Carbazochrome sodium sulfonate slow-released tablet and its preparing method

A technology of sodium carboxysulfonate and sustained-release tablets, which is applied in pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of poor compliance, inconvenience in using injections, and low blood drug concentration And other issues

Inactive Publication Date: 2007-06-27
SHANDONG INST OF PHARMA IND
View PDF0 Cites 7 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Injectables are notoriously inconvenient and poorly compliant for patients
When taking carbosulfonium sodium tablets, the drug will be in contact with the gastrointestinal mucosa at a high concentration after dissolution, which is likely to produce irritation, so adverse reactions such as loss of appetite, stomach discomfort, nausea and vomiting will occur; and because its biological half-life is only 1.5 Therefore, the maintenance time of the effective blood drug concentration in the body after oral administration is very short, and the patient needs to take it 3 to 4 times a day, so the compliance is also poor, especially the time interval between taking the medicine at night and the morning is long, and the blood drug concentration is very low in the morning , the phenomenon of "peaks and valleys" appears, the drug effect cannot be exerted smoothly, and the toxic and side effects are also large, so it is considered to develop carbosulfonate sustained-release tablets

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
  • Carbazochrome sodium sulfonate slow-released tablet and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1 Sodium Carbosulfonate Hydrophilic Gel Matrix Tablet

[0046] prescription:

[0047] Sodium carbosulfonate 30g

[0048] HPMC K4M 50g

[0049] Lactose 80g

[0050] 95% ethanol appropriate amount

[0051] Magnesium Stearate 1.5g

[0052] Talc powder 1.5g

[0053] Preparation Process:

[0054] Take carbosulfonium sodium raw material, pulverize and pass through a 120-mesh sieve, mix evenly with HPMC K4M and lactose, moisten with 95% ethanol and granulate, dry at 50°C and granulate, add magnesium stearate and talc, Mix evenly and tablet.

[0055] For the release test, the release rate of the sample was measured according to the first method of Appendix XC of the Chinese Pharmacopoeia in 2005, Part Two of the Chinese Pharmacopoeia Edition. First use 900ml of dilute hydrochloric acid (9→1000) as solvent, rotate at 100 rpm, take samples at 1 and 2 hours, then change to 900ml of buffer salt with pH 6.8 as solvent, operate in the same way, take samples at 4 and 8...

Embodiment 2

[0061] Example 2 Sodium carbene sulfonate waxy matrix tablet

[0062] prescription:

[0063] Sodium carbosulfonate 30g

[0064] Octadecanol 30g

[0065] Lactose 90g

[0066] Magnesium Stearate 1.5g

[0067] Talc powder 1.5g

[0068] Preparation Process:

[0069] The crude drug of sodium carbosulfonate is crushed and passed through a 120-mesh sieve, mixed evenly with lactose, molten stearyl alcohol is added therein, mixed evenly and then granulated, magnesium stearate and talcum powder are added, mixed evenly and pressed into tablets.

[0070] The release test is the same as in Example 1, and the results are as follows:

[0071] Time (hours) cumulative release %

[0072] 1 26.8%

[0073] 2 39.3%

[0074] 4 65.1%

[0075] 8 94.3%

Embodiment 3

[0076] Example 3 Sodium carbosulfonate non-erodible matrix tablet

[0077] prescription:

[0078] Sodium carbosulfonate 30g

[0079] Ethylcellulose 45g

[0080] Lactose 75g

[0081] 95% ethanol appropriate amount

[0082] Magnesium Stearate 1.5g

[0083] Talc powder 1.5g

[0084] Preparation Process:

[0085] The crude drug of sodium carbosulfonate is crushed and passed through a 120-mesh sieve, mixed evenly with lactose, ethyl cellulose, magnesium stearate and talcum powder, and the whole powder is directly compressed into tablets.

[0086] The release test is the same as in Example 1, and the results are as follows:

[0087] Time (hours) cumulative release %

[0088] 1 23.4%

[0089] 2 36.9%

[0090] 4 60.3%

[0091] 8 87.6%

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 present invention is slow released carbazochrome sodium sulfonate matrix tablet and its preparation process. The recipe of the slow released carbazochrome sodium sulfonate matrix tablet includes carbazochrome sodium sulfonate 5-85 wt%, matrix material 10-90 wt%, diluent 0-80 wt%, and proper amount of adhesive and lubricant. It is prepared through mixing material powder and direct tabletting; or pelletizing the mixture of materials except lubricant, mixing with lubricant and tabletting; or preparing fast release part, preparing slow releasing part and double-layered tabletting. The pelletizing may be wet pelletizing, dry pelletizing, smelting palletizing, etc.

Description

Technical field: [0001] The invention belongs to the technical field of drug sustained-release preparations, and in particular relates to a sustained-release matrix tablet containing the active ingredient sodium carbosulfonate and a preparation method thereof. technical background: [0002] The chemical name of sodium carbosulfonate is: 1-methyl-6-oxo-2,3,5,6-tetrahydroindole-5-semicarbazone-2-sodium sulfonate, the molecular weight is 376.32, and the structural formula is as follows: [0003] [0004] Sodium carbosulfonate is easily soluble in hot water, slightly soluble in water, and almost insoluble in ethanol or chloroform. [0005] Sodium carbosulfonate is modified on the basis of the structure of Anluoxue, and its water solubility is enhanced by 50 times, which is very beneficial to the preparation of sustained-release preparations, and its hemostatic effect is also more excellent. [0006] Sodium carbosulfonate is a new generation of vascular strengthening agent, w...

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): A61K9/22A61K31/404A61K47/10A61K47/12A61K47/14A61K47/32A61K47/34A61K47/36A61K47/38A61K47/44A61P7/04
Inventor 陈修毅
Owner SHANDONG INST OF PHARMA IND
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap