Hydrophilic and lipophilic balanced microemulsion formulations of free-form and/or conjugation-stabilized therapeutic agents such as insulin
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-038/38
C07K-014/62
출원번호
US-0958383
(1997-10-27)
발명자
/ 주소
Ekwuribe Nnochiri Nkem
Ramaswamy Muthukumar
Radhakrishnan Balasingam
Allaudeen HameedSulthan S.
출원인 / 주소
Protein Delivery, Inc.
대리인 / 주소
Barret
인용정보
피인용 횟수 :
63인용 특허 :
24
초록▼
A therapeutic formulation comprising a microemulsion of a therapeutic agent in free and/or conjugatively coupled form, wherein the microemulsion comprises a water-in-oil (w/o) microemulsion including a lipophilic phase and a hydrophilic phase, and has a hydrophilic and lipophilic balance (HLB) value
A therapeutic formulation comprising a microemulsion of a therapeutic agent in free and/or conjugatively coupled form, wherein the microemulsion comprises a water-in-oil (w/o) microemulsion including a lipophilic phase and a hydrophilic phase, and has a hydrophilic and lipophilic balance (HLB) value between 3 and 7, wherein the therapeutic agent may for example be selected from the group consisting of insulin, calcitonin, ACTH, glucagon, somatostatin, somatotropin, somatomedin, parathyroid hormone, erythropoietin, hypothalamic releasing factors, prolactin, thyroid stimulating hormones, endorphins, enkephalins, vasopressin, non-naturally occurring opioids, superoxide dismutase, interferon, asparaginase, arginase, arginine deaminease, adenosine deaminase, ribonuclease, trypsin, chymotrypsin, papain, Ara-A (Arabinofuranosyladenine), Acylguanosine, Nordeoxyguanosine, Azidothymidine, Dideoxyadenosine, Dideoxycytidine, Dideoxyinosine Floxuridine, 6-Mercaptopurine, Doxorubicin, Daunorubicin, or I-darubicin, Erythromycin, Vancomycin, oleandomycin, Ampicillin; Quinidine and Heparin. In a particular aspect, the invention comprises an insulin composition suitable for parenteral as well as non-parenteral administration, preferably oral or parenteral administration, comprising insulin covalently coupled with a polymer including (i) a linear polyalkylene glycol moiety and (ii) a lipophilic moiety, wherein the insulin, the linear polyalkylene glycol moiety and the lipophilic moiety are conformationally arranged in relation to one another such that the insulin in the composition has an enhanced in vivo resistance to enzymatic degradation, relative to insulin alone. The microemulsion compositions of the invention are usefully employed in therapeutic as well as non-therapeutic, e.g., diagnostic, applications.
대표청구항▼
[ What is claimed is:] [1.] A composition for presentation or delivery of an insulin-methyl(ethyleneglycol).sub.7 -O-hexanoic acid conjugate, said composition:(a) comprising a water-in-oil (w/o) microemulsion including:(i) a lipophilic component; and(ii) a hydrophilic component; and(iii) a therapeut
[ What is claimed is:] [1.] A composition for presentation or delivery of an insulin-methyl(ethyleneglycol).sub.7 -O-hexanoic acid conjugate, said composition:(a) comprising a water-in-oil (w/o) microemulsion including:(i) a lipophilic component; and(ii) a hydrophilic component; and(iii) a therapeutically effective amount of insulin conjugated to 1, 2, and/or 3 methyl(ethyleneglycol).sub.7 -O-hexanoic acid conjugates; and(b) having an HLB value between 3 and 7.
연구과제 타임라인
LOADING...
LOADING...
LOADING...
LOADING...
LOADING...
이 특허에 인용된 특허 (24)
Speaker Tully J. (Philadelphia PA) Speaker Tycho J. (Philadelphia PA) Collett John H. (Sale GB2), Adjuvant-enhanced sustained release composition and method for making.
Vanlerberghe Guy (Commune de Villevaude FRX) Handjani Rose-Marie (Paris FRX), Aqueous dispersions of lipid spheres and compositions containing the same.
