Changing Healthcare Worldwide

FURTHER PRE-CLINICAL RESULTS ON TDS® IBUPROFEN

Release issued 11/25/2001

The study, the second in a series of three overseen by Prof. Derek Willoughby and completed by Dr. Chandan A.S. Alam, of the Department of Experimental Pathology of the William Harvey Institute at St. Bartholomew's and the Royal London School of Medicine and Dentistry and Dr. Atholl Johnston of St. Georges Hospital Medical School, measured the ability of the TDS technology to deliver Ibuprofen across the skin in a sufficient dose to accomplish a therapeutic outcome without a patch or other appliance. Data from the study confirms company claims that the TDS technology enables rapid penetration and increased blood concentrations of Ibuprofen. The analysis of the samples from this trial was performed at St. Georges Medical School under full GLP protocol. This trial expands documentation of the fifth drug delivered successfully utilizing the TDS technology.

The model for the study was the white rat and two different variations of TDS Ibuprofen identified in the previous pilot trial were trialed against a control of Ibuprofen in alcohol. Each of the three formula variations were applied to 12 animals per formula. Blood samples were obtained at baseline, two hours, four hours and six hours. Both formulations were successful at delivering a dose of the drug with average blood levels of the test material- delivered Ibuprofen at 22.4 micrograms per mL at 2 hours, 28.5 micrograms per mL at 4 hours and 26.3 at 6 hours.

The company anticipates that therapeutic outcome studies suggested by this data will be performed shortly. This data is particularly encouraging in light of the fact that rats and mice metabolize Ibuprofen at a rate five times faster than human metabolism, but the TDS was nevertheless successful at achieving and maintaining a detectable blood level in the animals over six hours from a single dose. The need for alternative dosing capability as provided by transdermal means is particularly felt in the case of analgesics and narcotic pain relievers. Many patients poorly tolerate NSAIDs or non-steroidal anti-inflammatory drugs including ibuprofen due to gastro-intestinal distress and liver metabolism issues. Patients must be particularly careful about consuming alcohol with many of these drugs due to interactions between them. Narcotics, while highly effective pain relievers are also very dosesensitive with potentially lethal side effects for over-dose. The TDS can effectively mitigate all of these issues with both NSAIDs and narcotics.

The TDS accomplishes the therapeutic outcome that the drug is designed for with much smaller doses than oral equivalents as demonstrated in the company's successful pre-clinical studies of Morphine Sulphate. By bypassing the gut and first-pass circulation from the gut to the liver, GI distress and liver metabolites are eliminated or minimized. The TDS can be modified to deliver a concentrated dose to a local area, which is not broadly distributed throughout the body. This capability, coupled with the smaller doses possible with the TDS(tm) enables much safer narcotic dosing that virtually eliminates the possibility of overdose and greatly reduces tolerance- building that leads to addiction. TransDermal Technologies is actively seeking a licensing partner or partners interested in exploiting this technology.

The TDS(tm) is a platform system that is designed to be modified for each application and is believed to enable the rapid, safe and effective delivery of many medicaments across intact skin by means of its sprayed on or applicator applied lotions.

Company Contact: Kenneth B. Kirby - k.kirby@transdermaltechnologies.com / 800-282-5511 / 561- 848-9100