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Physiologically active substance bound to biotin moiety, and composition for oral administration including same

A physiologically active substance, biotin technology, applied in the field of compositions for oral administration, can solve problems such as low permeability of intestinal membrane, and achieve the effect of promoting penetration and excellent oral absorption in vivo

Pending Publication Date: 2022-01-11
D&D PHARMATECH INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, a problem with peptide and protein drugs when administered orally is that they decompose due to enzymatic attack, and the intestinal membrane has low permeability

Method used

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  • Physiologically active substance bound to biotin moiety, and composition for oral administration including same
  • Physiologically active substance bound to biotin moiety, and composition for oral administration including same
  • Physiologically active substance bound to biotin moiety, and composition for oral administration including same

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Experimental program
Comparison scheme
Effect test

Embodiment approach

[0162] According to one embodiment of the present invention, [the method] may comprise a purification step after the separation step. Separation and purification steps can be performed using size exclusion chromatography, high performance liquid chromatography, or ion exchange chromatography, but are not limited thereto.

[0163] Another aspect of the present invention provides a composition for oral composition comprising a PSA as hereinbefore described bonded to a biotin moiety.

[0164] The physiologically active substance bonded to a biotin moiety according to one embodiment of the present invention can be transported by active transport via a sodium-dependent multivitamin transporter by bonding to biotin (a type of water-soluble vitamin B7). Absorption, thereby promoting intestinal membrane permeability and intestinal absorption.

[0165] A further aspect of the present invention provides a pharmaceutical composition comprising a PSA as described hereinabove bonded to a ...

Embodiment approach 1 to 3

[0235] 1) preparation example

[0236] Using DMSO solvent added with 0.3% triethylamine (TEA, Sigma) as the reaction solvent, prepared the polypeptide-biotin part of the polypeptide with SEQ.ID.No.12 described in the following Table 5 and the above Table 3 A 1:2 molar ratio mixture between said biotin moieties (using B1, B2 and B3, respectively; polypeptide of SEQ.ID.No. 12: B1, B2 or B3). The mixture was allowed to react at room temperature for at least 30 minutes, and the reaction was terminated by adding the same volume of 1% trifluoroacetic acid as the volume of the mixture.

[0237] [table 5]

[0238]

[0239]

[0240] 2) Separation, purification and confirmation

[0241] The reaction products of Embodiments 1 to 3 above were separated and purified using reverse-phase high-performance liquid chromatography (hereinafter referred to as "HPLC").

[0242] A SUPERSIL ODS-1 column (10x250 mm, 5 μm, LB Science, South Korea) was used as a column. Using 30%-50% solvent B...

Embodiment approach 4 to 9

[0251] Using the same method as in Embodiments 1 to 3, a polypeptide-biotin moiety was prepared by bonding a biotin moiety to the polypeptides of SEQ.ID.No.8 and 13, as shown in Table 6 below.

[0252] [Table 6]

[0253]

[0254] [Evaluation]

[0255] Reaction rate and yield

[0256]The reaction rate was found by comparing the HLPC peak areas of Embodiments 1 to 3 under HPLC analysis of the mixture with the biotin moiety based on the amount of polypeptide added in the initial mixture obtaining step.

[0257] The yield of the present invention was found by quantifying the amount of final purified material based on the amount of polypeptide added in the initial mixture obtaining step. The results are shown in Table 7 below.

[0258] [Table 7]

[0259] Embodiments 1 to 3 Binding position C40 reaction speed >99％ Yield 80％

[0260] Measurement of Oral Absorption Rates of Embodiments 1 to 3

[0261] To confirm the rate of oral absorptio...

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Abstract

The present invention relates to: a physiologically active substance to which a biotin moiety is bound; and a composition for oral administration comprising same. A physiologically active substance to which a biotin moiety is bound according to the present invention has the effect of having excellent oral absorption into the body.

Description

technical field [0001] The present invention relates to a physiologically active substance bonded to a biotin moiety, and a composition for oral administration comprising the physiologically active substance. More specifically, the present invention relates to a biotin moiety-bonded physiologically active substance having excellent oral absorption in vivo, and a composition for oral administration comprising the physiologically active substance. Background technique [0002] In recent years, with economic progress and accelerated development of science and technology, diets have become westernized and consumption of high-calorie, high-fat food products has been increasing. Therefore, the population suffering from diabetes and obesity etc. due to various metabolic diseases is rapidly increasing. [0003] Diabetes mellitus is a disease with multiple complications, and its treatment requires dietary restriction, which significantly reduces the patient's quality of life. There...

Claims

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Application Information

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IPC IPC(8): A61K47/54A61K47/64A61K38/26A61K38/16A61K9/00A61P3/10A61P3/04A61P19/10A61P1/16A61P1/00A61P25/28C07K5/097C07K5/083C07K5/117C07K5/062C07D495/04C07D519/00
CPCA61K47/545A61K47/64A61K38/26A61K38/16A61K9/0053A61P3/10A61P3/04A61P19/10A61P1/16A61P1/00A61P25/28C07K5/0821C07K5/1024C07K5/0606C07K5/081C07D495/04C07D519/00A61K47/551A61K47/56A61K38/00C07K14/605C07K14/62A61K47/65A61K47/61A61K31/4188C07K14/00
Inventor J·申O·全E·J·朴
Owner D&D PHARMATECH INC
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