IPC분류정보
국가/구분 |
United States(US) Patent
등록
|
국제특허분류(IPC7판) |
|
출원번호 |
US-0498015
(2009-07-06)
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등록번호 |
US-8273371
(2012-09-25)
|
우선권정보 |
GB-0315012.5 (2003-06-27) |
발명자
/ 주소 |
- Martens, Johan Adriaan
- Kirschhock, Christine Eva Antonia
- Kremer, Sebastien Philippe Brigitte
- Aerts, Alexander Jan Maria Herman Eugeen
- Van Den Mooter, Guy
- Van Humbeeck, Jan
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출원인 / 주소 |
|
대리인 / 주소 |
|
인용정보 |
피인용 횟수 :
0 인용 특허 :
9 |
초록
▼
The invention describes a new class of crystalline silica material having two levels of porosity and structural order. At the first level, building units are nanoslabs of uniform size having zeolite framework. At the second structural level, nanoslabs are assembled, e.g. linked through their corners
The invention describes a new class of crystalline silica material having two levels of porosity and structural order. At the first level, building units are nanoslabs of uniform size having zeolite framework. At the second structural level, nanoslabs are assembled, e.g. linked through their corners, edges or faces following patterns imposed by interaction with cationic surfactant or triblock copolymer molecules. After evacuation of these molecules, microporosity is obtained inside the nanoslabs, and a precise mesoporosity between the nanoslabs depending on the tiling pattern of the zeolite nanoslabs, as evidenced by X-ray diffraction. These materials are useful for the fixation of biologically active species, such as poorly soluble drugs.
대표청구항
▼
1. A pharmaceutical composition for the immediate release of a poorly soluble drug, comprising said poorly soluble drug and a substantially ordered mesoporous silica, wherein the drug molecules are loaded on the mesoporous silica material, wherein the water solubility of said biologically active spe
1. A pharmaceutical composition for the immediate release of a poorly soluble drug, comprising said poorly soluble drug and a substantially ordered mesoporous silica, wherein the drug molecules are loaded on the mesoporous silica material, wherein the water solubility of said biologically active species is below 2.5 mg/ml, wherein the molecular weight of said poorly soluble drug is between about 200 and 1,000 Daltons, and wherein said ordered silica has one level of porosity or structural order, has a highly ordered, two-dimensional hexagonal (P6mm) honeycomb mesostructure, which upon calcination at 500° C. yields porous structures with high BET surface areas of 690 to 1040 m2/g and pore volumes up to 2.5 cm3/g, ultra large d(100) spacings of 7.45-45 nm, and silica wall thicknesses of 3.1 to 6.4 nm, and has a pore size in the range 6 nm to 14 nm and is obtained in the absence of an alpha-tocopherol polyethylene glycol ester templating biomolecule. 2. The pharmaceutical composition according to claim 1, wherein said poorly soluble drug belongs to Class II or Class IV of the Biopharmaceutical Classification System. 3. The pharmaceutical composition according to claim 1, wherein the water solubility of said poorly soluble drug is between 0.1 and 1 mg/ml. 4. The pharmaceutical composition according to claim 1, wherein said poorly soluble drug is selected from the group consisting of chlorothiazide, hydrochlorothiazide, nimodipine, flufenamic acid, furosemide, mefenamic acid, bendroflumethiazide, benzthiazide, ethacrinic acid, nitrendipine, itraconazole, saperconazole, troglitazone, prazosin, atovaquone, danazol, glibenclamide, griseofulvin, ketoconazole, carbamazepine, sulfadiazine, florfenicol, acetohexamide, ajamaline, benzbromarone, benzyl benzoate, betamethasone, chloramphenicol, chlorpropamide, chlorthalidone, clofibrate, diazepam, dicumarol, digitoxin, ethotoin, glutethimide, hydrocortisone, hydroflumethiazide, hydroquinine, indomethacin, ibuprofen, ketoprofen, naproxen, khellin, nitrazepam, nitrofurantoin, novalgin, oxazepam, papaverine, phenylbutazone, phenytoin, prednisolone, prednisone, reserpine, spironolactone, sulfabenzamide, sulfadimethoxine, sulfamerazine, sulfamethazine, sulfamethoxypyridazine, succinylsulfathiazole, sulfamethizole, sulfamethoxazole, sulfaphenazole, sulfathiazole, sulfisoxazole, sulpiride, testosterone, diaminopyrimidines, trimethoprim, diaveridine, ormetoprim and pyrimethamine. 5. The pharmaceutical composition according to claim 1, wherein said poorly soluble drug is present in an amount from 0.5% to 50% by weight of the composition. 6. A process for producing a pharmaceutical composition comprising a poorly soluble drug loaded on a substantially ordered mesoporous silica, wherein the water solubility of said poorly soluble drug is below 2.5 mg/ml, wherein the molecular weight of said poorly soluble drug is between about 200 and 1,000 Daltons, and wherein said ordered silica has a highly ordered, two-dimensional hexagonal (P6 mm) honeycomb mesostructure, which upon calcination at 500° C. yields porous structures with high BET surface areas of 690 to 1040 m2/g and pore volumes up to 2.5 cm3/g, ultra large d(100) spacings of 7.45-45 nm, and silica wall thicknesses of 3.1 to 6.4 nm, and wherein said ordered silica has one level of porosity or structural order, has a pore size in the range of 6 nm to 14 nm, and is obtained in the absence of an alpha-tocopherol polyethylene glycol ester templating biomolecule, wherein a physical mixture of said biologically active species and said substantially ordered mesoporous silica is suspended in an appropriate solvent other than a supercritical fluid, and the suspended mixture is stirred until the poorly soluble drug is substantially entirely fixed or entrapped within the pores of the ordered mesoporous silica. 7. The pharmaceutical composition according to claim 1, wherein immediate release means a release of at least 60% of the drug under physiological conditions (pH, temperature) within at most 30 minutes for drug loadings within a range from about 5% to 40% by weight of a pharmaceutical composition comprising said poorly soluble drug loaded on said substantially ordered mesoporous silica material. 8. The pharmaceutical composition according to claim 1, wherein the substantially ordered mesoporous silica is SBA-15. 9. The pharmaceutical composition according to claim 1, wherein the water solubility of said poorly soluble drug is between 0.2 μg/ml and 0.1 mg/ml.
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