Dear Reader: Innovations across the entire package - Pharma ...

More documents

Recommendations

Info

Excipients & Actives for Pharma No. 26, 2011 The most immediate benefit is consistent performance in terms of binding, viscosity and adhesion – plus enhanced stability opens the door for entirely new applications. Formulation with sensitive APIs Formulation stability For example, you can now use Kollidon ® as an alternative to cellulose when working with oxygen-sensitive ingredients. What’s more, the transparent inner lining is compatible with NIR testing – so packaging can remain sealed until the product is actually being used, retaining Kollidon’s original freshness. Thanks to PeroXeal, the best PVP portfolio on the market just got even better. Opens new opportunities for formulation with 0 2 -sensitive APIs Greater choice Provides an alternative to cellulose Greater choice Formulation with sensitive APIs Longer shelf life Formulation stability Allows stable formulaions by reduced API degradation constant K values Improved performance and reliability Longer shelf life Extends excipient shelf life up to 4 years FIGURE 4 Benefits of the new packaging concept to our customers Page 4
Excipients & Actives for Pharma No. 26, 2011 CROSPOVIDONE Binding properties and flow behavior of different crospovidone grades C.Tissen, M.Hilkens, J.Lorenz, P.Kleinebudde Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University Duesseldorf, Germany INTRODUCTION | Crospovidone is a superdisintegrant commonly used in quantities of 2-5 % (w/w) to accelerate the disintegration of tablets. Several grades of Kollidon CL are commercially available and differ only in particle size distribution. The drawbacks of traditional disintegrants are often poor flowability or a negative influence on the compactibility of tableting mixtures. However, robust mechanical properties and low friability should be achieved in order to facilitate further production steps, e.g. coating processes. Therefore, a combination of a dry binder and a disintegrant is often required to improve the mech anical properties of a tablet while still ensuring complete disintegration. The purpose of this study was to investigate the binding properties of crospovidone grades of different particle size distributions and elucidate their influence on tensile strength. METHODS AND MATERIALS | Materials Crospovidone (Kollidon CL, Kollidon CL-F, Kollidon CL-SF, BASF SE, Ludwigshafen, Germany), alpha-lactose monohydrate (Tablettose ® 80, Meggle, Wasserburg, Germany), dicalcium phosphate (Dicaphos ® AN, *Budenheim, Germany), magnesium stearate (Welding, Hamburg, Germany). Methods / Particle size distribution The particle size distribution of the various Kollidon CL grades was analyzed using laser light diffraction (Helos, Sympatec GmbH, Clausthal-Zellerfeld, Germany). Measurements were performed in triplicate with a dry dispersing unit (Vibri, Rhodos T4.1, Sympatec GmbH, Claustha-Zellerfeld, Germany) at 1.0 bar. Flowability The flowability of the tabletting mixtures was analyzed in duplicate with a ring shear tester (RST-01.c, RST-CONTROL 95 Schulze Schuettguttechnik, Wolfenbuettel, Germany). Consolidation stress and unconfined yield strength were used to characterize flowability. Normal stress during pre-shearing was 5000 Pa. Compression of tablets Table 1 shows tabletting mixtures containing different ratios of filler (Tablettose 80, Dicaphos AN) and disintegrant (Kollidon CL; Kollidon CL-F, Kollidon CL-SF). Each formulation was blended for 20 minutes in a laboratory-scale Turbula mixer (Turbula T2F, Bachofen AG Maschinenfabrik, Basel, Switzerland). Afterwards, 0.5% w/w magnesium stearate was added as a lubricant and the mixtures were blended for two further minutes. Each mixture was compressed to flat-faced tablets of 12 mm diameter at 153 and 255 MPa, using a rotary die press (Pressima, IMA Kilian, Cologne, Germany). Crushing forces were determined with a hardness tester (HT-1, Sotax, Basel, Switzerland) and subsequently calculated as tensile strength according to Fell and Newton [1]. TABLE 1 Fraction [%] Filler 100 95 90 80 60 40 0 Disintegrant 0 5 10 20 40 60 100 Tabletting mixtures Disintegration testing The disintegration time for 12 tablets of each batch was measured with a disintegration tester (Erweka ZT 32, Heusenstamm, Germany) according to Ph.Eur. Because of the extreme turbidity of the disintegration medium after a few seconds, all batches were analyzed without using a beaker. RESULTS AND DISCUSSION | Discussion The tensile strength of the lactose/crospovidone tablets varied from 0.9 to 5.1 N/mm² (Figure 1). Irrespective of the amount of Kollidon CL, the tablets exhibited no increase in tensile strength. In contrast, crospovidone grades with smaller particle sizes led to improved tensile strength. The higher the amount of Kollidon CL-F and Kollidon CL-SF, the higher the tensile strength of the resulting tablets. As the particle size of crospovidone decreased, the detected tensile strength increased (Figure 2). The tensile strength of tablets is known to be affected by the variation in particle size of the excipients used. Smaller particles facilitate interparticulate bonding during the compression process, resulting in tablets with improved hardness [2]. Consequently, tablets with Kollidon CL-SF exhibited the highest values. Even 20% (w/w) almost doubled the determined tensile strength. All crospovidone grades could successfully be compressed to tablets without filler; tablets consisting of pure Kollidon CL-SF exhibited the highest tensile strength. Page 5
Page 1 and 2: Excipients & Actives for Pharma No.
Page 3: Excipients & Actives for Pharma No.

Dear Reader: Innovations across the entire package - Pharma ...

You also want an ePaper? Increase the reach of your titles

Delete template?

Save as template?