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Guanidine hydrochloride sustained release preparation and preparation method thereof

A technology of guanfacine hydrochloride and sustained-release preparations, which can be applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. The pharmacokinetic parameters such as the degree of availability are not ideal, so as to achieve the effect of less toxic and side effects, high production efficiency, and convenient long-term treatment

Active Publication Date: 2012-07-18
ZHONGSHUAI PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the sustained-release preparations obtained by common preparation methods often have the following problems: large batch-to-batch variation, poor release stability, and unsatisfactory pharmacokinetic parameters such as in vivo bioavailability

Method used

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  • Guanidine hydrochloride sustained release preparation and preparation method thereof
  • Guanidine hydrochloride sustained release preparation and preparation method thereof
  • Guanidine hydrochloride sustained release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] The raw and auxiliary materials of the guanfacine hydrochloride sustained-release preparation of the present invention consist of:

[0049] Taking g as the unit, the weight of each raw and auxiliary material in the original formula of guanfacine hydrochloride sustained-release preparation was enlarged by 5 to 15 times. 232.5g of lactose, 75g of fumaric acid, 250g of hydroxypropyl methylcellulose, 175g of polyacrylic resin, 3g of micronized silica gel, 3g of magnesium stearate and 120g of water.

[0050] The preparation method of guanfacine hydrochloride slow-release preparation of the present invention:

[0051] Prepare various raw materials and auxiliary materials according to the composition of raw materials and auxiliary materials of the above-mentioned guanfacine hydrochloride sustained-release tablets, prepare guanfacine hydrochloride 11.48g, lactose 232.5g, fumaric acid 75g, hydroxypropyl methylcellulose 250g, polyacrylic acid 175g of resin was crushed until it p...

Embodiment 2

[0052] Embodiment 2: basically the same as Embodiment 1, the difference is:

[0053] The raw and auxiliary materials of the guanfacine hydrochloride sustained-release preparation of the present invention consist of:

[0054] Taking g as the unit, the weight of each raw and auxiliary material in the original formula of the guanfacine hydrochloride sustained-release preparation was enlarged by 5 to 15 times. Mannitol 190g, citric acid 100g, hydroxypropyl cellulose 300g, polyacrylic resin 135g, micropowder silica gel 3g, sodium stearyl fumarate 5g and 5% povidone aqueous solution 100g.

Embodiment 3

[0055] Embodiment 3: basically the same as Embodiment 1, the difference is:

[0056] Taking g as the unit, the weight of each raw and auxiliary material in the original formula of guanfacine hydrochloride sustained-release preparation was enlarged by 5 to 15 times. Lactose 200g, microcrystalline cellulose 30g, fumaric acid 100g, ethyl cellulose 250g, polyacrylic resin 150g, micropowder silica gel 3g, magnesium stearate 3g and water 120g. .

[0057] Taking the guanfacine hydrochloride sustained-release tablet prepared in Example 1 as the test sample, the release test method is as follows:

[0058] Get the product obtained in Example 1, according to the release assay method (the second method of two appendix X D of Chinese Pharmacopoeia 2010 edition), adopt the dissolution assay device, the rotating speed is 100rpm, and temperature is 37 ℃, and release medium is the hydrochloric acid buffering of pH 2.2 Liquid 900ml, the sampling time points are: 1 hour, 4 hours, 8 hours and 2...

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Abstract

The invention discloses guanidine hydrochloride sustained release preparation and a preparation method thereof. The guanidine hydrochloride sustained release preparation is mainly prepared by guanidine hydrochloride, a filling agent, sustained release materials and potential of hydrogen (pH) sensitive materials. The preparation method comprises the steps of firstly preparing all raw materials according to proportion, evenly mixing the guanidine hydrochloride, the filling agent, the sustained release materials and the pH sensitive materials at high speed, granulating and drying the evenly mixed powder, finally adding a flow agent, a lubrication agent and an adhesion agent, tableting according to a general method, and achieving guanidine hydrochloride sustained release tablets. The guanidine hydrochloride sustained release preparation is small in side effect, obviously reduces difference of preparation of different batches, improves stability of samples, is convenient long term curing of patients and improves compliance of medicine. A patient can take the guanidine hydrochloride sustained release tablets once a day, so that effective drug concentration in bodies can be guaranteed for 24 hours, and nervous centralis side reactions caused by the fact that a blood concentration peak value is high due to general preparation is reduced.

Description

technical field [0001] The invention relates to pharmaceutical preparation technology in the field of pharmacy, in particular to a guanfacine hydrochloride sustained-release preparation and a preparation method thereof. Background technique [0002] Guanfacine hydrochloride is an antihypertensive drug used to treat moderate to severe hypertension. The chemical name is N-amidino-2-(2,6-dichlorophenyl)acetamide monohydrochloride, and its molecular formula is: C 9 h 9 Cl 2 N 3 O HCl, the molecular weight is 282.55, and the structural formula is: [0003] [0004] Guanfacine hydrochloride is a white to off-white crystalline powder, insoluble in water and ethanol, and has a relatively high solubility in methanol (>30mg / mg). [0005] Guanfacine hydrochloride is selective alpha 2 -Adrenoceptor potentiator, first used in the treatment of moderate to severe hypertension, in the form of tablets for oral administration, sold under the trade name Tenex in the United States ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K9/16A61K31/155A61K47/44A61K47/38A61K47/36A61K47/32A61K47/12A61P9/12
Inventor 邬向东王军任峰晓
Owner ZHONGSHUAI PHARMA SCI & TECH CO LTD
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