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Methods for producing an oralsuspension of teichoplanin or teichoplanin analogs

a technology of teichoplanin and oral suspension, which is applied in the directions of peptide delivery, emulsion delivery, saccharide peptide ingredients, etc., can solve the problems of inconvenient reconstitution process for both the pharmacist and the patient in need of teichoplanin treatment, incomplete administration of dose, and decreased patient compliance, so as to improve patient compliance, taste and stability, and reduce the ability to swallow

Inactive Publication Date: 2017-03-09
MAHER ILLYA KEITH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention is a stable suspension of teicoplanin that can be formulated in the form of an aqueous or non-aqueous vehicle. The suspension has improved taste, stability, and solubility by careful manipulation of the flavouring and sweetening agents, as well as particle size. This suspension is suitable for patient-friendly dosage forms for children, geriatrics, and others with decreased ability to swallow solid orals. It provides better patient compliance, improved stability, and does not have dose variation issues. The suspension has a particle size with most particles falling within the range of d90 being less than about 170 μητ.

Problems solved by technology

The reconstitution process is inconvenient for both the pharmacist and the patient in need of teicoplanin treatment due to the foaming of the lyophilized powder on addition of water, as taught in the prior art by Vecchio EP1806150 and Kruchek (Anaesthesia, 2010, 65, 1047).
Foaming of the teicoplanin solution can result in incomplete administration of the dose if administered orally before the foaming has subsided.
Additionally, the formulation is not flavored to mask the unpalatable bitterness of teicoplanin; thus this can significantly led to a decrease in patient compliance.
Furthermore, sterile water for injection is typically the vehicle for compounding this preparation and it lacks preservatives increasing the risk of contamination and exposure to pathogens (bacteria, viruses, fungi / yeast, and / or mold spores).
For patients already infected with staphylococci or clostridium difficile any exposure to additional pathogens due to a contaminant can worsen their outcome.

Method used

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  • Methods for producing an oralsuspension of teichoplanin or teichoplanin analogs

Examples

Experimental program
Comparison scheme
Effect test

example 1

Teicoplanin 20 mg / mL Oral Suspension

[0047]

1. Teicoplanin2000mg2. Colloidal silicon dioxide2mg3. Citric acid monohydrate0.3mg4. FD&C Red#30.05mg5. Strawberry flavoring0.05mg6. Propylene glycol15ml7. Water, Purifed15ml8. Sorbitol70ml

Procedure

[0048]1. Calculate the required quantity of each ingredient for the total amount to be prepared.[0049]2. Accurately weigh and / or measure each ingredient.[0050]3. Prepare the suspension using 2 (two) separate Beakers.[0051]4. Beaker 1: levigate teicoplanin (item 1) and colloidal silicon dioxide (item 2) in 30% sorbitol (item 8) (30 ml).[0052]5. Beaker 2: Dissolve citric acid (item 3), strawberry flavor (item 5) and FD&C Red #3 (item 4) in purified water (item 7).[0053]6. Add Beaker 2 to Beaker 1 while stirring then add propylene glycol (item 6) and stir well.[0054]7. Complete to the final volume with sorbitol (item 8) and mix well.

example 2

Teicoplanin 20 mg / mL Oral Suspension

[0055]

1. Teicoplanin2000mg2. Colloidal silicon dioxide2mg3. Sodium Citrate0.3mg4. FD&C Red#30.05mg5. Strawberry flavoring0.05mg6. Propylene glycol15ml7. Water, Purifed15ml8. Sorbitol70ml

Procedure

[0056]1. Calculate the required quantity of each ingredient for the total amount to be prepared.[0057]2. Accurately weigh and / or measure each ingredient.[0058]3. Prepare the suspension using 2 (two) separate Beakers.[0059]4. Beaker 1: levigate teicoplanin (item 1) and colloidal silicon dioxide (item 2) in 30% sorbitol (item 8) (30 ml).[0060]5. Beaker 2: Dissolve sodium Citrate (item 3), strawberry flavor (item 5) and FD&C Red #3 (item 4) in purified water (item 7).[0061]6. Add Beaker 2 to Beaker 1 while stirring then add propylene glycol (item 6) and stir well.[0062]7. Complete to the final volume with sorbitol (item 8) and mix well.

example 3

Teicoplanin 20 mg / mL Oral Suspension

[0063]

1. Teicoplanin2000mg2. Poloxamer 4071mg3. Citric acid monohydrate0.3mg4. FD&C Red#30.05mg5. Strawberry flavoring0.05mg6. Propylene glycol15ml7. Ethanol 95%5ml8. Water, Purifed10ml9. Sorbitol70ml

Procedure

[0064]1. Calculate the required quantity of each ingredient for the total amount to be prepared.[0065]2. Accurately weigh and / or measure each ingredient.[0066]3. Prepare the suspension using 2 (two) separate Beakers.[0067]4. Beaker 1: levigate teicoplanin (item 1) in 30% sorbitol (item 9) (30 ml), then add ethanol (item 7) and stir well.[0068]5. Beaker 2: dissolve citric acid (item 3), poloxamer 407 (item 2), strawberry flavor (item 5) and FD&C Red #3 (item 4) in purified water.[0069]6. Add Beaker 2 to Beaker 1 while stirring then add propylene glycol (item 6) and stir well.[0070]7. Complete to the final volume with sorbitol (item 8) and mix well.

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Abstract

A stable suspension of teicoplanin and one or more pharmaceutically acceptable additives and method for preparation wherein the teicoplanin is mixed with an aqueous or non aqueous suspension base and pharmaceutically acceptable additives and wherein the teicoplanin is milled to obtain a homogeneously dispersed suspension.

Description

RELATED APPLICATIONS[0001]This application claims priority to U.S. Provisional Application No. 62 / 215,425 filed Apr. 30, 2015. The entire contents of the above application are hereby incorporated by reference as though fully set forth herein.FIELD[0002]The present invention relates to the field of medicinal preparations containing peptides. More specifically, the present invention relates to preparations of teicoplanin, which is an antibiotic of the glycopeptide family, more particularly of the ristocetin type.BACKGROUND[0003]Teicoplanin is an antibiotic used in the prophylaxis and treatment of infections caused by Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus, Enterococcus faecalis and Clostridium. It is a semisynthetic glycopeptide antibiotic with a spectrum of activity similar to vancomycin. Its mechanism of action is to inhibit the polymerization of cell wall components in bacterial cell wall synthesis.[0004]Teicoplanin is complex glycoprotein mix...

Claims

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Application Information

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IPC IPC(8): A61K38/14A61K9/14A61K9/10
CPCA61K38/14A61K9/14A61K9/10A61K9/0095
Inventor MAHER, ILLYA KEITH
Owner MAHER ILLYA KEITH
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