Hiv treatment formulation of atazanavir and cobicistat

一种考比泰特、制剂的技术，应用在阿扎那韦和考比泰特的HIV治疗制剂领域，能够解决给药不方便、患者依从性损害等问题，达到降低丸剂负荷的效果

Inactive Publication Date: 2016-10-12
BRISTOL MYERS SQUIBB HLDG IRELAND UNLTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If there are too many separate pills to swallow at too many intervals, dosing becomes inconvenient and adherence to treatment is less likely
Similarly, patient compliance can also be severely compromised if pills or other dosage units are difficult to swallow by themselves

Method used

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  • Hiv treatment formulation of atazanavir and cobicistat
  • Hiv treatment formulation of atazanavir and cobicistat
  • Hiv treatment formulation of atazanavir and cobicistat

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1 - Manufacturing method

[0054] Manufacture of Atazanavir (ATV) Granules

[0055] Below is a description of the method used to manufacture ATV granulation for ATV / COBI film coated tablets. Materials can be pre-screened when required.

[0056]1. Add microcrystalline cellulose (intragranular part), atazanavir sulfate, stearic acid, sodium starch glycolate (intragranular part), crospovidone (intragranular part) and hydroxypropyl cellulose to a suitable in a mixer, and blend the materials.

[0057] 2. Wet granulate the premix from step 1 with water.

[0058] 3. Wet mill the granulation from step 2 using a suitable Comil.

[0059] 4. Dry the granules from step 3 in a suitable fluid bed drier.

[0060] 5. Size the dry pellet from step 4 using the appropriate Comil.

[0061] 6. Add microcrystalline cellulose (extragranular fraction), sodium starch glycolate (extragranular fraction), and crospovidone (extragranular fraction) to the granules from step 5 and ble...

Embodiment 2

[0076] Example 2 Batch size and formulation

[0077] Representative batch sizes and formulations for ATV / COBI film-coated tablets are provided in Tables 1 and 2, respectively.

[0078]

[0079]

[0080]

[0081] NOTE: The amount of atazanavir (as free base) is theoretically equivalent to 87.8% atazanavir sulfate.

[0082] The amount shown is equivalent to 150 mg corbytide (without silicon dioxide). The amount of corbitide-on-silica was adjusted based on the drug content factor (DCF) for corbitide-on-silica, with a concomitant adjustment in microcrystalline cellulose.

[0083] q.s. = adequate; NA = not applicable.

Embodiment 3

[0084] Example 3 - The composition of an ATV / COBI film-coated tablet with 300 mg (as free base) of atazanavir sulfate / 150 mg of corbitide is set forth in Table 3 below:

[0085]

[0086] The amount of atazanavir (as free base) is theoretically equivalent to 87.8% atazanavir sulfate. The amount is 87.8% based on a theoretical determination "as is"; 341.7 mg of atazanavir sulfate is equivalent to 300 mg of atazanavir. Adjustments may be made "as is" based on actual assays of the drug lot batches used in the manufacture of the drug product.

[0087] Corbytate Pharmaceuticals is Corbytate on silica. The amount shown is equivalent to 150 mg corbytide (without silicon dioxide). The amount of corbitide-on-silica was adjusted based on the drug content factor (DCF) for corbitide-on-silica, with a concomitant adjustment in microcrystalline cellulose.

[0088] (NC = Non-Compendial NF = National Formulary Ph.Eur. = European Pharmacopoeia USP = United States Pharmacopoeia).

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PUM

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Abstract

Formulations of the HIV compounds atazanavir and cobicistat, and methods of treatment utilizing these formulations, are set forth.

Description

[0001] Cross references to related applications [0002] This application claims priority to US Provisional Application Serial No. 61 / 887,574, filed October 7, 2013, which is hereby incorporated by reference in its entirety. field of invention [0003] The present invention relates to two-drug combinations containing antiretroviral compounds, useful formulations against HIV. In particular, the present invention relates to bilayer combination formulations of atazanavir and cobicistat. Additionally, the present invention relates to fixed dose combination tablets of atazanavir and corbitide having good physical properties and low levels of degradants, and efficient delivery of the two active pharmaceutical components. The invention also relates to methods of administering these formulations to a patient in need of treatment. Background of the invention [0004] HIV-1 (Human Immunodeficiency Virus-1) infection remains a major medical problem, with tens of millions of people wo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24
CPCA61K9/2054A61K9/209A61K31/4418A61K31/5377A61P31/12A61P31/18A61P43/00A61K2300/00A61K9/2095
Inventor O.M.Y.库F.尼法J.陶N.K.科塔拉S.A.瓦里亚
Owner BRISTOL MYERS SQUIBB HLDG IRELAND UNLTD
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