Assessment of Processing and Polymorphic Form Effect on the Powder and Tableting Properties of Microcrystalline Celluloses I and II

Rojas, John; Lopez, A. Ciro; Gamboa, Yudy; González, Christian; Montoya, Fernando

doi:10.1248/cpb.59.603

Cited by 14 publications

(15 citation statements)

References 17 publications

(16 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Production of MCCII pellets using a response surface design MCCII was obtained from cotton linters as reported previously [8]. Approximately, 30g of MCCII was wetted with 30 ml of distilled water and passed through a #20 mesh sieve (841 µm size) with a force ≤ 11.2 N/cm 2 measured with a load cell (LCGD-10K, Omega Engineering, Inc., Stamford, CT).…”

Section: Methodsmentioning

confidence: 99%

“…These phenomena provide a high absorption and moisture retaining properties. The retained water molecules could act as a lubricant during extrusion, and control the pellet shape during spheronization [8]. The aim of this study was to evaluate the impact of spheronization frequency and time, wetting level and sample load on the morphology and particle properties of the resulting MCCII pellets employing a response surface design.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Assessment of the Production Variables on the Pelletization Properties of Microcrystalline Cellulose Ii (Mccii)

Rojas

Correa

2017

Int J Pharm Pharm Sci

Self Cite

View full text Add to dashboard Cite

Objective: To study microcrystalline cellulose II (MCCII) as new pelletization aid using the extrusion/spheronization technology. Methods:The effect of the spheronization rate and spheronization time was assessed by a response surface design. The shape descriptors and physical properties of pellets were taken as response variables. Approximately, 30 g of MCCII were hydrated, passed through a # 20 mesh sieve and spheronizated at frequencies of 6, 9 and 12 Hz and residence times of 15, 240 and 480 s in 9 experimental runs. In a separate experimental set, moisture levels of 25, 50, 75, 100 and 125% were employed at the optimal operating conditions of 6 Hz and 480 s. A microscopy analysis was used to evaluate the shape descriptors. Pellets properties such as compressibility, friability, porosity, strength, flow rate and mass were also evaluated.Results: Pellets having a small size and a high value of shape descriptors related to morphology were obtained employing a spheronization rate and spheronization time of 6Hz and 480s and 100% wetting level. The spheronization time increased pellet densification but decreased the total porosity. Pellet mass was also favoured by using high spheronization rates. A high moisture level (>100%) rendered pellets having a large size, mass, low porosity and good yield. Conversely, pellet size decreased as sample load increased, whereas porosity and compressibility increased as sample load augmented. Conclusion:MCCII offers the potential for use as an alternative pelletization agent rendering pellets having a good flowability, high mechanical strength and low friability at the optimal operational conditions.

show abstract

Section: Methodsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Assessment of the Production Variables on the Pelletization Properties of Microcrystalline Cellulose Ii (Mccii)

Rojas

Correa

2017

Int J Pharm Pharm Sci

Self Cite

View full text Add to dashboard Cite

show abstract

“…It is denser, but less crystalline and ductile than microcrystalline cellulose I (MCCI). Further, microcrystalline cellulose II (MCCII) shows a lower degree of polymerization and faster compact disintegration than MCCI products independent of the processing conditions (9)(10)(11). However, there are no reported studies that evaluate the suitability of MCCII as disintegrant.…”

Section: Introductionmentioning

confidence: 99%

Functional Assessment of Four Types of Disintegrants and their Effect on the Spironolactone Release Properties

2012

Self Cite

View full text Add to dashboard Cite

Abstract. Spironolactone is a drug derived from sterols that exhibits an incomplete oral absorption due to its low water solubility and slow dissolution rate. In this study, formulations of spironolactone with four disintegrants named as croscarmellose sodium, crospovidone, sodium starch glycolate and microcrystalline cellulose II (MCCII) were conducted. The effect of those disintegrants on the tensile strength, disintegration time and dissolution rate of spironolactone-based compacts was evaluated using a factorial design with three categorical factors (filler, lubricant, and disintegrant). The swelling values, water uptake and water sorption studies of these disintegrants all suggested that MCCII compacts disintegrate by a wicking mechanism similar to that of crospovidone, whereas a swelling mechanism was dominant for sodium starch glycolate and croscarmellose sodium. The disintegration time of MCCII and sodium starch glycolate remained unchanged with magnesium stearate. However, this lubricant delayed the disintegration time of crospovidone and croscarmellose sodium. MCCII presented the fastest disintegration time independent of the medium and lubricant employed. The water sorption ratio and swelling values determined sodium starch glycolate followed by croscarmellose sodium as the largest swelling materials, whereas crospovidone and MCCII where the least swelling disintegrants. The swelling property of sodium starch glycolate and croscarmellose sodium was strongly affected by the medium pH. The disintegration time of spironolactone compacts was faster when starch was used as a filler due to the formation of soft compacts. In this case, the type of filler employed rather than the disintegrant had a major effect on the disintegration and dissolution times of spironolactone.

