Changing Healthcare Worldwide

THERAPEUTIC OUTCOME CONFIRMED FOR TRANSDERMAL IBUPROFEN

Release issued 02/05/2002

The study, the third 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(R) to deliver a therapeutic dose of Ibuprofen across the skin 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 bio-available and bio- active Ibuprofen. The kinetics analysis of the samples from the previous 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 the best formulation of TDS(R) Ibuprofen of two effective variations identified in the kinetics segments of the study trial was tested against a control of alcohol. The inflammation model for this trial was the plueral edema model. A pleural edema is created in the rat's thoracic cavity in both experimental and control groups. The experimental group received a dose of Ibuprofen delivered via the TDS (R) and the control group received only alcohol on the back. The animals are anesthetized throughout the procedure to avoid ingestion of the test materials. The animals are dosed at baseline and the volumes of fluid withdrawn from the pleural cavities at the end of six hours are compared between the experimental and control groups. The number of cells in the fluid is also compared. In the experimental group, 20% less fluid was recovered and the number of cells was less. The difference between the experimental and control groups was expressed as a two-tailed p Value confidence interval of 0.0006. This outcome demonstrates that the Ibuprofen was delivered across the skin in the test group and accomplished a significant reduction in the inflammation which had been induced in the subject animals.

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(R) can effectively mitigate all of these issues with both NSAIDs and narcotics. The TDS(R) accomplishes the therapeutic outcome that the drug is designed for with much smaller doses than oral equivalents as demonstrated in this trial. 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(R) 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(R) 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(R) 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