Microstructural imaging of early gel layer formation in HPMC matrices

Bajwa, Gurjit S.; Hoebler, Katrin; Sammon, Chris; Timmins, Peter; Melia, Colin D.

doi:10.1002/jps.20656

Cited by 65 publications

(43 citation statements)

References 28 publications

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“…Surface sensitive [10,11] ATR-FTIR imaging Quantitative Surface sensitive [12][13][14][15][16][17] Transmission-FTIR imaging Quantitative Unrealistic tablet needed (thickness <20µm) [18] An advantage of MRI is the ease of sampling. A slice or line can be selected in a tablet completely immersed in the dissolution fluid, as MRI is a 3D technique.…”

Section: Time Resolution Specificitymentioning

confidence: 99%

Simultaneous FTIR Spectroscopic Imaging and Visible Photography to Monitor Tablet Dissolution and Drug Release

Kazarian

Weerd

2007

Pharm Res

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A method to study tablet dissolution simultaneously by Fourier transform infraredattenuated total reflection (FTIR-ATR) imaging and macro-photography is described. Such a combined approach appeared important as the results of macro-photography, which have been provided by a number of authors, led to contradictory interpretations. The macro-photographs of a pharmaceutical tablet during exposure to water show a number of 'fronts' moving into the tablet. These fronts are obviously related to water penetration into and dissolution of the tablet, but the exact nature can not be derived from photographic evidence. Therefore, the combination of macro-photography and FTIR-ATR imaging was developed and used to interpret the physical changes leading to the observed fronts. The quantitative results obtained by FTIR-ATR imaging enabled the attribution of the three observed fronts (inside to outside) to: 1. True water penetration, possibly combined with (partial) dissolution of buflomedyl pyridoxal phosphate (BPP) 2. Total gellification of hydroxypropyl-methylcellulose (HPMC) 3. Erosion front IntroductionIn recent years, a number of new approaches has been reported to study the behaviour of pharmaceutical tablets during dissolution. These studies aim to generate an understanding of the processes in a dissolving tablet. This is a welcome addition to the standard dissolution tests, which obtain the amount of dissolved active ingredient as a function of time, but do not provide indications on the underlying mechanisms of tablet dissolution.

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Section: Time Resolution Specificitymentioning

confidence: 99%

Simultaneous FTIR Spectroscopic Imaging and Visible Photography to Monitor Tablet Dissolution and Drug Release

Kazarian

Weerd

2007

Pharm Res

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“…The mechanism by which PVA-based Opadry® coating (AMB and II) act as a moisture barrier appears to be absorption of water followed by entrapment of the water by hydrogen bonding, preventing subsequent water penetration into the pellet core. This phenomenon is similar to the initial phase of water ingress that occurs with high molecular weight HPMC-based matrix tablets where water uptake occurs first by capillary action, then the porous channels are rapidly blocked by HPMC swelling and the newly formed swollen HPMC gel layer will act as a diffusion barrier (16). Therefore, a certain amount of water needs to enter the PVA-based film before closure of the porous network occurs.…”

Section: Alternative Drug Layered Pellet Water Barriersmentioning

confidence: 67%

Stability Enhancement of Drug Layered Pellets in a Fixed Dose Combination Tablet

Burke

Cook

et al. 2013

AAPS PharmSciTech

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Abstract. The purpose of this research was to develop a stable fixed dose combination tablet for a model DPP-IV inhibitor and metformin hydrochloride. The dipeptidyl peptidase IV (DPP-IV) inhibitor was particularly challenging to formulate due to its significant chemical instability and moisture sensitivity. Various formulation strategies were investigated and placed on accelerated stability to determine the lead approach and critical quality attributes. The lead formulation investigated was a drug layered pellet containing the DPP-IV inhibitor, which was further coated with various seal coats and moisture barriers, then compressed into a tablet with compression aids and granulated metformin hydrochloride. The investigations revealed that the drug layered pellets compressed into a fixed dose combination tablet yielded a unique stability enhancement. The stability was highly dependent on the final tablet water content and could be further improved by the addition of moisture barrier coatings. A fundamental understanding of the key critical quality attributes for the fixed dose combination product containing a DPP-IV inhibitor and metformin hydrochloride as an oral solid dosage form were established. This research identified a formulation approach to enable a successful commercial product to be developed.

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“…This may be attributed to the higher ionic strength of the phosphate buffer medium, which normally decreases the drug-release rate from the HPMC matrix tablets, which can diminish the discriminatory ability of the method. The mechanism of slowing the drug release from the HPMC matrix tablets in the presence of different salts was studied previously (43)(44)(45). One of the possible explanations for the slower release is the competition of the polymer chains with the ionic constituents for the water molecules; therefore, there is less water available for the polymer hydration and consequently the drug release from matrix tablet is slower.…”

Section: Development Of Dissolution Methods Using Apparatus 1 and Appamentioning

confidence: 99%

A Novel Beads-Based Dissolution Method for the In Vitro Evaluation of Extended Release HPMC Matrix Tablets and the Correlation with the In Vivo Data

Klančar¹,

Markun²,

Baumgartner

et al. 2012

AAPS J

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Abstract. The aim of this work was to establish alternative in vitro dissolution method with good discrimination and in vivo predictability for the evaluation of HPMC extended release matrix tablets. For this purpose, two different HPMC matrix tablet formulations were first evaluated by a range of conventional dissolution testing methods using apparatus 1, apparatus 2, and apparatus 3 according to US Pharmacopoeia. Obtained results showed low discrimination between the tested samples. Afterward, a novel dissolution testing method which combines plastic beads and apparatus 3 was developed with the aim to better mimic the mechanical forces that occur in vivo. Results showed that sufficiently large mechanical stress with high dips per minute program setting (apparatus 3) was needed to obtain in vitro discriminative results, which are in accordance with the in vivo data. The in vivo relevance of the method was confirmed with the establishment of the level A in vitro-in vivo correlation.

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Microstructural imaging of early gel layer formation in HPMC matrices

Cited by 65 publications

References 28 publications

Simultaneous FTIR Spectroscopic Imaging and Visible Photography to Monitor Tablet Dissolution and Drug Release

Simultaneous FTIR Spectroscopic Imaging and Visible Photography to Monitor Tablet Dissolution and Drug Release

Stability Enhancement of Drug Layered Pellets in a Fixed Dose Combination Tablet

A Novel Beads-Based Dissolution Method for the In Vitro Evaluation of Extended Release HPMC Matrix Tablets and the Correlation with the In Vivo Data

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