Pharmaceutical Manufacturing, Packaging, and Product Development Studies

Case Study of an Insoluble Compound with Poor Bioavailability

• IriSys’ first use of and success with technology in 1997
• Client needed to move into clinic as soon as possible
• IriSys suggested a lipid based dosage form
• IriSys improved bioavailability from 5% to 90%
• IriSys’ formulation enabled client to enter the clinic, satisfy investors, obtain additional financing and soon thereafter, file an Initial Public Offering
• The drug product is currently in Phase III in the form of a tablet.  If the tablet dosage form, requiring significantly more time, had been pursued initially, essential data would have been delayed substantially, from 1 to 2 years and as a result, investors may have responded less aggressively.

Case Study of a Formulation Content Uniformity Issue due to the
Low Dosage Strength

• Compound was highly potent, a low dosage was indicated
• Chemical compatibility of compound was determined using a matrix of excipients selected from lipophilic and hydrophilic vehicles and surfactants
• Candidate formulations were prepared using compatible excipients expected to provide desirable microemulsion properties
• IriSys developed a self microemulsifying system
• Phase III trials initiated

Case study of a Compound Characterized by Insolubility in Water, Poor Solubility in Oil, and Acid Lability

• Poor bioavailability demonstrated in early clinical trials
• IriSys developed a semi solid matrix which was liquefied by heating for capsule filling
• Capsules were enteric coated to protect active ingredient from degradation in acid
• Dog and human studies showed significant improvement in bioavailability

Case Study of an Insoluble Compound

• Client specified that compound must move into clinic as soon as possible
• IriSys developed a pharaceutical formulation that provided acceptable bioavailability, stability and indication of efficacy
• Drug product is currently in advanced clinical trials

Case Study of a Water Sensitive Compound

• IriSys developed a semi solid matrix to stabilize the orally bioavailable oncology compound
• Hydroxypropyl Methylcellulose (HPMC) V-Caps, a gelatin alternative for hygroscopic formulations, were used
• A U.S. Patent was filed for a novel formulation specific to the compound
• Drug product currently in Phase I.
  

Cast Study of a Compound Prone to Deliquescence at Room Temperature

• IriSys protected drug by incorporating it into a multicomponent liquid vehicle, all work performed under nitrogen
• Moisture uptake was used to determine formulation acceptability
• Drug product entering Phase I