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Combination formulations comprising darunavir and etravirine

A technology for dosage forms and oral preparations, which can be used in medical preparations containing active ingredients, pill delivery, antiviral agents, etc., and can solve problems such as physical difficulties, exceeding the convenient size limit, and large size.

Inactive Publication Date: 2010-07-28
TIBOTEC PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The combination tablet would therefore weigh 1425.2mg and be large in size, exceeding the convenient size limit, making it difficult for the patient to take such a large tablet both perceptually and practically
This makes tablet loading the number one problem to be tackled with combination tablets

Method used

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  • Combination formulations comprising darunavir and etravirine
  • Combination formulations comprising darunavir and etravirine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0105] 1) Preparation of spray-dried powder

[0106] The feed mixture for the spray-dried formulation was prepared by dissolving TMC125 and polymer in a solvent and adding microcrystalline cellulose. The polymer types, solvents and amounts of components used are listed under feed mixture (iv) mentioned above. The feed mixture was then passed through a high pressure nozzle in co-current mode into an SD-12.5-N, closed loop spray drying chamber. The resulting solid pharmaceutical composition is collected from the cyclone and post-vacuum dried at elevated temperature to reduce residual solvent levels. The dry powder is sieved, and the powder sieve with a particle size between 45-100 microns is retained.

[0107] 2) Preparation of Combination Tablets

[0108] Table 1: Composition of Combination Tablets

[0109] ingredient name

[0110] ingredient name

[0111] Spray-dried TMC125 in HPMC was mixed with microcrystalline cellulose (MCC), croscarmellose sodi...

Embodiment 2

[0119] 1) Preparation of spray-dried powders

[0120] The preparation of spray-dried TMC125 was carried out as described in Example 1.

[0121] 2) Preparation for rolling ( roller compaction ) bulk mixture

[0122] Table 4

[0123] Component mg / tablet

[0124] The ingredients were hand passed through a 1 mm stainless steel screen and then mixed in a 100 l Gallay tumble mixer at 10 rpm for 10 minutes. In Gerteis Polygran TM Roller compaction on 250 / 100 / 3 roller compactor.

[0125] Table 5: Roller compaction settings

[0126]

[0127] Table 6: Results of rolled material

[0128]

[0129] Table 7: Final Blending and Tabletting

[0130] Material mg / tablet

[0131] Except for magnesium stearate, all ingredients were passed through a 1mm stainless steel sieve, and then in 100 lGallay TM Mix for 10 minutes at 10 rpm in a tumble blender. The sieved magnesium stearate was then added to the mixture and mixed at the same speed for an a...

Embodiment 3

[0147] Example 3 : coating

[0148] Table 12: Dissolution Rates of Coated and Uncoated TMC125

[0149] Dissolution of TMC125 in Combination Tablets in Experiment 2

[0150] time (minutes)

5

10

15

20

30

45

60

120

180

210

1030daN uncoated

1266daN uncoated

1030daN coating

1266daN coating

31.67

16.77

21.99

46.35

14.60

27.45

37.79

57.37

20.96

37.80

46.23

65.95

28.70

46.96

52.07

75.10

42.77

62.47

60.11

80.93

52.56

80.84

67.31

84.83

61.74

89.56

72.54

93.07

76.12

98.21

83.87

96.29

81.10

99.61

88.91

98.15

88.90

99.34

91.43

[0151] Table 13: Dissolution Rates of Coated and Uncoated TMC114

[0152] Dissolution of TMC114 in Combination Tablets in Experiment 1

[0153] time (minutes)

5

10

15

20

30

45

60

120

...

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Abstract

This invention relates to solid oral dosage forms of the HIV inhibitors containing a combination of TMC114 and TMC125.

Description

field of invention [0001] The present invention relates to a solid oral dosage form of an HIV inhibitor comprising a combination of TMC114 and TMC125. Background of the invention [0002] Human immunodeficiency virus (HIV) infection, the known cause of acquired immunodeficiency syndrome (AIDS), remains a major medical problem for its treatment. HIV is able to escape immune pressure, adapt to a variety of cell types and growth conditions, and develop resistance to currently available drug therapies. The latter include nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), nucleotide reverse transcriptase inhibitors (NtRTIs), HIV-protease inhibitors (PIs), fusion inhibitors and Recent CCR5 and integrase inhibitors. [0003] Although each of these drugs is effective at suppressing HIV when used alone, they all face the emergence of drug-resistant mutants. This has led to the use of combination therapy of several anti-HI...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/34A61K31/505A61P31/18
CPCA61K31/505A61K9/2077A61K9/1652A61K9/146A61K31/34A61P31/18A61K2300/00
Inventor J·F·M·沃尔斯波尔斯E·M·J·詹斯
Owner TIBOTEC PHARMA
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