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Para-aminosalicylate colon positioning drug delivery system

A sodium aminosalicylate and colon-localized technology, which is applied in the digestive system, drug combination, pharmaceutical formula, etc., can solve the problems of large adverse reactions and low local concentration, so as to reduce toxic and side effects, eliminate irritation, and reduce dosage Effect

Active Publication Date: 2009-12-02
上海新菲尔生物制药工程技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The technical problem to be solved by the present invention is to overcome the shortcomings of low local concentration and large adverse reactions in the existing ordinary tablets and enteric-coated tablets of sodium p-aminosalicylate, and provide a kind of medicine that can overcome the above-mentioned shortcomings, and Sodium p-aminosalicylate pellets or granules with better colon localization effect

Method used

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  • Para-aminosalicylate colon positioning drug delivery system
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  • Para-aminosalicylate colon positioning drug delivery system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1 Preparation of pellets or granules by sugar-coated pan method

[0047] 1. System kernel

[0048] Steps (1)-(5) were carried out at 5°C, and steps (1)-(3) and (5) were carried out under dark light conditions.

[0049] (1) Take 500g of sodium p-aminosalicylate (100% pass through 500 mesh), mix it with 300g PVP-k30 and 100g Eudragit S100 and use it as material A (900g in total); dissolve 100g Eudragit S100 in 100g 20% Aqueous ethanol was used as feed B (200 g in total).

[0050] The overall formulation is: 50% sodium p-aminosalicylate, 30% binder (PVP-k30) and 20% backbone material (Eudragit S100).

[0051] (2) Take and mix 450gA and 22.5gB of materials respectively to make semi-dry and semi-wet soft materials, and pass through a 20-mesh upper screen to make fine particles as intermediate C.

[0052] (3) Put the intermediate C into the rotating sugar-coating pot, alternately add material A and material B while rotating, and continuously sieve and classify, put...

Embodiment 2

[0058] Example 2 Sugar-coated pellets or granules

[0059] 1. System kernel

[0060] Steps (1)-(5) are carried out at room temperature (25°C), and steps (1)-(3) and (5) are carried out under dark light conditions.

[0061] (1) Take 980g of sodium p-aminosalicylate original drug (100% pass through 400 mesh), mix with 10g copovidone and 5g cellulose acetate phthalate as material A (total 995g); 5g cellulose acetate Phthalate was dissolved in 250 g of 50% ethanol in water as feed B (255 g total).

[0062] The overall formulation is: 98% sodium p-aminosalicylate, 1% binder (copovidone) and 1% backbone material (cellulose acetate phthalate).

[0063] (2) Take and mix the materials 19.6gA and 19.6gB respectively to form a semi-dry semi-wet soft material, and pass through a 20-mesh upper screen to make fine particles as intermediate C.

[0064] (3) Put the intermediate C into the rotating sugar-coating pot, alternately add material A and material B while rotating, and continuously...

Embodiment 3

[0070] Example 3 Sugar-coated pellets or granules

[0071] 1. System kernel

[0072] Steps (1)-(5) are carried out at room temperature (30°C), and steps (1)-(3) and (5) are carried out under dark light conditions.

[0073] (1) Mix 880g (100% through 80 mesh) of the original drug of sodium p-aminosalicylate with 40g hydroxypropyl methylcellulose (HPMC), 10g microcrystalline cellulose and 30g sodium carboxymethylcellulose as a material A (960 g in total); 40 g of Eudragit L100 was dissolved in 320 g of an 80% ethanol aqueous solution by mass as material B.

[0074] The overall formulation is: 88% sodium p-aminosalicylate, 3% binder (sodium carboxymethylcellulose), 8% backbone material (HPMC and Eudragit L100) and 1% porogen (microcrystalline cellulose).

[0075] (2) Take and mix 76.8g of material A and 19.2g of material B to form a semi-dry and semi-wet soft material, and pass through a 10-mesh upper screen to make fine particles as intermediate C.

[0076] (3) Put the interm...

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Abstract

The invention relates to a para-aminosalicylate colon positioning drug delivery system which is a pellet or a particle. The inner part of the system is a kernel which contains the following components according to the mass percent: 50-98 percent of para-aminosalicylate, 1-30 percent of adhesive and 1-20 percent of skeleton material; and the surface of the kernel is coated with a layer of coatings which is 1 percent-40 percent of the mass of the whole pellet or the particle and contains film forming agent, sticking resistant agent and plasticizer. The invention also discloses a method for preparing the formulation, which comprises a sugar coating pot method, an extrusion-rolling method and a fluidized bed preparation method. Compared with the prior common tablet and a colon positioning tablet, the formulation has the better colon positioning effect, has the characteristics of increased specific surface area and good dissolving effect, is beneficial to absorbing and can reduce the poison and side effect caused by fast drug release by an individual difference of the formulation with a large dose, such as tablets, and the like.

Description

technical field [0001] The invention relates to a colonic positioning drug delivery system for sodium p-aminosalicylate. Background technique [0002] After oral administration, the drug is generally absorbed or degraded before reaching the colon, while with rectal administration, the drug can directly enter the rectum or colon for local or systemic treatment. However, when administered rectally, the drug is limited to the rectum and descending colon, and cannot reach the transverse colon and ascending colon. Therefore, the development of colon-localized drug delivery system is of great significance for the drugs used for the treatment of local lesions of the colon, and the drugs that need to be located in the colon to avoid being degraded by gastrointestinal enzymes. [0003] At present, colon-targeted drug delivery systems can be roughly divided into the following categories according to the drug release principle: enzyme-controlled drug delivery systems, pH-controlled dr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/606A61K47/26A61K47/32A61K47/34A61K47/36A61K47/38A61K47/40A61K47/42A61P1/00A61P1/04A61K47/10
Inventor 王懋杨学成
Owner 上海新菲尔生物制药工程技术有限公司
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