A Comparative Evaluation of the Properties of some Tablet Disintegrants

Gissinger, D.; Stamm, A.

doi:10.3109/03639048009068720

Cited by 66 publications

(24 citation statements)

References 2 publications

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“…In the case of tablets with high concentrations of L-HPC, L-HPC swelled significantly, that is, the maximum swelling rate of L-HPC was approximately ten-fold that of microcrystalline cellulose. 18) However, the high concentration of L-HPC in tablets interferes with the rapid disintegration function (increasing disintegration time) due to the decrease in the degree of wetting (increasing wetting time). 4) We previously reported that the disintegration time of tablets prepared with PH-102 and L-HPC significantly decreased (25→5 s) with increasing tablet porosity (approximately, 25→45%).…”

Section: Discussionmentioning

confidence: 99%

Preparation of Rapidly Disintegrating Tablet Using New Types of Microcrystalline Cellulose (PH-M Series) and Low Substituted-Hydroxypropylcellulose or Spherical Sugar Granules by Direct Compression Method.

et al. 2001

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Recently, the clinical usefulness of tablets that are rapidly disintegrated by saliva (rapidly disintegrating tablet), an attractive dosage form for patient-oriented pharmaceutical preparations, has been reported.2) Previously, we formulated rapidly disintegrating tablets containing meclizine hydrochloride, an antidinic agent, using microcrystalline cellulose (Avicel PH-102 ® : mean particle size, 100 mm), a conventional pharmaceutical excipient, and low-substituted hydroxypropylcellulose (L-HPC: mean particle size, 50 mm), a good disintegrant, by the direct compression method at a low compression force (1-6 kN).3) Bi et al. 4) also reported the preparation of compressed tablets that can rapidly disintegrate in the mouth, using Avicel PH-102 and L-HPC with ethenzamide and ascorbic acid as model drugs. However, patients often complain of a feeling of roughness in their mouths after taking these tablets, due to the surface texture and the large particle size. Generally, the rough texture of particles with size below 15 mm is not felt in the mouth. 5-7)Therefore, in this study we attempted to formulate a new type of rapidly disintegrating tablet with good texture using excipients with particle size smaller than that of PH-102 by the direct compression method. Although the most suitable disintegration time is not confirmed, we set the desirable disintegration time at 15 s based on information on the disintegration time of commercially available preparations with the characteristic of rapid disintegration.8) The microcrystalline cellulose PH-M series is a new type of pharmaceutical excipient that is spherical and has a very small particle size, and is used as an ingredient in cosmetics. To decrease the sensation of roughness in the mouth, we prepared rapidly disintegrating tablets using microcrystalline cellulose (Avicel PH-M-06 ® ) with a small particle size (mean particle size, 7 mm) instead of PH-102 in the formulation of tablets containing acetaminophen or ascorbic acid as the model drug for tableting study. Furthermore, to improve the fluidity of excipients in the tableting process, we investigated the usability of spherical sugar granules 9) instead of L-HPC in combination with PH-M-06. ExperimentalMaterials Acetaminophen (JP XIII) and ascorbic acid (JP XIII) were purchased from Maruishi Seiyaku Co. (Osaka, Japan). Microcrystalline cellulose (Avicel ® PH-102, PH-M-06, PH-M-15, PH-M-25, JP XIII) and L-HPC (LH-11 ® , JP XIII) were kindly supplied by Asahi Chemical Industry Co., Tokyo, Japan and Shin-Etsu Chemical Co., Tokyo, Japan, respectively. Spherical sugar granules (water-soluble sugar granule, Nonpareil ® , hereafter abbreviated as NP), sucrose starch spheres (NP-101), purified sucrose spheres (NP-103), purified lactose spheres (NP-107) and purified D-mannitol spheres (NP-108) were kindly supplied by Freund Industry Co., Tokyo, Japan. All other reagents were of analytical grade.Physical Characteristics of Crystalline Cellulose The particle size distribution of crystalline cellulose was measured using a ce...

