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Multi-unit slow-release preparation

A multi-unit, preparation technology, applied in the field of pharmacy, can solve the problems of insufficient strength, low release bioavailability, and irregular release.

Active Publication Date: 2007-06-27
GUANGZHOU PUIS PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, further studies in humans have shown that the pellets with good in vitro release are basically not released in the human body, and the bioavailability is very low compared with ordinary tablets, and the in vitro release cannot be accelerated by reducing the amount of methacrylate copolymer. Improve bioavailability
Even if the amount of methacrylate copolymer is very low and the in vitro release is fast, it still shows irregular release and low bioavailability in vivo, which cannot meet the standard requirements (see below)
The possible reason is that there is too little methacrylate copolymer, the coating of the pellets is uneven and the strength is not enough
Change to a pH-dependent acrylate copolymer and a mixture of pellets with different in vitro release rates. Although the in vitro release is good, the in vivo performance is either the same as that of ordinary tablets or the bioavailability is very low.

Method used

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  • Multi-unit slow-release preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1: Preparation details

[0039] 1.1 Preparation of pellet cores containing erythromycin derivatives

[0040] Add clarithromycin, citric acid (monohydrate), binder and surfactant into an appropriate amount of 50% (V / V) ethanol solution, stir well and maintain stirring. Put the inert core in the fluidized bed bottom spray device, adjust the appropriate air speed and temperature, and coat the above suspension on the core. The obtained ball core is dried until the water content is less than 4%.

[0041] Prescription (mg / tablet): clarithromycin 250mg, citric acid (monohydrate) 32mg, hypromellose 35mg, sodium lauryl sulfate 4.4mg, inert core 75mg.

[0042] 1.2 Ball core coated with slow-release film

[0043] Neutral methacrylate (Eudragit NE30D), hypromellose, polyethylene glycol 6000 and talcum powder are fully stirred and kept stirring, and the above-mentioned obtained ball core is placed in a fluidized bed bottom spray device, and a suitable The air speed and t...

Embodiment 2

[0047] Embodiment 2 bioavailability test

[0048] 2.1 Drugs

[0049] The above-mentioned preparation (T), 250mg / grain; control drug (R): Klacid (Klacid  Clarithromycin tablets, produced by Italy Abbott Pharmaceuticals Co., Ltd. and repackaged by Shanghai Abbott Pharmaceuticals Co., Ltd.), 250mg / tablet.

[0050] Bioequivalence standard: "Pharmacopoeia of the People's Republic of China" 2000 Edition Appendix XIXB Guidelines for human bioavailability and bioequivalence testing of pharmaceutical preparations.

[0051] 2.2 Experimental design and methods

[0052] A single-dose, two-period crossover design was adopted. 20 healthy subjects (average age 23.0±2.42 years old) were randomly divided into two groups A and B, 10 people in each group, and the test drug or control drug was crossed orally in phase I and II respectively, and a one-week washout period was passed before the cross medication .

[0053] Phase I trial: 10 subjects in group A took 500 mg of the control drug ora...

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Abstract

An orally taken slow-release multi-unit medicine is composed of multiple micro-pills including at least one erythromycin derivative and at least one organic carboxylic acid. Said micro-pill is wrapped by a water-insoluble medicine-permeable polymer film containing the water-soluble clamycin.

Description

technical field [0001] The present invention belongs to the field of pharmacy. Disclosed is an oral multi-unit sustained-release preparation of erythromycin derivatives that can reduce the number of daily doses. More specifically, the present invention is a clarithromycin multi-unit sustained-release preparation administered once a day. technical background [0002] Erythromycin derivatives include clarithromycin (6-methylerythromycin A), roxithromycin, azithromycin, etc., which are a class of semi-synthetic antibacterial drugs, which usually need to be administered two or three times a day, and a course of treatment is usually 10-14 days. Too many doses lead to poor compliance. [0003] Developing their sustained-release formulations could improve medication compliance. One such sustained-release preparation is the monolithic sustained-release tablet. Another possibility is a multi-unit sustained-release preparation, such as sustained-release pellets containing the abo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61K31/7052A61K9/16A61P31/04
Inventor 贝庆生谢俊雄
Owner GUANGZHOU PUIS PHARMA FACTORY