Mill Patrick James (Beaconfield EN) Cresswell Michael Alan (High Wycombe EN) Feinberg Joseph George (London EN), Conjugates of acid polysaccharides and complex organic substances.
Huper Fritz (Wuppertal DT) Rauenbusch Erich (Wuppertal DT) Schmidt-Kastner Gunter (Wuppertal DT) Bomer Bruno (Leverkusen DT) Bartl Herbert (Odenthal-Hahnenberg DT), Crosslinked copolymers of ab
상세보기
Eckenhoff James B. (Los Altos CA) Cortese Richard (Los Gatos CA) Landrau Felix A. (Milpitas CA), Dosage system and method of using same.
Woodle Martin C. (Menlo Park CA) Martin Francis J. (San Francisco CA) Yau-Young Annie (Los Altos CA) Redemann Carl T. (Walnut Creek CA), Liposomes with enhanced circulation time.
Harris J. Milton ; Veronese Francesco Maria,ITX ; Caliceti Paolo,ITX ; Schiavon Oddone,ITX, Multiarmed, monofunctional, polymer for coupling to molecules and surfaces.
Davis Frank F. (19 Farmingdale Rd. East Brunswick NJ 08816) Van Es Theodorus (313 Overbrook Rd. Piscataway NJ 08854) Palczuk Nicholas C. (45 W. Franklin St. Bound Brook NJ 08805), Non-immunogenic polypeptides.
Appelgren Curt H. (Kungsbacka SEX) Eskilsson Eva C. (Mlnlycke SEX) Uvdal Jonas P. (Gothenburg SEX), Process for preparing rapidly disintegrating granulates.
Eckenhoff James B. (Los Altos CA) Cortese Richard (Los Gatos CA) Landrau Felix A. (Milpitas CA), Rate controlled dispenser for administering beneficial agent.
Gillespie, Roger John; Lerpiniere, Joanne; Gaur, Suneel; Adoms, David Reginald; Knutsen, Lars Jacob Stray; Ward, Simon Edward, 4-Quinolinemethanol derivatives as purine receptor antagonists (1).
Cheu, Elizabeth L. S.; Choi, Lewis Siu Leung; Chou, Doug Ta Hung; Davidoff, Allen W.; Ezrin, Alan M.; Jung, Grace; Plouvier, Bertrand M. C.; Yifru, Aregahegn S., Drug conjugates of ion channel modulating compounds.
Ekwuribe, Nnochiri N.; Radhakrishnan, Balasingam; Price, Christopher H.; Anderson, Jr., Wes; Ansari, Aslam M., Methods of activating a receptor using amphiphilic drug-oligomer conjugates.
Ekwuribe, Nnochiri N.; Price, Christopher H.; Ansari, Aslam M.; Odenbaugh, Amy L., Methods of synthesizing substantially monodispersed mixtures of polymers having polyethylene glycol moieties.
Ekwuribe, Nnochiri N.; Price, Christopher H.; Ansari, Aslam M.; Odenbaugh, Amy L., Mixtures of calcitonin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same.
Ekwuribe,Nnochiri N.; Price,Christopher H.; Ansari,Aslam M.; Odenbaugh,Amy L., Mixtures of calcitonin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same.
Ekwuribe, Nnochiri N.; Price, Christopher H.; Ansari, Aslam M.; Odenbaugh, Amy L., Mixtures of drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same.
Ekwuribe, Nnochiri N.; Price, Christopher H.; Ansari, Aslam M.; Odenbaugh, Amy L., Mixtures of growth hormone drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same.
Ekwuribe, Nnochiri N.; Price, Christopher H.; Ansari, Aslam M.; Radhakrishnan, Balasingam; Odenbaugh, Amy L., Mixtures of insulin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same.
Ekwuribe,Nnochiri N.; Price,Christopher H.; Ansari,Aslam M.; Radhakrishnan,Balasingam; Odenbaugh,Amy L., Mixtures of insulin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same.
Rosendahl, Mary S.; Mantripragada, Sankaram B.; Gomez, Eliana B., Use of hydrophobic organic acids to increase hydrophobicity of proteins and protein conjugates.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.