Porous drug matrices and methods of manufacture thereof
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-009/14
A61K-009/00
A61K-031/335
A01N-043/02
출원번호
US-0022776
(2011-02-08)
등록번호
US-8821938
(2014-09-02)
발명자
/ 주소
Straub, Julie
Altreuter, David
Bernstein, Howard
Chickering, III, Donald E.
Khattak, Sarwat
Randall, Greg
출원인 / 주소
Acusphere, Inc.
대리인 / 주소
Pabst Patent Group LLP
인용정보
피인용 횟수 :
0인용 특허 :
55
초록▼
Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous so
Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.
대표청구항▼
1. A pharmaceutical composition comprising: a porous matrix comprising paclitaxel and albumin, wherein the matrix has a transaxial pressure (“TAP”) density of less than or equal to 1.0 g/ml; andthe matrix yields, upon contact with an aqueous medium, paclitaxel particles having a mean diameter betwee
1. A pharmaceutical composition comprising: a porous matrix comprising paclitaxel and albumin, wherein the matrix has a transaxial pressure (“TAP”) density of less than or equal to 1.0 g/ml; andthe matrix yields, upon contact with an aqueous medium, paclitaxel particles having a mean diameter between 0.1 and 5 μm;wherein an aqueous dissolution rate of the paclitaxel particles is increased relative to unprocessed paclitaxel. 2. A pharmaceutical composition comprising: a porous matrix comprising paclitaxel and albumin, wherein the matrix has a transaxial pressure (“TAP”) density of less than or equal to 1.0 g/ml; andthe matrix yields, upon contact with an aqueous medium, paclitaxel particles having a total surface area of at least 0.9 m2/ml;wherein an aqueous dissolution rate of the paclitaxel particles is increased relative to unprocessed paclitaxel. 3. The pharmaceutical composition of claim 1, wherein the paclitaxel particles consist essentially of paclitaxel and albumin. 4. The pharmaceutical composition of claim 2, wherein the paclitaxel particles consist essentially of paclitaxel and albumin. 5. A pharmaceutical composition comprising: a porous matrix comprising docetaxel and albumin, wherein the matrix has a transaxial pressure (“TAP”) density of less than or equal to 1.0 g/ml; andthe matrix yields, upon contact with an aqueous medium, docetaxel particles having a mean diameter between 0.1 and 5 μm;wherein an aqueous dissolution rate of the docetaxel particles is increased relative to unprocessed docetaxel. 6. A pharmaceutical composition comprising: a porous matrix comprising docetaxel and albumin, wherein the matrix has a transaxial pressure (“TAP”) density of less than or equal to 1.0 g/ml; andthe matrix yields, upon contact with an aqueous medium, docetaxel particles having a total surface area of at least 0.9 m2/ml;wherein an aqueous dissolution rate of the docetaxel particles is increased relative to unprocessed docetaxel. 7. The pharmaceutical composition of claim 5, wherein the docetaxel particles consist essentially of docetaxel and albumin. 8. The pharmaceutical composition of claim 6, wherein the docetaxel particles consist essentially of docetaxel and albumin. 9. A method of treating cancer comprising administering to a subject in need thereof a pharmaceutical composition comprising: a porous matrix comprising paclitaxel and albumin, wherein the matrix has a transaxial pressure (“TAP”) density of less than or equal to 1.0 g/ml; andthe matrix yields, upon contact with an aqueous medium, paclitaxel particles having a mean diameter between 0.1 and 5 μm;wherein an aqueous dissolution rate of the paclitaxel particles is increased relative to unprocessed paclitaxel. 10. The method of claim 9, wherein the paclitaxel particles consist essentially of paclitaxel and albumin. 11. The method of claim 9, wherein the pharmaceutical composition is administered parenterally. 12. The method of claim 11, wherein the pharmaceutical composition is administered intravenously. 13. A method of treating cancer comprising administering to a subject in need thereof a pharmaceutical composition comprising: a porous matrix comprising docetaxel and albumin, wherein the matrix has a transaxial pressure (“TAP”) density of less than or equal to 1.0 g/ml; andthe matrix yields, upon contact with an aqueous medium, docetaxel particles having a mean diameter between 0.1 and 5 μm;wherein an aqueous dissolution rate of the docetaxel particles is increased relative to unprocessed docetaxel. 14. The method of claim 13, wherein the docetaxel particles consist essentially of docetaxel and albumin. 15. The method of claim 13, wherein the pharmaceutical composition is administered parenterally. 16. The method of claim 15, wherein the pharmaceutical composition is administered intravenously. 17. The method of claim 9, wherein the pharmaceutical composition is an aqueous solution or suspension. 18. The method of claim 13, wherein the pharmaceutical composition is an aqueous solution or suspension.
연구과제 타임라인
LOADING...
LOADING...
LOADING...
LOADING...
LOADING...
이 특허에 인용된 특허 (55)
Cupps Thomas Lee (Oxford OH) Bogdan Sophie Eva (Maineville OH), 5-(2-imidazolinylamino)benzimidazole compounds useful as alpha-2-adrenoceptor agonists.
Bagchi Pranab (Webster NY) Scaringe Raymond P. (Rochester NY) Bosch H. William (Bryn Mawr PA), Co-microprecipitation of nanoparticulate pharmaceutical agents with crystal growth modifiers.
