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Application of andrographolide in the preparation of a pharmaceutical for treatment of inflammatory bowel disease, andrographolide enteric targeting micropellet, and method for preparation thereof

a technology of enteric targeting and andrographolide, applied in the field of medicine, can solve the problems of insufficient effective treatment methods in the clinic, inability to completely alleviate the conditions of disease, and decrease the incidence of complications, so as to improve the specific surface area, reduce the glass transition temperature and the minimum film forming temperature (mfft), and increase the drug release rate

Inactive Publication Date: 2017-08-10
TIANJIN TASLY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0044]A specific pH-dependent technique has been used, namely the joint use of two pH-dependent polymers, to make it enteric targeting release in bodies of different colon pH values.
① The first type of enteric coating material, e.g. Eudragit L 100-55, has been used in the enteric coating layer, ensuring that the medicine does not release in the stomach until exposing the drug layer by quick dissolution after reaching the duodenum. ② The second type of coating material (e.g. the Eudragit S 100), as the middle layer, is used as a skeleton in the drug layer, among which the drug is uniformly distributed. Gradually, the drug is released by dissolution of enteric coating layer when the micropellet reaches the duodenum. Under low pH condition, however, the drug is released a little; only when approaching the end of small intestine at pH close to 7, the drug is released quickly, because the Eudragit S 100 in the drug layer has a retarding effect in the low pH condition.

Problems solved by technology

Their definite cause and pathogenesis have not yet been eradicated and therefore there are insufficient effective treatment methods in clinic.
Although these drugs are proven to be able to change the natural process of disease, they can not completely alleviate the conditions of disease and decrease the incidence of complications.
Moreover, the chemicals of glucocorticoid and immunosuppressive agents often cause obvious adverse reaction and longtime administration will likely result in damage to the body.
On the other hand, the colon drug delivery has been regarded as a difficult issue in R&D for a long time, which is determined by colon's own physiological characteristics.
It is well-known that the colon is located in the bottom half of the digestive tract, that drugs are very difficult to reach the colon when administrated orally and that enema administration is both inconvenient and painful.
Although this technique has overcome defects of difference among individuals in the pH-dependent OCSDDS, there are problems.
Because the monosaccharide, e.g. the Guar gum is dissolved in water and the drug will be soon released from pores formed by dissolution of monosaccharide after entering the body, it is difficult to ensure that effective amount of drug reaches the colon.
Once being embedded into the polymer chain, it will not only affect the extensibility of polymer chain, but also destroy the integrity of polymer membrane, which will make the coating membrane crisped and easily broken.
Hence, the risk is increased that the membrane may be early broken during transportation or by gastrointestinal peristalsis.

Method used

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  • Application of andrographolide in the preparation of a pharmaceutical for treatment of inflammatory bowel disease, andrographolide enteric targeting micropellet, and method for preparation thereof
  • Application of andrographolide in the preparation of a pharmaceutical for treatment of inflammatory bowel disease, andrographolide enteric targeting micropellet, and method for preparation thereof
  • Application of andrographolide in the preparation of a pharmaceutical for treatment of inflammatory bowel disease, andrographolide enteric targeting micropellet, and method for preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1-1

Preparation of Enteric-Coated Tablet

[0091]Extraction of andrographolide: the leaves of Andrographis paniculata was soaked in 95% (v / v) ethanol and the resulting ethanol liquid was decolored with activated carbon and the ethanol is recovered by distillation to give a concentrated liquid. The liquid was allowed to stand still to have coarse crystal. Said coarse crystal was added with 15 times (15×) 95% (v / v) ethanol, dissolved by heating, decolored with activated carbon and filtered immediately. The resultant liquid was allowed to stand still to give a light-yellow crystal by recrystallization. The obtained crystal is refined by washing with distilled water, chloroform and methol to have the final product of andrographolide.

[0092]Appropriate amount of excipient was added into afore-obtained andrographolide to prepare the enteric-coated tablet by a conventional method.

[0093]The extracting method was the same as the EXAMPLE 1-1.

[0094]Appropriate amount of excipient was added into afore-...

example 1-3

Preparation of Granule

[0095]

andrographolide100 g microcrystalline cellulose50 glactose50 gstarch50 gsurcose250 g to prepare 500 g granule

Method:

[0096]The extracting method was the same as the EXAMPLE 1-1. In addition, andrographolide and other excipients were screened with 100-mesh sifter, mixed well to prepare into the soft material by using appropriate amount of water, granulated with 14-mesh and sorted out.

example 1-4

Preparation of Intestinal Suppository

[0097]The materials were mixed well according to the formula of EXAMPLE 1-3, into which the matrix was added to prepare the intestinal suppository by a conventional method.

2. Examples and Preparative Examples of Andrographolide pH-Dependent Enteric Targeting Micropellet

[0098]It should be noted that the percentage of examples preparative examples referred to percentage by weight.

Example 2-1

[0099]Andrographolide enteric targeting micropellet was composed of a blank pellet, a drug layer and an enteric coating layer, wherein said drug layer was composed of following formula (g):

anti-BlankEurdragitstickingpelletAndrographolideS100plasticizeragentSurfactant20050152.14.51.00

[0100]Wherein, said blank pellet was a blank sucrose pellet with a diameter of 600 μm; said plasticizer was the triethyl citrate; said anti-sticking agent was the talc and said surfactant was the SDS (sodium dodecyl sulfate);

[0101]The enteric coating layer included the Eudragit L100-...

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Abstract

The present invention relates to an andrographolide enteric targeting micropellet and method for preparation thereof; furthermore, the present invention also relates to uses of andrographolide and andrographolide enteric targeting micropellets in the preparation of a pharmaceutical for treatment of inflammatory bowel disease.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application is a divisional of U.S. patent application Ser. No. 14 / 910,173, filed on Feb. 4, 2016, which is U.S. national phase filing of PCT / CN2014 / 083810, filed on Aug. 6, 2014, all of which claim priority to Chinese Patent Application No. 20130338444.1, filed on Aug. 6, 2013, the entire contents of each of which are incorporated by reference herein in their entireties.FIELD OF THE INVENTION[0002]Present invention relates to the field of medicine. More specifically, the invention relates to an andrographolide enteric targeting micropellet and method for preparation thereof. Also, present invention relates to an application of andrographolide and andrographolide enteric targeting micropellet in the preparation of a medicine for treatment of inflammatory bowel disease.BACKGROUND OF THE INVENTION[0003]Andrographolide (C20H30O5) is the diterpene lactone compound extracted from the plant Andrographis Paniculata. It is one of the main co...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/16B01J2/00A61K31/365
CPCA61K9/1682A61K31/365B01J2/006A61K9/1635A61K9/1676A61K9/5026A61K9/5078A61P1/00A61P1/04A61P29/00A61P31/00A61K9/16
Inventor SUN, HENRYMA, XIAOHUIGUO, ZHIXINLIN, SENWANG, GENBEIYAN, LULUZHANG, LIHUAZHOU, SHUIPINGZHANG, SHUNNAN
Owner TIANJIN TASLY PHARMA CO LTD
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