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Section: Discussionmentioning

confidence: 99%

Preparation of Rapidly Disintegrating Tablet Using New Types of Microcrystalline Cellulose (PH-M Series) and Low Substituted-Hydroxypropylcellulose or Spherical Sugar Granules by Direct Compression Method.

et al. 2001

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“…The effectiveness of crospovidone has been claimed to be due to its high capillary activity through wicking with little swelling action (2,17,18), mainly by swelling (19), or by strain recovery or latent viscoelastic recovery (20). Sodium starch glycolate is reported to work via rapid uptake of water and swelling (16,18). Microcrystalline cellulose, commonly used as filler in tablet formulations, is not considered to be a superdisintegrant but reported to possess good wicking properties and hydrogen bonds between adjacent matchstick-like bundles that break when exposed to water (21).…”

Section: Introductionmentioning

confidence: 99%

“…Croscarmellose sodium is reported to aid disintegration by rapid swelling and wicking upon contact with water (2,15,16). Wicking is a "whipping" action where material-air or material-material interface is spontaneously replaced by material-water interface and thus helps in maintaining capillary flow.…”

Section: Introductionmentioning

confidence: 99%

Functionality of Disintegrants and Their Mixtures in Enabling Fast Disintegration of Tablets by a Quality by Design Approach

Desai

Liew

et al. 2014

AAPS PharmSciTech

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Abstract. Investigation of the effect of disintegrants on the disintegration time and hardness of rapidly disintegrating tablets (RDTs) was carried out using a quality by design (QbD) paradigm. Ascorbic acid, aspirin, and ibuprofen, which have different water solubilities, were chosen as the drug models. Disintegration time and hardness of RDTs were determined and modeled by executing combined optimal design. The generated models were validated and used for further analysis. Sodium starch glycolate, croscarmellose sodium, and crospovidone were found to lengthen disintegration time when utilized at high concentrations. Sodium starch glycolate and crospovidone worked synergistically in aspirin RDTs to decrease disintegration time. Sodium starch glycolate-crospovidone mixtures, as well as croscarmellose sodium-crospovidone mixtures, also decreased disintegration time in ibuprofen RDTs at high compression pressures as compared to the disintegrants used alone. The use of sodium starch glycolate in RDTs with highly water soluble active ingredients like ascorbic acid slowed disintegration, while microcrystalline cellulose and crospovidone drew water into the tablet rapidly and quickened disintegration. Graphical optimization analysis demonstrated that the RDTs with desired disintegration times and hardness can be formulated with a larger area of design space by combining disintegrants at difference compression pressures. QbD was an efficient and effective paradigm in understanding formulation and process parameters and building quality in to RDT formulated systems.

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“…Gissinger and Stamm compared water absorption, contact angle, swelling volume, and disintegration times of a range of disintegrants (Gissinger and Stamm, 1980). They ranked the efficacy mainly according to the disintegration time and concluded that modified starch and cellulose, low-substituted hydroxypropylcellulose, polacrilin potassium, and crospovidone are superior to other disintegrants.…”

Section: Introductionmentioning

confidence: 99%

Assessment of disintegrant efficacy with fractal dimensions from real-time MRI

Quodbach

Moussavi

Tammer

et al. 2014

International Journal of Pharmaceutics

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A B S T R A C TAn efficient disintegrant is capable of breaking up a tablet in the smallest possible particles in the shortest time. Until now, comparative data on the efficacy of different disintegrants is based on dissolution studies or the disintegration time. Extending these approaches, this study introduces a method, which defines the evolution of fractal dimensions of tablets as surrogate parameter for the available surface area. Fractal dimensions are a measure for the tortuosity of a line, in this case the upper surface of a disintegrating tablet. High-resolution real-time MRI was used to record videos of disintegrating tablets. The acquired video images were processed to depict the upper surface of the tablets and a box-counting algorithm was used to estimate the fractal dimensions. The influence of six different disintegrants, of different relative tablet density, and increasing disintegrant concentration was investigated to evaluate the performance of the novel method. Changing relative densities hardly affect the progression of fractal dimensions, whereas an increase in disintegrant concentration causes increasing fractal dimensions during disintegration, which are also reached quicker. Different disintegrants display only minor differences in the maximal fractal dimension, yet the kinetic in which the maximum is reached allows a differentiation and classification of disintegrants.

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A Comparative Evaluation of the Properties of some Tablet Disintegrants

Cited by 66 publications

References 2 publications

Preparation of Rapidly Disintegrating Tablet Using New Types of Microcrystalline Cellulose (PH-M Series) and Low Substituted-Hydroxypropylcellulose or Spherical Sugar Granules by Direct Compression Method.

Preparation of Rapidly Disintegrating Tablet Using New Types of Microcrystalline Cellulose (PH-M Series) and Low Substituted-Hydroxypropylcellulose or Spherical Sugar Granules by Direct Compression Method.

Functionality of Disintegrants and Their Mixtures in Enabling Fast Disintegration of Tablets by a Quality by Design Approach

Assessment of disintegrant efficacy with fractal dimensions from real-time MRI

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