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Colonic delivery using Zn/pectin beads with a Eudragit coating

A colon and pectin technology, applied in the directions of capsule delivery, microcapsules, peptide/protein components, etc., can solve problems such as aggravating the discomfort of the original disease and the bad feeling of patients

Inactive Publication Date: 2010-08-04
DA VOLTERRA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Even though the diarrhea is usually not severe and stops quickly (spontaneously or after completion of antibiotic therapy), the patient feels bad about it and exacerbates the discomfort of the original illness for which the antibiotic was prescribed;

Method used

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  • Colonic delivery using Zn/pectin beads with a Eudragit coating
  • Colonic delivery using Zn/pectin beads with a Eudragit coating
  • Colonic delivery using Zn/pectin beads with a Eudragit coating

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0268] Example 1: Development of a sensitive, quantitative and specific assay for β-lactamase L1

[0269] Hydrolysis of nitroceftin is a well-known technique for quantification of penicillinase activity. However, the usual format is in a single tube and is not suitable for the analysis of large numbers of samples. This example describes the development and fit for purpose qualification of this assay performed in a 96-well microplate format.

[0270] A stock solution of nitroceftin was obtained by dissolving dry powder of nitroceftin in dimethyl sulfoxide (DMSO) at a concentration of 10 mM. Stock solutions were stored at -20°C and diluted 100-fold immediately before use in 50 mM sodium phosphate buffer (Hepes buffer) pH 7.0 containing 0.1 mg / ml bovine serum albumin (BSA). The choice of buffer is described in Table 1.

[0271] Add 20 μl of the solution to be analyzed to 180 μl of the diluted nitrocefamin. The kinetics of nitrocefaxifen hydrolysis was measured by absorbance m...

Embodiment 2

[0278] Example 2: Instability of β-lactamase L1 in raw pectin mixtures and the role of metal counterions

[0279] 0.3 ml of β-lactamase L1 (Eurogentec, Belgium, approximately 10 mg / mL by μBCA assay) was mixed with 10 g of a 6% pectin solution (low methoxylated amidated pectin (Unipectine ), Texturant Systems, cat#OG175C) mixed; the pH of the pectin solution was not adjusted.

[0280] Under the condition of stirring (200rpm) at room temperature, the pectin / β-lactamase L1 mixture was added dropwise to 40ml of calcium chloride (6 %) of the beaker.

[0281]After further incubation to equilibrate free and bound calcium ions, the beads were recovered by filtration and washed 3 times in 200 ml of purified water to remove excess free calcium. At this stage, the beads are referred to as "gelled beads".

[0282] The beads were dried in an oven at 37°C for 2 hours, resulting in dried beads.

[0283] 2x5 drop and 2x15 drop samples were taken at the outlet of the needle to measure init...

Embodiment 3

[0288] Example 3: Optimization of metal ions for gelling pectin, and effect of pH of pectin solution

[0289] To determine the effect of pectin solution parameters and zinc ions, an experiment comparing 4 formulations was carried out. The design scheme was established according to the factorial design Design Expert 6.0.10, Stat-Ease, Minneapolis. Check two parameters:

[0290] (a) pH of pectin solution: 4.0 and 7.0.

[0291] (b) Metal cations in the gelling water bath: Ca 2+ (CaCl 2 ) or Zn 2+ (Zinc acetate is abbreviated as ZnAc)

[0292] Beads were prepared as described in Example 2. However, since the stability of pectin decreases with increasing pH, the concentration of pectin solution was reduced from 6% to 4%.

[0293] Encapsulation yield was measured by assaying the enzymatic activity of β-lactamase L1, as described in Example 1.

[0294] Five beads were dissolved in 20 ml at 4°C in the presence or absence of 1% pectinase (Pectinase from Aspergillus aculeatus, P...

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Abstract

Drug delivery systems that can deliver therapeutic and / or diagnostic agents to the colon are disclosed. The systems include pectin beads crosslinked with zinc or any divalent cation of interest, which beads are then coated with Eudragit TM -type polymers. The drug delivery systems are orally administrable, but can deliver the active agents to the colon, or, in some embodiments, to various other positions in the gastro-intestinal tract. The agents can be used to diagnose, treat, prevent, or investigate a variety of conditions, including infectious diseases, inflammatory diseases, cancers and the like. Certain agents, such as metallo-dependent enzymes, for example, ss-lactamase Ll from Stenotrophomonas maltophilia, as well as agents that inactivate macrolide, quinolone, fluoroquinolone or glycopeptide antibiotics, can reduce the quantity of residual antibiotics reaching the colon following antibiotic therapy.

Description

field of invention [0001] The present invention is in the field of oral drug delivery systems for administering active agents, such as metallo-specific enzymes, to the colon. Background of the invention [0002] Drug delivery systems that specifically deliver active agents to the colon have been recognized as having important therapeutic advantages. Many colonic conditions will be treated more effectively if the active ingredient is delivered locally. Examples of such colonic disorders include Crohn's disease, ulcerative colitis, colorectal cancer, and constipation. [0003] Colonic release may also benefit patients when delayed absorption is necessary for therapeutic considerations. Examples include the treatment of conditions such as nocturnal asthma or colic (Kinget R. et al. (1998), Colonic Drug Targeting, Journal of Drug Targeting, 6, 129). [0004] Colonic release can also be used to administer therapeutically active polypeptides. Peptides are usually administered ...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K38/00
CPCA61K38/191A61K38/50A61K38/465A61K38/13A61K9/5073A61K38/43A61K38/46A61K9/5026A61K38/19A61P1/04A61P1/10A61P29/00A61P31/04A61P35/00A61P37/02
Inventor A·安德里蒙H-C·于盖
Owner DA VOLTERRA
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