OzmoCAP®: The Extended Release Capsule

Advantages of extended release (also known as controlled release) oral dosage forms:

• Reduced frequency of daily dosing. By extending the release of a drug over time, it is often possible to maintain an efficacious level of that drug in the blood stream without the need to swallow medicine multiple times per day. This can provide for improved patient compliance.

• Blunted Cmax/increased Cmin. For a number of drugs, safety issues are directly linked to the blood levels. By metering the drug into the blood stream, oral extended release dosage forms blunt the maximum blood level (Cmax). At the same time, the drug’s extended release can result in a higher level of drug in the bloodstream at the next dosing time (Cmin). Overall, therefore, extending the drug release can increase the time that the drug is within the therapeutic window.

• Reduced local gastro-intestinal tract irritation. With immediate release dosage forms, all the drug is delivered in a relatively narrow region of the GI tract. By more slowly metering out the drug release, extended release dosage forms can reduce side effects associated with high local concentrations of drug in the GI tract.

• Potential line extension. In some cases, the benefits afforded to patients by extended release drug delivery options can also result in patentable inventions.

OzmoCAP® allows rapid development of oral extended release drug products:

• OzmoCAP® provides known in vivo drug delivery rates set by the OzmoCAP® formulation independent of the drug’s properties (e.g., solubility as a function of pH). This means that a clinical trial can determine if a drug will be viable with extended release without the complexity of whether the dosage form itself performs as expected.
• OzmoCAP® delivers the drug with options for release rates, all with good in vitro-in vivo correlation (IVIVC): fast, medium, and slow. This allows a clinical trial to determine an optimized release rate based on the drug’s in vivo performance without having to factor in the uncertainties of dosage form performance. For example, OzmoCAP® will show if a drug is well-absorbed throughout the GI tract or whether that absorption is limited. It will also enable companies to examine strategies to overcome some issues such as solubility in the lower GI tract.
• Because the OzmoCAP® dosage form is a capsule rather than a coated tablet, the OzmoCAP® team can quickly develop a formulation and suitable analytical methods and produce clinical supplies of the drug product (under GMP) ready to ship to a pack/label site.

Producing Your OzmoCAP® Drug Product

The OzmoCAP® team will rapidly develop and produce your controlled release drug product in proprietary OzmoCAP® capsules. This starts with development in our R&D facility and continues to shipment of supplies for animal testing. Here are the steps:

1. 1. The OzmoCAP® technical team will develop the target product profile (TPP) for your product, making sure the desired OzmoCAP® meets the determined needs. The team can also provide expert help in designing the animal testing protocol to best meet the project objectives.
   2. The OzmoCAP® team will formulate the active and produce filled capsules with the desired release rate(s). The capsules can include additives designed to improve bioavailability such as added acids, surfactants, crystal growth inhibitors, and cyclodextrins. The active can also be in the form of a solid dispersion or even some types of liquids (e.g., oils).
   3. The team will develop suitable dissolution methods.
   4. The dissolution performance of the capsules will be confirmed using the developed dissolution method.
   5. OzmoCAP® capsules will be shipped to animal laboratories for testing.
   6. The OzmoCAP® technical team will work with the client to interpret the results of the study and help with the subsequent steps as requested.