Tablet formulation development focusing on the functional behaviour of water uptake and swelling

Lenz, Jan; Finke, Jan Henrik; Bunjes, Heike; Kwade, Arno; Juhnke, Michael

doi:10.1016/j.ijpx.2021.100103

Cited by 4 publications

(4 citation statements)

References 52 publications

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“…24 Thus, uptake of the disintegrating medium into the tablet (wicking) followed by the swelling of the disintegrant added are the prerequisites for efficient/ faster tablet disintegration. 13 It was envisaged in the present work that co-processing of crospovidone with the hydrogel isolated from the seeds of O. basilicum Ocimum basilicum would yield co-processed material with improved disintegrant functionality. [25][26][27] The average pore radius of the co-processed crospovidone was 4.27A o and was more than the average pore radius of the crospovidone (3.99A o ).…”

Section: Optimization Of Vaginal Tablet Of Solid Dispersion Of Clotri...mentioning

confidence: 83%

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Development of Vaginal Tablet of Clotrimazole Prepared by Applying the Concept of Percolatio Threshold

Rajan,

Mustaqeem,

Akbar

et al. 2023

IJDDT

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Clotrimazole is the drug of choice in the treatment of vulvovaginal candidiasis and belongs to biopharmaceutical classification system (BCS) class IIb. Therefore, it should be presented in appropriate form adopting a suitable formulation approach to ensure its fast and complete release in the vagina. Solid dispersion of clotrimazole was prepared using microcrystalline cellulose as a carrier material after confirming their miscibility into each other by the ‘melting point depression’ method. Vaginal tablets of the solid dispersion of clotrimazole were prepared by direct compression using co-processed crospovidone as a novel disintegrant (1.5% w/w) to ensure fast disintegration of the tablet. Co-processed crospovidone was selected as a novel disintegrant and its proportion in the formulation was decided by applying the concept of percolation threshold. The superior functionality of co-processed crospovidone as a disintegrant was because of its larger pore size i. e., 4.27Ao than the pore size of crospovidone 3.99Ao. The faster ingress of water through the larger pores leads to the fast disintegration of the tablet. Rapid release of the drug from the disintegrated tablet dosage form was confirmed by performing in-vitro antifungal studies. The statistical analysis of the data obtained after applying the student ‘t’ test indicated that there was a difference in the means of zone of inhibitions between the tablets of optimized composition and the tablets the plain clotrimazole at p less than 0.5.

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Section: Optimization Of Vaginal Tablet Of Solid Dispersion Of Clotri...mentioning

confidence: 83%

“…The graph of the kinetic constant of water uptake versus disintegrant content was plotted for all the compositions containing crospovidone and co-processed crospovidone separately. 7,13 The percolation thresholds were determined after analyzing the graphs.…”

Section: Preparation Of Two Sets Of Vaginal Tablet Formulations Of So...mentioning

confidence: 99%

Development of Vaginal Tablet of Clotrimazole Prepared by Applying the Concept of Percolatio Threshold

Rajan,

Mustaqeem,

Akbar

et al. 2023

IJDDT

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“…This might indicate that pore penetration and disintegrant functionality were not influenced by the porosity of these formulations, resulting in a similar outcome after the analysis regarding water content and volume. Swelling of the Eudragit EPO particles was not expected at a pH of 7 [44]. A maximum volume increase followed by a fast decrease to a nearly constant value was observed after 50 s for tablets containing 5% NaCMCXL.…”

Section: Tablet Water Uptake and Swellingmentioning

confidence: 84%

Tablet Disintegration and Dispersion under In Vivo-like Hydrodynamic Conditions

et al. 2022

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Disintegration and dispersion are functional properties of tablets relevant for the desired API release. The standard disintegration test (SDT) described in different pharmacopoeias provides only limited information on these complex processes. It is considered not to be comparable to the biorelevant conditions due to the frequent occurrence of high hydrodynamic forces, among other reasons. In this study, 3D tomographic laser-induced fluorescence imaging (3D Tomo-LIF) is applied to analyse tablet disintegration and dispersion. Disintegration time (DT) and time-resolved particle size distribution in close proximity to the tablet are determined in a continuously operated flow channel, adjustable to very low fluid velocities. A case study on tablets of different porosity, which are composed of pharmaceutical polymers labelled with a fluorescent dye, a filler, and disintegrants, is presented to demonstrate the functionality and precision of the novel method. DT results from 3D Tomo-LIF are compared with results from the SDT, confirming the analytical limitations of the pharmacopoeial disintegration test. Results from the 3D Tomo-LIF method proved a strong impact of fluid velocity on disintegration and dispersion. Generally, shorter DTs were determined when cross-linked sodium carboxymethly cellulose (NaCMCXL) was used as disintegrant compared to polyvinyl polypyrrolidone (PVPP). Tablets containing Kollidon VA64 were found to disintegrate by surface erosion. The novel method provides an in-depth understanding of the functional behaviour of the tablet material, composition and structural properties under in vivo-like hydrodynamic forces regarding disintegration and the temporal progress of dispersion. We consider the 3D Tomo-LIF in vitro method to be of improved biorelevance in terms of hydrodynamic conditions in the human stomach.

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“…Research on the water-sorption kinetics in ASDs is rare. Bunjes et al [8] showed that the water-sorption kinetics in tablets made of microcrystalline cellulose and either eudragit, hydroxypropylmethylcellulose acetyl-succinate, or PVP-covinyl acetate (PVPVA) are quite different. However, a methodology to predict the watersorption kinetics in ASDs has not been proposed yet.…”

Section: Introductionmentioning

confidence: 99%

Predicting the Water Sorption in ASDs

2022

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Water decreases the stability of amorphous solid dispersions (ASDs) and water sorption is, therefore, unwanted during ASD storage. This work suggests a methodology to predict the water-sorption isotherms and the water-sorption kinetics in amorphous pharmaceutical formulations like ASDs. We verified the validity of the proposed methodology by measuring and predicting the water-sorption curves in ASD films of polyvinylpyrrolidone-based polymers and of indomethacin. This way, the extent and the rate of water sorption in ASDs were predicted for drug loads of 0.2 and 0.5 as well as in the humidity range from 0 to 0.9 RH at 25 °C. The water-sorption isotherms and the water-sorption kinetics in the ASDs were predicted only based on the water-sorption isotherms and water-sorption kinetics in the neat polymer on the one hand and in the neat active pharmaceutical ingredient (API) on the other hand. The accurate prediction of water-sorption isotherms was ensured by combining the Perturbed-Chain Statistical Association Theory (PC-SAFT) with the Non-Equilibrium Thermodynamics of Glassy Polymers (NET-GP) approach. Water-sorption kinetics were predicted using Maxwell–Stefan diffusion coefficients of water in the ASDs.

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Tablet formulation development focusing on the functional behaviour of water uptake and swelling

Cited by 4 publications

References 52 publications

Development of Vaginal Tablet of Clotrimazole Prepared by Applying the Concept of Percolatio Threshold

Development of Vaginal Tablet of Clotrimazole Prepared by Applying the Concept of Percolatio Threshold

Tablet Disintegration and Dispersion under In Vivo-like Hydrodynamic Conditions

Predicting the Water Sorption in ASDs

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