The six finalists for the CPhI Innovation Awards 2010 have been chosen by the judging panel
Stable solid solution prepared with Soluplus via hot melt extrusion process
Following extensive scrutiny by the judging panel, the six finalists in the CPhI Innovation Awards 2010 have been selected.
Each company will have 20 minutes to present its innovation to the judges on the first morning of the show, and the bronze, silver and gold winners will be announced at the exhibitor party that evening.
The shortlisted companies are: BASF, EmulTech, Microinnova Engineering, SynCo Bio Partners, Thermo Fisher Scientific and Zeon Corporation.
BASF (10.00 – 10.20am) will be presenting Soluplus, a new chemical entity and the first excipient in the market especially designed to form stable solid solutions via hot melt extrusion. It has outstanding solubilisation properties and offers considerable enhancement in the drug release and bioavailability of poorly soluble APIs, BASF says.
Hot melt extrusion has become increasingly important in pharmaceuticals due to its ability to molecularly dissolve a novel drug in a solid solution. The comparably low Tg (glass transition temperature) and melt viscosity of Soluplus enable a more efficient and robust hot melt extrusion process. Furthermore, Soluplus can be extruded at low temperatures, which is beneficial for heat-sensitive APIs.
Soluplus is available in commercial scale from a validated manufacturing process operated under cGMP requirements, and Soluplus is now opening new doors in the pharmaceutical innovation field by enabling many promising drug candidates to reach the market that could not have been formulated with conventional excipients.
Dutch contract development organisation Emultech (10.30 – 10.50am) is also focusing on enhanced drug delivery, but through the development of controlled microspheres. The company’s Emulsion Technology for Micro Encapsulates (ET4ME) is the basis for the development of highly defined microspheres for parenteral, pulmonary and mucosal drug delivery.
Highly defined polymer drug delivering microspheres
Microspheres have long been hailed to be the ideal carrier for challenging and specific drugs. Size, release rate and site of action could be tuned, achieving optimal therapeutic dosage. Using ET4ME, EmulTech can offer development of all kinds of microspheres for controlled drug delivery, encapsulating small molecules to proteins, antigens, etc.
The key benefits of the versatile technology include:
The company is currently working on several development projects, including a targeted chemotherapy; a sustained release anaesthetic products for the treatment of chronic pain; a single shot multiple release vaccine; and several projects to improve the delivery of specific antigens.
Microinnova Engineering (11.00 – 11.20am) has developed three different concepts on full manufacturing scale that bring together the flexibility of batch processing, the performance advantages of continuous processing and the further benefits of process intensification by using microreactors, micro heat exchangers and ultrasound.
200 litres per hour manufacturing plant
Plant redesign concept: This concept integrates microreactors or other microstructured components into existing production plants to achieve considerable improvements. The starting point of this concept is one single process step or similar processes in existing chemical and pharmaceutical plants.
Unit operation concept: The unit operation concept realises, in the form of a SKID construction, a chemical process step in a plant with all related aggregates and measuring devices. That way, individual reaction steps in a continuous process can be achieved without changing the other process steps. This concept is a typical solution for inefficient or difficult process steps. Savings can be generated by higher yields, lower raw material consumption and/or less energy.
Modular multipurpose concept: The modular multi-purpose plant concept combines the advantages of batch technology and continuous process management. The variably combinable and replaceable modules, such as the feed module, the reactor module or the residence-time module, make it possible to create temporary chemical plants for a wide range of different purposes adjusted to the respective product. This concept generates a solution for maximising flexibility and performance.
All manufacturing concepts are commercially available and Microinnova will present three case studies illustrating practical examples of each of the three concepts.
SynCo Bio Partners (11.30 – 11.50am) was contracted by a Japanese biotech company to establish a production process to enable the GMP manufacturing of a live biotherapeutic bulk drug substance and drug product for use in Phase I clinical trials.
The product consists of a live biotherapeutic (a live non-pathogenic micro-organism) used to deliver a therapeutic compound to a specific location within a patient’s body. The product is used in combination with standard chemotherapy in which the micro-organism is specifically targeted to a solid tumour and delivers an enzyme at the tumour site where it converts the chemotherapeutic prodrug (administered separately) to its active form.
The majority of live biotherapeutics are administered orally. However, this product is a parenteral, which adds to the complexity of GMP manufacturing. A parenteral is usually an aseptically produced product, so free of any micro-organisms; however this product is a micro-organism!
The production process developed was seemingly simple, with fermentation of the micro-organism at 100 L scale, harvest and buffer exchange using microfiltration to replace fermentation broth with formulation buffer. However, since culture purity must be absolutely maintained throughout the process as a live biotherapeutic cannot be sterilised prior to entry into the filling facility, the biggest challenge to develop the production process as a fully closed system, in which aseptic handling throughout was key.
A further complication was to ensure that the bulk drug substance was produced, filled into vials (drug product) and frozen within 24 hours, as the live micro-organism is not stable for long periods at room temperature.
Despite these challenges, SynCo has developed and fully validated the production process to enable the production of the bulk drug substance and frozen drug product for the client on time and within budget; GMP manufacture for clinical trial supply will commence in Q1 2011.
Thermo Fisher Scientific (12.00 – 12.20pm) has taken the advanced technology of Raman spectrometry and packaged it in a very small, robust and easy-to-use instrument that not only tests the materials with the press of a button, but returns meaningful answers that don’t require sophisticated interpretation (i.e. a simple ‘pass’ or ‘fail’ result for a given material).
The Thermo Scientific TruScan is a rugged, handheld Raman spectrometer that allows customers to realise huge time and cost savings and to improve quality processes. In many cases, it allows users to test 100% of all incoming materials on the loading dock or on the warehouse floor in under a minute, rather than only testing a statistical sample.
In addition to its dramatically reduced size and heightened ease-of-use, TruScan revolutionises the process by scanning materials right through transparent packaging. In doing so, it allows many materials to be identified without opening them, such as frequently counterfeited drugs like Heparin, malaria tablets and bottles of Viagra. As a result, TruScan saves customers a significant amount of time and money (cost savings of US$1m per year, per instrument).
TruScan’s intuitive user interface and managed workflow minimise user error and ensure even novice users are quickly up and running. Its embedded workflow software ensures the correct Standard Operating Procedure (SOP) or method is followed for each sample, backed by three levels of password-protected user authorisation. The built-in bar code reader minimises transcription errors
Designed for use in 21 CFR Part 11-compliant environments, TruScan has UL and CE certification. It also has built-in self-test diagnostics, including system checks at the start of every measurement, and system calibration to NIST and ASTM standards
Zeon Corporation (12.30 – 12.50pm) has developed a high performance ether solvent, CycloPentyl Methyl Ether (CPME), for process innovation and green chemistry.
This new solvent is an alternative to ether solvents such as THF, diethylether and dioxane, which have some inherent drawbacks of low boiling point, easy peroxide formation, easy solubility in water and inefficient recovery from water.
CPME’s features include high boiling point (106°C), as well as preferable characters: low formation of peroxides; relative stability under acidic or basic conditions; formation of azeotropes with water; a low affinity for water; and small evaporation energy compared with other ethers coupled with narrow explosion range.
These advantages enable some conventional reaction sequences in one pot or easier process as a result of solvent unification and facile isolation of the products, which contribute green chemistry and cost reduction.