Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Maleic acid trimebutine slow release tablet comprising quick release part and preparing method thereof

A technology of trimebutine maleate and sustained-release tablets, applied in the direction of ester active ingredients, sugar-coated pills, pill delivery, etc., can solve the problems of slow onset of action and low bioavailability, and achieve good absorption and definite curative effect , the effect of taking convenience

Active Publication Date: 2007-03-14
KAIKAII YUANSHENG PHARMA CO LTD
View PDF1 Cites 12 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This zero-order release has certain shortcoming, because trimebutine maleate is slightly soluble in water, t1 / 2 is 2.7h (Ke about 0.25h -1 ), when the zero-order drug release rate is 25mg / h, according to the single-compartment model, it can be calculated that the cumulative drug release in the body can reach 80% after 24 hours [Edited by Tu Xide, Pharmacy, People's Health Publishing House, 2002, Beijing, 955 page], which leads to slow onset of action and low bioavailability, and the effective treatment of gastrointestinal diseases should take effect quickly in order to reduce the suffering of patients
Therefore, zero-order release controlled-release formulations are not suitable for trimebutine maleate

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
  • Maleic acid trimebutine slow release tablet comprising quick release part and preparing method thereof
  • Maleic acid trimebutine slow release tablet comprising quick release part and preparing method thereof
  • Maleic acid trimebutine slow release tablet comprising quick release part and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] The preparation of embodiment 1 trimebutine maleate bilayer tablet (1000)

[0037] prescription:

[0038] 1. Immediate release layer

[0039] Trimebutine Maleate 150g

[0040] Microcrystalline Cellulose 50g

[0041] Tartaric acid 10g

[0042] Magnesium Stearate 1g

[0043] Talc powder 1g

[0044] 5% povidone absolute ethanol solution appropriate amount

[0045] A total of 1000 capsules

[0046] 2. Sustained release layer:

[0047] Trimebutine Maleate 150g

[0048] Lactose 10g

[0049] Hypromellose HPMC (K4M) 100g

[0050] Tartaric acid 10g

[0051] Magnesium Stearate 1g

[0052] Talc powder 1g

[0053] 5% povidone absolute ethanol solution appropriate amount

[0054] A total of 1000 capsules

[0055] Preparation Process:

[0056] 1. Immediate-release granules: weigh trimebutine maleate, tartaric acid, and microcrystalline cellulose in the prescribed amount of the immediate-release layer, mix wel...

Embodiment 2

[0060] Embodiment 2 trimebutine maleate sustained release tablet

[0061] Prescription: (based on 1000 tablets)

[0062] 1. Immediate Release Granules

[0063] Trimebutine Maleate 150g

[0064] Lactose 20g

[0065] Tartaric acid 10g

[0066] 5% povidone absolute ethanol solution appropriate amount

[0067] 2. Sustained-release granules:

[0068] Trimebutine Maleate 150g

[0069] Lactose 70g

[0070] Hypromellose HPMC (K4M) 200g

[0071] Tartaric acid 10g

[0072] 5% povidone absolute ethanol solution appropriate amount

[0073] Preparation Process:

[0074] 1. Immediate-release granules: weigh trimebutine maleate, tartaric acid, and lactose in the prescription amount of the immediate-release layer, mix well, add povidone ethanol solution to make a soft material, pass through a 24-mesh sieve twice to obtain granules, and dry at 40°C 30 minutes.

[0075] 2. Sustained-release granules: take by weighing the prescription amount of the sustained-release layer, trimebutin...

Embodiment 3

[0078] The mensuration of embodiment 3 release rate

[0079] Get the trimebutine maleate slow-release tablet that obtains under embodiment 1, embodiment 2, according to release assay method (Chinese Pharmacopoeia version in 2005 two appendix XD first method), adopt dissolution assay (Chinese Pharmacopoeia 2005 edition two appendix XC first method) device, with 0.01mol / L hydrochloric acid solution 900ml as solvent, rotating speed is 100 revolutions per minute, operate according to law. Sampling 5ml at 1, 2, 3, 4, 6, 8, and 12 hours respectively, filtering, taking 2ml of the subsequent filtrate, putting it in a 10ml measuring bottle, adding 0.01mol / L hydrochloric acid solution to dilute to the mark as the test solution. In addition, accurately weigh an appropriate amount of trimebutine maleate reference substance, add 0.01mol / L hydrochloric acid solution to dissolve, quantitatively dilute to a solution with a concentration of about 20 μg / ml, and use it as the reference substance...

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

PropertyMeasurementUnit
wavelengthaaaaaaaaaa
Login to View More

Abstract

This invention concerns a the maleic acid trimebutine sustained-releasing tablets with rapid releasing part and preparation of pharmaceutical pharmaceuticals, including double slice and tablet mixed and suppressed by particles with different releasing characteristics, it is found in the invention that after the maleic acid trimebutine and fumaric acid being mixed and granulated, the stability and compressibility of the maleic acid trimebutine is improved, and its citation moist is lowered, and it can be used for preparation of the praeparatum of the present invention, the present invention includes the rapid releasing part and sustained-releasing part.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a trimebutine maleate sustained-release tablet with an immediate-release part and a preparation process thereof. technical background [0002] Trimebutine maleate (English name: trimebutine maleate, abbreviation: TMB), structural formula such as [0003] [0004] Down: [0005] Trimebutine maleate is a gastrointestinal motility rhythm regulator different from cholinergic drugs and antidopamine drugs. It is clinically used to treat gastrointestinal symptoms caused by chronic gastritis (abdominal fullness, abdominal pain, nausea, belching) and irritable bowel syndrome. [0006] The relevant characteristics of trimebutine maleate are as follows: [0007] 1. Different from other digestive system drugs, it can have a bidirectional effect of promoting or inhibiting the movement of the digestive tract due to the difference in the physiological state of the digestive tract. Normaliz...

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): A61K9/28A61K31/24A61P1/04
Inventor 涂家生胡泽开何宜成
Owner KAIKAII YUANSHENG PHARMA CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com