Eickhoff W. Mark (Downingtown PA) Mueller Karl R. (Pexton PA) Engers David A. (Collegeville PA), Formulations of compounds as nanoparticulate dispersions in digestible oils or fatty acids.
Kruse Lawrence I. ; Chang An-Chih ; DeHaven-Hudkins Diane L. ; Farrar John J. ; Gaul Forrest ; Kumar Virendra ; Marella Michael Anthony ; Maycock Alan L. ; Zhang Wei Yuan, Kappa agonist compounds pharmaceutical formulations and method of prevention and treatment of pruritus therewith.
Bruno Joseph A. (Blue Bell PA) Doty Brian D. (Phoenixville PA) Gustow Evan (Ardmore PA) Illig Kathleen J. (Phoenixville PA) Rajagopalan Nats (Phoenixville PA) Sarpotdar Pramod (Malvern PA), Method of grinding pharmaceutical substances.
Na George C. (Fort Washington PA) Rajagopalan Natarajan (Phoenixville PA), Method of preparing nanoparticle compositions containing charged phospholipids to reduce aggregation.
Cleland Jeffrey L. (San Carlos CA) Lim Amy (San Bruno CA) Powell Michael Frank (San Francisco CA), Methods and compositions for microencapsulation of adjuvants.
Desai Neil P. (Los Angeles CA) Soon-Shiong Patrick (Los Angeles CA) Sandford Paul A. (Los Angeles CA) Grinstaff Mark W. (Pasadena CA) Suslick Kenneth S. (Champaign IL), Methods for in vivo delivery of substantially water insoluble pharmacologically active agents and compositions useful th.
Soon-Shiong Patrick (Los Angeles CA) Desai Neil P. (Los Angeles CA) Grinstaff Mark W. (Pasadena CA) Sandford Paul A. (Los Angeles CA) Suslick Kenneth S. (Champaign IL), Methods for in vivo delivery of substantially water insoluble pharmacologically active agents and compositions useful th.
Bernstein Howard (Cambridge MA) Straub Julie A. (Winchester MA) Brush Henry T. (Somerville MA) Wing Richard E. (Cambridge MA), Microencapsulated fluorinated gases for use as imaging agents.
Bagchi Pranab (Webster NY) Stewart Robert C. (Spencerport NY) McIntire Gregory L. (West Chester PA) Minter John R. (Rochester NY), Microprecipitation of micro-nanoparticulate pharmaceutical agents.
Bagchi Pranab (Webster NY) Karpinski Piotr H. (Fairport NY) McIntire Gregory L. (West Chester PA), Microprecipitation of nanoparticulate pharmaceutical agents.
Bagchi Pranab ; McIntire Gregory L. ; Minter John R., Microprecipitation of nanoparticulate pharmaceutical agents using surface active material derived from similar pharmace.
Wong Sui-Ming (Collegeville PA) Cooper Eugene R. (Berwyn PA) Xu Shugian (Exton PA), Polyalkylene block copolymers as surface modifiers for nanoparticles.
Dugstad Harald,NOX ; Foss Per Antonius,NOX ; Klaveness Jo,NOX ; Rongved P.ang.l,NOX ; Skurtveit Roald,NOX, Polymeric surfactant-encapsulated microbubbles and their use in ultrasound imaging.
DeLuca Patrick P. (Lexington KY) Kanke Motoko (Fukuyama JPX) Sato Toyomi (Tokyo CA JPX) Schroeder Hans G. (Encinitas CA), Porous microspheres for drug delivery and methods for making same.
Straub, Julie; Bernstein, Howard; Chickering, III, Donald E.; Khattak, Sarwat; Randall, Greg, Porous paclitaxel matrices and methods of manufacture thereof.
Bosch H. William (Bryn Mawr PA) Marcera Donna M. (Collegeville PA) Mueller Ronald L. (Downingtown PA) Swanson Jon R. (Macungie PA) Mishra Dinesh S. (Harleysville PA), Process for preparing therapeutic compositions containing nanoparticles.
Desai Neil P. ; Tao Chunlin ; Yang Andrew ; Louie Leslie ; Zheng Tianli ; Yao Zhiwen ; Soon-Shiong Patrick ; Magdassi Shlomo,ILX, Protein stabilized pharmacologically active agents, methods for the preparation thereof and methods for the use thereof.
Ruddy Stephen B. (Schwenksville PA) Eickhoff W. Mark (Downingtown PA) Liversidge Gary (West Chester PA), Site-specific adhesion within the GI tract using nanoparticles stabilized by high molecular weight, linear poly (ethylen.
Wong Sui-Ming (Collegeville PA) Newington Ian M. (Hazlemere GB2) Liversidge Elaine M. (West Chester PA) McIntire Gregory L. (West Chester PA) Pitt Alan R. (Sandridge GBX) Shaw Jack M. (Aberdeen MD), Sulfated nonionic block copolymer surfactants as stabilizer coatings for nanoparticle compositions.
Liversidge Gary G. (West Chester PA) Conzentino ; Jr. Philip (West Chester PA) Cundy Kenneth C. (Pottstown PA) Sarpotdar Pramod P. (Malvern PA), Surface modified NSAID nanoparticles.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.