Highly-soluble sulbenicillin sodium colon-targeted starch capsule and preparation method thereof

A technology of sulbenicillin sodium and starch capsules, which is applied in the field of highly soluble sulbenicillin sodium colon-targeted starch capsules and its preparation, which can solve the problems of unstable release and large-scale burst release of film-layer drugs, and achieve low cost , easy to operate, simple process effect

Inactive Publication Date: 2018-06-26
HUNAN ERKANG XIANGYAO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these methods are more or less flawed. The pH value type material is alkaline and degrades with the pH. After entering the intestinal environment, the pH value from the front of the small intestine to the colon gradually increases, and the alkaline material is not at the pH of the colon. Only when the condition begins to dissolve, but before reaching the colon, most of the pH value type materials are not dissolved, and a small part of the material dissolves, but the rupture of some membrane layers may lead to a large amount of sudden release of the drug
However, the use of colonic bacteria degradable materials may also cause the instability of release due to individual differences and differences in bacterial flora.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Preparation of Sulbenicillin Sodium

[0024] Add the crude sulbenicillin sodium to 95% ethanol, add 0.5% (w / v) activated carbon, stir and dissolve at 50°C for 30 minutes, filter out the activated carbon while it is hot, cool the filtrate to 0°C, crystallize for 5 hours, filter, Dry to obtain refined sulbenicillin sodium; ultrasonicate the refined sulbenicillin sodium under ultrasonic conditions, and then put it into microwave conditions and microwave at 150°C for 40 minutes to obtain uniform, stable and highly soluble sulphonic acid Benzillin Sodium.

Embodiment 2

[0026] Prepare hard capsules according to the conventional process: fill the refined sulbenicillin sodium in the tapioca starch capsule shell, and use the sealing material (mixed solution of HPMC5%, PVA11%, ethanol 34%, water 60%) to fit the capsule shell seal at the place to make hard capsules; prepare colon enteric coating liquid, its formula is made up of hypromellose phthalate, 95% ethanol, succinate, and the weight percent of each component is: hypromellose 7.0% of phthalate, 90.0% of 95% ethanol, and 3.0% of succinate; the above-mentioned colon enteric coating solution is used to coat the starch capsule to obtain the colon enteric starch capsule of the present invention.

[0027] The in vitro dissolution test of the capsule was carried out, and the results were as follows: the dissolution rate of the capsule was less than 1% in 3 hours in 37 ℃, pH=6.8 artificial intestinal fluid; 10% in 1 hour in 37 ℃, pH=7.4 artificial intestinal fluid; 37 ℃, pH=7.8 More than 90% dissol...

Embodiment 3

[0029] Prepare hard capsules according to the conventional process: fill the refined sulbenicillin sodium in the tapioca capsule shell, and use sealing materials (HPMC5%, PVA11%, ethanol 34%, water 60%) to seal the joint of the capsule shell , prepared into starch hard capsules; preparation of colonic enteric coating liquid, its formula is made up of cellulose acetate trimellitate, 95% ethanol, octenyl succinate starch, and the weight percentage of each component is: cellulose acetate 7.0% trimellitate, 90.0% 95% ethanol, 3.0% octenyl succinate starch; coat the capsule with the above colonic enteric coating solution to obtain the colonic enteric starch capsule of the present invention.

[0030]The in vitro dissolution test of the capsule was carried out, and the results were as follows: the dissolution rate of the capsule was less than 1% in 2 hours in artificial gastric juice at 37 ℃; About 4% was dissolved in 1 hour in artificial intestinal juice; 92% was dissolved in 1 hour...

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PUM

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Abstract

The invention provides a highly-soluble sulbenicillin sodium colon-targeted starch capsule and a preparation method thereof. According to the invention, a starch capsule is used and is filled with sulbenicillin sodium, the nested part of a capsule shell is sealed with a sealing material so as to prepare a hard capsule, and the prepared hard capsule is coated with a colon-soluble coating solution;and the colon-soluble coating solution is prepared by mixing a coating material, a coating solvent and a plasticizer. The invention has the following advantages: the prepared highly-soluble sulbenicillin sodium colon-targeted starch capsule has the triple effects of colon targeting performance, rapid disintegration and slow drug release, prolongs the circulation time of oral sulbenicillin sodium in the body and improves the absorption efficiency of sulbenicillin sodium; compared with the prior art where special colon-soluble capsule shells are selected, the highly-soluble sulbenicillin sodiumcolon-targeted starch capsule of the invention is high in filling percentage, and a coating process adopted in the invention is stable in process, easy to operate and suitable for large-scale industrial production; after coating, the starch hard capsule prepared by using the method can maintain the color and transparency of the original capsule and improve patient compliance; and the preparation method does not need special equipment, and is simple in process, easy to operate and low in cost.

Description

technical field [0001] The invention relates to a highly soluble sulbenicillin sodium colon-targeting starch capsule and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] Sulbenicillin sodium belongs to broad-spectrum semi-synthetic penicillin antibiotics. It is effective against the following infections caused by sensitive bacteria such as Pseudomonas aeruginosa, Proteus, and E. coli: (1) Respiratory system infections, such as acute and chronic bronchitis, bronchiectasis, bronchial Pneumonia, pneumonia, etc.; (2) abdominal infection, such as peritonitis, cholecystitis, cholangitis, etc.; (3) urinary system infection, such as pyelonephritis, cystitis, urethritis, etc.; (4) gynecological infection, such as uterine appendages (5) superficial suppurative diseases, such as folliculitis, cellulitis, tonsillitis, postoperative wound infection, traumatic or burn infection, etc.; (6) sepsis; (7) subacute Bacterial endocarditis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/48A61K47/36A61K47/38A61K47/10A61K47/14A61K47/32A61K31/43A61P31/04
CPCA61K9/4816A61K9/4891A61K31/43A61K47/10A61K47/14A61K47/32A61K47/36A61K47/38
Inventor 帅放文王向峰章家伟
Owner HUNAN ERKANG XIANGYAO PHARMA
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