Effects of hardness on the disintegration time and the dissolution rate of uncoated caffeine tablets

Kitazawa, Shigeru; Johno, Ikuo; Ito, Yoko; Teramura, Shigeo; Okada, Jutaro

doi:10.1111/j.2042-7158.1975.tb09397.x

Cited by 69 publications

(35 citation statements)

References 7 publications

(1 reference statement)

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“…For instance, a good correlation between hardness (crushing tolerance) and disintegration time was obtained by Kitazawa and co-workers for conventional uncoated tablets containing caffeine. 17) For rapidly disintegrating tablets, the same good relationship between crushing tolerance and disintegration time was obtained. These two parameters increased with increasing particle size of PH-102 and PH-M-06 (Figs.…”

Section: Discussionmentioning

confidence: 66%

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: 66%

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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“…Studies from literature suggest that there is a relationship between tablet hardness and disintegration time. Basically, when the hardness increases, the disintegration time increases [23]. In other words the higher the crushing force the longer the disintegration time will be.…”

Section: Friability and Disintegrationmentioning

confidence: 99%

Wet Granulation to Overcome Liquisolid Technique Issues of Poor Flowability and Compactibility: A Study to Enhance Glibenclamide Dissolution

Javaheri¹,

Carter²,

Elkordy³

2014

Journal of Pharmaceutics and Drug Development

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The aim of this study is to apply wet granulation on liquisolid powders to overcome issues of poor powder flowability and compressibility especially with using high viscosity liquid vehicles. Different liquisolid formulations were made using three excipients where the effect of each excipient used in the dissolution of the model hydrophobic drug (Glibenclamide) was evaluated. The Glibenclamide tablets were formulated using PEG 400, Synperonic PE/L44 and Cremophor ELP, at a 10 %w/w in liquid vehicle drug concentration. The carrier (Avicel®PH102) was used followed by colloidal silicon dioxide (coating material) that converted the wet mixture into dry powder. Potato starch, 5%w/w, as a disintegrant was mixed with the mixture manually for 10 minutes and was finalized by adding 0.75% of magnesium stearate as a lubricant. The final powder (depending on its flowability and compactability) was then compacted automatically using a single-punch tableting machine to give tablets with 4mg unit drug dose. Prepared liquisolid compacts were characterised via B.P. quality control tests. In this study, a novel discovery was achieved to overcome the major problems with liquisolid preparations (flowability and compactability). This new technique is the wet granulation process to be applied with liquisolid powders just before the compaction stage of the powders into tablets. Consequently, it was found that by application of wet granulation to liquisolid powder admixture, the large-scale production of liquisolid compacts is feasible and can be easily applied by pharmaceutical industry. As with some liquisolid vehicles especially high viscosity although very good to enhance dissolution usually formulations are studied in powder forms [1,2].Keywords: Liquisolid compacts; Granulation; Glibenclamide; Flowability and compactibility; Dissolution rate; Wettability Abstract Oral drug delivery is the main and most common route of administration. There are various types of dosage forms that can be formulated, and tablets are known to be the most common type. Tablets can be manufactured by several stages where the final stage is the compression of the powder held within a confined space. In addition, the use of tablets as dosage form became of interest to the pharmaceutical industry, thus the formulation of tablet with variety of forms were formulated [3]. Tablets are solid preparations each containing a single dose of one or more active ingredients and produced via compression of uniform volumes of particles. The secret behind the difference between each tablet is in the type of excipients used. Pharmaceutical industry use different excipients, diluents, disintegrants and lubricants to ensure that tablets of specified quality are prepared. However, one excipient can affect the properties of the tablets. Thus, it can be said that each excipient added has a specific role in the formulation of the oral tablets. ISSN: 2348-9782In addition, the In-vitro dissolution study found that granulated liquisolid tablets enhanced not only the flowability an...

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“…Crushing tolerance and porosity have been reported to be linked to the disintegration of tablets, 5,6) although they do not strongly correlate with disintegration time in the mouth of rapidly disintegrating tablet. Disintegration time in the mouth is influenced by powder compactibility.…”

Section: Resultsmentioning

confidence: 99%

“…Therefore, we evaluated factors related to disintegration time in the mouth. Crushing tolerance and porosity have been reported to be linked to tablet disintegration, 5,6) however these parameters are not closely correlated with disintegration time in the mouth. We focused on an analysis of the compaction process using a single punch machine equipped with several force analysis elements, and found a novel factor that predicted in vivo disintegration time of rapidly disintegrating tablets.…”

mentioning

confidence: 99%

A Novel Method for Predicting Disintegration Time in the Mouth of Rapidly Disintegrating Tablet by Compaction Analysis Using TabAll

Shibata

Yamamoto

Fujii

et al. 2004

CHEMICAL & PHARMACEUTICAL BULLETIN

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A tableting process analyzer (TabAll) was used to predict disintegration time in the mouth of rapidly disintegrating tablet. Analyzer profiles recorded upper punch displacement and die wall force encountered during tablet processing. Changes in the mixing ratio of spherical sugar granules and microcrystalline cellulose or lactose affected upper punch displacement and die wall force profiles. Analysis of the compaction process revealed a strong association between disintegration time in the mouth and stationary time, relaxation time of upper punch displacement, and relaxation time of die wall force; disintegration time in the mouth decreased as the three parameters increased. Thus, analysis of the compaction process is useful for predicting disintegration time in the mouth of rapidly disintegrating tablet, which can assist the formulation of new rapidly disintegrating tablets.

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Effects of hardness on the disintegration time and the dissolution rate of uncoated caffeine tablets

Cited by 69 publications

References 7 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.

Wet Granulation to Overcome Liquisolid Technique Issues of Poor Flowability and Compactibility: A Study to Enhance Glibenclamide Dissolution

A Novel Method for Predicting Disintegration Time in the Mouth of Rapidly Disintegrating Tablet by Compaction Analysis Using TabAll

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