IPC분류정보
국가/구분 |
United States(US) Patent
등록
|
국제특허분류(IPC7판) |
|
출원번호 |
US-0152780
(2011-06-03)
|
등록번호 |
US-8445027
(2013-05-21)
|
발명자
/ 주소 |
- Hughes, Patrick M.
- Boix, Michele
- Sarrazin, Christian
- Do, Marina
|
출원인 / 주소 |
|
대리인 / 주소 |
|
인용정보 |
피인용 횟수 :
19 인용 특허 :
126 |
초록
▼
Biocompatible intraocular implants, such as microparticles, include a prostamide component and a biodegradable polymer that is effective in facilitating release of the prostamide component into an eye for an extended period of time. The prostamide component may be associated with a biodegradable pol
Biocompatible intraocular implants, such as microparticles, include a prostamide component and a biodegradable polymer that is effective in facilitating release of the prostamide component into an eye for an extended period of time. The prostamide component may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. Or, the prostamide component may be encapsulated by the polymeric component. The present implants include oil-in-oil emulsified implants or microparticles. Methods of producing the present implants are also described. The implants may be placed in an eye to treat or reduce at least one symptom of an ocular condition, such as glaucoma.
대표청구항
▼
1. A method for producing therapeutic polymeric microparticles, comprising encapsulating a prostamide component with a polymeric component to form a population of prostamide-encapsulated microparticles by an oil-in-oil emulsion process, wherein the polymeric component comprises a poly(lactide-co-gly
1. A method for producing therapeutic polymeric microparticles, comprising encapsulating a prostamide component with a polymeric component to form a population of prostamide-encapsulated microparticles by an oil-in-oil emulsion process, wherein the polymeric component comprises a poly(lactide-co-glycolide) (PLGA) copolymer, the oil-in-oil emulsion process comprising: forming a first composition comprising a prostamide component, a poly(lactide-co-glycolide) (PLGA) copolymer, and an organic solvent;forming a second oil-containing composition;mixing the first composition and the second oil-containing composition to form an oil-in-oil emulsion;drying the emulsion to form a dried emulsion product;contacting the dried emulsion product with a solvent to form a solvent-containing composition;removing the solvent from the solvent-containing composition to form a population of microparticles having a maximum particle diameter less than about 200 μm and comprising the prostamide component and the polymeric component; andterminally sterilizing the polymeric microparticles, wherein at least 80% of the prostamide component remains stable after sterilization; and wherein the prostamide component comprises a compound having the formula (I) wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A is an alkylene or alkenylene radical having from two to six carbon atoms, which radical may be interrupted by one or more oxide radicals and substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups wherein said alkyl radical comprises from one to six carbon atoms; B is a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical, selected from the group consisting of hydrocarbyl aryl and heteroaryl radicals having from four to ten carbon atoms wherein the heteroatom is selected from the group consisting of nitrogen, oxygen and sulfur atoms; X is —N(R4)2 wherein R4 is selected from the group consisting of hydrogen, a lower alkyl radical having from one to six carbon atoms, wherein R5 is a lower alkyl radical having from one to six carbon atoms; Z is ═O or represents 2 hydrogen radicals; one of R1 and R2 is ═O, —OH or a —O(CO)R6 group, and the other one is —OH or —O(CO)R6, or R1 is ═O and R2 is H, wherein R6 is a saturated or unsaturated acyclic hydrocarbon group having from 1 to about 20 carbon atoms, or —(CH2)mR7 wherein m is 0 or an integer of from 1 to 10, and R7 is cycloalkyl radical, having from three to seven carbon atoms, or a hydrocarbyl aryl or heteroaryl radical, as defined above, or a pharmaceutically-acceptable salt thereof. 2. The method of claim 1, wherein the prostamide component comprises bimatoprost. 3. The method of claim 1, wherein the PLGA copolymer has a lactide/glycolide ratio of 75/25, a molecular weight of about 63 kilodaltons, and an inherent viscosity of about 0.6 dL/g. 4. The method of claim 1, wherein the drying comprises evaporating the oil-in-oil emulsion to form an evaporated product. 5. The method of claim 4, wherein contacting the dried emulsion product with a solvent to form a solvent-containing composition comprises suspending the evaporated product in the solvent before removing the solvent from the solvent-containing composition. 6. The method of claim 2, wherein the microparticles have a release rate of the prostamide component of about 0.7% per day in vitro. 7. A method for producing therapeutic polymeric microparticles, comprising encapsulating bimatoprost with a polymeric component to form a population of bimatoprost-encapsulated microparticles by an oil-in-oil emulsion process, wherein the polymeric component comprises a poly(lactide-co-glycolide) (PLGA) copolymer, the oil-in-oil emulsion process comprising: forming a first composition comprising bimatoprost, a poly(lactide-co-glycolide) (PLGA) copolymer, and an organic solvent;forming a second oil-containing composition;mixing the first composition and the second oil-containing composition to form an oil-in-oil emulsion;evaporating the oil-in-oil emulsion to form an evaporated product;contacting the evaporated product with a solvent to form a solvent-containing composition; andremoving the solvent from the solvent-containing composition to form a population of microparticles having a maximum particle diameter less than about 200 μm and comprising bimatoprost and the polymeric component. 8. The method of claim 1, wherein the population of microparticles formed by the method has a mean particle diameter from about 30 μm to about 50 μm. 9. The method of claim 1, wherein prostamide component comprises about 10% wt/wt of the microparticles. 10. The method of claim 1, wherein the prostamide component comprises about 5% wt/wt of the microparticles. 11. The method of claim 7, wherein the organic solvent is acetonitrile.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.