Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1998-06-16
2000-10-17
Azpuru, Carlos A.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
A61F 214
Patent
active
061327557
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to a new drug release system for the controlled release of drugs over a long period of time.
According to the invention, a transcorneal system for the controlled supply of drugs avoiding the gastrointestinal tract is claimed, which consists essentially of a device which makes it possible to administer a medicinal composition over a long period of time whilst avoiding the corneal skin layers.
The apparatus according to the invention consists essentially of a reservoir for the drug and at least one--typically several--micro-pins provided with capillary openings which are connected to the reservoir in such a way that the drug in the form of a solution containing the active substance passes from the reservoir into the micro-pins. When the transcorneal system is placed on the skin, the Stratum corneum and possibly the epidermis are penetrated by the micro-pins so as to provide direct access to the innervated layer of the skin. In this way the drug can pass from the reservoir through the capillary openings of the micro-pins into vascularised sections of the skin from where it is absorbed into the bloodstream through the capillary circulatory system. Instead of the micro-pins, micro-blades may be used, which scratch the skin when the system is applied.
An essential advantage of the system according to the invention is that the skin barrier for transdermally administered drugs, namely the Stratum corneum, is circumvented with the system according to the invention.
It is precisely the individually different properties of the uppermost horny layer in patients which are the reason for problems such as insufficient bioavailability and allergies when active substances are administered transdermally. One particular advantage of transcorneal administration is that this method of administration is not restricted to those active substances which penetrate through the skin, as is the case with transdermal administration, for example. Examples of suitable active substances include pain killers such as morphine, naltrexone, fentanyl, oxymorphone; anti-Parkinson's agents such as L-dopa, pramipexole; heart and circulatory drugs, nitroglycerin, drugs to combat high blood pressure and vasodilatory disorders, such as clonidine, nifidepine, verapamil and diltiazam; anticoagulants such as heparin and hirudin; agents for long-term therapy in cancers and immune diseases; agents for the long-term treatment of addiction; peptides; ACE-inhibitors; neurokinin antagonists; and hormones such as oestradiol.
Usually, the active substance is present in the form of a solution to allow satisfactory travel through the capillary openings of the micro-pins of the transcorneal system. Theoretically, all physiologically acceptable solvents or solvent mixtures in which the active substance is soluble in a sufficient quantity may be used. The phrase "sufficient quantity" is taken to mean those concentrations of active substance in the solvent which make it possible to administer a therapeutically effective quantity of active substance.
The preferred solvents are water and ethanol. If it should be necessary, solubilisers and complexing agents may be used to increase the solubility of the active substance in the solvent. Delicate active substances may be mixed with additives to increase their shelf life.
The system according to the invention contains a reservoir for storing the active substance solution, whilst a liquid-conveying connection between the reservoir and the micro-pins makes it possible for the drug to be conveyed from the reservoir through the capillary openings of the micro-pins and below the Stratum corneum, so that the drug can be introduced directly into the bloodstream whilst avoiding the outer horny layers.
The transportation of the drug--e.g. in the form of an aqueous solution--may be either "passive", i.e. achieved by the existing concentration gradient between the concentration of the active substance solution in the reservoir and in the blood, or "active", e.g. by means of an overpressure stored in the
REFERENCES:
patent: 3964482 (1976-06-01), Gerstel et al.
Eicher Joachim
Zierenberg Bernd
Azpuru Carlos A.
Boehringer Ingelheim KG
Devlin M-E M.
Raymond R. P.
Stempel A. R.
LandOfFree
Transcorneal drug-release system does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Transcorneal drug-release system, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Transcorneal drug-release system will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-465905