Extended release biodegradable ocular implants

a biodegradable, ocular implant technology, applied in the direction of drugs, prostheses, immunological disorders, etc., can solve the problems of more serious vision loss, slow or sudden painless loss of vision, and macula break down

Inactive Publication Date: 2008-10-02
ALLERGAN INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Macular degeneration results in a break down the macula, the light-sensitive part of the retina responsible for the sharp, direct vision needed to read or drive.
The wet form of the disease usually leads to more serious vision loss.
Macular degeneration can produce a slow or sudden painless loss of vision.
This leakage causes retinal cells to die and creates blind spots in central vision.
Macular edema (“ME”) can result in a swelling of the macula.
A major problem with topical and oral drug administration is the inability of the drug to achieve an adequate (i.e. therapeutic) intraocular concentration.
Unfortunately, these high drug plasma levels commonly l...

Method used

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  • Extended release biodegradable ocular implants
  • Extended release biodegradable ocular implants
  • Extended release biodegradable ocular implants

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Dexamethasone Three Implant Extended Release System

[0114]A bioerodible implant system for extended delivery of dexamethasone was made by mixing the active agent dexamethasone (Pharmacia Corp., Peapack, N.J.) separately with each of the following three different polymers:

[0115]1. poly (D,L-lactide) (R104, Boehringer Ingelheim GmbH, Germany),

[0116]2. poly(D,L-lactide-co-glycolide) as a 75:25 (wt % / wt %) blend of lactide:glycolide (RG755, Boehringer Ingelheim GmbH, Germany), and;

[0117]3. poly (D,L-lactide) (R203, Boehringer Ingelheim GmbH, Germany), so as to obtain three different dexamethasone-polymer mixes.

[0118]R203 and R104 both are poly(D,L-lactide) polymers, but with different molecular weights. The molecular weight for R203 is about 14,000, while the molecular weight for R104 is about 3,500. RG755 is a poly(lactide-co-glycolide) co-polymer. The molecular weight of RG755 is about 40,000.

[0119]The dexamethasone and one of the three polymers specified above were thor...

example 2

In vitro Release of Dexamethasone from Three Implant Extended Release System

[0121]Cumulative release of dexamethasone from the three implant system of Example 1 was measured in vitro. The three implant system was placed in a glass vial filled with receptor medium (0.1 M phosphate solution, pH 4.4, at 37 degrees C.). To allow for “infinite sink” conditions, the receptor medium volume was chosen so that the concentration would never exceed 5% of saturation. To minimize secondary transport phenomena, e.g. concentration polarization in the stagnant boundary layer, the glass vial was placed into a shaking Water bath at 37° C. Samples were taken for HPLC analysis from the vial at defined time points. The concentration values were used to calculate the cumulative release data, as shown in Table 1 and the corresponding FIG. 1. In Table 1 “Day” is the day of the in vitro measurement of the cumulative amount of dexamethasone released from the three implants, “Cum.” is an abbreviation for cumm...

example 3

In vivo Release of Dexamethasone from Three Implant Extended Release System

[0124]The three implant system of Example 1 was implanted into the vitreous of the eyes of eight rabbits. This was carried out by loading the three implants of Example 1 into a simple trocar with a sample holder and plunger, making an incision through the lower front sclera, inserting the trocar through the scleral incision, and depressing the trocar plunger to deposit the three implants of Example 1 into the vitreous. The in vivo vitreous concentrations of dexamethasone were monitored by vitreous sampling, using LC / MS (liquid chromatography and mass spectrometry). The dexamethasone concentrations for each eye were measured at days 7, 30, 60, 90, 120, 150, 180, 210 and 240 and 360 for the three implant system of Example 1. The averaged results of one mixed concentration measurement are set forth by the two left hand side columns of Table 2.

[0125]Comparison studies were also carried out using single (Posurdex)...

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Abstract

Biodegradable implants sized and suitable for implantation in an ocular region or site and methods for treating ocular conditions. The implants provide an extended release of an active agent at a therapeutically effective amount for a period of time between 50 days and one year, or longer.

Description

BACKGROUND[0001]This invention relates to implants and methods for treating an ocular condition. In particular the present invention relates to implants and methods for treating an ocular condition by implanting into an ocular region or site an extended release bioerodible implant comprising an active agent and a bioerodible polymer. The bioerodible implants of this invention have varying and extended release rates to provide for improved kinetics of release of one or more active (therapeutic) agents over time.[0002]An ocular condition can include a disease, aliment or condition which affects or involves the eye or one of the parts or regions of the eye. Broadly speaking the eye includes the eyeball and the tissues and fluids which constitute the eyeball, the periocular muscles (such as the oblique and rectus muscles) and the portion of the optic nerve which is within or adjacent to the eyeball. An anterior ocular condition is a disease, ailment or condition which affects or which i...

Claims

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Application Information

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IPC IPC(8): A61F2/00A61K31/56A61P27/02A61K9/00A61K9/14A61K9/20A61K31/57
CPCA61K9/0051A61K9/204A61K31/573A61K47/34A61K31/57A61P27/02A61P29/00A61P37/08
Inventor NIVAGGIOLI, THIERRYSHIAH, JANE GUOLIN, QING
Owner ALLERGAN INC
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