A new generation of starch products as excipient in pharmaceutical tablets. I. Preparation and binding properties of high surface area potato starch products

doi:10.1016/0378-5173(95)04383-7

International Journal of Pharmaceutics

Volume 134, Issues 1–2, 28 May 1996, Pages 27-36

https://doi.org/10.1016/0378-5173(95)04383-7 Get rights and content

Abstract

A new pharmaceutical excipient with a high binding capacity was prepared from potato starch by enzymatic degradation, followed by suitable dehydration of the precipitated and filtered retrograded starch to produce high specific surface area products. Thermal dehydration methods like drying at room or elevated temperature and spray-drying resulted in particulate solids with low specific surface area, as measured by nitrogen adsorption, and low compactibility. Both freeze-drying and chemical desiccation, like washing with ethanol or acetone, produced powders with strongly increased specific surface area and increased binding capacity. The compactibility of the final products showed a positive correlation with the specific surface area, changing at high surface areas into constant compactibility. Moreover, the binding capacity appeared to increase with the moisture content of the products.

References (9)

J. Herman et al.
Modified starches as hydrophilic matrices for controlled oral delivery. II. In vitro drug release evaluation of thermally modified starches
Int. J. Pharm.
(1989)
G.H.P. Te Wierik et al.
Preparation, characterization and pharmaceutical application of linear dextrins. VI. General applicability and mechanism of programmed release from amylodextrin tablets
J. Contr. Release
(1993)
G.H.P. Te Wierik et al.
Preparation, characterization and pharmaceutical application of linear dextrins. V. Study on the binding properties of amylodextrin, metastable amylodextrin and metastable amylose
Int. J. Pharm.
(1994)
A.W. Arends-Scholte et al.
Zetmeelprodukten als tabletteerhulpstof, werkwijze voor het bereiden daarvan alsmede werkwijze voor het maken van tabletten
(1994)

There are more references available in the full text version of this article.

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This process is achieved in four stages: atomization of the feed dispersion by a pneumatic system, contact of the sprayed droplets with hot air, fast drying of the sprayed droplets, and separation of the dried particles from the drying air (Master, 1991). This technique has been extensively applied in the to prepare free flowing granules, agglomerates, or spherical particles in a narrow particle size range as well as to develop new excipients for direct compression (Bolhuis, Kussendrager, & Langridge, 2004; Limwong, Sutanthavibul, & Kulvanich, 2004; Te Wierik et al., 1996). It has also been used to modify the physicochemical properties of carbohydrate.
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Research paperA new generation of starch products as excipient in pharmaceutical tablets. I. Preparation and binding properties of high surface area potato starch products

Abstract

Int. J. Pharm.

J. Contr. Release

Int. J. Pharm.

Zetmeelprodukten als tabletteerhulpstof, werkwijze voor het bereiden daarvan alsmede werkwijze voor het maken van tabletten

Research paper
A new generation of starch products as excipient in pharmaceutical tablets. I. Preparation and binding properties of high surface area potato starch products