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Polycarbophil enteric coated medicinal composition

A polycarbophil and drug technology, which is applied in the field of polycarbophil enteric-coated pharmaceutical compositions, can solve the problems of inability to guarantee complete disintegration, large preparation specifications and inconvenience to swallow, etc.

Inactive Publication Date: 2010-07-28
REGENEX PHARMA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, polycarbophil calcium preparations are used for the treatment of irritable bowel syndrome and have the following four main disadvantages: 1. Incomplete disintegration and decalcification: after polycarbophil calcium contacts with acidic environment, surface polycarbophil Calcium phenanthrene will quickly decalcify to form free polycarbophil. Free polycarbophil and free carboxyl groups have strong viscosity in the digestive juice, forming a gel-like protective layer to wrap the inner polycarbophil The surface of the calcium, preventing moisture from entering the inner layer, thereby preventing further decalcification of the inner polycarbophil calcium
3. Adverse reactions caused by high calcium: the pharmaceutical composition containing polycarbophil calcium, the calcium ions released in the gastrointestinal tract are easily absorbed by the body
4. The preparation specification is too large and difficult to swallow: the current polycarbophil calcium preparation specification is 625 mg / tablet, and the tablet weight is generally 1 gram / tablet; the daily dose per person is generally 1-4 tablets
Therefore, the clinical weight of polycarbophil calcium tablets is too large, which is inconvenient for the elderly and children to swallow
[0010] In order to solve the problem of incomplete disintegration of polycarbophil calcium, polycarbophil calcium chewable tablets (trade name: Mitrolan) have been developed.
But chewing will make polycarbophil calcium absorb water and swell in advance in the mouth, causing difficulty in swallowing, and there are also problems that may be caused by incomplete decalcification (oral acidity is close to neutral) and high calcium
EP0273209, US5215754 disclose a kind of polycarbophil calcium preparation, contain components such as microcrystalline cellulose, magnesium stearate, cross-linked polyvinylpyrrolidone, polyvinylpyrrolidone, silica gel and stearic acid, and add caramel and carry out Coating, a marketed product (trade name: Fibercon) has been developed according to the above-mentioned patent, but this tablet cannot be guaranteed to disintegrate within 60 minutes, so that the curative effect cannot be guaranteed
EP0488139 and US5213806 disclose a polycarbophil calcium preparation that can rapidly disintegrate in gastric juice, containing polycarbophil calcium and cellulose derivatives. Although this method greatly improves the disintegration problem, decalcification may not The disadvantages of thoroughness, insufficient water absorption in the stomach, and possible adverse reactions caused by high calcium have not been eliminated.
A patent (CN1662247) applied abroad in China discloses a medicinal combination of polycarbophil magnesium for the same indication. Although it avoids the problem of excessive calcium absorption, it also needs to remove magnesium in the stomach. After absorbing water, it also brings about adverse reactions that may be caused by excessive magnesium absorption.
In addition, polycarbophil magnesium still has the problems of incomplete disintegration and low water absorption capacity in acid
[0011] Therefore, there is still no preparation technology to comprehensively solve the above problems

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 4

[0041] Mix the main drug and excipients in Example 1 evenly, place them in a tumbling coating granulator to make pellets, after drying, place them in a coating pot or in a fluidized bed, and spray the enteric coating liquid to coat them. coating to obtain enteric-coated pellets with a diameter ranging from 0.5mm to 3mm. The pellets are filled into capsules to obtain polycarbophil enteric-coated capsules.

Embodiment 5

[0043] Weigh the main drug and excipients according to the prescription amount in Example 1, and after mixing evenly, use a fluidized bed or a spheroid coating granulator to wrap the main drug and auxiliary material mixture on the blank pellets. Then coat the enteric coating solution on the pellets in a fluidized bed or spheroid coating granulator, and the diameter of the pellets ranges from 0.5mm to 3mm. The pellets are packed into capsules to obtain polycarbophil enteric-coated capsules.

[0044] In order to illustrate the enteric-coated effect of medicine of the present invention, we have carried out experiment according to disintegration time limit assay method (two appendix X A of Chinese Pharmacopoeia version in 2005):

Embodiment 1-5

[0046] Example 1-5 sample disintegration time limit detection result

[0047] The test results show that the enteric-coated preparation of polycarbophil has remarkable enteric-coating characteristics: in 0.1mol / L HCL solution, there is no disintegration within 2 hours, while in the solution of phosphate buffer (pH6.8) It only takes a few minutes to disintegrate rapidly, which shows that the medicine of the present invention is not easy to disintegrate in acidic gastric juice, but can disintegrate rapidly in intestinal environment.

[0048] In order to further verify the curative effect of polycarbophil enteric-coated preparation, 6 healthy beagle dogs are divided into three groups, single-dose cross administration method, oral administration, give the polycarbophil enteric-coated tablet (500mg / Tablets), commercially available polycarbophil calcium tablets (625mg / tablet) and blank tablets (control group), twice a day, two tablets each time. Immediately after adminis...

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PUM

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Abstract

The invention relates to a pharmaceutical enteric soluble medicine compound and the method for preparing the same, comprising core of pharmaceutical and shaping for medical use and enteric soluble membrane coating the core. Said enteric soluble medicine compound can be released in intestine quickly, and avoid pharmaceutical swelling in acid gastric.

Description

technical field [0001] The present invention relates to a kind of pharmaceutical composition and preparation method thereof for preventing and / or treating constipation and diarrhea, more specifically, the present invention relates to containing polycarbophil (Polycarbophil) and pharmaceutically acceptable excipient A pharmaceutical composition comprising a core and a coating film comprising an enteric polymer surrounding the core. Background technique [0002] Irritable bowel syndrome is a disease that can cause abnormal defecation even in the absence of organic disorders, usually caused by functional abnormalities in the distal digestive tract, generally divided into the following subcategories: spastic contraction of the terminal colon, etc. Constipation type caused by delayed delivery of contents; diarrhea type caused by increased peristalsis and other promotion of contents delivery; alternate type in which constipation and diarrhea are repeated sequentially. Abnormal bo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/78A61K9/32A61K9/34A61K9/16A61K9/58A61K9/60A61K47/38A61K47/36A61K47/40A61K47/26A61K47/34A61P1/10A61P1/12A61K47/32A61K47/42
Inventor 卢智俊
Owner REGENEX PHARMA LTD