show abstract

mentioning

confidence: 99%

“…For this reason, this excipient is ideal to formulate rapidly disintegrating compacts compared to other cellulosic excipients. 7,8) Processing such as spray drying and wet granulation improved compactibility, dilution potential, flow and powder density due to the transformation of a fiber morphology to a more regularly-shaped particle without changing the apparent plastic deformation mechanism under consolidation. 9) Since MCCII shows lower mechanical properties compared to microcrystalline cellulose I, it is an ideal candidate for coprocessing with a more brittle deforming material having a high surface area such as fumed silica (200 m 2 /g).…”

mentioning

confidence: 99%

Effect of Silicification on the Tableting Performance of Cellulose II: A Novel Multifunctional Excipient

Rojas

Kumar

2012

CHEMICAL & PHARMACEUTICAL BULLETIN

Self Cite

View full text Add to dashboard Cite

The effect of silicification on the tableting performance of microcrystalline cellulose II (MCCII) was assessed through coprocessing with fumed silica via spray drying and wet granulation at the 98 : 2, 95 : 5, 90 : 10 and 80 : 20 ratios. Compacts produced by spray drying and wet granulation rendered better tensile strength than MCCII. The Kawakita and Heckel models implied that silicification increased compressibility and decreased the plastic deforming behavior and densification by die filling at the early stage of compression for MCCII. It also decreased the sensitivity to hydrophobic lubricants such as magnesium stearate, especially for the spray-dried products due to the competing effect with magnesium stearate. Further, silicification decreased the high elastic recovery typical of MCCII due to the increase in specific surface area and fragmenting behavior which contributed to the formation of stronger compacts. Moreover, silicification did not affect the fast disintegrating properties and release rates of poorly soluble drugs such as griseofulvin formulated in tablets compared to those of Prosolv ® SMCC 50 and Prosolv ® SMCC 90. The new silicified materials are appropriate to formulate fast disintegrating tablets by direct compression.Key words coprocessed excipient; direct compression; fumed silica; microcrystalline cellulose II Ideally, during a formulation process a combination of a plastic and brittle material is necessary for optimum tableting performance.1) This combination prevents the storage of too much elastic energy during powder compression, which is associated to the formation of weak compacts and the tendency for capping and lamination.2) Further, excipients with one of these two types of deformation can be coprocessed to produce a synergistic effect by selectively overcoming the disadvantages of the individual components. Such combinations can help improving functionalities such as compaction performance, compressibility and sensitivity to moisture. The products so formed are physically modified in a way that they do not lose their chemical structure and stability. In other words, excipients maintain their independent chemical properties; while, synergistically increase their functional performance.3) Typically, coprocessed materials exhibit superior properties than the parent individual components. The randomized embedding of the components in the particles minimizes their anisotropic behavior. So, deformation can occur along any plane and multiple clean surfaces are formed during the compaction process.4) A major limitation of a coprocessed excipient is that the ratio of the components in a mixture is fixed and in developing a new formulation, a fixed ratio of the excipients may not be an optimum choice for the drug at the dose per tablet under development. 5,6) Microcrystalline cellulose II (MCCII), a new allomorph of cellulose was recently introduced as a new multifunctional excipient, especially due to its great ability to uptake water independent of the processing employed. For this re...

show abstract

Assessment of Processing and Polymorphic Form Effect on the Powder and Tableting Properties of Microcrystalline Celluloses I and II

Cited by 14 publications

References 17 publications

Assessment of the Production Variables on the Pelletization Properties of Microcrystalline Cellulose Ii (Mccii)

Assessment of the Production Variables on the Pelletization Properties of Microcrystalline Cellulose Ii (Mccii)

Functional Assessment of Four Types of Disintegrants and their Effect on the Spironolactone Release Properties

Effect of Silicification on the Tableting Performance of Cellulose II: A Novel Multifunctional Excipient

Contact Info

Product

Resources

About