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Spray-dried granules containing pranlukast and processes for the preparation thereof

A technology of drying granules and granules, which is applied in the direction of active ingredients of heterocyclic compounds, pill delivery, respiratory diseases, etc., and can solve problems such as long-term, organic solvent residue, environmental pollution, etc.

Active Publication Date: 2007-05-02
YUHAN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In the PCT publication, however, the preparation of the solid dispersion involves dissolving pranlukast and (hydroxypropyl)methylcellulose or (hydroxypropyl)cellulose in an organic solvent (i.e., a mixture of dichloromethane and methanol solvent), so it may cause problems such as environmental pollution and potential toxicity of organic solvent residues
In addition, drying (for example, spray drying) is complicated and takes a long time due to the need to use a large amount of organic solvents to completely dissolve pranlukast, which makes industrial production difficult

Method used

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  • Spray-dried granules containing pranlukast and processes for the preparation thereof
  • Spray-dried granules containing pranlukast and processes for the preparation thereof
  • Spray-dried granules containing pranlukast and processes for the preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Preparation of spray-dried granules

[0040] 20g of polyvinylpyrrolidone (PVP), 12g of Solutol  HS 15 (BASF), and 28g of Poloxamer  407 (BASF) was dissolved in 500ml of purified water. Then 100 g of pranlukast was added to the resulting solution with stirring at 18000-20000 rpm using a homogenizer to generate a suspension.

[0041] The suspension was spray dried using a micro spray dryer (Buchi 190) at an internal temperature of 120-130°C and an external temperature of 80-90°C to produce spray-dried granules. The average particle size of pranlukast in the spray-dried granules was determined according to the dynamic light scattering technique using an optical particle sizer AccuSizer 780A (ParticleSizing Systems. Inc. Santa Barbara, Calif., U.S.A). As a result, the average particle size of pranlukast in the spray-dried granules was 9.79 μm.

Embodiment 2-10

[0042] Examples 2-10: Preparation of spray-dried granules

[0043] In the same manner as in Example 1, spray-dried granules were prepared according to the components and contents in Table 1 below. Use 5ml of purified water per 1g of pranlukast.

[0044] Example

Ingredients (g)

Granularity(*)

(μm)

Pranlukast

pvp

Solutol 

HS 15

Cremophor 

RH40

Poloxamer

407

2

100

20

-

12

28

11.52

3

100

20

15

-

35

10.84

4

100

20

21.6

-

38.4

9.30

5

75

15

16.2

-

28.8

9.35

6

75

15

11.25

-

26.25

12.29

7

100

20

-

10

50

7.94

8

100

20

-

15

60

8.97

9

100

10

...

Embodiment 11

[0047] Example 11: Preparation of spray-dried granules

[0048] 10g of polyvinylpyrrolidone, 15g of Cremophor  RH 40 (BASF), and 37.5g of Poloxamer  407 (BASF) was dissolved in 500ml of purified water. A suspension was thus produced by adding 100 g of pranlukast to the resulting solution under stirring with a magnetic stirrer. Then, use a homogenizer to homogenize the suspension at 18,000-20,000rpm for 10 minutes, and spray dry it with a fluidized bed granulator (Glatt) at an internal temperature of 110-130°C and a spray pressure of 1.0-2.0bar. A spray-dried granule is produced. The average particle size of pranlukast in the spray-dried granules was determined in the same manner as in Example 1. As a result, the average particle size of pranlukast in the spray-dried granules was 11.30 μm.

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Abstract

The invention provides a spray-dried granule comprising pranlukast, a water-soluble polymer and a surfactant, and a method for producing the granule. The average particle size of the pranlukast in the granule is 0.5-20 um. Thereby, not only adhesion cohesiveness and solubility of the pranlukast but also elution rate and bioavailability thereof can be improved even without coating the pranlukast with saccharides such as lactose. As a result, the dose can remarkably be reduced from that of conventional formulations. Furthermore, since the formulation can be produced without using an organic solvent, the formulation is suitable for mass-production on an industrial scale.

Description

field of invention [0001] The invention relates to a spray-dried granule containing pranlukast and a preparation method thereof. Background technique [0002] Pranlukast (chemical name: 4-oxa-8-[4-(4-phenylbutoxy)benzamido]-2-(tetrazol-5-yl)-4H-1-benzopyridine Fylfuran hemihydrate), which potently antagonizes leukotriene C4 and leukotriene D4, is used in the treatment of bronchial asthma and allergic rhinitis. [0003] The currently commercially available pranlukast is capsules (Onon capsules, 112.5mg / grain of pranlukast, two capsules each time, Donga Pharmaceutical Co., Ltd.). [0004] However, pranlukast is a very viscous and poorly water soluble drug. Therefore, when pranlukast is formulated into tablets or capsules, it sticks to punches, molds, etc., thereby making continuous production difficult. Furthermore, based on its low bioavailability, therapeutic doses of 200 mg or greater are generally recommended. [0005] In view of these problems, various studies have be...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/20A61K9/48A61K31/41A61P11/02A61P11/06A61P11/08
CPCA61K9/0095A61K9/1629A61K9/1682A61K9/20A61K9/48A61K31/41
Inventor 朴永俊朴诗妍
Owner YUHAN
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