Effect of granule properties on rough mouth feel and palatability of orally disintegrating tablets

Kimura, Shin-ichiro; Uchida, Shinya; Kanada, Ken; Namiki, Noriyuki

doi:10.1016/j.ijpharm.2015.02.023

Cited by 71 publications

(47 citation statements)

References 14 publications

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“…For solid oral multiparticulate dosage forms, important texture attributes include roughness, hardness, fracturability and cohesiveness, depending on the specific form …”

Section: Discussionmentioning

confidence: 99%

Evidence of acceptability of oral paediatric medicines: a review

Mistry

Batchelor

2017

Journal of Pharmacy and Pharmacology

125

109

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Objectives The aim of this review was to map the currently available evidence on acceptability of oral paediatric medicines to aid in the selection of suitable platform formulations for the development of new acceptable paediatric products. Methods This process used a defined search strategy of indexed publications and included methods to assess the quality of the evidence retrieved. Key findings Taste/palatability was the most extensively studied area of paediatric medicine acceptability yet standard methods or criteria that define what is classed as acceptable to children is still to be defined. There have been many reports on the acceptability of medicines to paediatric populations yet major gaps in the acceptability knowledge base exist including the shape and dimensions of tablets, minitablets and capsules swallowed whole in infants and children; size and overall volume of multiparticulates; volume of liquids completely swallowed in infants and children; duration of retention within the oral cavity, size and taste of orodispersible tablets, lozenges and chewable tablets and the number of solid units dosed at each time point. Conclusions The review highlights where further information is required to support knowledge around acceptability of age-appropriate medicines. An algorithm to aid in selection of a formulation that is likely to be acceptable based on the age range to be treated by the medicine is presented as a result of this review. IntroductionThere is much evidence to support the need for age-appropriate medicines to treat paediatric patients. Pharmaceutical products for the paediatric population have a number of considerations that may not apply to adult products. In particular, the acceptability of a product needs to be clearly defined for paediatric populations and this is currently an area of great interest.The importance and incentive to study the acceptability, including palatability, of paediatric formulations was discussed in the reflection paper [1] and endorsed in the latest European Paediatric guideline on pharmaceutical development of formulations for paediatric use.[2] Before this regulatory change, there was no requirement for medicines to be demonstrated to be acceptable to children. Guidance issued by the European Medicines Agency (EMA) in 2013 states that patient acceptability must be an integral part of paediatric formulation development and described in the paediatric investigation plan (PIP).[3] Acceptability has previously been defined as 'an overall ability of the patient and caregiver (defined as "user") to use a medicinal product as intended (or authorised)'.[4] The palatability of paediatric medicines is one of the most important formulation factors in the acceptability of liquid medicines with potential to influence adherence to therapeutic regimens and outcomes.[5] Palatability has been defined as, 'the overall appreciation of a (often oral) medicine by organoleptic properties such as vision (appearance), smell, taste, aftertaste and mouth feel (e.g. texture, cooli...

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“…For solid oral multiparticulate dosage forms, important texture attributes include roughness, hardness, fracturability and cohesiveness, depending on the specific form …”

Section: Discussionmentioning

confidence: 99%

Evidence of acceptability of oral paediatric medicines: a review

Mistry

Batchelor

2017

Journal of Pharmacy and Pharmacology

125

109

View full text Add to dashboard Cite

show abstract

“…The maximum particle size with which patients do not feel the sandy feeling or rough sensation on the tongue is around 200 µm, so the particle size of MS was envisaged to be less than 200 µm to avoid any rough mouth feel 25 . Such a formulation would have all the advantages and convenience of ODT dosage form and would simultaneously provide sustained release of the drug.…”

Section: Domperidone (5-chloro-1-[1-[3-(2-oxo-23-dihydro-1h-benzimidmentioning

confidence: 99%

“…The particle size of MS was well within ≤ 200 µm limit and would thus avoid any gritty feeling in the mouth after disintegration. It is well known that particle size above 200 µm causes rough mouth feel though threshold particle size within ODT required for feeling roughness has been determined to be >200μm because of the palatability of the exicipients like mannitol used in ODT 25,41 .…”

