Peptide as absorption enhancer and composition containing same
View Patent ↗As described herein, an peptide of SEQ ID NO: 1 is modified at the terminal end. Specifically, the carboxyl-group of the leucine at the terminal end of the amino acid sequence FCIGRL (SEQ ID NO: 1) is modified with a —CONH 2 . This modified peptide is used as a permeation enhancer to boost the mucous membrane permeation, thereby noticeably increasing the bioavailability of a drug that is administered together with the modified peptide. The drug to be administered with the modified peptide can be cyclosporine A.
1. A composition for enhancing mucous membrane permeability, the composition comprising an amino acid sequence FCIGRL (SEQ ID NO:1), wherein the carboxyl group (—COOH) of Leucine at the terminal end of the amino acid sequence is modified into —CONH 2 ; and
an active component, wherein the active component is not linked to the peptide.
2. The composition for enhancing mucous membrane permeability of claim 1 , wherein the active component is cyclosporine A.
3. The composition for enhancing mucous membrane permeability of claim 2 , wherein the composition further comprises a pharmaceutically acceptable additive or adjuvant.
4. The composition for enhancing membrane permeability of claim 1 , wherein the mucous membrane is a mucous membrane with the expressed tight junction.
5. The composition for enhancing membrane permeability of claim 4 , wherein the mucous membrane is a mucous membrane of small intestine, nasal cavity, oral cavity, skin, lung, vagina, rectum, or large intestine.
6. A preparation comprising:
a peptide having an amino acid sequence FCIGRL (SEQ ID NO:1), wherein the carboxyl group (—COOH) of Leucine at the terminal of the amino acid sequence is modified into —CONH 2 ; and
an active component, wherein the active component is cyclosporine A and is not linked to the peptide.
7. The preparation of claim 6 , wherein the preparation is taken by oral, nasal, buccal, transdermal, transpulmorary, rectal, or vaginal administration.
8. The preparation of claim 6 , wherein the preparation further comprises a pharmaceutically acceptable additive or adjuvant.
9. The preparation of claim 6 , wherein the preparation is for enhancement of mucous membrane permeability.
10. The preparation of claim 6 , wherein the preparation contains 0.001 to 50 wt % of the peptide.
11. A method of enhancing permeation of an active component through mucous membranes in a subject comprising administering to a subject in need thereof an active component and a peptide respectively,
wherein the peptide has an amino acid sequence FCIGRL (SEQ ID NO:1) wherein the carboxyl group (—COOH) of Leucine at the terminal end of the amino acid sequence is modified into —CONH 2 and the peptide boosts the mucous membrane permeation of the active component, and
the active component is a cyclosporine A and is not linked to the peptide.
12. The method of claim 11 , wherein the mucous membrane is selected from a group consisting of a mucous membrane of small intestine, a mucous membrane of nasal cavity, a mucous membrane of oral cavity, a mucous membrane of skin, a mucous membrane of lung, a mucous membrane of vagina, a mucous membrane of rectum, and a mucous membrane of large intestine.
13. The method of claim 12 , wherein the active component and peptide are in the form of a dosage form selected from the group consisting of a liquid, capsules, granules and tablets.
14. The method of claim 13 , wherein the liquid dosage form is selected from the group consisting of an aqueous solution, suspension, and an emulsion.
15. The method of claim 11 , wherein the peptide opens a tight junction between adjacent cells in the mucous membrane.
16. The method of claim 11 , wherein the active component and the peptide are administered once a day or multiple times a day.
17. The method of claim 11 , wherein the peptide is administered in an amount of 0.0001 mg/kg to 100 mg/kg.
18. The method of claim 13 , wherein the dosage form further comprises a pharmaceutically acceptable additive or adjuvant.