Dissolution Behavior and Bioavailability of Phenytoin from a Ground Mixture with Microcrystalline Cellulose

Yamamoto, Keiji; Nakano, Masahiro; Arita, Takaichi; Takayama, Yoshikazu; Nakai, Yusuke

doi:10.1002/jps.2600651017

Cited by 84 publications

(34 citation statements)

References 2 publications

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“…More, research work has been done using dry milling conditions for co-grinding. 7,14) The properties of milled product are dominated by the surface properties of the crystal face. In the case of poorly water soluble substances, the newly created surface is hydrophobic and thus poorly wettable.…”

mentioning

confidence: 99%

“…The enhancement of dissolution rate which results in improvement of bioavailability of poorly soluble drugs has been demonstrated by various investigators. [14][15][16] In an earlier study 4) we had investigated the effect of cogrinding of RHCL with different hydrophilic carriers such as polyvinyl pyrrolidone (PVP), hydroxypropylmethyl cellulose (HPMC), HPC and sodium alginate. As a continuation, the present study was undertaken to investigate the effect of cogrinding RHCL with different superdisintegrants, namely crospovidone (CP), croscarmellose sodium (CCS) and sodium starch glycolate (SSG), using a ball mill, in order to determine the potential effect on dissolution rate and bioavailability of RHCL.…”

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confidence: 99%

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Enhanced Dissolution and Bioavailability of Raloxifene Hydrochloride by Co-grinding with Different Superdisintegrants

Jagadish¹,

Yelchuri²,

K³

et al. 2010

Chem. Pharm. Bull.

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The present study investigated the effect of co-grinding raloxifene HCL (RHCL) with different superdisintegrants, namely crospovidone (CP), croscarmellose sodium (CCS) and sodium starch glycolate (SSG), using a ball mill, in order to determine the potential effect on dissolution rate and bioavailability of raloxifene hydrochloride (RHCL). The dissolution studies of the co-ground compositions and the corresponding physical mixtures were carried out in U.S. Pharmacopeia (USP) Type II apparatus. The solid state interactions of the co-ground and the physical mixtures were evaluated by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The pharmacokinetics of co-ground mixture (1 : 5 RHCL : CP) and milled RHCL was evaluated following oral administration (25 mg/kg) in healthy female Sprague-Dawley rats. DSC studies showed that the crystalline nature of RHCL was reduced after co-grinding with superdisintegrants, while co-grinding with CP resulted in significant particle-size reduction of the mixture. Significant enhancement in dissolution rate was observed with coground mixture of RHCL with CP (1 : 5). The extent of the mean plasma exposures of RHCL was 7-fold higher in animals treated with co-ground mixture of RHCL, CP (1 : 5) compared to animals treated with milled RHCL. Co-grinding of RHCL with CP, reduced drug crystallinity, increased the rate and extent of dissolution, and improved bioavailability.

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confidence: 99%

mentioning

confidence: 99%

Enhanced Dissolution and Bioavailability of Raloxifene Hydrochloride by Co-grinding with Different Superdisintegrants

Jagadish¹,

Yelchuri²,

K³

et al. 2010

Chem. Pharm. Bull.

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“…Yamamoto and the author 10) found that poorly water-soluble griseofulvin showed higher serum concentrations when it was administered in the form of amorphous mixture with micro-crystalline cellulose. Another poorly water-soluble drug, phenytoin 11) showed higher serum concentrations when a ground mixture with micro-crystalline cellulose was administered than theˆne powder of phenytoin alone was administered (Fig. 1).…”

