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Zileuton-containing membrane-controlled slow release pellets and preparation method thereof

A technology of sustained-release pellets and zileuton, which is applied in the direction of bulk delivery, respiratory diseases, and drug combinations, can solve the problems of large individual differences in absorption, hidden dangers of drug safety, and difficult reproducibility, and achieve inter-individual The effect of small difference, improvement of clinical effective rate, and avoidance of burst release effect

Inactive Publication Date: 2013-07-10
STAIDSON (BEIJING) BIOPHARMACEUTICALS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the matrix sustained-release tablet is a single-unit drug delivery system, and if the quality of a single sustained-release tablet is defective, it will cause a burst release effect and bring hidden dangers to medication safety; at the same time, the drug release behavior between different batches of sustained-release tablets The reproducibility is difficult to control, and the absorption in the body varies greatly among individuals; in addition, zileuton itself has a certain stimulating effect on the gastrointestinal tract, and patients have adverse reactions such as nausea and vomiting after taking it

Method used

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  • Zileuton-containing membrane-controlled slow release pellets and preparation method thereof
  • Zileuton-containing membrane-controlled slow release pellets and preparation method thereof
  • Zileuton-containing membrane-controlled slow release pellets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Embodiment 1 preparation containing pill core

[0052] Prescription: Zileuton 3000g

[0053] Sucrose (thinner) 1500g

[0054] Starch (binder) 500g

[0055] Preparation process: Weigh an appropriate amount of zileuton, sucrose, and starch, pass through an 80-mesh sieve respectively, mix evenly according to the prescription ratio, add an appropriate amount of 70% ethanol to prepare a soft material, and extrude through a sieve plate of an extruder to obtain a strip-shaped material. Put the strip material in the spheronizer, adjust the speed of 1500rpm and the spheronization time for 5 minutes to make the particles completely spheroidized, take out the pellets and dry them, heat-treat at 40°C for 12 hours, and then sieve the pellets with a size of 0.5-0.9mm to obtain the pellet core. Results The obtained pill-containing core was smooth and round in appearance, low in friability, and suitable for coating.

Embodiment 2

[0057] Preparation of pill-containing cores

[0058] Prescription: Zileuton 3000g

[0059] Microcrystalline cellulose (thinner) 1100g

[0060] Preparation process: the same as the preparation method in Example 1, wherein when the strip-shaped material is placed in a spheronizer for spheronization, the rotational speed is adjusted to 800 rpm and the spheronization time is 15 minutes.

Embodiment 3

[0062] Preparation of pill-containing cores

[0063] Prescription: Zileuton 3000g

[0064] Starch (thinner) 1250g

[0065] Povidone (adhesive) 200g

[0066] Preparation process: with embodiment 1.

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Abstract

The invention discloses zileuton-containing membrane-controlled slow release pellets and a preparation method thereof. The zileuton-containing membrane-controlled slow release pellets contain quick release coated pellets and slow release coated pellets in a weight part ratio of 1:3-1:7, wherein the coated pellets consist of zileuton-containing medicated pellet cores and coatin layers wrapped outside the medicated pellet cores; and the weight part ratio of the medicated pellet cores to the coating layer is 5:1-15:1. The drup release rate of the zileuton-containing membrane-controlled slow release pellets is stable and controllable, and the clinical effectiveness is obviously improved; meanwhile, adverse effect occurrence of the gastrointestinal tract is also greatly reduced; and the pellets have a simple preparation process and high repeatability and are suitable for scale-up production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a film-controlled slow-release pellet containing zileuton and a preparation method thereof. Background technique [0002] Zileuton (Zileuton) chemical name: N-hydroxy N-[1-(2-benzothiophene) ethyl] urea, first synthesized by ABBOT laboratory in the United States in 1988, FDA approved the drug officially in December 1996 Listed in the United States, it is used for the prevention and treatment of chronic asthma in people over the age of 12. [0003] Zileuton is a new type of 5-lipoxygenase inhibitor, and its mechanism of action is: by inhibiting the activity of 5-lipoxygenase to antagonize the synthesis of leukotrienes, thereby effectively controlling the development of asthmatic inflammation (leukotriene It is a highly active inflammatory substance synthesized by arachidonic acid catalyzed by 5-lipoxygenase, and plays an important role in the pathogenesis of asthma). As ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/381A61P11/06
Inventor 谭剑平蒋立新常坦然
Owner STAIDSON (BEIJING) BIOPHARMACEUTICALS CO LTD
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