Loxoprofen sodium sustained-release pellet

A technology of loxoprofen sodium and sustained-release pellets, which is applied in the direction of microcapsules, medical preparations of non-active ingredients, and respiratory diseases, etc., which can solve the problems of poor ease of use, reduce irritation, and reduce drug administration The effect of frequency and avoiding side effects

Active Publication Date: 2016-07-20
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Loxoprofen sodium includes loxoprofen sodium anhydrate, monohydrate or dihydrate, among which loxoprofen sodium dihydrate is recorded in the Japanese Pharmacopoeia Prescription and Chinese Ministry of Standards, which is a water-soluble drug At present, the oral dosage form of this drug that has been listed in the domestic and foreign markets is mainly loxoprofen sodium tablet, and the dosage is 180mg per day, which is taken in three times, and the convenience of use is poor.

Method used

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  • Loxoprofen sodium sustained-release pellet
  • Loxoprofen sodium sustained-release pellet
  • Loxoprofen sodium sustained-release pellet

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Embodiment 1 loxoprofen sodium sustained-release pellet capsule (2000)

[0027] prescription:

[0028] 1) Drug-loaded pill core

[0029]

[0030] 2) Isolation layer coating solution

[0031]

[0032] 3) Sustained release layer coating solution

[0033] Surelease water-based dispersion 180g

[0034] Distilled water 120g

[0035] Preparation Process:

[0036] 1) Preparing drug-loaded pill cores: Pass loxoprofen sodium, starch, and microcrystalline cellulose through an 80-mesh sieve respectively, mix evenly according to the prescription ratio, add 50% ethanol, prepare soft materials, and pass through the sieve plate of the extruder Extrude the strips, put the strips into a spheronizer, and spheronize to obtain round particles. After drying at 50°C for 12 hours, sieve 0.6-1.25mm pellets to obtain the core of the pellets containing The appearance of the pill core is smooth, round and hard, suitable for coating.

[0037]2) Prepare the coating solution for the iso...

Embodiment 2

[0041] Embodiment 2 loxoprofen sodium sustained-release pellet capsules (2000)

[0042] prescription:

[0043] 1) drug-loaded pill core is the same as embodiment 1

[0044] 2) Isolation layer coating solution

[0045]

[0046] 3) Sustained release layer coating solution

[0047] Surelease Aqueous Dispersion 240

[0048] Distilled water 160g

[0049] Preparation process: with embodiment 1.

Embodiment 3

[0050] Embodiment 3 loxoprofen sodium sustained-release pellet capsules (2000)

[0051] prescription:

[0052] 1) drug-loaded pill core is the same as embodiment 1

[0053] 2) Isolation layer coating solution

[0054]

[0055] 3) Sustained release layer coating solution

[0056] Surelease water-based dispersion 270g

[0057] Distilled water 180g

[0058] Preparation process: with embodiment 1.

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Abstract

The invention provides a loxoprofen sodium sustained-release pellet. The pellet comprises a drug-loaded pellet core, an isolating layer coating the drug-loaded pellet core and a sustained-release layer coating the isolating layer, wherein the weight ratio of the drug-loaded pellet core to the isolating layer to the sustained-release layer is 80:(1-15):(2-20). The loxoprofen sodium sustained-release pellet shows an excellent release characteristic in vitro, the frequency of administration can be reduced, the medication compliance of patients can be improved, the blood concentration can be stabilized, and toxic and side effects of drugs on the stomach and intestines can be reduced. The invention further discloses a method for preparing the loxoprofen sodium sustained-release pellet. The method is simple in process, and is easy to industrially produce.

Description

technical field [0001] The invention belongs to the field of pharmacy, and relates to loxoprofen sodium sustained-release pellets and a preparation method thereof. Background technique [0002] Loxoprofen Sodium (Loxoprofen Sodium), the first propionic acid precursor non-steroidal anti-inflammatory drug (NSAIDs), was first developed by Sankyo Co., Ltd. in Japan, and was launched in Japan in July 1986. The trade name is Lesong . After oral administration, the drug is metabolized into a trans-OH active drug in the body, inhibiting the biosynthesis of prostaglandins, that is, by binding to cyclooxygenase, covering the active center of the enzyme, thereby blocking the enzyme from catalyzing the conversion of arachidonic acid into PG Metabolism, exert analgesic, anti-inflammatory and antipyretic effects. As a new type of NSAIDs, loxoprofen sodium is different from other drugs in that it is a prodrug, which has no activity itself, and becomes active only after being rapidly conv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/216A61K47/38A61P29/00A61P19/02A61P11/00
CPCA61K9/5073A61K31/216A61K47/38
Inventor 栾立标万东伟
Owner CHINA PHARM UNIV
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