Functionality of Cross-Linked Polyvinylpyrrolidone as a Spheronization Aid: A Promising Alternative to Microcrystalline Cellulose

Liew, Celine Valeria; Gu, Li; Soh, Josephine L. P.; Heng, Paul Wan Sia

doi:10.1007/s11095-005-5279-3

Cited by 41 publications

(31 citation statements)

References 29 publications

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“…This meant that MCC grades with a larger W 710 μm value and smaller SSA tend to generate a smaller Torque max . The relationship between packing abilities of MCC powders (bulk and tapped densities) and wet mass consistency has been well established and explained (3)(4)(5)(6). Variables which had very large error bars (confidence intervals) spanning the positive and negative regions were not deemed to have significant effects.…”

Section: Wet Massing Behavior Determined Using Mixer Torque Rheometrymentioning

confidence: 99%

“…From the encouraging performance of crospovidone to aid in extrusion-spheronization, Liew et al (3) concluded that for any given material to serve as a competent spheronization aid, the internal water repository has to possess adequate capacity and rigidity to modulate the amount of water released under pressure for lubrication during extrusion. While many previously proposed materials have the ability to absorb water, these materials lacked the rigidity and binding ability (of MCC) to regulate water distribution by coping with the pressures exerted during extrusion-spheronization.…”

Section: Introductionmentioning

confidence: 99%

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Importance of Small Pores in Microcrystalline Cellulose for Controlling Water Distribution during Extrusion–Spheronization

et al. 2008

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Abstract. The purpose of this research was to investigate the effects of particle size on the wet massing behavior of microcrystalline cellulose (MCC). In this study, a series of six fractionated MCC grades were customized and specially classified to yield different particle size varieties of the standard grade, Comprecel M101. All seven MCC grades were extensively characterized for the physical properties and wet massing behavior using mixer torque rheometry. Effects of MCC physical properties on the maximum torque (Torque max ) were determined using partial least squares (PLS) analysis. Most physical properties varied systematically with particle size and morphological changes. Marked differences were observed in the small pore volumes (V highP ) and BET surface areas of the MCC grades. Variables that exerted dominant influences on Torque max were identified. In particular, the significance of V highP in governing wet mass consistency was established. The role of V highP has not been reported in any study because this small but significant variation is likely to be obliterated or compensated by variation in other physical properties from MCC grades from different suppliers. The findings demonstrated the role of small pores in governing the wet mass consistency of MCC and provide a better understanding of MCC's superior performance as a spheronization aid by the ability to fulfill the function as a molecular sponge to facilitate pellet formation during wet granulation processes.

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Section: Wet Massing Behavior Determined Using Mixer Torque Rheometrymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Importance of Small Pores in Microcrystalline Cellulose for Controlling Water Distribution during Extrusion–Spheronization

et al. 2008

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“…A socalled spheronization aid is generally needed to provide the moistened bulk (paste) with the above-stated rheological properties (5). In this respect, microcrystalline cellulose (MCC) is widely regarded as a key excipient due to its potential for retaining large amounts of moistening liquid that imparts binding, lubricating and plasticizing properties to the mass (1,(6)(7)(8).…”

Section: Introductionmentioning

confidence: 99%

The Use of ß-Cyclodextrin in the Manufacturing of Disintegrating Pellets with Improved Dissolution Performances

et al. 2008

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Abstract. It has recently been highlighted that the release behavior of pellets containing microcystalline cellulose (MCC) as the spheronizing agent may be impaired by the lack of disintegration. Although alternative spheronizing excipients have been proposed, their overall advantages have not thoroughly been assessed. In the present work, the possible use of β-cyclodextrin (βCD) was therefore explored for the manufacturing of pellets with a potential for effective disintegration and immediate release of poorly soluble active ingredients. MCC/βCD powder formulations containing no drug or model drugs with different water solubility, able to form inclusion compounds with the employed cyclodextrin, were pelletized by agglomeration in rotary fluid bed equipment. By applying successive statistical experimental designs, the most critical formulation and operating parameters were identified and optimal manufacturing processes were ultimately set up. High yields of pellets provided with satisfactory physical-technological characteristics were obtained using powder formulations with up to 80% βCD. Based on dissolution testing results, the suitability of βCD for the preparation of disintegrating MCCcontaining pellets with improved dissolution performance was finally demonstrated.

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“…Crospovidone is a synthetic, cross-linked homopolymer of N-vinyl-2-pyrrolidone that is free flowing and nonirritating [10][11][12]. Although the linear poly(vinylpyrrolidone) is water soluble, cross-linking leads to the hydrophilic, but water-insoluble, crospovidone.…”

Section: Introductionmentioning

confidence: 99%

“…Polyplasdone ® is the product name for a family of crospovidone products available from International Specialty Products (now Ashland Specialty Ingredients). The totally synthetic production of crospovidone minimizes lot-tolot variability observed with MCC [11]. A well-characterized polymer that is considered biocompatible and nontoxic, crospovidone is generally regarded as safe for use in oral dosage forms administered to humans.…”

Section: Introductionmentioning

confidence: 99%

A Quality by Experimental Design Approach to Assess the Effect of Formulation and Process Variables on the Extrusion and Spheronization of Drug-Loaded Pellets Containing Polyplasdone® XL-10

et al. 2015

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Abstract. Successful pellet production has been reported in literature with cross-linked poly(vinylpyrrolidone), Polyplasdone ® XL-10 and INF-10. In the present study, a quality by experimental design approach was used to assess several formulation and process parameter effects on the characteristics of Polyplasdone ® XL-10 pellets, including pellet size, shape, yield, usable yield, friability, and number of fines. The hypothesis is that design of experiments and appropriate data analysis allow optimization of the Polyplasdone product. High drug loading was achieved using caffeine, a moderately soluble drug to allow in vitro release studies. A five-factor, two-level, half-fractional factorial design (Resolution V) with center point batches allowed mathematical modeling of the influence of the factors and their two-factor interactions on five of the responses. The five factors were Polyplasdone ® level in the powder blend, volume of water in the wet massing step, wet mixing time, spheronizer speed, and spheronization time. Each factor and/or its two-factor interaction with another factor influenced pellet characteristics. The behavior of these materials under various processing conditions and component levels during extrusionspheronization have been assessed, discussed, and explained based on the results. Numerical optimization with a desirability of 0.974 was possible because curvature and lack of fit were not significant with any of the model equations. The values predicted by the optimization described well the observed responses. The hypothesis was thus supported.

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Functionality of Cross-Linked Polyvinylpyrrolidone as a Spheronization Aid: A Promising Alternative to Microcrystalline Cellulose

Cited by 41 publications

References 29 publications

Importance of Small Pores in Microcrystalline Cellulose for Controlling Water Distribution during Extrusion–Spheronization

Importance of Small Pores in Microcrystalline Cellulose for Controlling Water Distribution during Extrusion–Spheronization

The Use of ß-Cyclodextrin in the Manufacturing of Disintegrating Pellets with Improved Dissolution Performances

A Quality by Experimental Design Approach to Assess the Effect of Formulation and Process Variables on the Extrusion and Spheronization of Drug-Loaded Pellets Containing Polyplasdone® XL-10

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