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In This Issue:
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| Formulation Challenges - Enteric Coating of Hard Gelatin Capsules |
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| Authors: Paul Smith, PhD & Manish Ghimire, PhD
The majority of multiparticulate delayed release formulations are comprised of enteric-coated pellets, filled into (uncoated) hard gelatin capsules (HGCs). There is, however, considerable interest in enteric coating of the HGC body:
1. Many new chemical entities present challenges due to instability in acidic gastric fluids or because of irritation to the gastric mucosa. Limited availability of API during the early stages of drug development, coupled with aggressive project timelines, often prohibits the development of an enteric-coated pellet or tablet formulation. The ability to encapsulate the drug within a HGC, which is subsequently enteric-coated, therefore circumvents the necessity to perform expensive and time-consuming formulation development at this stage.
2. Many nutraceuticals benefit from enteric coating; however poor compaction characteristics can prevent high-speed tablet operations. In such cases, enteric-coated HGCs become the presentation of choice.
The enteric coating of HGCs is a challenging and sensitive process. It is essential to create a seal at the union of the two halves of the capsule; without an affective seal enteric failures will be inevitable. The most common approach is “banding,” applying a thin band of gelatin around the seam. Although effective, banding is a time-consuming and expensive process which requires specialized equipment. An alternative strategy is the application of a suitable subcoat onto the HGC prior to enteric coating. The composition of the subcoat is critical in order to achieve good enteric protection. The film should be strong enough to form a robust seal across the capsule join, sufficiently flexible to prevent cracking and exhibit good adhesion to the gelatin substrate.
Nutrateric® nutritional enteric coating system is an aqueous, delayed release coating system approved for nutraceutical and pharmaceutical applications. Colorcon® has developed a procedure for the enteric coating of unbanded HGCs, utilizing a suitable subcoat and <5% weight gain of Nutrateric.
For details, please contact your local Colorcon representative.
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| Recent Advances in Continuous Film Coating Technology for both Delayed and Immediate Release Applications |
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 Author: Charles Cunningham
Improvements in continuous coater design and processes have been developed to ensure uniform and consistent coating from start-to-finish, minimizing or eliminating the potential for product loss. Colorcon conducted two studies evaluating these improvements in both delayed and immediate release applications.
The first study investigated a delayed release coating on mineral oil soft gelatin capsules using Nutrateric nutritional enteric coating in a 24” diameter fully-perforated continuous coating pan (Thomas Engineering Inc.). Three trials evaluated the effects of coating application levels and process throughput on enteric performance.
Consistent enteric performance was achieved for each trial. All soft gels passed disintegration testing, irrespective of whether they were sampled from start-up, continuous, or shut-down modes. Nutrateric coatings provided gastric resistance at low weight gains (3.5%) with high throughput rates.
Study link (PDF 855 KB)>>
The second study evaluated application of a PVA-based Opadry® II complete film coating system on Calcium plus vitamin D tablets in a 30” diameter fully-perforated continuous coating pan (O’Hara Technologies). The tablets were assessed for color development and uniformity in both batch and continuous modes.
In these trials, color development and color uniformity were achieved in a fraction of the time required for a traditional batch coater. Coated tablet throughput rates as high as 1300kg/hour were achieved with no variability in tablet appearance during start-up, shut-down or discharge.
Study link (PDF 571 KB) >>
As manufacturers strive to improve efficiency and reduce costs, innovations in both machinery and film-coating systems offer many opportunities. In these studies, both Opadry II immediate release and Nutrateric delayed release coating systems were well suited for continuous coater applications – making greater profits and higher quality output an attainable goal.
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| Rheometry and Surface Property Analysis of PVA-Based Coatings |
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Author: Charles Cunningham
Opadry II complete film coating systems are fully formulated and optimized for high productivity in film coating processes. The Opadry II 85 series coating systems are based on polyvinyl alcohol (PVA) and designed for immediate release applications. These coatings exhibit exceptionally high adhesion characteristics as well as low viscosity at high solids concentration.
In recent work published by Pfizer, scientists investigated the rheometric and surface tension properties of Opadry II 85 series coatings as related to dosage forms and excipient combinations produced by roll compaction. The effect of pigment addition to the coating systems was also studied.
It was found that the addition of pigments had an influence on suspension viscosity yet all formulations, irrespective of pigment type, did not exceed 250 cP at solids concentrations as high as 25%. Increasing water content did influence the wetting and spreading characteristics of the droplets, but this was also found to be dependent on the ratio of specific excipients in the tablet formulation.
The work conducted by Pfizer helped to address some of the fundamental properties of this coating system as related to optimization of the total tablet formulation for their specific product. Opadry II 85 series film coating systems offer formulators great flexibility in tailoring the use of the coating to address the technical requirements of the tablet formulation and coating process.
