Ilaprazole enteric coated tablet and preparation method thereof

A technology of ilaprazole and ilaprazole calcium, which is applied in the direction of pill delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of poor reproducibility of enteric-coated effects, changes in drug release behavior of preparations, Affect the clinical efficacy and other issues, to achieve the effect of improving drug bioavailability, eliminating irritation, and releasing rapidly and stably

Inactive Publication Date: 2012-07-11
LIVZON PHARM GRP INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Enteric-coated tablets are a single-dose drug, and the reproducibility of the enteric-coated effect is not good, which may easily cause intestinal irritation due to high local concentration, and errors or defects in the preparation of individual tablet products will lead to the drug release behavior of the overall preparation Changes that affect clinical efficacy

Method used

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  • Ilaprazole enteric coated tablet and preparation method thereof
  • Ilaprazole enteric coated tablet and preparation method thereof
  • Ilaprazole enteric coated tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1: Extrusion spheronization method prepares the pellet core containing ilaprazole sodium

[0037] Table 1 contains the pellet core prescription of ilaprazole sodium

[0038] material

amount (g)

Microcrystalline Cellulose pH101

320

pregelatinized starch

80

Ilaprazole Sodium

72

sodium hydroxide

62

Hydroxypropyl Methyl Cellulose 5cp

10

water

120

[0039] Weigh Mcc pH101 and pregelatinized starch, mix through a 60-mesh sieve; weigh the active ingredient (i.e. ilaprazole sodium) and sodium hydroxide, mix through a 60-mesh sieve; mix the above two. Weigh 5cp of hydroxypropyl methylcellulose (HPMC) and disperse it with a small amount of hot water, then add the remaining amount of water to dissolve it, and make pulp (8% (m / m)). The above-mentioned mixed material and slurry are made into a soft material, and the soft material is extruded and spheronized. The operating ...

Embodiment 2

[0042] Embodiment 2: Extrusion spheronization method prepares the pellet core containing ilaprazole magnesium

[0043] Table 3 contains the prescription of micropellet core of ilaprazole magnesium

[0044] material

[0045] Weigh Mcc pH101 and starch, mix through 80-mesh sieve; weigh active ingredient (i.e. ilaprazole magnesium) and magnesium hydroxide, mix through 80-mesh sieve; mix the above two. Weigh 15 cp of hydroxypropyl methylcellulose (HPMC) and disperse it with a small amount of hot water, then add the remaining amount of water to dissolve it, and make pulp (5% (m / m)). The above-mentioned mixed material and slurry are made into a soft material, and the soft material is extruded and spheronized. The main parameters are controlled as follows: the particle size die is 0.2mm, the extrusion speed is 20-30rpm, and the spheronization speed is 2000-2500rpm. 522.4 g of light yellow pellet cores were obtained, with a yield of 99.7%. Direct drying or fluidized bed d...

Embodiment 3

[0046] Embodiment 3: Extrusion spheronization method prepares the pellet core containing ilaprazole lithium

[0047] Table 4 contains the pellet core prescription of ilaprazole lithium

[0048] material

[0049] Weigh Mcc pH101 and lactose, mix through a 100-mesh sieve; weigh the active ingredient (i.e. ilaprazole lithium) and sodium carbonate, mix through a 100-mesh sieve; mix the above two. Povidone K30 was weighed, dissolved in 100 g of 25% (v / v) ethanol aqueous solution, and made into slurry (5% (m / m)). The above-mentioned mixed material and slurry are made into a soft material, and the soft material is extruded and spheronized. The main parameters are controlled as follows: the particle size die is 0.4mm, the extrusion speed is 20-40rpm, and the spheronization speed is 1500-2500rpm. 535.8 g of pellet cores were obtained with a yield of 99.8%. Direct drying or fluidized bed drying at 30°C.

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Abstract

The invention provides an ilaprazole enteric coated tablet and a preparation method thereof. The ilaprazole enteric coated tablet comprises enteric coated pellets and a pharmaceutically-acceptable tablet auxiliary material, wherein each enteric coated pellet comprises a pellet core, an isolating layer and an enteric coated layer; and the pellet core comprises ilaprazole or a pharmaceutically-acceptable salt thereof and a stabilizing agent. The enteric coated pellet tablet made from ilaprazole has high acid resistance; in a prescription, barrier substances such as an acid resisting agent, a surfactant, an organic solvent, a hydrophobic substance and the like are not contained, so that the health and safety of a human body are better facilitated; in the preparation method, an organic solvent is not used, so that operation is easy, and active substances are released quickly and stably; and moreover, the pellets in the tablet can be widely and uniformly distributed into an intestinal tract after administration, a dosage is poured out in a scatter way, and the distribution area of a medicament on the surface of the intestinal tract is increased, so that the stimulation of the medicament on the intestinal tract can be reduced or eliminated, and the bioavailability of the medicament is enhanced.

Description

technical field [0001] The invention relates to an enteric-coated tablet containing a proton pump inhibitor and a preparation method thereof, in particular to an enteric-coated tablet containing ilaprazole or a pharmaceutically acceptable salt thereof and a preparation method thereof. Background technique [0002] Ilaprazole is the latest generation of proton pump inhibitor developed by Ilyang Pharmaceutical Co., Ltd. and Livzon Pharmaceutical Co., Ltd. in Korea. It is widely used in various acid-related gastrointestinal diseases, such as duodenal Ulcers, gastric ulcers, reflux esophagitis, etc. Compared with other PPIs, ilaprazole has the strongest antacid activity, no individual differences in treatment, and stronger acid control ability at night, etc., and is expected to become the core product in the PPI market. [0003] Ilaprazole is not stable in acidic and neutral media, and is easily destroyed in gastric acid. Therefore, enteric-coated tablets are currently used dom...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/4439A61K47/32A61K47/34A61K47/36A61K47/38A61P1/04
Inventor 侯雪梅金鑫陈乔柏张丽
Owner LIVZON PHARM GRP INC
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