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Alpha1-receptor antagonist slow-release pill preparation and its preparation method

A technology of receptor antagonists and sustained-release pellets, which can be applied to medical preparations containing active ingredients, pill delivery, anti-tumor drugs, etc., and can solve problems such as unrealized and unavailable tamsulosin sustained-release curves

Inactive Publication Date: 2008-10-22
AMOREPACIFIC CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, a satisfactory sustained-release profile of tamsulosin cannot be obtained due to the rapid dissolution of the enteric-coated substance upon entering the small intestine
[0007] Accordingly, the inventors of the present invention have endeavored to develop pellet formulations capable of maintaining therapeutically effective levels of α1-receptor antagonists in the blood for a sufficient period of time without initial burst release of the drug, and have found A pellet formulation of a controlled-release sphere core coated with a layer of substance and a water-insoluble polymer shows a satisfactory constant release profile of the drug, which has not been achieved in the art

Method used

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  • Alpha1-receptor antagonist slow-release pill preparation and its preparation method
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  • Alpha1-receptor antagonist slow-release pill preparation and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1: Preparation of slow-release pellet preparation

[0046] (1) Preparation of pellets containing active ingredients

[0047] 1.0 g of tamsulosin hydrochloride (Ragactives, Spain), 747 g of microcrystalline cellulose and 16 g of talc were thoroughly mixed in a centrifugal fluidized bed granulator (GPCG-1, Glatt, Germany) for about 1 minute. The binder solution (120g Eudragit in 580g water TM L30D-55) is sprayed onto the mixture in the granulator to form pellets. The pellet preparation conditions are listed in Table 1. The pellets thus obtained were spherical particles with a diameter of 0.5 to 1.4 mm, as shown in Table 2.

[0048]

[0049]

[0050]

[0051] Particle size (μm)

Weight (g)

Proportion(%)

＞1400

0.45

0.45

710～1400

9.77

9.76

[0052] 500～710

88.39

88.34

355～500

1.45

1.45

＜355

-

-

total

100.06 ...

Embodiment 2

[0059] Embodiment 2: Preparation of slow-release pellet preparation

[0060] (1) Preparation of pellets containing active ingredients

[0061] 24.25 g of doxazosin mesylate (Cipla, India), 400 g of microcrystalline cellulose, 295.75 g of calcium hydrogen phosphate, and 40 g of talc were fully granulated in a centrifugal fluidized bed granulator (GPCG-1, Glatt, Germany). Mix for about 1 minute. The binder solution (133.3g Eudragit in 600g water TM L30D-55) is sprayed onto the mixture in the granulator to form pellets. The pellet preparation conditions are listed in Table 1. The pellets thus obtained were spherical particles with a diameter ranging from 0.5 to 1.4 mm, as shown in Table 5.

[0062]

[0063] Particle size (μm)

Weight (g)

Proportion(%)

＞1400

8.78

8.79

710～1400

79.22

79.28

500～710

11.41

11.42

355～500

0.52

0.52

＜355

-

-

total

...

Embodiment 3

[0068] Embodiment 3: Preparation of slow-release pellet preparation

[0069] (1) Preparation of pellets containing active ingredients

[0070] 50 g of alfuzosin hydrochloride (Heumann PCS, Germany), 550 g of microcrystalline cellulose, 120 g of calcium hydrogen phosphate, and 40 g of talc were thoroughly mixed in a centrifugal fluidized bed granulator (GPCG-1, Glatt, Germany) for about 1 minute. The binder solution (133.3g Eudragit in 600g water TM L30D-55) is sprayed onto the mixture in the granulator to form pellets. The pellet preparation conditions are listed in Table 1. The pellets thus obtained were spherical particles with a diameter ranging from 0.7 to 1.4 mm, as shown in Table 7.

[0071]

[0072] Particle size (μm)

Weight (g)

Proportion(%)

＞1400

4.48

4.48

710～1400

91.96

92.04

500～710

3.24

3.24

355～500

0.23

0.23

＜355

-

-

total

...

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Abstract

A sustained-release pellet formulation comprising: a pellet core comprising an alpha1-receptor antagonist, a pellet-forming susbstance and a pharmaceutically acceptable excipient and a coating layer comprising an enteric coating substance and a water-insoluble polymer, which is coated on said pellet core maintains a therapeutically effective drug level in the blood for a sufficient time without an initial burst and sustains the release of the drug even in the small intestine due to the water-insoluble polymer in the coating layer.

Description

field of invention [0001] The present invention relates to a sustained-release pellet formulation of an α1-receptor antagonist for treating urinary disorders associated with benign prostatic hyperplasia and a preparation method thereof. Background of the invention [0002] alpha 1 Activation of the receptors causes smooth muscle cells to contract, which brings about such effects as constricting the vasculature, raising blood pressure and constricting the urinary tract to restrict urine flow. block alpha 1 Compounds for the receptor exert the opposite effect. [0003] Therefore, α 1 Receptor antagonists are potentially effective therapeutic agents for hypertension, congestive heart failure and other cardiovascular diseases. Furthermore, specific α1-receptor antagonists such as tamsulosin, alfuzosin, doxazosin and terazosin have also been developed for the treatment of urinary symptoms indicative of benign prostatic hyperplasia. α1-receptor antagonists work by blocking α1...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K9/22
CPCA61K31/18A61K31/505A61K9/1652A61K9/5026A61P13/02A61P13/08A61P35/00A61P43/00A61K9/28A61K9/20
Inventor 中光炫申永姬宾圣娥金正铸
Owner AMOREPACIFIC CORP
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