Aqueous preparation containing oligopeptides and etherified cyclodextrin
First Claim
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1. An aqueous pharmaceutical composition comprising:
- an oligopeptide of formula I
cyclo-(n-Arg-nGly-nAsp-nD-nE)
(I)in whichD and E each, independently of one another, denote Gly, Ala, β
-Ala, Asn, Asp, Asp(OR), Arg, Cha, Cys, Gln, Glu, His, Ile, Leu, Lys, Lys(Ac), Lys(AcNH2), Lys(AcSH), Met, Nal, NIe, Orn, Phe, 4-Hal-Phe, homoPhe, Phg, Pro, Pya, Ser, Thr, Tia, Tic, Trp, Tyr or Val;
R denotes alkyl having 1-18 C atoms;
Hal denotes F, Cl Br or I;
Ac denotes alkanoyl having 1-10 C atoms, aroyl having 7-11 C atoms or aralkanoyl having 8-12 C atoms; and
n denotes H, R, benzyl or aralkyl radical having 7-18 C atoms on the alpha-amino function of the corresponding amino acid, with the proviso that at least one amino acid has a substituent n, where n denotes R,and where, if the amino acids are optically active, both the D and L forms are included,and physiologically acceptable salts thereof;
and an etherified β
-cyclodextrin having a water solubility of greater than 1.8 mg/ml in water.
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Abstract
The present invention relates to an aqueous pharmaceutical preparation of oligopeptides comprising an oligopeptide of the formula I, cyclo-(n-Arg-nGly-nAsp-nD-nE), and a partially etherified β-cyclodextrin having a water solubility of greater than 1.8 mg/ml of water, and to the preparation of the aqueous pharmaceutical preparation.
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23 Claims
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1. An aqueous pharmaceutical composition comprising:
- an oligopeptide of formula I
cyclo-(n-Arg-nGly-nAsp-nD-nE)
(I)in which D and E each, independently of one another, denote Gly, Ala, β
-Ala, Asn, Asp, Asp(OR), Arg, Cha, Cys, Gln, Glu, His, Ile, Leu, Lys, Lys(Ac), Lys(AcNH2), Lys(AcSH), Met, Nal, NIe, Orn, Phe, 4-Hal-Phe, homoPhe, Phg, Pro, Pya, Ser, Thr, Tia, Tic, Trp, Tyr or Val;R denotes alkyl having 1-18 C atoms; Hal denotes F, Cl Br or I; Ac denotes alkanoyl having 1-10 C atoms, aroyl having 7-11 C atoms or aralkanoyl having 8-12 C atoms; and n denotes H, R, benzyl or aralkyl radical having 7-18 C atoms on the alpha-amino function of the corresponding amino acid, with the proviso that at least one amino acid has a substituent n, where n denotes R, and where, if the amino acids are optically active, both the D and L forms are included, and physiologically acceptable salts thereof; and an etherified β
-cyclodextrin having a water solubility of greater than 1.8 mg/ml in water.- 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)
- an oligopeptide of formula I
Specification