Dissolution mechanism and rate of solid dispersion particles of nilvadipine with hydroxypropylmethylcellulose

Okimoto, Kazuto; Miyake, Mari; Ibuki, Rinta; Yasumura, Mituru; Ohnishi, Norio; Nakai, Tomoya

doi:10.1016/s0378-5173(97)00274-3

Cited by 85 publications

(46 citation statements)

References 13 publications

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“…The K-chemistry grades of HPMC and, in particular, K100M contain more irregularly shaped particles with rough surfaces than any of the other grades of cellulose ethers. This is attributed to the higher Hpo/Meo substitution ratio and molecular size which result in more complex surfaces (Gustafsson et al, 1999;Okimoto et al, 1997).…”

Section: 11-morphology Of Cellulose Ether Powdersmentioning

confidence: 99%

Tribo-electric charging and adhesion of cellulose ethers and their mixtures with flurbiprofen

Ghori

Šupuk

Conway

2014

European Journal of Pharmaceutical Sciences

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The pervasiveness of tribo-electric charge during pharmaceutical processing can lead to the exacerbation of a range of problems including segregation, content heterogeneity and particle surface adhesion. The excipients, hydroxypropyl methylcellulose (HPMC) and methylcellulose (MC), are often used in drug delivery systems and so it is important to understand the impact of associated factors on their charging and adhesion mechanisms, however, little work has been reported in this area. Such phenomena become more prominent when excipients are introduced to a powder mixture alongside the active pharmaceutical ingredient(s) (APIs) with inter-and intra-particulate interactions giving rise to electrification and surface adhesion of powder particles. The aim of this study was to understand the impact of material attributes (particle size, hydroxypropoxyl (Hpo) to methoxyl (Meo) ratio and molecular size) on the charging and adhesion characteristics of cellulose ethers. Furthermore, a poorly compactible and highly electrostatically charged drug, flurbiprofen, was used to develop binary powder mixtures having different polymer to drug ratios and the relationship between tribo-electric charging and surface adhesion was studied. Charge was induced on powder particles and measured using a custom built device based on a shaking concept, consisting of a Faraday cup connected to an electrometer. The diversity in physicochemical properties has shown a significant impact on the tribo-electric charging and adhesion behaviour of MC and HPMC.Moreover, the adhesion and electrostatic charge of the API was significantly reduced when MC and HPMC were incorporated and tribo-electric charging showed a linear relationship (R 2 = 0.81-0.98) with particle surface adhesion, however, other factors were also involved. It is anticipated that such a reduction in charge and particle surface adhesion would improve flow and compaction properties during processing.

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Section: 11-morphology Of Cellulose Ether Powdersmentioning

confidence: 99%

Tribo-electric charging and adhesion of cellulose ethers and their mixtures with flurbiprofen

Ghori

Šupuk

Conway

2014

European Journal of Pharmaceutical Sciences

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“…The image of silymarin revealed drug particles with a reduced specific surface area due to some aggregation and agglomeration. Morphological images of HPMC E 15LV exhibited cylindrical shape and similar to fiber (20). The photomicrographs of physical mixtures showed individual particles of silymarin and carrier without any surface adsorption.…”

Section: Characterization Of Solid Dispersionsmentioning

confidence: 94%

Silymarin-solid dispersions: Characterization and influence of preparation methods on dissolution

Sonali¹,

Tejal²,

Thakkar³

et al. 2010

Acta Pharmaceutica

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Seeds of milk thistle (Silybum marianum L. Gaertn, Asteraceae) have been used in medicine for over 2,000 years. Silymarin (SLM), an antihepatotoxic phytocomplex, is a mixture of flavonolignans which has been widely used as a therapeutic agent for a variety of acute and chronic liver diseases. Silymarin is practically insoluble in water; therefore, upon oral administration, its absorption rate in the gastrointestinal tract is low, providing only about 20 to 40 % bioavailability (1).Several approaches have been attempted to improve oral bioavailability of silymarin, complexation with a phospholipid (2), formation of an inclusion complex with b-cyclodextrin and hydroxypropyl-b-cyclodextrin (3), solid dispersion with a hydrophilic polymer such as PEG 6000 (4), selfmicroemulsifying systems (5), co-precipitates (6) and a complex with crosslinked polymers (7). The influence of preparation methodology of silymarin solid dispersions using a hydrophilic polymer on the dissolution performance of silymarin was investigated. Silymarin solid dispersions were prepared using HPMC E 15LV by kneading, spray drying and co-precipitation methods and characterized by FTIR, DSC, XRPD and SEM. Dissolution profiles were compared by statistical and model independent methods. The FTIR and DSC studies revealed weak hydrogen bond formation between the drug and polymer, while XRPD and SEM confirmed the amorphous nature of the drug in co-precipitated solid dispersion. Enhanced dissolution compared to pure drug was found in the following order: co-precipitation > spray drying > kneading methodology (p < 0.05). All preparation methods enhanced silymarin dissolution from solid dispersions of different characteristics. The co-precipitation method proved to be best and provided a stable amorphous solid dispersion with 2.5 improved dissolution compared to the pure drug.

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“…12 The use of hydrophilic polymers as carriers for the dissolution enhancement of poorly water-soluble drug is increasing. 13,14 Various hydrophilic carriers such as polyethylene, 15 polyvinylpyrrolidone 16 and sugars 17 have been investigated for improvement of dissolution characteristics and bioavailability of poorly water soluble drugs. Polyvinylpyrrolidone (PVP) has been used for the preparation of solid dispersion of loratadine using rotary evaporation and spray-drying solvent evaporation techniques.…”

Section: -10mentioning

confidence: 99%

Enhancement of Dissolution Profile of Poorly Water Soluble Loratadine by Solid Dispersion Technique

Uddin

Chowdhury

Hasan

et al. 2017

Dhaka Univ. J. Pharm. Sci

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This study was carried out to improve the dissolution properties of loratadine by solid dispersion technique. A series of solid dispersions of loratadine in PVP K-30 (1:1, 1:3 and 1:5) were prepared by kneading technique. The prepared solid dispersions were characterized by various physicochemical properties (fourier transform infrared spectroscopy, X-ray diffraction and scanning electron microscopy) and the dissolution characteristics were compared with loratadine and the physical mixtures of loratadine. It was revealed from the physicochemical analyses that there was a good compatibility between drug and carrier. On the other hand, the drug release from the prepared binary solid dispersions was significantly enhanced in comparison to both drug alone and the physical mixtures. Finally solid dispersion of loratadine: PVP K-30 prepared as 1:5 ratio was found to be described by non-Fickian release mechanism and was selected as the best formulation in this study.

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Dissolution mechanism and rate of solid dispersion particles of nilvadipine with hydroxypropylmethylcellulose

Cited by 85 publications

References 13 publications

Tribo-electric charging and adhesion of cellulose ethers and their mixtures with flurbiprofen

Tribo-electric charging and adhesion of cellulose ethers and their mixtures with flurbiprofen

Silymarin-solid dispersions: Characterization and influence of preparation methods on dissolution

Enhancement of Dissolution Profile of Poorly Water Soluble Loratadine by Solid Dispersion Technique

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