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Nalbuphine-based formulations and uses thereof

A technology of sodium buphine and preparations, which is applied in the field of sodium buphine preparations and their uses, and can solve the problems of unfavorable rapid release of active components, unpleasant strong taste of active components, etc.

Inactive Publication Date: 2013-04-03
DEBREGEAS & ASSOCIES PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] Another difficulty with the use of oral dosage forms of nabuphine is the particularly unpleasant strong taste of the active ingredient, which prevents its direct use in solution
This requires the usual galenic artefacts (flavoring or coatings) to mask the above mentioned taste, which is detrimental to the immediate release of the active ingredient

Method used

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  • Nalbuphine-based formulations and uses thereof
  • Nalbuphine-based formulations and uses thereof
  • Nalbuphine-based formulations and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] Example 1: 30mg tablet

[0077] formula

[0078] raw material

unit (mg)

％

Nabuphine / HCl

30.00

4.69

Povidone (PVP)

242.01

37.80

Mannitol (granulated carrier)

349.49

54.58

Crospovidone

12.81

2.00

Anhydrous Colloidal Silica

0.64

0.10

Sodium Stearyl Fumarate

3.20

0.50

Talc

2.14

0.33

total

640.29

100.00

[0079] The preparation is obtained by the following process:

[0080] Weighing raw materials (balances);

[0081] Mix sodium buphine, purified water and povidone (spiral mixer);

[0082] Dissolving and compounding the mixture (GPCG3 fluidized bed, Würster and peristaltic pump);

[0083] coating mannitol with the above mixture and drying the coated mannitol to obtain granules;

[0084] Sieve the above particles (mesh diameter 600 μm diameter, vibrating sieve, mesh diameter 630 μm, 500 μm and 400 ...

Embodiment 2

[0088] Example 2: 30mg tablet

[0089] formula

[0090] raw material

unit (mg)

％

Nabuphine / HCl

30.00

18.65

Talc

4.47

2.70

Anhydrous Colloidal Silica

0.74

0.45

Avicel PH 200 (granulated carrier)

23.17

14.00

Tablettose 80 (granulated carrier)

79.44

48.00

Povidone

7.45

4.50

Magnesium stearate

0.74

0.45

Sepifilm LP014

14.89

9.00

Crospovidone

3.72

2.25

96°Alcohol (96°Alcohol Surfin Pharma)

/

/

purified water

/

/

total

320.15

100.00

[0091] The preparation is obtained by the following process:

[0092] Weighing raw materials (balances);

[0093] Mix Sodium Buphine, Talc and Tablettose and Avicel

[0094] A binder solution is obtained by mixing povidone and purified water;

[0095] spraying the above binder solution onto the...

Embodiment 3

[0101] Example 3: 10mg tablet

[0102] formula

[0103]

[0104] The preparation is obtained by the following process:

[0105] Weighing raw materials (balances);

[0106] Homogenize for 5 minutes at 150 rpm in a cubic mixer (8 L) (Nabuphine, Avicel PH200, Talc, Aerosil 200、Tablettose 80 and PVP K30);

[0107]Lubricate the above mixture with magnesium stearate for 1 minute at 150 rpm;

[0108] The above mixture (G009, diameter 9) was compressed on a Korsch apparatus;

[0109] Coating solutions were prepared on magnetic plates with Sepifilm LP014 and purified water;

[0110] The above compressed mixture was aqueous coated in LAF GPCG 1.

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Abstract

An immediate-release oral pharmaceutical formulation comprising nalbuphine, or a pharmaceutically acceptable salt thereof, and at least one hydrophilic granulation substrate, one hydrophilic binder and one lubricant.

Description

technical field [0001] The subject of the present invention is a pharmaceutical formulation comprising nalbuphine and its use for the treatment of pain. Background technique [0002] Pain is a very common dysfunction and one of the most commonly treated symptoms. [0003] Millions of individuals frequently suffer from recurrent pain without receiving treatment that is completely satisfactory in improving symptoms. [0004] Morphine derivatives have been widely used to treat pain in the past, and their use has grown substantially over the past decade. [0005] Nalbuphine is a semi-synthetic opioid derivative of the receptor kappa-agonist and receptor μ-antagonist classes, belonging to the phenanthrene family. This molecule is classified by WHO in Classification Table IIA. Its analgesic activity is equivalent to that of morphine and ten times greater than that of tebuzocine. [0006] It is also used for anesthesia. Its other advantages are a lower incidence of respiratory...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/28A61K9/50A61K31/485A61K49/10G01N1/00
CPCA61K9/2866A61K31/485A61K9/5078A61K9/2018A61K9/0053A61K9/5047A61K9/1676A61P25/00A61P25/04A61P25/30A61P25/36A61P29/00A61K9/20A61K9/28A61K9/50A61K9/2009A61K9/2013A61K9/2027
Inventor 克里斯托弗·勒邦帕斯卡·祖普利大卫·奥利维尔·保罗
Owner DEBREGEAS & ASSOCIES PHARMA