Study link (PDF 112 KB) >>
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| Educational Programs |
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Colorcon Formulation School®
Colorcon Formulation School brings together leading experts from industry, academia and Colorcon Technical Centers to provide valuable information on the theory and practical approach to core formulation. In most cases, the format will be a two-day forum; one day of practical work and one day of presentations, including one or more industry speakers.
The Formulation School conducts a range of classes including Fundamentals, School for Matrices, and School for Multi-Particulates.
Here are brief descriptions:
Fundamentals – includes excipient selection, different manufacturing techniques, troubleshooting, and other topics such as regulatory, API characterization, scale-up considerations and new technologies.
School for Matrices – includes best practices to formulate matrices, the importance of QbD, gastro-retentive systems, processing options and the influence of tablet shape and film coating on matrices.
School for Multi-Particulates (MP) – includes features and benefits of the different types of MPs, drug loading best practices, principles of extrusion spheronization, mini-tablet formulation guidelines and equipment review and more.
Here is what some recent attendees had to say about the Colorcon Formulation School:
"The Colorcon speakers were well prepared and fielded the topics with comfort and ease. The special guest speakers were a bonus. I found both speakers to be fascinating and inspiring." Joan Murphy – Teva, USA
"I was very impressed with the expertise of all the various presenters and the capabilities of Colorcon." Eric Liimatta – Albemarle, USA
For more information on our Educational Programs, please click here.
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| Conversation with… |
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Dr. Kamlesh Oza
“What have you done for me lately?” has been the mantra in world culture for quite some time. As far back as the 80’s, Janet Jackson even wrote a hit song about it. However, during our conversation with Dr. Kamlesh Oza, he maintains a different attitude. He asks, “What can we do for you?”
Dr. Oza is the General Manager - Film Coatings at Colorcon, Inc. in West Point, PA. When asked about his team’s focus he began to reminisce even further back than the 80’s. “At Colorcon we have a product range that came out of innovation from the 1960’s, and, we did not stop there. We continued to innovate to offer the first in “lakes” (pigments for pharma use), then liquid dispersions for sugar coating and a ready-to-use dispersion system that made the job easier to get a color match from batch-to-batch and converted an art form to a science.”
He proceeded to describe how the Company has been innovative, developing unique patented technology, such as Opadry®, a ready-to-use powder for film coating and Opadry® II, a fast aqueous film coating. Realizing he could go on and on about the products, Dr. Oza stopped and said, “You know, we don’t just sell a product, we give support that is needed in a competitive environment to maintain and achieve a best-in-class position. We ask, 'What can we do for our customers?'”
Dr. Oza described some of the value-added services that Colorcon offers... 1) Product authentication technologies in the form of unique color, shape with covert and overt markers.
2) Optimize customer’s color inventories by formulating new dosage forms with the most economical, productive and state-of-the art products from existing inventories. 3) Our Brand Enhancement initiative allows our customers to have a trademark and branding option to make their product stand out.
Always thinking about the customer’s needs, it is evident that Dr. Oza’s enthusiasm speaks volumes for the exciting direction that Colorcon is taking with innovation. Continuously looking to improve products and services for their customers, Dr. Oza concluded our conversation with this comment. “'Cheaper, better, faster' will have new meaning for the industry, as this will come with a full service model from Colorcon for solid oral doses. Ultimately, we want to be the 'Formulation Partner.'”
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| Dont Forget About... |
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Starch 1500® Partially Pregelatinized Maize Starch
 Starch 1500 is a unique pharmaceutical excipient combining several properties in a single product. Starch 1500 performs the multiple functions of a binder, disintegrant, and flow-aid while having lubricant properties. It is extremely versatile, being effective in a variety of processing methods for solid oral dosage forms, such as direct compression, wet granulation, dry granulation/roller compaction and encapsulation. Starch 1500 is particularly effective with moisture sensitive actives and low dose applications and exhibits synergy, enhancing the functionality of other commonly used excipients in formulations.
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| Don’t Miss This... |
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CRS Satellite Meeting
Hilton Vienna Danube
March 24-25, 2009
Vienna, Austria |
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CRS has organized a two-day satellite meeting in Vienna, as a forum for technical exchanges concerning the challenges and opportunities that multiparticulate systems may present. We highly recommend that you attend this event, where internationally renowned multiparticulate experts will present and discuss their experiences and latest work on the subject.
The topics will guide you to select most appropriate technology attributes for your API, how to reduce formulation and process development time, and discuss how you should get your product to the market with sound science based data and robust formulation and production. Please make a note in your calendar and secure an early registration, as space is limited.
For more information on the event content, venue and registration, please click here.
We look forward to seeing you in Vienna, March 24-25, 2009.
This event is co-sponsored by Colorcon, Inc. and Evonik Industries
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