Section: Reviews Of Research Work Basic Studies On Interactions Of Omentioning

confidence: 99%

From Physical Pharmacy to Clinical Pharmacology

Nakano

2005

YAKUGAKU ZASSHI

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Research works on molecular interactions in solutions were carried out at School of Pharmacy, the University of Wisconsin under the direction of Prof. T. Higuchi and at Faculty of Pharmaceutical Sciences, Kyoto University under the direction of Prof. H. Sezaki. Studies on permeation of drugs through polymer membranes were carried out at Faculty of Pharmacy and Pharmaceutical Sciences, University of Alberta, Edmonton, Canada and at Pharmaceutical Chemistry Research Laboratories at Food and Drug Directorate, Department of Health and Welfare, Canada. Studies on modiˆcation of delivery patterns by means of pharmaceutical approaches were carried out at Faculty of Pharmaceutical Sciences, Hokkaido University. Topics related to modiˆcation of drug delivery patterns include employment of amorphous forms such as ground mixture with micro-crystalline cellulose and coprecipitate with polyvinylpyrrolidone, use of biodegradable polymers such as polylactic acid and polycarbonates, gel-forming materials such as konjac, agar and hydroxypropylcellulose, and physicochemical systems such as complexation. Works related to drug delivery and disposition of drugs in humans were carried out at Department of Pharmacy, Kumamoto University Hospital. Topics related to drug delivery in humans include injections containing anticancer drugs for intra-arterial administration, lidocaine gels for dermal anesthesia, glucagon solution for nasal administration. Topics related to disposition of drugs in humans include clinical pharmacokinetic studies in infants and elderly and medical uses of adsorbents.

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“…Co-grinding can be done either in a dry or in wet condition (Takahashi et al, 1985;Miyamae et al, 1994). However, a common disadvantage one usually encounters with wet grinding or milling is partial dissolution of the drug which more often results in uncontrolled re crystallization (Ahuja et al, 2007;Yamamoto et al, 1976). In the past, investigators have successfully used co-grinding under dry conditions for improving the solubility of poorly soluble drugs (Florence et al, 1976;Etman and Nada., 1999;Nada, 1997;Garg et al, 2009).…”

Section: Introductionmentioning

confidence: 99%

Dissolution rate and bioavailability enhancement of co-ground mixtures of paliperidone, with different hydrophilic carriers

Pandey¹,

Rath²,

Dwivedi³

2013

Int Curr Pharm J

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Co-ground mixtures of poorly water soluble drug Paliperidone (PAL) with different hydrophilic carriers [Polyvinylpyrrolidine (Plasdone K-25 and Plasdone S-630), Hydroxypropyl methyl cellulose (HPMC), Hydroxypropylcellulose (HPC) and Sodium alginate were prepared to improve the dissolution rate of PAL. Co-grinding with PVP, especially with PVP- S630 (Vinyl pyrrolidone/ vinyl acetate co-polymer), was more effective in reduction of particle size than milling of drug alone. DSC studies indicated that crystalline nature of drug was reduced after co-grinding with PVP grades as compared to their corresponding physical mixtures. The hydrophilic carriers other than PVP did not reduce the crystalline nature of the drug significantly. X-ray diffraction (XRD) was carried out for selected batches to confirm DSC results. Significant enhancement in dissolution rate as well as extent was observed with co-ground mixtures of drug and PVP. Among all the prepared batches in this study, co-ground mixture of PAL and Plasdone S-630 in 1:1 ratio showed best results in terms of extent of dissolution as well as dissolution rate in water. This effect was not only due to particle size reduction, but also loss of crystalline nature of the drug during co-grinding. PVP was found to be a better carrier among the different hydrophilic carriers used in the study for improving the dissolution characteristics of PAL. The extent of the mean plasma exposures of PAL was 7-fold higher in animals treated with co-ground mixture of PAL, Plasdone S630 (1:1) compared to animals treated with Pure PAL.DOI: http://dx.doi.org/10.3329/icpj.v2i3.13632 International Current Pharmaceutical Journal, February 2013, 2(3): 70-77

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Dissolution Behavior and Bioavailability of Phenytoin from a Ground Mixture with Microcrystalline Cellulose

Cited by 84 publications

References 2 publications

Enhanced Dissolution and Bioavailability of Raloxifene Hydrochloride by Co-grinding with Different Superdisintegrants

Enhanced Dissolution and Bioavailability of Raloxifene Hydrochloride by Co-grinding with Different Superdisintegrants

From Physical Pharmacy to Clinical Pharmacology

Dissolution rate and bioavailability enhancement of co-ground mixtures of paliperidone, with different hydrophilic carriers

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