Slow releasing micropill containing active component of indapamide and method for preparing the same

A technology of sustained-release pellets and indapamide, which is used in pharmaceutical formulations, bulk delivery, blood diseases, etc., can solve the problems of sudden release of sustained-release tablets and difficult quality control, and achieve increased safety, high yield and Reproducible, easy-to-industrial effect

Inactive Publication Date: 2005-11-23
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, sustained-release tablets are easily affected by operating conditions such as pressure in large-scale production, making it difficult to control the quality, and most of the sustained-release tablets are prone to burst release

Method used

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  • Slow releasing micropill containing active component of indapamide and method for preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1, the preparation of blank pellet

[0040] 1

2

lactose

starch

sucrose

Talc powder

Magnesium stearate

100g

30g

40g

20g

10g

microcrystalline cellulose

starch

hypromellose

silica

Magnesium stearate

80g

60g

20g

20g

20g

[0041] B. Preparation process

[0042] Mix the prescription amount of lactose (or microcrystalline cellulose) and starch evenly, add the binder prepared by sucrose or hypromellose, use a granulator (or coating pan) to start and roll the pellets to the required The mesh number is 15-30 mesh (lubricant and glidant are added while rolling the pellets), dried, and the best 18-25 mesh is screened out.

Embodiment 2

[0043] Embodiment 2, the preparation of quick-release pellets

[0044] 1

2

Blank pellets

Indapamide

hypromellose

Talc powder

polyethylene glycol

water

120g

1.5g

2g

10g

0.4g

100ml

Blank pellets

Indapamide

Polyvinylpyrrolidone

Talc powder

polyethylene glycol

70% ethanol

120g

1.5g

5g

15g

0.3g

100ml

[0045] B. Preparation process

[0046] Add indapamide, hypromellose (or polyvinylpyrrolidone) and talcum powder described in the prescription into water or 70% ethanol respectively, and stir for 20 minutes to form a uniform mixed solution. In the fluidized bed (or coating pan), the temperature of the pellets was kept at 30° C., and the mixed solution was evenly sprayed on the outer layer of the blank pellets obtained in Example 1 to obtain immediate-release pellets.

Embodiment 3

[0047] Embodiment 3, the preparation of sustained-release pellets

[0048] 1

2

medicated pellets

Acrylic resin NE30D

triethyl citrate

Talc powder

water

150g

20g

3.5g

5g

150ml

medicated pellets

Acrylic RS30D

Acrylic resin RL30D

triethyl citrate

Talc powder

water

150g

15g

1.5g

3.8g

11.3g

135ml

3

4

medicated pellets

Ethyl cellulose

Hypromellose

0.1% diethyl phthalate

75% ethanol

150g

10g

2g

5g

100ml

medicated pellets

Aqueous dispersion of ethyl cellulose

Talc powder

water

150g

15g

10g

100ml

[0049] B. Preparation process

[0050] Put the quick-release pellets obtained in Example 2 into a fluidized bed (or coating pan), and keep the temperature of the pellets at 2...

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PUM

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Abstract

A slowly-releasing micropill containing indapamide as its active component is composed of pill core, quick-releasing layer and slow-releasing layer. It is prepared through proportionally mixing filler, adhesive and lubricant, granulating to become (10-30)-mesh pill cores, dissolving indapamide and high-molecular adhesive in solvent, spraying it on the surface of pill cores, dissolving the retarder, pore-forming agent and plasticizer of antisticking agent in solvent, and spraying it on the surface micropill. Its advantages are high slow releasing effect within 24 hr and no sudden release.

Description

technical field [0001] The invention belongs to the technical field of drug sustained-release preparations, and more specifically relates to a sustained-release pellet containing an active ingredient of indapamide and a preparation method thereof. technical background [0002] Indapamide is a sulfonamide diuretic, which acts by inhibiting the reabsorption of water and electrolytes in the cortical dilution segment of the distal renal tubules. The possible mechanisms include the following aspects: regulation of calcium influx in vascular smooth muscle cells; Prostaglandin PGE that stimulates free vasodilation 2 and prostaglandin PGI 2 Synthesis; reduce blood vessel hypersensitivity to vasopressor amine, thereby inhibiting vasoconstriction and achieving antihypertensive effect. Common preparations currently on the domestic market include: Indapamide Tablets (Shoubishan) from Tianjin Lisheng Pharmaceutical Factory, Indapamide Tablets (Najuli) imported from France Servier Pharm...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K9/52A61K31/404A61P7/10
Inventor 任晓文马晋徐为人连潇嫣李洪起
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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