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DRY PROCESSING OF ATAZANAVIR

2020-10-07 09:19:14

Key Words：DRY PROCESSING OF ATAZANAVIR

Claims

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1. Process for producing oral dosage forms, more specifically tablets, comprising atazanavir and adhesion enhancers, wherein said dosage forms are produced by means of dry compaction or by means of direct compression, and the atazanavir to adhesion enhancer weight ratio is from 5: 1 to 1 :7.

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2. Process according to Claim 1 , comprising the steps

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(a) mixing of atazanavir with an adhesion enhancer and optionally further pharmaceutical excipients;

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(b) compaction to give a slug;

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(d) compression of the resulting granules to give tablets, where appropriate with addition of further pharmaceutical excipients; and

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(e) optionally covering of the tablets with a film, with the granulation conditions in step (c) being chosen such that the D 50 value of the particle size distribution of the granules lies between 100 and 450 μηι.

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3. Process according to Claim 2, wherein the compaction (b) is carried out in a roll granulator and the rolling force is from 2 to 70 kN/cm, preferably 5 to 50 kN/cm.

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4. Process according to Claim 1, comprising the steps

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(a) mixing of atazanavir with an adhesion enhancer and optionally further pharmaceutical excipients; and

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(d) direct compression of the resulting mixture to give tablets, and

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(e) optionally covering of the tablets with a film.

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5. Process according to Claim 4, wherein the mixture resulting from step (a) has a particle size distribution D 50 value of from 50 to 250 μιη.

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6. Process according to any of Claims 1 to 5, wherein a stabilizing agent is added.

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7. Process according to Claim 6, where the stabilizing agent is citric acid.

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8. Process according to any of Claims 1 to 7, wherein atazanavir is used in an amount of from 20 to 60% by weight, based on the total weight of all substances used.

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9. Process according to any of Claims 1 to 8, wherein particulate atazanavir with a particle size distribution D 50 value of from 5 to 150 μιη is used. 10. Tablets obtainable according to any of Claims 1 to 9.

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1 1. Tablets according to Claim 10 having a friability of less than 3%, a content uniformity of from 95 to 105% and a hardness of from 30 to 200 N, said tablets comprising from 50 to 300 mg of atazanavir.

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12. Tablet comprising atazanavir and adhesion enhancers, with the atazanavir to adhesion enhancer weight ratio being from 5: 1 to 1 :7 and said tablet having a bimodal pore size distribution.

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13. Intermediate obtainable by dry compaction of atazanavir together with an adhesion enhancer, with the atazanavir to adhesion enhancer weight ratio being from

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5: 1 to 1 :7.

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14. Intermediate according to Claim 13, wherein the density of the intermediate is from 0.8 to 1.3 g/cm 3, preferably 0.9 to 1.20 g/cm 3.

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15. Sachet or stick pack comprising an intermediate according to either of Claims 13 and 14.

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