IPC분류정보
| 국가/구분 |
United States(US) Patent
등록
|
| 국제특허분류(IPC7판) |
|
| 출원번호 |
US-0414484
(2009-03-30)
|
| 등록번호 |
US-8263131
(2012-09-11)
|
|
발명자
/ 주소 |
- Rabinow, Barrett
- White, Randy
- Sun, Chong-Son
- Wong, Joseph Chung Take
- Kipp, James E.
- Doty, Mark
- Rebbeck, Christine L.
- Papadopoulos, Pavlos
|
| 출원인 / 주소 |
- Baxter International Inc.
|
| 대리인 / 주소 |
Marshall, Gerstein & Borun LLP
|
| 인용정보 |
피인용 횟수 :
0 인용 특허 :
175 |
초록
▼
The present invention relates to compositions of submicron- to micron-size particles of antimicrobial agents. More particularly the invention relates to a composition of an antimicrobial agent that renders the agent potent against organisms normally considered to be resistant to the agent. The compo
The present invention relates to compositions of submicron- to micron-size particles of antimicrobial agents. More particularly the invention relates to a composition of an antimicrobial agent that renders the agent potent against organisms normally considered to be resistant to the agent. The composition comprises an aqueous suspension of submicron- to micron-size particles containing the agent coated with at least one surfactant selected from the group consisting of: ionic surfactants, non-ionic surfactants, biologically derived surfactants, and amino acids and their derivatives. The particles have a volume-weighted mean particle size of less than 5 μm as measured by laser diffractometry.
대표청구항
▼
1. A method for treating a subject infected with Candida albicans strain c43, the method comprising the step of administering itraconazole to a subject infected with Candida albicans strain c43, wherein the Candida albicans strain c43 has a MIC greater than 8 μg/mL for itraconazole, wherein the itra
1. A method for treating a subject infected with Candida albicans strain c43, the method comprising the step of administering itraconazole to a subject infected with Candida albicans strain c43, wherein the Candida albicans strain c43 has a MIC greater than 8 μg/mL for itraconazole, wherein the itraconazole is formulated as an aqueous suspension of submicron- to micron-size particles containing itraconazole coated with at least one surfactant selected from the group consisting of ionic surfactants, non-ionic surfactants, surface-active biological molecules, and amino acids and their derivatives, and wherein the particles have a volume-weighted mean particle size of less than 5 μm as measured by laser diffractometry. 2. The method of claim 1, wherein itraconazole has a solubility in a water-miscible first solvent that is greater than in a second aqueous solvent, and the aqueous suspension is prepared by: (i) dissolving itraconazole in the first solvent to form a solution;(ii) mixing the solution with the second solvent to define a pre-suspension; and(iii) adding energy to the pre-suspension to form particles having an average effective particle size of less than 5 μm, wherein the first or second solvent comprises one or more surfactants selected from the group consisting of nonionic surfactants, ionic surfactants, surface-active biological molecules, and amino acids and their derivatives. 3. The method of claim 1, wherein the ionic surfactant is selected from the group consisting of: anionic surfactants, cationic surfactants, zwitterionic surfactants, and combinations thereof. 4. The method of claim 1, wherein the surfactant is selected from the group consisting of bile salts, polyalkoxyethers, hydroxyethylstarch, polyethylene-660-hydroxystearate, albumin, and phospholipids. 5. The method of claim 1, wherein the aqueous suspension further comprises a pH adjusting agent. 6. The method of claim 1, wherein the aqueous suspension further comprises an osmotic pressure adjusting agent. 7. The method of claim 1, wherein itraconazole is present in the suspension in an amount from about 0.01% to about 50% w/v. 8. The method of claim 1, wherein the surfactant is present in the suspension in an amount from about 0.001% to about 5% w/v. 9. The method of claim 1, wherein the step of administering is by a route selected from the group consisting of parenteral, oral, buccal, periodontal, rectal, nasal, pulmonary, topical, intravenous, intramuscular, intracerebral, subcutaneous, intradermal, intralymphatic, pulmonary, intraarticular, intrathecal, and intraperitoneal. 10. The method of claim 1, wherein itraconazole is present in an amount of from about 0.01% to about 50% w/v, the aqueous suspension comprises an osmotic pressure adjusting agent, and the surfactant is present in an amount of from about 0.001% to about 5% w/v.
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