Section: B) Characterization Of Ms I)appearance and Particle Sizementioning

confidence: 99%

Formulation and development of orodispersible sustained release tablet of domperidone

Patil

Tiwari

Repka

et al. 2015

Drug Development and Industrial Pharmacy

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Abstract:Commercially available domperidone orodispersible tablets (ODT) are intended for immediate release of the drug but none of them have been formulated for sustained action. The aim of the present research work was to develop and evaluate orodispersible sustained release tablet (ODT-SR) of domperidone, which has the convenience of ODT and benefits of controlled release product combined in one. The technology comprised of developing sustained release microspheres (MS) of domperidone, followed by direct compression of MS along with suitable excipients to yield ODT-SR which rapidly disperses within 30 seconds and yet the dispersed MS maintain their integrity to have a sustained drug release. The particle size of the MS was optimized to be less than 200 μm to avoid the grittiness in the mouth. The DSC thermograms of MS showed the absence of drug-polymer interaction within the microparticles, while SEM confirmed their spherical shape and porous nature. Angle of repose, compressibility and Hausner's ratio of the blend for compression showed good flowability and high percent compressibility. The optimised ODT-SR showed disintegration time of 21 seconds and matrix controlled drug release for 9 h. Invivo pharmacokinetic studies in Wistar rats showed that the ODT-SR had a prolonged MRT of 11.16 h as compared 3.86 h of conventional tablet. The developed technology is easily scalable and holds potential for commercial exploitation.

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“…We aimed at manufacturing uniform and fine granules (100-200 µm), which are desirable for imparting good handling during processing and a good mouthfeel. 11,12) Experimental Materials Ibuprofen (IBU) was kindly provided from BASF Japan Ltd. (Tokyo, Japan), GM was purchased from Taiyo Chemical Industry Co., Ltd. (Saitama, Japan), SA was purchased from Wako Pure Chemical Industries, Ltd. (Osaka, Japan) and PEG6000 was purchased from Wako Pure Chemical Industries, Ltd. US2 was kindly provided by Fuji Chemical Industries Co., Ltd. (Tokyo, Japan), DCPD was kindly provided by Kimura Sangyo Co., Ltd. (Tokyo, Japan).…”

Section: Highlighted Paper Selected By Editor-in-chiefmentioning

confidence: 99%

Melt Adsorption as a Manufacturing Method for Fine Particles of Wax Matrices without Any Agglomerates

Shiino

Fujinami

Kimura

et al. 2017

CHEMICAL & PHARMACEUTICAL BULLETIN

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We have focused on melt adsorption as manufacture method of wax matrices to control particles size of granules more easily than melt granulation. The purpose of present study was to investigate the possibility of identifying a hydrophobic material with a low melting point, currently used as a meltable binder of melt granulation, to apply as a novel carrier in melt adsorption. Glyceryl monostearate (GM) and stearic acid (SA) were selected as candidate hydrophobic materials with low melting points. Neusilin US2 (US2), with a particle diameter of around 100 µm was selected as a surface adsorbent, while dibasic calcium phosphate dihydrate (DCPD), was used as a non-adsorbent control to prepare melting granules as a standard for comparison. We prepared granules containing ibuprofen (IBU) by melt adsorption or melt granulation and evaluated the particle size, physical properties and crystallinity of granules. Compared with melt granulation using DCPD, melt adsorption can be performed over a wide range of 14 to 70% for the ratio of molten components. Moreover, the particle size; d50 of obtained granules was 100-200 µm, and these physical properties showed good flowability and roundness. The process of melt adsorption did not affect the crystalline form of IBU. Therefore, the present study has demonstrated for the first time that melt adsorption using a hydrophobic material, GM or SA, has the potential capability to control the particle size of granules and offers the possibility of application as a novel controlled release technique.

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Effect of granule properties on rough mouth feel and palatability of orally disintegrating tablets

Cited by 71 publications

References 14 publications

Evidence of acceptability of oral paediatric medicines: a review

Evidence of acceptability of oral paediatric medicines: a review

Formulation and development of orodispersible sustained release tablet of domperidone

Melt Adsorption as a Manufacturing Method for Fine Particles of Wax Matrices without Any Agglomerates

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