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1.发明申请CELLULOSE DERIVATIVES FOR INHIBITING CRYSTALLIZATION OF POORLY WATER-SOLUBLE DRUGS 审中-公开用于抑制不溶性水溶性药物结晶的纤维素衍生物公开(公告)号：US20150004237A1
公开(公告)日：2015-01-01
申请号：US14368911
申请日：2013-01-09
Inventor： Kevin J. Edgar , Bin Li , Lynne Taylor , Grace Ilevbare , Stephanie M. Williams , Haoyu Liu
IPC: A61K47/38 , A61K31/427 , A61K31/357 , A61K31/536 , A61K31/40 , A61K31/05 , C08B3/00 , A61K31/352
CPC classification number: A61K47/38 , A61K9/146 , A61K31/05 , A61K31/352 , A61K31/357 , A61K31/40 , A61K31/427 , A61K31/536 , A61K31/70 , C08B3/00
Abstract: Provided are cellulose esters useful for inhibiting solution crystallization of drugs. Specific polymers include cellulose esters of formula I: wherein n of the ω-carboxyalkanoyl group, is 3, 4, 6, or 8 to provide a ω-carboxyalkanoyl group chosen from succinoyl, glutaroyl, adipoyl, sebacyl, and suberyl groups; and wherein R is chosen from: a hydrogen atom; and an alkanoyl group chosen from acetyl, propionyl, butyryl, valeroyl, hexanoyl, nonanoyl, decanoyl, lauroyl, palmitoyl, and stearoyl groups; wherein there is a total degree of substitution of the alkanoyl group and the ω-carboxyalkanoyl group of at least 2.0; and wherein the polymer comprises m repeating units where n=1 to 1,000,000, or 10 to 100,000, or 100 to 1,000, such as 1 to 6,000. Embodiments further include compositions comprising cellulose esters and poorly water-soluble drugs, which compositions exhibit greater solubility and stability in solution as compared to the drugs alone.
Abstract translation: 提供用于抑制药物溶液结晶的纤维素酯。 特定聚合物包括式I的纤维素酯：其中ω-羧基烷酰基的n为3,4,6或8，以提供选自琥珀酰基，戊二酰基，己二酰基，癸二酰基和辛二酸基的ω-羧基烷酰基; 并且其中R选自：氢原子; 和选自乙酰基，丙酰基，丁酰基，戊酰基，己酰基，壬酰基，癸酰基，月桂酰基，棕榈酰基和硬脂酰基的烷酰基; 其中烷酰基和ω-羧基烷酰基的总取代度为至少2.0; 并且其中所述聚合物包含m个重复单元，其中n = 1至1,000,000，或10至100,000，或100至1,000，如1至6,000。 实施方案还包括包含纤维素酯和水溶性差的药物的组合物，与单独的药物相比，该组合物在溶液中表现出更大的溶解度和稳定性。
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公开(公告)号：US12162962B2
公开(公告)日：2024-12-10
申请号：US17836338
申请日：2022-06-09
Inventor： Kevin J. Edgar , Brittany L. B. Nichols , Junyi Chen , Charles Frazier , Lynne S. Taylor , Laura I. Mosquera-Giraldo , Ann Norris
Abstract: A method for the synthesis of alkyl ω-carboxy(hydroxyethyl) polysaccharides is described. The method includes methylating or ethylating a polysaccharide or providing a methylated or ethylated polysaccharide, hydroxyethylating the methylated or ethylated polysaccharide, and oxidizing the hydroxyethylated polysaccharide to form the ω-carboxy(hydroxyethyl) polysaccharide. A method for the synthesis of oxidized polysaccharides is also described. The method includes hydroxypropylating a polysaccharide and oxidizing the hydroxypropylated polysaccharides. A method for the production of a solid capable of forming a hydrogel is also described. The method includes combining a first solution comprising an oxidized oligo(hydroxypropyl) polysaccharide bearing one or more ketone groups with a second solution comprising an amine substituted polysaccharide to form a third solution, and removing solvent from the third solution to form the solid, or adding an additional solvent to the third solution to precipitate the solid. Novel polysaccharides and hydrogels prepared according to these methods are also described.
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公开(公告)号：US20250101139A1
公开(公告)日：2025-03-27
申请号：US18974476
申请日：2024-12-09
Applicant: Virginia Tech Intellectual Properties, Inc.
Inventor： Kevin J. Edgar , Brittany L.B. Nichols , Junyi Chen , Charles Frazier , Ann Norris
Abstract: A method for the synthesis of alkyl ω-carboxy(hydroxyethyl) polysaccharides is described. The method includes methylating or ethylating a polysaccharide or providing a methylated or ethylated polysaccharide, hydroxyethylating the methylated or ethylated polysaccharide, and oxidizing the hydroxyethylated polysaccharide to form the ω-carboxy(hydroxyethyl) polysaccharide. A method for the synthesis of oxidized polysaccharides is also described. The method includes hydroxypropylating a polysaccharide and oxidizing the hydroxypropylated polysaccharides. A method for the production of a solid capable of forming a hydrogel is also described. The method includes combining a first solution comprising an oxidized oligo(hydroxypropyl) polysaccharide bearing one or more ketone groups with a second solution comprising an amine substituted polysaccharide to form a third solution, and removing solvent from the third solution to form the solid, or adding an additional solvent to the third solution to precipitate the solid. Novel polysaccharides and hydrogels prepared according to these methods are also described.
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公开(公告)号：US20220298265A1
公开(公告)日：2022-09-22
申请号：US17836338
申请日：2022-06-09
Inventor： Kevin J. Edgar , Brittany L.B. Nichols , Junyi Chen , Charles Frazier , Lynne S. Taylor , Laura I. Mosquera-Giraldo , Ann Norris , Benjamin Adams
Abstract: A method for the synthesis of alkyl ω-carboxy(hydroxyethyl) polysaccharides is described. The method includes methylating or ethylating a polysaccharide or providing a methylated or ethylated polysaccharide, hydroxyethylating the methylated or ethylated polysaccharide, and oxidizing the hydroxyethylated polysaccharide to form the ω-carboxy(hydroxyethyl) polysaccharide. A method for the synthesis of oxidized polysaccharides is also described. The method includes hydroxypropylating a polysaccharide and oxidizing the hydroxypropylated polysaccharides. A method for the production of a solid capable of forming a hydrogel is also described. The method includes combining a first solution comprising an oxidized oligo(hydroxypropyl) polysaccharide bearing one or more ketone groups with a second solution comprising an amine substituted polysaccharide to form a third solution, and removing solvent from the third solution to form the solid, or adding an additional solvent to the third solution to precipitate the solid. Novel polysaccharides and hydrogels prepared according to these methods are also described.
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