Stable non-dihydrate azithromycin oral suspensions

A technology for oral suspension and azithromycin, applied in the field of reducing the conversion of non-dihydrated azithromycin, reducing the conversion of non-dihydrated azithromycin, oral suspension formulations

Inactive Publication Date: 2006-08-23
PFIZER PRODS ETAT DE CONNECTICUT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the very bitter taste of azithromycin, appropriate flavoring is required to ensure patient compliance and reduce vomiting after swallowing

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0103] Stability of non-dihydrated azithromycin in aqueous and flavored oral suspensions

[0104] Evaluation of the stability of different forms of non-dihydrated azithromycin in aqueous and flavored oral suspensions. In particular, non-dihydrate azithromycin forms G, M, N, F and J, respectively, are used in POS Formulation II. These POS formulations were made by mixing with 18ml of water. The suspension was then stored at 5°C or 30°C for 1, 5 and 10 days. Suspensions of bulk azithromycin forms G, M, N, F and J were also made up with 18 ml of water and kept under the same conditions.

[0105] At the end of the holding time, the suspension was filtered and the suspended solids were collected as described above. These solids were then analyzed using SS-NMR to quantify the presence of azithromycin dihydrate (Form A) in the recovered azithromycin samples on a weight percent basis (wt%).

[0106] Storage time after making

[0107] NA = not analyzed

[0108] Table 1 s...

Embodiment 2

[0114] Effects of different flavoring agents and sucrose on form transformation

[0115] To evaluate proposed excipients, active doses of azithromycin and desired amounts of potential excipients were suspended in a 0.1 M phosphate buffer system corrected to pH 8.16. The buffer system is achieved by adding 13.738g of NaH 2 PO 4 ·H 2 O was dissolved in 900 ml of water, the pH was corrected to 8.16 using sodium hydroxide, and the solution was diluted in 1 L of water. Once samples are prepared in buffer, store at room temperature for the desired shelf life of the finished product. The azithromycin product was then isolated by filtration and the resulting solid filtrate was analyzed using the solid state NMR method described above for the dihydrate form, which can be present quantitatively.

[0116] The effect of different flavor components and sucrose on the conversion of azithromycin form G to azithromycin dihydrate (form A) in suspension was evaluated as described below.

...

Embodiment 3

[0127] Identification of Flavor Components that Facilitate Form Conversion of Azithromycin

[0128] In Example 1, form conversion of azithromycin was shown when the non-dihydrated azithromycin was prepared in a flavored suspension suitable for use as an oral suspension dosage form. Moreover, a high conversion rate was produced in the suspension containing Trusil artificial banana flavor compared to the suspension containing B&C banana flavor, which shows that Trusil artificial banana flavor contains a higher amount of Conversion enhancers or more effective conversion enhancers.

[0129] In order to evaluate the effect of the different components of the suspension flavor on the conversion of the non-dihydrated azithromycin form, for the main components of artificial vanilla milk, Trusil cherry flavor, B&C banana flavor or Trusil banana flavor in Example 2 Confirmation was performed and quantification was performed using gas chromatography. Sucrose was also analyzed.

[0130]...

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PUM

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Abstract

This invention relates to a powder for oral suspension, and an oral suspension made there from, which comprises non-dihydrate azithromycin and an azithromycin conversion stabilizing excipient, wherein said excipient reduces the conversion of the form of azithromycin, when placed in suspension, to another form of azithromycin. This invention further relates to a method for reducing the conversion of a form of non-dihydrate azithromycin, in an oral suspension, by adding a surface tension reducing excipient that reduces the surface tension of the aqueous vehicle. Furthermore, this invention relates to a method for reducing the conversion of a non-dihydrate azithromycin, in an unflavored oral suspension, by raising the viscosity of the oral suspension, and in a flavored oral suspension by lowering the viscosity of the oral suspension.

Description

Background of the invention [0001] Azithromycin, also known as 9-deoxy-9a-aza-9a-methyl-9a-homoerythromycin A, exists as a dihydrate as well as a large number of non-dihydrate forms. [0002] Azithromycin is administered for the treatment of a variety of infections, particularly infections of the urinary tract, bronchi, lungs, sinuses, and middle ear. [0003] In the treatment of pediatric patients, azithromycin is administered as a dosage form of oral suspension, which is administered by single or multiple courses of treatment. The oral suspension dosage form is preferred for pediatric therapeutic use because it provides better control over the amount of azithromycin administered and because many pediatric patients are unable to swallow other oral dosage forms. However, since azithromycin has a very bitter taste, suitable flavoring is required to ensure patient compliance and reduce vomiting after swallowing. More recently, oral suspensions of azithromycin have included azi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/26A61K47/36A61K47/38A61K47/40A61K31/7048
Inventor 史蒂文·W·科利尔威廉·J·柯拉托洛巴巴拉·A·约翰逊布伦丹·J·墨菲
Owner PFIZER PRODS ETAT DE CONNECTICUT
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