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Stable solid formulation of a GC-C receptor agonist polypeptide suitable for oral administration

A drug and dosage form technology, applied in the field of stable solid preparations of guanylate cyclase-C receptor agonist polypeptides suitable for oral administration, can solve the problems of inconvenient freezing

Active Publication Date: 2011-09-14
硬木药品公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, freezing is inconvenient for commercial distribution of drugs and storage for patients

Method used

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  • Stable solid formulation of a GC-C receptor agonist polypeptide suitable for oral administration
  • Stable solid formulation of a GC-C receptor agonist polypeptide suitable for oral administration
  • Stable solid formulation of a GC-C receptor agonist polypeptide suitable for oral administration

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-15

[0087] Example 1-15: Preparation of Linaclotide Preparations

[0088] The linaclotide formulations of Examples 1-15 were produced essentially as described in Formulation Protocol A, wherein Table 1 provides the amounts of cation, sterically hindered primary amine, binder, linaclotide, and beads, while Table 1 2 provides the conditions for coated beads:

[0089] Table 1

[0090]

[0091]

[0092] * "Cation" means a divalent cation contained in the salt used in the examples, "amine" means a sterically hindered primary amine, and [ ] means a molar ratio of cation and / or amine to linaclotide.

[0093] ** The concentration of linaclotide in this and all following examples was determined based on the peptide content and chromatographic purity listed on the certificate of analysis provided for each manufacturing batch of linaclotide active pharmaceutical ingredient (API). quantity.

[0094] Table 2

[0095]

Embodiment 16

[0096] Example 16: Preparation of Linaclotide Preparations

[0097] The linaclotide formulation of Example 16 was produced essentially as described in formulation protocol B, wherein Table 3 provides the amounts of cation, sterically hindered primary amine, binder, linaclotide, and beads, while Table 4 provides Conditions for coated beads:

[0098] table 3

[0099]

[0100] Table 4

[0101]

Embodiment 17

[0102] Example 17: Preparation of Linaclotide Preparations

[0103] The linaclotide formulation of Example 17 was produced essentially as described in formulation protocol A, except that the formulation contained 22.96 mg of butylated hydroxyanisole (BHA), where Table 5 provides the cation, sterically hindered primary amine, binder , linaclotide and the amount of beads, while Table 6 provides the conditions for coating the beads.

[0104] table 5

[0105]

[0106] Table 6

[0107]

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Abstract

Solid, stable formulations of linaclotide suitable for oral administration are described herein as are methods for preparing such formulations. The formulations described herein contain a polypeptide consisting of the amino acid sequence Cys Cys GIu Tyr Cys Cys Asn Pro Ala Cys Thr GIy Cys Tyr ("linaclotide") or a pharmaceutically acceptable salt thereof. The linaclotide formulations described herein are stable and have a sufficient shelf life for manufacturing, storing and distributing the drug.

Description

technical field [0001] The present disclosure relates to solid formulations of guanylate cyclase-C receptor agonist polypeptides suitable for oral administration and methods of preparing such formulations. [0002] priority statement [0003] This application claims U.S. Application Serial No. 61 / 089,422 filed August 15, 2008 and U.S. Provisional Application entitled "Stable Solid Formulation of a GC-C Receptor Agonist Polypeptide Suitable for Oral Administration," filed August 3, 2009 priority. The entire contents of the aforementioned applications are incorporated herein by reference. Background technique [0004] Many therapeutic polypeptides are formulated in aqueous solutions because they are most active in this form. However, most polypeptides are not particularly stable in aqueous solutions, so formulations often have short half-lives and require refrigeration. Although aqueous solutions of polypeptides may be dried by freeze-drying, spray-drying, or other methods...

Claims

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Application Information

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IPC IPC(8): A61K38/00A61K9/50A61K9/16A61K9/20A61K9/48
CPCA61K9/4866A61K9/4858A61K9/2054A61K9/1611A61K38/10A61K9/485A61K9/1617A61K9/167A61K9/5078A61J3/00A61K9/1635A61K9/205A61K9/1623A61K38/12A61P1/00A61P1/04A61P1/10A61P1/14A61P43/00A61K9/0053A61K9/50A61K47/02A61K47/183A61K47/36B65D81/26G01N30/02G01N2030/027
Inventor A·弗雷津S·维托夫斯基A·格罗西H·赵M·德希亚Y·莫
Owner 硬木药品公司
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