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Oral administration composition for delivering salicylic acid medicines to intestinal tract

A composition and drug technology, applied in the directions of drug combination, drug delivery, antipyretic drugs, etc., can solve the problems of affecting the efficacy of drugs, and the efficacy of salicylic acid drugs cannot be sustained for a long time.

Inactive Publication Date: 2015-01-07
HEFEI PINGGUANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Salicylic acid drugs have the problem that the drug effect cannot be sustained for a long time, mainly because the active ingredient of the drug is released too quickly, and it is likely that the drug has not yet reached the desired site of action, such as in the rectum, the active ingredient has been released, which seriously affects The effect of medicine

Method used

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  • Oral administration composition for delivering salicylic acid medicines to intestinal tract
  • Oral administration composition for delivering salicylic acid medicines to intestinal tract

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Example 1: Preparation of sustained-release sulfasalazine pellets

[0052] (i) Coating solution containing drug

[0053] 242 g of a hydroxypropylmethylcellulose / polyethylene glycol mixture (Colorcon, Dartford, UK) were dissolved in 2850 g of water by vigorous stirring. Then 68 g of micronized sulfasalazine was stirred well in the Opadry solution to form a homogeneous suspension. The suspension was made up with water to a weight of 3160 g.

[0054] (ii) Acidified sealant layer

[0055] 124g of Opadry (as above) and 6g of citric acid (Thornton and Ross) were dissolved in 1450g of water. The solution was made up to 1580 g with water.

[0056] (iii) Application of drug and sealant layers

[0057] The coating chamber of the Aeromatic-Fielder MP-1 fluidized bed coating machine is filled with 4000g of sucrose pellet cores (mesh size of 16-18, Paulaur, USA), wherein the volume of fluidizing air is 80m 3 / h, the inlet temperature is 70° C., the atomization pressure is 29 p...

Embodiment 2

[0061] Example 2: Preparation of Coated Capsules Containing Sulfasalazine Beadlets

[0062] (a) Capsule filling

[0063] The sulfasalazine pellets obtained in Example 1 were filled into No. 0 starch capsules (Capsugel, Greenwood, SC, U.S.): each capsule body was filled with 282 mg pellets, equivalent to 4 mg of sulfasalazine, In a water / isopropanol mixture, seal each capsule body with a cap.

[0064] (b) Capsule coating

[0065] 47.5 g Eudragit L100 and 15.8 g Eudragit S100 (Degussa, Darmstadt, Germany) were dissolved in a mixture comprising 714 g isopropanol and 24.3 g water. 12.2 g of dibutyl sebacate (plasticizer) and 15.8 g of talc (anti-adherent) were mixed into the coating solution.

[0066] 2400 filled capsules were transferred to the coating pan of a Hi-coater (Vector Corporation, USA) and rotated at 18 rpm. The inlet temperature is set at 40°C and the air flow is 1.16m 3 / min(41ft 3 / min), the capsule was heated for 10 minutes. The coating dispersion was then c...

Embodiment 3

[0069] Example 3: Long-Term Stability of Coated Capsules Containing Sulfasalazine Beadlets

[0070]The table below lists the sulfasalazine and impurity content of capsules prepared in Example 2 and stored for 30 months in HDPE bottles with child-resistant polypropylene caps at 25°C / 60%RH.

[0071]

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Abstract

The invention discloses an oral administration composition for delivering salicylic acid medicines to the intestinal tract. The composition comprises sustained release components, capsules and delayed release components, wherein the capsules are coated on the outer sides of the sustained release components and are coated by the delayed release components; the sustained release components comprise drug cores, organic acid layers and alkali-containing ethyecellulose layers; organic acids are coated on the outer side of the drug cores; the alkali-containing ethyecellulose is coated on the outer sides of the organic acids; the drug cores comprise sulfasalazine and / or 5-aminosalicylic acid; the capsules are prepared from gel, hydroxypropyl methyl cellulose or starch; and the delayed release components comprise polymers with enteric solubility. After the composition is subjected to oral administration during use, the medicine is delivered to the intestines, the drug release is controlled in the intestines to provide sustained release of the medicine, the salicylic acid medicines reach a to-be-treated area at enough concentration, and last for long time in the area, so that a local treatment effect is provided.

Description

technical field [0001] The invention relates to the technical field of drugs for treating gastrointestinal diseases, in particular to an oral composition for delivering salicylic acid drugs to the intestinal tract. Background technique [0002] Salicylates are used to treat inflammatory diseases of the gastrointestinal tract, such as Crohn's disease and ulcerative colitis. Sulfasalazine (SASP) and 5-aminosalicylic acid (5-ASA) are suitable for patients in chronic phase and mild to moderate activity phase. It is generally believed that SASP cannot prevent Crohn's disease recurrence. For those who cannot tolerate SASP or are allergic, 5-ASA can be used instead. For rectal and sigmoid and descending colon lesions, SASP or 5-ASA preparations can be used as enemas and administered through the anus. SASP and 5-ASA preparations should not be used in patients with severe liver and kidney diseases, infants, hemorrhagic constitution and those allergic to salicylic acid preparations...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/635A61K31/606A61K9/52A61K47/38A61K47/12A61K47/02A61K47/18A61K47/32A61P1/00A61P29/00A61P1/04A61P13/12
Inventor 王康林马婕武玉虹葛宪奎
Owner HEFEI PINGGUANG PHARMA
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