Supercharge Your Innovation With Domain-Expert AI Agents!

Guanfacine hydrochloride sustained-release preparation and preparation method thereof

A technology for guanfacine hydrochloride and sustained-release preparations, which is applied in pharmaceutical formulations, medical preparations containing active ingredients, and drug delivery, and can solve the problem of unsatisfactory pharmacokinetic parameters such as bioavailability in vivo, large batch-to-batch differences, and Poor release stability and other issues, to achieve good stability and dissolution characteristics, reduce the production of impurities, and reduce the effect of production energy consumption

Active Publication Date: 2014-04-09
郑州大明药物科技有限公司
View PDF1 Cites 1 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Guanfacine hydrochloride sustained-release preparation and preparation method thereof
  • Guanfacine hydrochloride sustained-release preparation and preparation method thereof
  • Guanfacine hydrochloride sustained-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Based on the specification of 1 mg free guanfacine effective content in each sustained-release preparation, the raw material composition of each guanfacine hydrochloride sustained-release tablet is: guanfacine hydrochloride 1.14 mg, pregelatinized starch 41.6 mg, hydroxymethyl cellulose Sodium Sulfate 46mg, Hydroxyethylcellulose 36mg, Citric Acid 17mg, Magnesium Lauryl Sulfate 4mg and Croscarmellose Sodium 4.26mg.

[0035] In this embodiment, according to the above-mentioned specifications of 1 mg free guanfacine hydrochloride effective content in each sustained-release preparation, the raw materials for producing 5000 guanfacine hydrochloride sustained-release tablets consist of: 5.7 g of guanfacine hydrochloride, 208 g of pregelatinized starch, Hydroxymethylcellulose sodium 230g, hydroxyethylcellulose 180g, citric acid 85g, magnesium lauryl sulfate 20g and croscarmellose sodium 21.3g.

[0036] In addition, according to the raw material composition of 5000 guanfacine h...

Embodiment 2

[0038] Based on the specification of free guanfacine effective content of 1 mg in each sustained-release preparation, the raw material composition of each guanfacine hydrochloride sustained-release tablet is: guanfacine hydrochloride 1.14 mg, pregelatinized starch 40 mg, hydroxymethylcellulose Sodium 49.4mg, hydroxyethylcellulose 30mg, tartaric acid 20.6mg, polyethylene glycol 4000 4.4mg and cross-linked polyvinylpyrrolidone 4.26mg.

[0039] In this embodiment, according to the specification of free guanfacine effective content of 1 mg in each sustained-release preparation mentioned above, the raw materials for producing 5000 guanfacine hydrochloride sustained-release tablets consist of: 5.7 g of guanfacine hydrochloride, 200 g of pregelatinized starch, Hydroxymethylcellulose sodium 247g, hydroxyethylcellulose 150g, tartaric acid 103g, polyethylene glycol 4000 22g and cross-linked polyvinylpyrrolidone 21.3g.

[0040] In addition, according to the raw material composition of 50...

Embodiment 3

[0042] Based on the specification of 1 mg free guanfacine effective content in each sustained-release preparation, the raw materials of each guanfacine hydrochloride sustained-release tablet are: guanfacine hydrochloride 1.14 mg, pregelatinized starch 57 mg, Eudragit 100 80.8 mg, malic acid 22.86mg, polyethylene glycol 4000 5.4mg and croscarmellose sodium 6mg.

[0043] In this embodiment, according to the specification of 1 mg free guanfacine effective content in each sustained-release preparation mentioned above, the raw materials for producing 5000 guanfacine hydrochloride sustained-release tablets are composed of: 5.7 g of guanfacine hydrochloride, 285 g of pregelatinized starch, Eudragit 100 404g, malic acid 114.3g, polyethylene glycol 4000 27g and croscarmellose sodium 30g.

[0044] In addition, according to the raw material composition of 5000 guanfacine hydrochloride sustained-release tablets, 2500 guanfacine hydrochloride sustained-release tablets with an effective fre...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a guanfacine hydrochloride sustained-release preparation and a preparation method thereof. The guanfacine hydrochloride sustained-release preparation is prepared from guanfacine hydrochloride, filler, a medicine carrier material, a pH regulator, a lubricating agent and a disintegrating agent. The preparation method comprises the steps of crushing and sieving the guanfacine hydrochloride, the filler, the pH regulator and the medicine carrier material respectively, uniformly mixing the guanfacine hydrochloride with the filler, the pH regulator and the medicine carrier material in a mixing machine, then sequentially adding the lubricating agent and the disintegrating agent into the mixing machine and mixing uniformly, and finally, tabletting with a conventional method to prepare the guanfacine hydrochloride sustained-release tablets with various specifications. Due to the utilization of the method for preparing the guanfacine hydrochloride sustained-release preparation, the operation process can be effectively simplified, impurities in the finished preparation are reduced and the medicine safety is improved; besides, the prepared guanfacine hydrochloride sustained-release preparation has good stability and dissolution characteristic.

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] The U.S. FDA has approved guanfacine hydrochloride extended-release tablets for the treatment of attention-deficit and hyperactivity disorder in children and adolescents aged 6 to 17. It is the first selective alpha2a-adrenergic receptor agonist approved to date for this indication globally. The chemical name of guanfacine hydrochloride 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] Preclinical studi...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/165A61P25/14A61P25/00
Inventor 刘志庆贾晓璐王翠侠朱赞梅苗海敏蒲薇薇王娜
Owner 郑州大明药物科技有限公司
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com