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Formulation of fast-dissolving efavirenz capsules or tablets using super-disintegrants

A technology of disintegrating agent and capsule, applied in the field of preparing said tablet or capsule

Inactive Publication Date: 2001-05-23
BRISTOL MYERS SQUIBB PHARMA CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In these cases, the dissolution of the drug from the dosage form in the gastrointestinal tract may be the limiting factor in determining the rate and extent of drug absorption into the body

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1: wet granulation 100mg capsule preparation

[0051] Preparation method: Mix efavirenz and sodium starch glycolate in the granule, then add sodium lauryl sulfate aqueous solution and carry out wet granulation. The wet material is then dried in a fluid bed, drying tray or other suitable dryer. The dried granules can then be milled to achieve a suitable particle size distribution prior to mixing with the other ingredients. The mixture is then filled into two hard gelatin capsule shells.

[0052] Ingredient Amount in each capsule %

[0053] efavirenz 100mg 39.06

[0054] Sodium Lauryl Sulfate 5mg 1.95

[0055] Lactose hydrate 57mg 22.26

[0056] Magnesium Stearate 4mg 1.56

[0057] Sodium starch glycolate (in granules) 80mg 31.25

[0058] Sodium starch glycolate (extragranular) 10mg 3.91

Embodiment 2

[0059] Capsule total weight 256mg Embodiment 2: Wet granulation 100mg capsule preparation

[0060] Preparation method: granulate efavirenz and sodium intragranular starch glycolate with an aqueous solution of sodium lauryl sulfate. The wet material is then dried in a fluid bed, drying tray or other suitable dryer. The dried granules can then be milled to achieve a suitable particle size distribution prior to mixing with the other ingredients. The mixture is then filled into two hard gelatin capsule shells.

[0061] Ingredient Amount in each capsule %

[0062] efavirenz 100mg 21.93

[0063] Sodium Lauryl Sulfate 5mg 1.10

[0064] Sodium starch glycolate (in granule) 50mg 10.96

[0065] Sodium starch glycolate (extragranular) 10mg 2.19

[0066] Lactose hydrate 277mg 60.75

[0067] Talc 8mg 1.75

[0068] Colloidal silicon dioxide 4mg 0.88

[0069] Stearic acid 2mg 0.44

[0070] Total capsule weight 456mg Example 3: wet granulation 300mg tablet formulation

[0071] Prep...

Embodiment 3

[0092] Embodiment 3 tablet formulations:

[0093] Time (minutes) % Dissolved

[0094] 10 78.0

[0095] 15 91.5

[0096] 30 100.0

[0097] 45 102.1

[0098] 60 102.9

[0099] Capsule and tablet samples made during the above manufacturing process were analyzed to determine dosage form uniformity. The content uniformity of capsules and tablets was determined according to the guidelines set forth by USP. The results are shown in Table 3. "RSD" as used in this specification means Relative Standard Deviation and is calculated according to USP guidelines.

[0100] table 3

[0101] Content homogeneity analysis

[0102] Embodiment 1 capsule:

[0103] Inclusion Uniformity 100.2+ / -1.7% (mean + / -RSD)

[0104] Embodiment 3 tablet:

[0105] Inclusion Uniformity 104.3+ / -0.7% (mean + / -RSD)

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PUM

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Abstract

The present invention provides improved oral dosage form formulations of efavirenz that are useful in the inhibition of human immunodeficiency virus (HIV), the prevention or treatment of infection by HIV, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS). In particular, the present invention relates to compressed tablets or capsules comprising efavirenz that contain one or more disintegrants that enhance the dissolution rate of the efavirenz in the gastrointestinal tract thereby improving the rate and extent of absorption of efavirenz in the body. The present invention also relates to the process of making such tablets or capsules.

Description

technical field [0001] The present invention provides improved oral dosage formulations of efavirenz for inhibiting human immunodeficiency virus (HIV), preventing or treating HIV infection, and treating acquired immunodeficiency syndrome (AIDS) caused by HIV infection. In particular, the present invention relates to compressed tablets or capsules containing efavirenz containing one or more disintegrants capable of increasing the rate of dissolution of efavirenz in the gastrointestinal tract, thereby improving the rate and extent of absorption of efavirenz in the body. The invention also relates to a process for the preparation of said tablet or capsule. Background technique [0002] In dose titration of patients, the aim is to achieve and maintain drug blood levels that exceed the minimum effective level required for a therapeutic response, but do not exceed the minimum toxic level. The absorption of a drug from an oral dosage form such as a tablet o...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/535A61K31/536A61K47/36A61P31/18
CPCA61K9/1652A61K9/2054A61K31/536A61K9/2059Y10S514/885A61P31/18A61K9/48
Inventor W·T·马科伊-莫雷赫德J·D·贝勒B·R·兰德曼
Owner BRISTOL MYERS SQUIBB PHARMA CO
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