Methods and compositions for sustained delivery of drugs

a topical delivery and composition technology, applied in drug compositions, metabolic disorders, cardiovascular disorders, etc., can solve the problems of limited drug delivery system, unique and fairly challenging hurdles for drug delivery, limited transdermal systemic delivery of drugs, etc., to achieve the effect of enhancing uptake and maintaining the health of ideas

a topical delivery and composition technology, applied in drug compositions, metabolic disorders, cardiovascular disorders, etc., can solve the problems of limited drug delivery system, unique and fairly challenging hurdles for drug delivery, limited transdermal systemic delivery of drugs, etc., to achieve the effect of enhancing uptake and maintaining the health of ideas

US20110104206A1Active Publication Date: 2011-05-05INTRATUS

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  • Methods and compositions for sustained delivery of drugs
  • Methods and compositions for sustained delivery of drugs
  • Methods and compositions for sustained delivery of drugs

Examples

Experimental program
Comparison scheme
Effect test

example 1

Treatment of Severe Dry Eye

[0112]Two human patients with preexisting symptomatic severe dry eye were treated as follows. The dry eye condition was assessed by the Schirmers tear test and corneal observations. Each subject received a single application of a lotion containing 1% of pilocarpine and 0.16% caffeine applied to the upper eyelid of the more severely affected eye by direct application of the lotion to the upper eyelid. The effect of treatment was then measured over six hours in regards to tear production and comfort level of the patient.

[0113]There was a rapid increase in tear production in both affected eyes in both subjects. There was an exponential increase in tear production in both patients within one hour of application that was sustained for six hours, as can be seen in FIG. 2.

[0114]Prior to treatment both patients ranked their comfort level of the affected eye as 0 on a scale of 0 to 4 with 0 being the most irritated and 4 being the most comfortable. After applicatio...

example 2

Intraocular Pressure

[0115]A normal human subject was selected to determine the effects of a single application of percutaneous upper eyelid application of a cream / lotion containing 0.2% timolol and 0.16% caffeine to the outer surface skin of one upper eyelid. The intraocular pressure was recorded in both the treated and untreated eye both before and after application of the composition. Additionally, the subject's vital signs, including pulse rate and blood pressure were recorded at the same time intervals as eye pressure was recorded. The effect of treatment was measured for over fifty two hours.

[0116]After a single application of timolol to one eyelid there was a rapid decline in intraocular pressure in both eyes as shown in FIG. 4. The treated eye showed a 73% drop in intraocular pressure within four hours of treatment, which returned to baseline eye pressure within 52 hours. The untreated eye rapidly dropped intraocular pressure by 50% within the same time frame as the treated e...

example 3

Effects of Topical Application of Physostigmine to One Eyelid

[0118]A normal human subject was selected to determine the effects of a single application of percutaneous upper eyelid application of a cream / lotion containing 5% physostigmine, a parasympathetic agonist, 0.16% caffeine to the outer surface skin of one upper eyelid. The effects on tear production, intraocular pressure and pupilary constriction were measured in both the treated and untreated eye both before and after application of the composition. Additionally, the subject's vital signs, including pulse rate and blood pressure were recorded at the same time intervals as eye pressure was recorded. The effect of treatment was measured for over twelve hours. Prior to treatment, the treated eye showed a dryness level of 0, while the untreated eye had a dryness level of 2 mm by Schirmers measurement.

[0119]After a single application of physostigmine to one eyelid there was a rapid increase in tear production from 0 to 5 mm in t...

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Abstract

The present disclosure relates to methods and compositions for the topical sustained delivery of therapeutic agents. Topical application of compositions containing a muscle fasciculating agent result in the sustained release of any therapeutic agent contained within the composition. More particularly, topical application of such compositions to the outer surface of the eyelid of a patient results in increased absorption and sustained release of the therapeutic agent into the eyes or systemically.

Description

CROSS-REFERENCE OF RELATED APPLICATION[0001]This application claims priority to provisional application, U.S. Application No. 61 / 256,614, filed Oct. 30, 2009 and U.S. Application Ser. No. 61 / 289,471, filed Dec. 23, 2009, both of which are incorporated herein by reference thereto.TECHNICAL FIELD[0002]The present invention relates generally to methods and compositions for the controlled topical delivery of drugs. More specifically, the present invention relates to methods and compositions for delivery of one or more drugs to the eye, a specified area of the eye or systemically to a remote target by topical application to at least one upper eyelid and optionally at least one lower eyelid. More specifically, these methods comprise applying a preparation containing the desired drug or combination of drugs to the surface of at least one upper eyelid and optionally at least one lower eyelid, thereby causing transfer of the drug or drugs from the eyelid into the eye or systemic circulation ...

Claims

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Application Information

Patent Timeline
05 May 2011
Publication
US20110104206A1
IPC
A61K31/522; A61K38/28; A61K36/185; A61K31/215; A61K39/08; A61P27/02; A61P3/10; A61P13/12; A61P9/12; A61P9/00; A61P25/34; A61P5/00; A61P35/04
CPC
A61K9/0019; A61K9/0048; A61K9/06; A61K31/519; A61K8/4953; A61K31/522; A61K47/38; A61Q1/10
Inventors
NANDURI, PADMA; DYER, T. AARON