Naftopidil suppository and preparation method thereof

A nafidil suppository, the technology of nafidil, which is applied in the directions of suppository delivery, pharmaceutical formulations, and medical preparations of inactive ingredients, etc., can solve gastrointestinal irritation, stomach discomfort or nausea, low dissolution rate, etc. problems, to reduce toxicity and side effects, improve bioavailability, and uniform drug dispersion

Active Publication Date: 2011-04-20
蚌埠丰原涂山制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Current market naftopidil solid preparation has tablet, capsule, drop, and these are all oral preparations, and in vitro dissolution rate is all relatively low, and blood drug concentration and bioavailability are also lower; Naftopidil has local stimulation It is more obvious when the concentration is higher. Ordinary oral preparations disintegrate rapidly after oral administration. Higher local concentrations can cause irritation to the gastrointestinal tract, which can cause stomach discomfort or nausea, edema, chills, AST elevation and Adverse reactions such as ALT elevation also have certain toxicity to the liver
In addition, the production of naftopidil into common preparations cannot give full play to the therapeutic effect of the drug. For patients, there is no obvious advantage in using other drugs and using this drug.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Weigh the raw materials according to the following ratio:

[0039] Naftopidil: 400g

[0040] Stearic acid: 700g (Hunan Erkang Pharmaceutical Co., Ltd., the same below)

[0041] Polyethylene glycol 1000: 200g (Hunan Erkang Pharmaceutical Co., Ltd., the same below)

[0042] Polyethylene glycol 4000: 300g (Hunan Erkang Pharmaceutical Co., Ltd., the same below)

[0043] Poloxamer (40): 100g (Hunan Erkang Pharmaceutical Co., Ltd., the same below)

[0044] White wax: 200g (Hunan Erkang Pharmaceutical Co., Ltd., the same below)

[0045] Sodium benzoate: 100g (Hunan Erkang Pharmaceutical Co., Ltd., the same below)

[0046]

[0047] Make 1000 capsules

[0048] The preparation method is as follows:

[0049] 1) Naftopidil and stearic acid are pulverized through a 120 mesh sieve and mixed uniformly for subsequent use;

[0050] 2) Melt polyethylene glycol 1000 and polyethylene glycol 4000 in a water bath at 80°C;

[0051] 3) Add 1) into 2) and s...

Embodiment 2

[0055] Weigh the raw materials according to the following ratio:

[0056] Naftopidil: 300g

[0057] Stearic acid: 600g

[0058] Polyethylene glycol 1000: 300g

[0059] Macrogol 4000: 300g

[0060] Poloxamer: 200g

[0061] White wax: 200g

[0062] Sodium benzoate: 100g.

[0063] The preparation method is as follows:

[0064] 1) Naftopidil and stearic acid are pulverized through a 100-mesh sieve and mixed uniformly for subsequent use;

[0065] 2) Melt polyethylene glycol 1000 and polyethylene glycol 4000 in a water bath at 60°C;

[0066] 3) Add 1) into 2) and stir to make it melt;

[0067] 4) Add poloxamer (40), white wax, and sodium benzoate into 3) and stir evenly to prepare a suppository paste filling;

[0068] 5) Wait for 4) to lower the temperature of the prepared paste filling to below 40°C, pour it into the mold, cool and solidify, remove the overflowing part, open the plug mold, and push it out.

Embodiment 3

[0070] Weigh the raw materials according to the following ratio:

[0071] Naftopidil: 400g

[0072] Stearic acid: 700g

[0073] Polyethylene glycol 1000: 200g

[0074] Polyethylene glycol 6000: 300g (Hunan Erkang Pharmaceutical Co., Ltd., the same below)

[0075] Poloxamer: 100g

[0076] White wax: 200g

[0077] Sodium benzoate: 100g.

[0078] The preparation method is as follows:

[0079] 1) Naftopidil and stearic acid are pulverized through a 110 mesh sieve and mixed uniformly for subsequent use;

[0080] 2) Melt polyethylene glycol 1000 and polyethylene glycol 6000 in a water bath at 80°C;

[0081] 3) Add 1) into 2) and stir to make it melt;

[0082] 4) Add poloxamer (40), white wax, and sodium benzoate into 3) and stir evenly to prepare a suppository paste filling;

[0083]5) Wait for 4) to lower the temperature of the prepared paste filling to below 40°C, pour it into a mold, cool and solidify, remove the overflowing part, open the plug mold, and push it out.

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PUM

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Abstract

The invention relates to naftopidil suppository and a preparation method thereof. The naftopidil suppository comprises the following components in part by weight: 10 to 25 parts of naftopidil, 10 to 60 parts of oleaginous substrate, 10 to 60 parts of water-soluble substrate, 1 to 10 parts of surfactant, 10 to 30 parts of hardening agent and 5 to 15 parts of absorbefacient. The suppository is uniformly dispersed, has high dissolution rate and improves the bioavailability and the effectiveness of medicaments.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a naftopidil suppository and a preparation method thereof. Background technique [0002] Naftopidil is a selective a1 receptor antagonist, which can relieve the sympathetic tension of the prostate and urethra caused by the stimulation of the receptor through a1 receptor blockade, reduce the internal pressure of the urethra, and improve benign prostatic hyperplasia Symptoms such as dysuria caused by it can also inhibit the rise in blood pressure caused by the a1 receptor, and also have calcium ion antagonism, and have antihypertensive effects on various animal models of hypertension. It is suitable for patients with hypertension, hyperlipidemia, diabetes, and benign prostatic hyperplasia. [0003] Current market naftopidil solid preparation has tablet, capsule, drop, and these are all oral preparations, and in vitro dissolution rate is all relatively low, and blood drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/02A61K31/495A61K47/44A61K47/42A61K47/40A61K47/34A61K47/14A61P3/06A61P3/10A61P9/12A61P13/08A61K47/10A61K47/12
Inventor 薛世静汪洪湖
Owner 蚌埠丰原涂山制药有限公司
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