Pharmaceutical compositions comprising cyclosporins
First Claim
1. A pharmaceutical composition comprising a cyclosporin as active ingredient,a hydrophilic phase component comprising1.1) a pharmaceutically acceptable di- or partial-ether of the formula
wherein R1 is C1-5 alkyl or tetrahydrofurfuryl, R2 is hydrogen, C1-5 alkyl or tetrahydrofurfuryl, and X is an integer from 1 to 6, or1.2) 1,2-propylene glycol;
2) a lipophilic phase component; and
3) a surfactant;
wherein said composition is a microemulsion pre-concentrate, which upon dilution with water to a ratio of 1;
1 parts by weight pre-concentrate to water or more of said water, is capable of providing an oil-in-water microemulsion having average particle size of less than about 1,000 Å
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Accused Products
Abstract
Pharmaceutical compositions comprising a cyclosporin, e.g. Ciclosporin or [Nva]2 -Ciclosporin, in "microemulsion pre-concentrate" and microemulsion form. The compositions typically comprise (1.1) a C1-5 alkyl or tetrahydrofurfuryl di- or partial-ether of a low molecular weight mono- or poly-oxy-alkane diol, e.g. Transcutol or Glycofurol, as hydrophilic component. Compositions are also provided comprising a cyclosporin and (1.1) and, suitably, also a saccharide monoester, e.g. raffinose or saccharose monolaurate. Dosage forms include topical formulations and, in particular, oral dosage forms.
389 Citations
26 Claims
- 1. A pharmaceutical composition comprising a cyclosporin as active ingredient,a hydrophilic phase component comprising
1.1) a pharmaceutically acceptable di- or partial-ether of the formula - space="preserve" listing-type="equation">R.sub.1 --[O--(CH.sub.2).sub.2 ].sub.x --OR.sub.2
wherein R1 is C1-5 alkyl or tetrahydrofurfuryl, R2 is hydrogen, C1-5 alkyl or tetrahydrofurfuryl, and X is an integer from 1 to 6, or 1.2) 1,2-propylene glycol; 2) a lipophilic phase component; and 3) a surfactant; wherein said composition is a microemulsion pre-concentrate, which upon dilution with water to a ratio of 1;
1 parts by weight pre-concentrate to water or more of said water, is capable of providing an oil-in-water microemulsion having average particle size of less than about 1,000 Å
.- View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25)
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26. An oral pharmaceutical composition comprising Ciclosporin or [Nva]2 -Ciclosporin as an active ingredient;
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1) a hydrophilic phase component which comprises a pharmaceutically acceptable C1-5 alkyl di-or partial-ether, or tetrahydrofurfuryl di-or partial-ether, of a mono- or poly-oxy-C2-12 -alkanediol, or 1,2-propylene glycol; 2) a lipophilic phase component which comprises a fatty acid triglyceride; and 3) a surfactant which comprises a polyoxyethylene glycolated natural or hydrogenated vegetable oil and monoglyceride; wherein said composition is a microemulsion pre-concentrate capable, on contacting with water, of forming an oil-in-water microemulsion having an average particle size of less than 1,000 Å
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Specification
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- Resources
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Current AssigneeNovartis Ag
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Original AssigneeSandoz Inc. (Novartis Ag)
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InventorsMeinzer, Armin, Richter, Friedrich, Hauer, Birgit, Posanski, Ulrich
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Primary Examiner(s)CHAN, Y CHRISTINA
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Application NumberUS07/990,734Time in Patent Office623 DaysField of Search424/455, 424/456, 424/457, 424/489, 514/9, 514/11, 514/885, 514/937, 514/938, 514/970, 514/963, 514/964, 514/974, 514/975, 530/317, 530/321, 530/322US Class Current424/455CPC Class CodesA61K 38/13 CyclosporinsA61K 9/1075 Microemulsions or submicron...A61K 9/4858 Organic compounds
