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Modified release pharmaceutical compositions comprising mycophenolate and processes thereof

A composition, the technology of mycophenolic acid, applied in the field of modified release pharmaceutical composition, can solve the problems of increasing toxicity and so on

Inactive Publication Date: 2011-02-09
PANACEA BIOTEC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Takahashi et al. (1995) concluded that patients with a low AUC of MPA appear to be at high risk of developing graft rejection, while high target concentrations can increase toxicity

Method used

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  • Modified release pharmaceutical compositions comprising mycophenolate and processes thereof
  • Modified release pharmaceutical compositions comprising mycophenolate and processes thereof
  • Modified release pharmaceutical compositions comprising mycophenolate and processes thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 3

[0088] 0 0.000

[0089] 0.33 5.202

[0090] 0.5 7.198

[0091] 0.67 6.736

[0092] 0.833 7.106

[0093] 1 6.619

[0094] 1.25 5.111

[0095] 1.5 4.941

[0096] 2 4.137

[0097] 2.5 3.761

[0098] 3 3.030

[0099] 3.5 2.649

[0100] 4 2.312

[0101] 4.5 3.109

[0102] 5 4.166

[0103]5.5 3.740

[0104] 6 2.816

[0105] 6.5 2.140

[0106] 7 1.753

[0107] 7.5 1.556

[0108] 8 1.585

[0109] 9 1.445

[0110] 10 1.283

[0111] 11 1.444

[0112] 12 1.413

[0113] 14 1.237

[0114] 16 1.102

[0115] 18 0.817

[0116] 22 0.972

[0117] 24 0.764

[0118] AUC of the compositions mentioned in Example 3 below 0-12 with AUC 12-24 The result of the ratio is as follows:

[0119] AUC 0-12 AUC 12-24 Ratio (AUC 0-12 : AUC 12-24 )

[0120] Average 26.51 11.671 2.27:1

Embodiment 1

[0121] Example 1: (80:20)SR:IR

[0122] Substance No. Composition Amount / tablet (mg)

[0123] Sustained Release (SR) layer

[0124] 1. Sodium mycophenolate mofetil (equivalent to 576mg mycophenolic acid) 630.98

[0125] 2. Lactose DCL21 5.5

[0126] 3. Aerosil 200 150.02

[0127] 4. Polyvinylpyrrolidone (PVP K-90) 55

[0128] 5. Hypromellose 55

[0129] 6. Polyethylene oxide (Polyox WSR 301) 110

[0130] 7. Polyvinylpyrrolidone (PVP K-30) 27.5

[0131] 8. Sufficient amount of isopropanol (lost during processing)

[0132] 9. Magnesium stearate 10.5

[0133] Immediate Release (IR) layer

[0134] 10. Sodium mycophenolate mofetil (equivalent to 148mg mycophenolate mofetil) 158.3

[0135] 11. Microcrystalline cellulose 44

[0136] 12. Polyvinylpyrrolidone (PVP K-30) 2.2

[0137] 13. Sufficient amount of isopropanol (lost during processing)

[0138] 14. Magnesium stearate 2.2

[0139] step:

[0140] i) Sodium mycophenolate mofetil, anhydrous lactose, colloidal silic...

Embodiment 2

[0157] Example 2: (80:20)SR:IR

[0158] Substance No. Composition Amount / tablet (mg)

[0159] Sustained Release (SR) layer

[0160] 1. Sodium mycophenolate mofetil (equivalent to 576mg mycophenolic acid) 630.98

[0161] 2. Lactose DCL21 5.5

[0162] 3. Aerosil 200 150.02

[0163] 4. Polyvinylpyrrolidone (PVP K-90) 55

[0164] 5. Hypromellose 55

[0165] 6. Polyethylene oxide (Polyox WSR 301) 110

[0166] 7. Polyvinylpyrrolidone (PVP K-30) 27.5

[0167] 8. Sufficient amount of isopropanol (lost during processing)

[0168] 9. Magnesium stearate 10.5

[0169] Immediate Release (IR) layer

[0170] 10. Sodium mycophenolate mofetil (equivalent to 148mg mycophenolate mofetil) 158.3

[0171] 11. Starch 1500 42

[0172] 12. Succinic acid 22

[0173] 13. Polyvinylpyrrolidone (PVP K-30) 2.5

[0174] 14. Sufficient amount of isopropanol (lost during processing)

[0175] 15. Magnesium stearate 2.5

[0176] step:

[0177] i) Sodium mycophenolate mofetil, anhydrous lactose, c...

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Abstract

Modified release pharmaceutical compositions comprising mycophenolate as the active agent or its pharmaceutically acceptable salts, esters, polymorphs, isomers, prodrugs, solvates, hydrates, or derivatives thereof, wherein the said composition exhibits a biphasic release profile when subjected to in- vitro dissolution and / or upon administration in- vivo are provided. The composition provides a drug release in a manner such that the drug levels are maintained above the therapeutically effective concentration (EC) constantly for an extended duration of time. Further, the difference between the maximum plasma concentration of the drug (Cmax) and the minimum plasma concentration of the drug (Cmjn), and in turn the flux defined as ((Cmax - Cmjn) / Cavg) is minimal. The present invention also provides process of preparing such dosage form compositions and prophylactic and / or therapeutic methods of using such compositions.

Description

technical field [0001] The present invention relates to a modified release pharmaceutical composition, the modified release pharmaceutical composition comprising mycophenolic acid or its pharmaceutically acceptable salt, ester, polymorph, isomer, prodrug, solvate, hydrate or its The derivative is used as an active agent, wherein said composition exhibits a biphasic release profile when undergoing dissolution in vitro and / or when administered in vivo. The composition essentially comprises an immediate release fraction (IR) and at least one delayed release fraction, and provides drug release in a manner such that drug levels are consistently maintained above therapeutically effective levels for an extended period of time. Concentration (EC) but below the level of toxic concentration (TC). In addition, the maximum plasma concentration of the drug (C max ) and the minimum plasma concentration of the drug (C min ) and is then defined as (C max -C min ) / C avg flux, compared to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/365
CPCA61K9/209A61K31/365A61P37/02A61P37/06
Inventor 拉杰什·贾殷苏克吉特·辛格
Owner PANACEA BIOTEC
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