ACRYL-EZE. Application Data. Enteric Coating of Tablets with Debossed Logos OBJECTIVES METHODS AND MATERIALS. Acryl-EZE - 1 -

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ACRYL-EZE Application Data Aqueous Acrylic Enteric System Enteric Coating of Tablets with Debossed Logos OBJECTIVES Concerns over film uniformity and film defects have led to an avoidance of debossed logos on enteric coated tablets. The aim of this study is to demonstrate that careful selection of tablet shape, logo design and logo placement will result in a robust enteric coating and avoid the need to subject tablets to the printing operation. METHODS AND MATERIALS A direct compression blend was prepared comprising aspirin (Rhodine 2371, Rhodia, Cranbury, NJ), microcrystalline cellulose (Emcocel 90M, JRS Pharma, Patterson, NY) and stearic acid (Purified vegetable grade powder, Oleotec Ltd., London, England). Aspirin 325mg tablets were compressed to the same breaking force using round 0.4062 compound radius compression tooling with varying engraving styles and logo placement (Natoli, St. Charles, MO). The characters ABC26 were chosen to represent a range of design complexity. The logos were placed centrally across the face of the tablet or around the perimeter of the tablet. A single stroke cut engraving style with a constant width, draft angle (40º), and depth, terminating with a full, single blend radius was compared to a panel cut with a flat area on the bottom surface. Plain, non-logo, tablets were also produced as a control. Figure 1. Central Logo Placement Figure 2. Perimeter Logo Placement Acryl-EZE - 1 -

A fully formulated aqueous enteric coating system based on Eudragit L100-55* (Acryl-EZE, Colorcon, WestPoint, PA) and an aqueous film coating system (Opadry, complete film coating system, Colorcon, West Point, PA) were used. The delayed release coatings were carried out in a fully perforated, side-vented pan. Tablets were coated directly with the delayed release coating system or after the application of a 2.0% weight gain sub-coat. Tablet samples were taken at a theoretical 6, 7, 8, 9 and 10 % (4 and 5% with sub-coat) delayed release coating weight gain for enteric performance testing and examination of logo definition. Enteric performance (acid resistance) was assessed using a variation of the enteric disintegration method (European Pharmacopoeia 3rd Edition 2001 supplement). Six delayed release-coated tablets were individually weighed and subjected to 0.1N HCL for 2 hours. The tablets that were still intact were removed from acid and reweighed to obtain the % acid uptake. Values less than 5% have been found to pass the acid phase of delayed release dissolution testing. 1 RESULTS Visual examination of the tablets after coating revealed that good logo clarity was maintained up to the 10% delayed release coating weight gain studied. The clarity of the logos was consistent irrespective of the logo design type or placement. Acid resistance testing showed that the tablets were robust and withstood acid penetration at less than the final delayed release coating weight gain of 10%. There was no difference in the results between the tablets of differing engraving styles or logo placement. Figure 3. Logo Placement Central No Sub-coat Perimeter No Sub-coat Acryl-EZE - 2 -

Figure 4. Acid Uptake Results No Sub-coat Figure 5. Logo Placement Central With Sub-coat Perimeter With Sub-coat Figure 6. Acid Uptake Results With Sub- coat Acid Uptake (%) Acid Uptake (%) Acryl-EZE - 3 -

Failures that did occur were found at the edges of the tablets rather than the logos. At no point in testing were defects found within the logos that resulted in enteric failure as had been historically expected. It was also found that the application of a sub-coat made little difference in logo clarity but significantly reduced the quantity of delayed release coating needed for good acid resistance. Sub-coat application primarily adds strength to the outer edges of the tablet core and reduces edge related defects when the tablet mechanical strength is deficient. CONCLUSIONS The use of typical logo engraving styles and logo placement had no effect on acid resistance or clarity of logos. The delayed release coating system used in this study exhibited good adhesion characteristics further contributing to the clarity of the logos and good enteric protection. Edge wear was found to be the most critical factor in enteric performance. Further processes for the branding and identification of tablets such as printing can be eliminated through proper selection of tablet shape, logo design and enteric coating system. Adapted from the poster presented at CRS Jul 2004. Acryl-EZE - 4 -

References 1. Jordan, M.P., Taylor, J., Hadfield, P.J.; A Comparison of the Performance Characteristics of Enteric Film Coating Systems, Contributed paper, AAPS National Meeting, October (2001). The information contained herein, to the best of Colorcon, Inc. s knowledge is true and accurate. Any recommendations or suggestions of Colorcon, Inc. with regard to the products provided by Colorcon, Inc. are made without warranty, either implied or expressed, because of the variations in methods, conditions and equipment which may be used in commercially processing the products, and no such warranties are made for the suitability of the products for any applications that you may have disclosed. Colorcon, Inc. shall not be liable for loss of profit or for incidental, special or consequential loss or damages. Colorcon, Inc. makes no warranty, either expressed or implied, that the use of the products provided by Colorcon, Inc., will not infringe any trademark, trade name, copyright, patent or other rights held by any third person or entity when used in the customer s application. For more information, contact your Colorcon representative or call: North America Europe/Middle East/Africa +1-215-699-7733 +44 (0)-1322-293000 Latin America India China +54-11-5556-7700 +91-832-6727373 +86-21-61982300 Acryl-EZE - 5 - You can also visit our website at www.colorcon.com Colorcon, 2009. The information contained in this document is proprietary to Colorcon and may not be used or disseminated inappropriately. All trademarks, except where noted, are property of BPSI Holdings, LLC. ads_acryleze_ent_coat_tab_v4_08.2016