What’s New at AAPS: Materials

The American Association of Pharmaceutical Scientists (AAPS) annual show took place in Denver, Colorado, on November 13-17.

Whilst it is nowhere near the size of CPhI Worldwide, several hundred exhibitors were present from the worlds of drug formulation and delivery, related equipment and machinery and analytical and CRO services, and some had innovations on show. Here we round the key ones in materials.

Capsugel was stressing is new EnTRinsic drug delivery technology. This is designed to provide oral delivery with full enteric protection and rapid release in the upper gastrointestinal (GI) tract, without the use of coatings. Tailored, two-piece enteric hard capsules are manufactured using pharmaceutical grades of 100% cellulosic derivatives and they release rapidly at pH 5.5, for optimal absorption in the upper GI tract.

The technology is said to be particularly suited to molecules like peptides, vaccines or live biotherapeutics, which are either sensitive to coating solutions or cannot withstand the heat associated with applying coatings. According to independent research cited by Capsugel, removing the need for enteric coating can save up to nine months’ time in Phase III trials. The use of EnTRinsic technology can also accelerate and simply prototype development and rapid in vivo testing of products requiring enteric protection of targeted release to the GI tract.

In parallel, Capsugel has launched its Vcaps Plus range of polymeric capsules. Based on hydroxypropyl methylcellulose (HPMC) from wood pulp, they are said to give immediate release in vivo performance comparable to that of gelatine; in tests with acetaminophen, their bioequivalence as measured in mean plasma concentration over 24 hours was basically identical.

Vcaps Plus are made via a newly developed gelation process, so that they avoid the addition of gelling systems and can release their contents independent of the pH and ionic strength of the test media. This reduction in variability, the company says, means that they “are quickly becoming a powerful new tool to reduce timelines in drug product development”.

In a similar field, Japan’s Nippon Soda has developed HPC VH/VH-FP, which is due to be launched in spring 2017 as the latest addition to its Nisso HPC range of excipients. Like them it is based on hydroxypropyl cellulose (HPC) and is manufactured by the same process. It is a water-soluble polymer that swells and becomes a hydro-gel in water

HPC VH and VH-FP is said to have the highest level of solution of viscosity for any HPC made from wood pulp, offering sustained release and viscosity enhancement when compared to existing Nisso HPC grades and other commonly used cellulose derivatives. It is more stable than other high-viscosity cellulose derivatives. Trials with Carbamazepine and Theophylline in tablet formulations showed VH-FP to have acceptable physical properties and the longest sustained drug release, the company states.

Opadry QX – the name comes from the words ‘quick’ and ‘flexible’ – is the latest extension to an established line of film coating systems from Colorcon. This is described as a low viscosity formulation that is mixed with water and ready for use in 25 minutes or fewer, even at up to 35% solids w/w, while staying well below the recommended level of viscosity.

Colorcon cites studies showing that Opadry QX achieves the typical weight gain of 3% in 31 minutes at 35% solids at a spray rate of 350-375 gram/minute. By comparison, the existing Opadry and Opadry II take 77 and 58 minutes at 15% and 20% solids respectively. All this means, the company says, “that films are applied faster, color uniformity reached earlier and all coated tablets have a uniform, defect-free finished appearance”.

Two major European-based players had line extensions in polymers. Evonik added the methacrylic polymer Eudragit FS 100 to its existing range of excipients for solubility enhancement and targeted treatment of diseases of the colon. Key properties are listed as excellent solubility enhancement, outstanding thermoelastic properties, high miscibility with APIs and other excipients and solubility in both common solvents and in intestinal conditions It can also form hydrogen bonds and/or ionic interactions for additional specific effects.

A poster at AAPS showed how solid dispersions of Nivedita Chemicals’ Felopidine, a drug with low water solubility, was prepared using Eudragit FS 100 as the carrier polymer by spray drying and melt extrusion. Different formulations achieved both colon targeting and significant solubility enhancement by comparison with the pure drug and physical mixtures, according to a research team at Evonik India.

BASF’s new Kollicoat MAE 100-55 is a methacrylic acid and ethyl acetate copolymer, similar in nature to Eudragit and positioned in direct competition with it, according to a company spokesman in Denver. The new product is a non-neutralized powder, in contrast to the pre-neutralized Kollicoat MAE 100 P and to Kollicoat MAE 30 DP, which is supplied as a dispersion.

BASF is seeking to position Kollicoat MAE 100-55 as a direct replacement for existing pH 5.5 enteric release coating polymers, stressing the major advantage of having larger dry powder particles than comparable 100-55 coating grades. Thus, it is significantly less dusty, while providing equivalent drug release: studies with Bupropion HCl tablets showed its release properties to be almost exactly the same as those of a comparable grade, the company said.


Nice Insight

Nice Insight, established in 2010, is the research division of That’s Nice, A Science Agency, providing data and analysis from proprietary annual surveys, custom primary qualitative and quantitative research as well as extensive secondary research. Current annual surveys include The Nice Insight Contract Development & Manufacturing (CDMO/CMO), Survey The Nice Insight Contract Research - Preclinical and Clinical (CRO) Survey, The Nice Insight Pharmaceutical Equipment Survey, and The Nice Insight Pharmaceutical Excipients Survey.