This section describes Improved Pharma’s offerings in two areas:
1. Synchrotron-based formulation design
2. Accelerated Formulation Development and Fast to IND (fIND)
Synchrotron-Based Formulation Design
Improper formulation selection or solid form selection can slow development and greatly increase costs. With the increased information Synchrotron-based studies provide, it is possible to greatly accelerate development by quickly finding the most stable and most soluble formulation.
· Formulations including improved formulations of existing products
o Improved Pharma uses its knowledge in solid-state chemistry and its access to Synchrotron facilities to design a solid form for formulation. In some cases Improved Pharma’s formulation design work will include the development of a preliminary IVIVC (in-vivo in-vitro correlation) dissolution test. Improved Pharma has extensive experience with amorphous formulations, spray drying, gel caps, SECs, coated particles, microencapsulation, roller compaction, granulation and other methods. Improved Pharma also has extensive experience with stabilizing unstable formulations. Improved Pharma can also resolve a wide range of formulation problems.
· Amorphous forms, polymorphs, solvates, salts, nanoparticles
o Utilizing Synchrotron-based analytical and pair distribution function data, Improved Pharma provides an expert assessment of the current status of your polymorph screening activities. These Synchrotron-based studies provide structural knowledge and also analytical information at/near the lowest possible detection limit. Improved Pharma may suggest additional experiments or approaches to determine which form is most stable. Improved Pharma can also use its superior expertise in solid state chemistry to design a solid form screening and selection process based on the structure and known properties of the starting drug. Finally, Improved Pharma can suggest when it is most appropriate to search for salts, cocrystals, or amorphous forms typically utilizing Synchrotron-based approaches
o Polymorphism and solid-state chemistry are the lynchpin in successful fast development. Improved Pharma uses its knowledge and expertise with Synchrotron-based data to get the solid-state chemistry right in a fast economical way. Thus stability, handling, and solubility problems are avoided and development is accelerated.
o Solubility – Getting the solid-state chemistry right is particularly important for poorly soluble compounds. For these materials, it is possible to gain substantial improvement in solubility by using the proper solid form – typically a salt, amorphous form or cocrystal. Additionally, materials milled to small particle size with surfactants provide another approach to enhancing solubility. Improved Pharma’s strategies are superior for poorly soluble compounds.
o Particle size – Improved Pharma has extensive experience with particle size issues and analytical methods to determine particle size. It is critical to understand particle size in the manufactured lot(s). Furthermore, in some cases, milling with surfactants is sufficient to achieve the desired solubility. Improved Pharma has the experience and knowledge to understand particle size effects on bioavailability and stability.
o An IVIVC or relationship can be extremely helpful in formulation design. Improved Pharma is capable of carrying out the screening experiments necessary to find a medium for an IVIVC, if possible. Improved Pharma could use dog or pig bioavailability data for these studies if requested.
Accelerated Formulation Development and Fast to IND (fIND)
Improved Pharma performs the following four steps to accelerate development of the best form and formulation.
1. Preformulation – Solid state chemistry and solid state properties
This step is key to finding the right form of your drug candidate. Improved Pharma helps you evaluate or discover new forms and select the best one for development. If needed, Improved Pharma can conduct a polymorph screen and determine the structure of the forms produced.
2. Amorphous screening or salt screening
If your molecule is poorly soluble Improved Pharma can perform amorphous screening and salt screening utilizing Synchrotron data to find the best form to take into the clinic and also the best form to insure good exposure in toxicology studies. Improved Pharma has high-level project directors who make sure the form chosen is the best for your particular needs.
Improved Pharma also selects the best formulation for the chosen form to ensure stability and good performance and verifies the stability of this form using structural information based on Synchrotron analysis and accelerated stability studies. Improved Pharma provides a protocol tailored to your specific needs.
3. Toxicity testing-Enhanced Exposure
Improved Pharma’s studies will lead to the best formulation for GLP studies and a method of testing using this formulation. Improved Pharma can arrange for GLP testing if required. Improved Pharma can avoid delays by close coordination with its closely linked GLP laboratories.
4. IND submission and GMP manufacturing
Improved Pharma’s studies will provide you with all of the information needed to manufacture Phase I supplies and can arrange for this manufacturing at a site nearby.
Thus, Improved Pharma has the skills and interest to work with you to make sure your molecule makes it to the clinic in an optimum formulation