ISP Pharmaceuticals Announces New Drug Solubility Initiative at CPhI 2009
Emphasis Will Be on R&D in Support of Ingredient and Processing Technology to Improve Solubility and Bioavailability of Drug Actives
Madrid, Spain, 14 October 2009 – ISP Pharmaceuticals announced that it has embarked upon a Drug Solubility Initiative in support of pharmaceutical companies working with drug actives that exhibit poor solubility. The ISP Drug Solubility Initiative is multi-faceted and will include R&D aimed at advancing the state of solubilization technology, the development and application of a broad portfolio of ingredients for use in solubilization as well as formulation services designed to enhance solubility using different processing approaches for a broad range of actives. The Initiative will see ISP expanding its facilities and personnel dedicated to solubilization efforts, the establishment of alliances with other companies involved in developing technologies for solubilization and outreach programs to the industry.
According to Philip Strenger, Senior Vice President – EMEA & Global Pharma for ISP, enhancing solubility is both a challenge and an opportunity for the pharmaceutical industry. “For the last several years, we have been hearing that more than 60% of drugs in the pharmaceutical developmental pipeline present solubility issues. But drug solubilization technology is much more than just a problem solver. It can open up a number of important opportunities for pharmaceutical companies, such as improved safety and efficacy, better patient compliance and the ability for pharmaceutical companies to maximize their intellectual property over a longer period of time,” he said. “At ISP, we are addressing the solubility issue on a number of fronts, using our expertise in material science and our broad portfolio of ingredients as the foundation for activities ranging from traditional formulation technologies to work with emerging formulation technologies. Every drug active will have its own range of requirements and each project will have physical and cost parameters within which we must work. We feel that by developing a database of solutions, we can help pharmaceutical companies develop workable commercial solutions, rapidly,” he added.
The industry’s biggest challenge
The solubility of a drug active plays an essential role in drug disposition, because the main pathway for drug absorption is the product of permeability and solubility. Today’s solubility dilemma exists in part because of the use of high throughput screening that focuses on compounds with high receptor affinity and selectivity at the expense of biopharmaceutical properties for formulation or delivery. Poor aqueous solubility is caused by two main factors: high hydrophobicity and highly crystalline structures.
The aqueous solubility of a compound is a critical determinant in its success or failure as a drug candidate. Better solubility, for example, will result in better absorption in the GI tract, reduced dosage level requirements and better bioavailability. Poor solubility has both commercial and therapeutic issues throughout the commercialization process. In the development phase, poor solubility can lead to inadequate exposure in both efficacy and toxicity studies. Higher dosages required to compensate for poor solubility can lead to side effects, food effects and intersubject variability. It can drive up overall costs for drug development and production and can lead to poor compliance by patients because of the high doses required to achieve a therapeutic effect.
According to Dr. Tim Bee, Sr. Director, Pharmaceuticals solving solubility problems lead to a number of desirable outcomes.”If we are able to make drugs more soluble, we can reduce development timelines and costs to introduce new drugs while helping to bring products to market more rapidly. It can reduce the dosage costs. We can improve safety and efficacy of the drugs we make and enhance convenience and compliance at the patient level. From a business standpoint, we can imagine creating new methods to reformulate failed or discontinued drugs and we can develop new delivery technologies that can extend the patent protection of existing drugs,” he said.
According to Strenger, ISP Pharmaceuticals is uniquely positioned and now committed to helping the pharmaceutical industry via its Drug Solubility Initiative. “Our business has broad capability for solubility enhancement and a number of touchpoints where we can support pharmaceutical companies along the commercialization process. We have the industry’s broadest ingredient portfolio for enhancing solubility. We have been conducting continuous research into solubility enhancement in our laboratories and will be expanding our efforts in this area. We have a contract services business that focuses on an important solid dispersion technology – spray drying. In fact, we are the only company in our industry that is actively working with both spray drying and hot melt extrusion technology to develop novel solid dispersion forms,” he said. “By solving the solubility dilemma, pharmaceutical companies will be able to offer better healthcare to the people of the world. And in so doing, will open up new opportunities for better business and improved profitability,” he added.