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Compositions and methods to improve oral absorption of antimicrobial agents

A technology of antimicrobial agents and biopolymers, applied in the direction of drug combination, resistance to vector-borne diseases, antibacterial drugs, etc., can solve problems such as poor safety or tolerance

Inactive Publication Date: 2008-01-02
CUBIST PHARMA INC +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present invention solves these problems, increases the overall uptake of the active drug into the plasma, allows the development of new oral antimicrobials that were not available before, and allows "stepdown therapy" (also Transitioning patients from parenteral to oral therapy) addresses an unmet medical need for antimicrobial agents that are poorly safe or well tolerated due to problems associated with low gastrointestinal uptake

Method used

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  • Compositions and methods to improve oral absorption of antimicrobial agents
  • Compositions and methods to improve oral absorption of antimicrobial agents
  • Compositions and methods to improve oral absorption of antimicrobial agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 10

[0139] Example 10: Ceftriaxone-calcium-carrageenan complex changes with time in the plasma concentration of ceftriaxone after intraduodenal (i.d.) administration in rats

[0140] About 40 mg ceftriaxone (CTX) eq. / kg of the complex described in Example 1 was suspended in water and administered i.d. to four rats together with 0.2 ml capmul (absorption enhancer). At specific time intervals, 0.6 ml of blood was collected from each rat and centrifuged. About 0.2 ml of plasma was then analyzed for CTX by HPLC. The results are shown in Table 7 below:

[0141] Table 7

[0142] i.d. time after administration (minutes)

Embodiment 11

[0143] Embodiment 11: CTX changes with time to the plasma concentration of ceftriaxone after intraduodenal (i.d.) administration of rats, with capmul as contrast

[0144] As a control, four rats were administered i.d. about 40 mg / kg CTX together with 0.2 ml capmul. See Chemotherapy 34:77-84 (1988). At specific time intervals, 0.6 ml of blood was collected from each rat and centrifuged. About 0.2 ml of plasma was then analyzed for CTX by HPLC. The results are shown in Table 8 below:

[0145] Table 8

[0146] i.d. time after administration (minutes)

Embodiment 12

[0147] Example 12: Changes in plasma concentration of ceftriaxone over time after i.v. administration to rats

[0148] For comparison purposes, approximately 20 mg / kg CTX was administered (i.v.) to four rats. At specific time intervals, 0.6 ml of blood was collected from each rat and centrifuged. About 0.2 ml of plasma was then analyzed for CTX by HPLC. The results are shown in Table 9 below:

[0149] Table 9

[0150] Research#

Pilot projects

Capmul:

OCTX

Capmul:

CTX

Emulsion

Capmul concentration

The total administered

Capmul(g)

Cmax

(μg / ml)

bioavailability

%

103-2

OCTX1 (C)

10∶1

N / A

36-57

48.5

103-6

1 = OCTX1(E)

2 = OCTX2(C)

1＝1∶1

2＝10∶1

1＝2.2∶1

2＝11∶1

1 = 21.6mg / mL

2 = N / A

1＝5-7

2＝44-55

3.3

44.6

103-7

1 = OCTX2(E)

2 = OCTX2(E)

1＝5∶1

2＝10∶1

1＝9∶1

2...

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PUM

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Abstract

The present invention provides compositions and methods for increasing absorption of antibacterial agents, particularly third generation cephalosporin antibacterial agents, in oral dosage solid and / or suspension forms. Specifically, the composition is comprised of a biopolymer that is preferably swellable and / or mucoadhesive, an antimicrobial agent, and a cationic binding agent contained within the biopolymer such that the binding agent is ionically bound or complexed to at least one member selected from the group consisting of the biopolymer and the antimicrobial agent.

Description

field of invention [0001] The present invention relates to compositions and methods for enhancing the intestinal absorption of antimicrobial agents and their pharmaceutically acceptable salts, esters, ethers or hydrates by using selected antimicrobial agents in combination with cation-binding agents and Biopolymers and optional absorption enhancers. Specifically, the present invention relates to compositions and methods for enhancing the intestinal absorption of third generation cephalosporin antimicrobials, carbapenem and lipopeptide antimicrobials. Background of the invention [0002] The gastrointestinal tract ("GI"), specifically the small intestine, is the primary site of absorption of nutrients and most bioactive agents. To accommodate the amount of absorption that occurs in the small intestine, the surface area is enlarged by the presence of villi and microvilli. However, before a bioactive compound can be transferred from the lumen to the blood, the compound may ha...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/36A61K9/16A61P31/00A61K9/22A61K9/52A61K31/546A61K38/00A61K38/12A61K38/14A61K47/12A61K47/14A61K47/48A61P31/04
CPCA61K9/1652A61K38/14A61K38/12A61K47/4823A61K47/61A61P31/00A61P31/04Y02A50/30A61K47/50A61K47/02
Inventor S-H·周J-S·李D·凯斯
Owner CUBIST PHARMA INC
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