Drug administration
First Claim
1. A composition useful for the prevention or treatment of a human or animal disorder or for the regulation of a human or animal physiological condition comprising, in admixture;
- as an active ingredient, a biologically-effective amount of a peptide specific for the particular disorder or condition; and
(b) as an adjuvant, a biocompatible, water-soluble, fusidic acid derivative which has the formula;
##STR3## wherein a dashed line represents a single or a double bond;
D represents a group having a molecular weight below about 600 daltons which renders an effective amount of said steroid water-soluble within a range of about pH 2 to about pH 12;
E and G each represent OAc, OH, a lower alkyl group or a lower heteroalkyl group;
W represents OAc or H; and
Q, V and X each represent H or OH, said steroid containing from two to three polar functions, exclusive of the function represented by D;
said adjuvant being capable of increasing peptide permeability of a human or animal mucosal surface across which the peptide is to be administered, in an amount effective to increase the permeability of said mucosal surface to said peptide.
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Accused Products
Abstract
Compositions and methods useful for the prevention or treatment of a human or animal disorder or for the regulation of a human or animal physiological condition are provided. The compositions used comprise, in admixture, a biologically-effective amount of a drug specific for the disorder or condition and a biocompatible, water-soluble, amphiphilic steroid, other than a natural bile salt, which is capable of increasing drug permeability of the human or animal body surface across which the drug is to be administered, in an amount effective to increase the permeability of the surface to the drug.
157 Citations
76 Claims
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1. A composition useful for the prevention or treatment of a human or animal disorder or for the regulation of a human or animal physiological condition comprising, in admixture;
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as an active ingredient, a biologically-effective amount of a peptide specific for the particular disorder or condition; and (b) as an adjuvant, a biocompatible, water-soluble, fusidic acid derivative which has the formula;
##STR3## wherein a dashed line represents a single or a double bond;
D represents a group having a molecular weight below about 600 daltons which renders an effective amount of said steroid water-soluble within a range of about pH 2 to about pH 12;E and G each represent OAc, OH, a lower alkyl group or a lower heteroalkyl group; W represents OAc or H; and Q, V and X each represent H or OH, said steroid containing from two to three polar functions, exclusive of the function represented by D;
said adjuvant being capable of increasing peptide permeability of a human or animal mucosal surface across which the peptide is to be administered, in an amount effective to increase the permeability of said mucosal surface to said peptide. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 22, 23, 24, 25, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 46, 47, 48)
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21. A composition useful for the prevention or treatment of a human or animal disorder or for the regulation of a human or animal physiological condition comprising, in admixture:
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(a) as an active ingredient, a biologically-effective amount of a peptide specific for the disorder or condition; (b) as an adjuvant, an ionized or partially ionized, water-soluble alkali salt of cephalosporin P1, P2, P3, P4 or P5 or a derivative thereof, said cephalosporin or derivative being capable of increasing peptide permeability of a human or animal mucosal surface across which the peptide is to be administered, in an amount effective to increase the permeability of said mucosal surface to said peptide. - View Dependent Claims (26)
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42. A composition useful for regulating blood glucose and free fatty acid levels comprising, in admixture:
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(a) as an active ingredient, a medically-effective amount of glucagon; and (b) as an adjuvant, an effective amount of a salt of tauro-24,25-dihydrofusidate. - View Dependent Claims (45)
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43. A composition useful for affecting human pregnancy comprising, in admixture:
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(a) as an active ingredient, a medically-effective amount of human chorionic gonadotropin; and (b) as an adjuvant, an effective amount of a salt of tauro-24,25-dihydrofusidate. - View Dependent Claims (69)
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44. A composition useful for regulating adrenocorticotropin synthesis and release comprising, in admixture:
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(a) as an active ingredient, a medically-effective amount of corticotropin-releasing hormone; and (b) as an adjuvant, an effective amount of a salt of tauro-24,25-dihydrofusidate. - View Dependent Claims (70)
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49. A pharmaceutical preparation in the form of a nasal spray or nose drops useful for the treatment of diabetes comprising a solution or suspension in a physiologically buffered sodium chloride solution of an admixture of a medically-effective amount of insulin as active ingredient and an effective amount of sodium tauro-24,25-dihydrofusidate as adjuvant.
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50. In a method of administering a peptide which comprises applying to a human or animal mucosal surface for absorption across said body surface a composition comprising, as an active ingredient, a peptide specific for a disorder or condition, the improvement which comprises:
- applying the peptide to the mucosal surface in admixture with biocompatible, water-soluble, fusidic acid derivative which has the formula;
##STR5## wherein a dashed line represents a single or a double bond;
D represents a group having a molecular weight below about 600 daltons which renders an effective amount of said steroid water-soluble within a range of about pH 2 to about pH 12;E and G each represent OAc, OH, a lower alkyl group or a lower heteroalkyl group; W represents OAc or H; and Q, V and X each represent H or OH, said steroid containing from two or three polar functions, exclusive of the function represented by D;
which biocompatible, water-soluble fusidic acid derivative acts an adjuvant being capable of increasing peptide permeability of the human or animal muscosal surface across which the peptide is to be administered, in an amount effective to increase the permeability of said mucosal surface to said peptide. - View Dependent Claims (51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 72, 73, 74, 75, 76)
- applying the peptide to the mucosal surface in admixture with biocompatible, water-soluble, fusidic acid derivative which has the formula;
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71. A method of administering a vaccine to a human being or animal to immunize said human being or animal against a particular disease which comprises applying to a human or animal mucosal surface for absorption across said muscosal surface a composition comprising, in admixture:
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(a) as a vaccinating agent, a biologically-effective amount of a peptide antigen or fragment thereof, said peptide antigen or fragment thereof, said peptide antigen being capable of eliciting an immune response protective against the particular disease; and (b) as an adjuvant, a biocompatible, water-soluble, fusidic acid derivative which has the formula;
##STR6## wherein a dashed line represents a single or a double bond;
D represents a group having a molecular weight below about 600 daltons which renders an effective amount of said steroid water-soluble within a range of about pH 2 to about pH 12;E and G each represent OAc, OH, a lower alkyl group or a lower heteroalkyl group; W represents OAc or H; and Q, V and X each represent H or OH, said steroid containing from two to three polar functions, exclusive of the function represented by D; said adjuvant being capable of increasing peptide antigen permeability of a human or animal mucosal surface across which the peptide is to be administered, in an amount effective to increase the permeability of said mucosal surface to said peptide.
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Specification