/0168-3659(95)00021-y

Cited by 175 publications

(91 citation statements)

References 27 publications

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“…The maximum measured dissolution medium uptake occurring over the duration of the experiment was estimated by subtracting the dry weight of the tablet from its wet weight at each time point (Tahara et al, 1995) as in equation 2.…”

Section: Modelling Of Swelling and Erosionmentioning

confidence: 99%

Evaluation of sesamum gum as an excipient in matrix tablets

Nep

Asare-Addo²,

Ngwuluka

et al. 2016

British Journal of Pharmacy

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In developing countries modern medicines are often beyond the affordability of the majority of the population. This is due to the reliance on expensive imported raw materials despite the abundance of natural resources which could provide an equivalent or even an improved function. The aim of this study was to investigate the potential of sesamum gum (SG) extracted from the leaves of Sesamum radiatum (readily cultivated in sub-Saharan Africa) as a matrix former. Directly compressed matrix tablets were prepared from the extract and compared with similar matrices of HPMC (K4M) using theophylline as a model water soluble drug. The compaction, swelling, erosion and drug release from the matrices were studied in deionized water, 0.1 N HCl (pH 1.2) and phosphate buffer (pH 6.8) using USP apparatus II. The data from the swelling, erosion and drug release studies were also fitted into the respective mathematical models. Results showed that the matrices underwent a combination of swelling and erosion, with the swelling action being controlled by the rate of hydration in the medium. SG also controlled the release of theophylline similar to the HPMC and therefore may have use as an alternative excipient in regions where Sesamum radiatum can be easily cultivated.

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Section: Modelling Of Swelling and Erosionmentioning

confidence: 99%

Evaluation of sesamum gum as an excipient in matrix tablets

Nep

Asare-Addo²,

Ngwuluka

et al. 2016

British Journal of Pharmacy

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“…Three methods have been reported for the pretreatment of the samples in SR-μCT experiments: (1) drying in an oven, (2) freeze-drying, and (3) absorbing as much liquid as possible with dry filter paper and storage at room temperature over silica gel. For methods (1) and (3), the matrix gel tablet tended to shrink, and the gel formed on the surface of the tablet core would collapse causing changes to the internal gel structure during the long process. However, the freeze-drying method was found to maintain the microstructure of the hydration layer as much as possible with its rapid cooling process.…”

Section: Samples Pretreatment For the Sr-μct Scanningmentioning

confidence: 99%

“…Among a variety of oral controlled release drug delivery systems, water swellable matrix systems, particularly those containing hydroxypropyl methylcellulose (HPMC), are widely used because of the relative simplicity of formulation compositions, ease of manufacturing, and low cost, as well as acceptance by regulatory authorities and applicability to drugs with a wide range of dose and solubility (1,2).…”

Section: Introductionmentioning

confidence: 99%

Quantification of Swelling and Erosion in the Controlled Release of a Poorly Water-Soluble Drug Using Synchrotron X-ray Computed Microtomography

Yin

Guo

et al. 2013

AAPS J

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Abstract. The hydration layer plays a key role in the controlled drug release of gel-forming matrix tablets. For poorly water-soluble drugs, matrix erosion is considered as the rate limiting step for drug release. However, few investigations have reported on the quantification of the relative importance of swelling and erosion in the release of poorly soluble drugs, and three-dimensional (3D) structures of the hydration layer are poorly understood. Here, we employed synchrotron radiation X-ray computed microtomography with 9-μm resolution to investigate the hydration dynamics and to quantify the relative importance of swelling and erosion on felodipine release by a statistical model. The 3D structures of the hydration layer were revealed by the reconstructed 3D rendering of tablets. Twenty-three structural parameters related to the volume, the surface area (SA), and the specific surface area (SSA) for the hydration layer and the tablet core were calculated. Three dominating parameters, including SA and SSA of the hydration layer (SA hydration layer and SSA hydration layer ) and SA of the glassy core (SA glassy core ), were identified to establish the statistical model. The significance order of independent variables was SA hydration layer > SSA hydration layer > SA glassy core , which quantitatively indicated that the release of felodipine was dominated by a combination of erosion and swelling. The 3D reconstruction and structural parameter calculation methods in our study, which are not available from conventional methods, are efficient tools to quantify the relative importance of swelling and erosion in the controlled release of poorly soluble drugs from a structural point of view.

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“…Natural and semi-synthetic gums or polymers, such as guar gum, xanthan gum, hydroxypropyl methylcellulose, ethylcellulose, hydroxypropylcellulose, and sodium carboxymethylcellulose, are being used as release retarding materials (10)(11)(12). Indeed, hydroxypropylmethylcellulose (HPMC) has received the most attention, likely due to its low toxicity and ease of manufacture (13).…”

Section: Introductionmentioning

confidence: 99%

Guar Gum, Xanthan Gum, and HPMC Can Define Release Mechanisms and Sustain Release of Propranolol Hydrochloride

2010

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Abstract. The objectives were to characterize propranolol hydrochloride-loaded matrix tablets using guar gum, xanthan gum, and hydroxypropylmethylcellulose (HPMC) as rate-retarding polymers. Tablets were prepared by wet granulation using these polymers alone and in combination, and physical properties of the granules and tablets were studied. Drug release was evaluated in simulated gastric and intestinal media. Rugged tablets with appropriate physical properties were obtained. Empirical and semi-empirical models were fit to release data to elucidate release mechanisms. Guar gum alone was unable to control drug release until a 1:3 drug/gum ratio, where the release pattern matched a Higuchi profile. Matrix tablets incorporating HPMC provided near zero-order release over 12 h and erosion was a contributing mechanism. Combinations of HPMC with guar or xanthan gum resulted in a Higuchi release profile, revealing the dominance of the high viscosity gel formed by HPMC. As the single rate-retarding polymer, xanthan gum retarded release over 24 h and the Higuchi model best fit the data. When mixed with guar gum, at 10% or 20% xanthan levels, xanthan gum was unable to control release. However, tablets containing 30% guar gum and 30% xanthan gum behaved as if xanthan gum was the sole rate-retarding gum and drug was released by Fickian diffusion. Release profiles from certain tablets match 12-h literature profiles and the 24-h profile of Inderal ® LA. The results confirm that guar gum, xanthan gum, and HPMC can be used for the successful preparation of sustained release oral propranolol hydrochoride tablets.

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Overall mechanism behind matrix sustained release (SR) tablets prepared with hydroxypropyl methylcellulose 2910

Cited by 175 publications

References 27 publications

Evaluation of sesamum gum as an excipient in matrix tablets

Evaluation of sesamum gum as an excipient in matrix tablets

Quantification of Swelling and Erosion in the Controlled Release of a Poorly Water-Soluble Drug Using Synchrotron X-ray Computed Microtomography

Guar Gum, Xanthan Gum, and HPMC Can Define Release Mechanisms and Sustain Release of Propranolol Hydrochloride

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