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Dry granulated formulations of azithromycin

A technology of azithromycin and dry granules, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and pill delivery, which can solve the problems of long holding time and increased adhesion

Inactive Publication Date: 2005-07-27
PFIZER PRODS ETAT DE CONNECTICUT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some tablet presses have a longer dwell time than others, allowing increased sticking

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107] Tablet Performance Index

[0108] The compression performance index of certain azithromycin formulations was evaluated to determine any mechanical disadvantages or attributes that may affect tablets of these azithromycin formulations. The evaluation was carried out in accordance with the method described in "Indices of Tableting Performance" H.E.N. Hiestand and D.P. Smith, Powder Technology 38 [1984] pp. 145-159.

[0109] Specifically, the Brittle Fracture Index (BFI) is calculated from the ratio of the material's normal tensile strength to its compromise tensile strength. The strain index (SI) was determined from a dynamic indentation hardness test. The Worst Case Bonding Index (Worst Case Bonding Index) was determined by evaluating the degree of bonded particles retained after decompression subjected to compression with a short dwell time and the plasticity mechanism of particle separation during decompression.

[0110] The tableting index of...

Embodiment 2

[0117] Azithromycin Dry Granules

[0118] The effect of the blending method and the effect of the azithromycin form on the dry granules was evaluated as follows.

[0119]Prepared by dry blending 35.2 wt% azithromycin, 54.8 wt% anhydrous dicalcium phosphate diluent, 4.0 wt% croscarmellose sodium disintegrant and 5.0 wt% magnesium stearate lubricant Compressed (slugs) formulations of azithromycin Forms A, M and F. Finally, 1.0 wt% magnesium stearate was added before tableting, and the total amount of lubricant was 6.0 wt%.

[0120] Dry granules were prepared by two different blending methods. 3 wt % lubricant was mixed with drug, diluent and disintegrant in a Turbula shaker-mixer (Willy A. Bachofen AG Maschinenfabrik, Basel, Switzerland) for 10 minutes using the long mixing method. The mixture was screened (20 mesh) and mixed for an additional 10 minutes. An additional 2 wt% lubricant was added and mixed in the Turbula shaker-mixer for an additional 2 min...

Embodiment 3

[0140] Azithromycin Configuration and Effect of Low and High Drug Loading

[0141] The effect of drug configuration on dry granulated tablets was studied using Forms A, F, J and M with low and high drug load formulations. The long-time blending method and test method described in Example 2 were used.

[0142] The low drug load formulation contained 35.2 wt% azithromycin, 54.8 wt% dicalcium phosphate anhydrous, 4.0 wt% croscarmellose sodium and 6.0 wt% magnesium stearate. The high drug load formulation contained 58.2 wt% azithromycin, 31.8 wt% dicalcium phosphate anhydrous, 4.0 wt% croscarmellose sodium and 6.0 wt% magnesium stearate.

[0143] Pre-compressed tablets were prepared as described in Example 2 and tested for hardness (kP scale). The results for low and high drug load particles are shown in Tables 3A and 3B, respectively.

[0144] The higher drug loading formulation achieved a target hardness of approximately 12 kP at a much lower compression force, wh...

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Abstract

This invention relates to a pharmaceutical formulation, in the form of a tablet, sachet or powder for suspension dosage form, which comprises dry granulated particles of a non-dihydrate form of azithromycin and, optionally, one or more pharmaceutically acceptable excipients. Preferably, the pharmaceutical formulation is a tablet containing between about 40%, by weight, to about 85% , by weight, non-dihydrate azithromycin. More preferably, the pharmaceutical formulation contains non-dihydrate azithromycin selected from the forms B, D, E, F, G, H, J, M, N, 0, P, Q, R, or mixtures thereof. Even more preferably, the invention relates to a pharmaceutical formulation wherein the dosage of azithromycin is 250 mgA, 500 mgA, 600 mgA or 1000 mgA. The present invention further relates to a dry granulated azithromycin particle, comprising a form of azithromycin, selected from forms D, E, F, G, H, J, M, N, 0, P, Q, R and mixtures of non-dihydrate forms, and at least one pharmaceutically acceptable excipient.

Description

Background of the invention [0001] Dry granulation is a method of forming granules by a compaction step followed by sizing of compacts into easily processable granules. It is often used to improve flow and / or increase the density of formulations, facilitating further manufacturing processes such as tableting, encapsulation and powder filling. Compressions are usually made directly from powder blends containing the active ingredient and other excipients including lubricants. [0002] Drug manufacturers prefer dry granulation techniques over wet granulation because the process is less time consuming and less expensive. However, dry granulation is generally limited to those cases where the drug or active ingredient has physical properties suitable for forming pharmaceutically acceptable granules and various dosage forms such as tablets. [0003] The addition of at least one excipient to the formulation is usually required and serves to increase the size of the final product tab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/20A61K9/48A61K31/16A61K31/70A61K31/7052A61K47/04A61K47/36A61K47/38A61P31/04A61P33/02
CPCA61K9/2054A61K31/70A61K9/2095A61K9/2009A61P31/04A61P33/02A61K9/20A61K31/7052A61K9/16
Inventor 巴巴拉·A·约翰逊厄恩斯特·S·奎安
Owner PFIZER PRODS ETAT DE CONNECTICUT
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