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Drug delivery system for administering fine particle under tenon's capsule

A technology of eyeball fascia and release system, which is applied in the direction of drug combination, drug delivery, antipyretics, etc., and can solve problems such as unresolved

Inactive Publication Date: 2006-09-20
SANTEN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, the method of intravenous administration of drug-macromolecule conjugates (see Invest. 247871 Bulletin), etc., but the above-mentioned problems have not yet been solved

Method used

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Examples

Experimental program
Comparison scheme
Effect test

manufacture example 1

[0028]Betamethasone (0.05 g) and polylactic acid (0.25 g) with a weight average molecular weight of about 20,000 (dispersion about 2.0) were dissolved in dichloromethane (0.5 mL) and benzyl alcohol (3.0 mL), and the resulting solution was obtained as Drug / polymer solution. A 0.2% (w / v) polyvinyl alcohol aqueous solution (400 mL) was homogenized (10000 rpm) in a homogenizer, and the drug / polymer solution was added dropwise thereto. After the mixture was dropped, the homogenization was continued for 10 minutes to prepare an O / W emulsion. This O / W type emulsion was stirred (200 rpm) with a stirrer for 3 hours. After stirring, the resulting suspension was centrifuged, and the supernatant was removed. To wash the precipitate, ultrapure water (30 mL) was added to disperse the precipitate, and the resulting dispersion was centrifuged again, and the supernatant was removed. Repeat this operation one more time. The washed precipitate was sieved to obtain granules. The obtained par...

manufacture example 2

[0030] Except using "dexamethasone (0.05g)" instead of "betamethasone (0.05g)" in Production Example 1, the same operation as Production Example 1 was carried out to obtain a particle size of 1 μm to 80 μm and a dexamethasone content of about 12% microspheres containing dexamethasone.

manufacture example 3

[0032] In addition to using "fluocinonide acetate (0.05g)" instead of "betamethasone (0.05g)" in Manufacturing Example 1, using "dichloromethane (3.0mL)" instead of "dichloromethane (0.5mL) and benzyl alcohol ( 3.0mL)", except that 2.0% (w / v) polyvinyl alcohol aqueous solution was used instead of 0.2% (w / v) polyvinyl alcohol aqueous solution, the same operation as in Production Example 1 was carried out to obtain fluorine acetate with a particle size of 3 μm to 70 μm. Microspheres containing fluocinolone acetate at a concentration of about 1%.

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PUM

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Abstract

It is intended to provide a continuous drug delivery system targeting a tissue in the posterior segment of eye which needs no frequent administration and shows little tissue invasion. Namely, a drug delivery system whereby a drug is selectively transferred into the posterior segment of eye, thereby lessening effects of the drug transfer on the anterior segment of eye. By administering fine grains containing a drug under Tenon's capsule, a drug delivery system ensuring the selective transfer of the drug toward the posterior segment of eye and maintenance of an efficacious drug concentration can be constructed.

Description

technical field [0001] The present invention relates to a drug release system for retina, choroid, optic nerve and other tissues at the back of the eyeball. Background technique [0002] There are many intractable diseases among the diseases of the retina, choroid, and optic nerve and other tissues at the back of the eye, and the development of effective therapeutic methods is currently expected. For eye diseases, the most common treatment is eye drops, but the drugs basically do not transfer to the retina, choroid and optic nerve and other tissues at the back of the eyeball. Furthermore, it is extremely difficult to maintain drug concentrations in tissues even if transferred. [0003] Therefore, intravenous injection, oral administration, and vitreous injection have been tried as methods of administering drugs for treating diseases of the posterior eyeball. In the case of intravenous injection or oral administration, the amount of transfer of the drug to the tissue of the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K47/34A61K31/573A61K45/00A61P27/02A61F9/00A61K9/00A61K9/16
CPCA61K31/573A61K9/0051A61K9/1647A61P27/02A61P29/00A61P31/00A61P35/00A61P37/00A61P7/00A61K9/10
Inventor 山田和人佐佐木恭正酒井宏之松野圣
Owner SANTEN PHARMA CO LTD
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