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Oral sustained releasing micropill of tuduranine and their preparation method

A technology for slow-release pellets and sinomenine, which is applied in the directions of pill delivery, sugar-coated pills, and pharmaceutical formulations to achieve good reproducibility.

Inactive Publication Date: 2006-10-11
SHANGHAI INST OF PHARMA IND CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, how to improve some shortcomings of sustained-release tablets is a very realistic problem from the perspective of clinical treatment.

Method used

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  • Oral sustained releasing micropill of tuduranine and their preparation method
  • Oral sustained releasing micropill of tuduranine and their preparation method
  • Oral sustained releasing micropill of tuduranine and their preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Ball core 200g, particle size 0.7mm

[0034] 70 grams of sinomenine hydrochloride

[0035] HPMC 10g

[0036] PEG6000 1g

[0037] 20 grams of water

[0038] (The above is the prescription of the medicine)

[0039] Surelease  70 grams

[0040] water 50g

[0041] (coating prescription)

[0042] use figure 1 The procedure shown for the preparation:

[0043] (1) Prescription of upper medicine is prepared into suspension, and its particle diameter is 10 microns;

[0044] (2) Place the inert ball core in the boiling drier 1, pass hot air from the bottom of the drier 1, make the inert ball core in a fluidized state, and put the suspension in step (1) from the bottom of the drier 1 After spraying through the nozzle 2, the suspension is sprayed on the inert ball core and dried;

[0045] Hot air temperature: 45°C, material temperature: 30°C, atomization pressure: 1.5bar; wind speed: 0.2-2 m / s

[0046] (3) Continue to pass in hot air to keep the inert ball core in ...

Embodiment 2

[0049] Ball core 200g

[0050] Sinomenine Hydrochloride 100g

[0051] HPMC 15g

[0052] PEG6000 1.5g

[0053] 30 grams of water

[0054] (The above is the prescription of the medicine)

[0055] Surelease  120 grams

[0056] HPMC 6g

[0057] 180g water

[0058] (coating prescription)

Embodiment 3

[0060] Ball core 200g

[0061] Sinomenine Hydrochloride 50g

[0062] HPMC 5.6g

[0063] PEG6000 0.8g

[0064] water 12 grams

[0065] (The above is the prescription of the medicine)

[0066] Eudragit  RS-100 20g

[0067] Eudragit  RL-100 3 grams

[0068] 2 g triacetic acid citrate

[0069] Talc powder 10g

[0070] 95% ethanol 250ml

[0071] (The above is the coating prescription)

[0072] The preparation method is the same as in the examples.

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Abstract

The invention discloses an oral sustained-release pellet of sinomenine or a salt thereof and a preparation method thereof. The sinomenine or its salt of the present invention is composed of an inert ball core loaded with a therapeutically effective amount of active ingredients and pharmaceutical adjuvants and a coating wrapped thereon, and the invention adopts a fluidization process for drug application and coating. The medicine on the core of the ball is carried out in a fluidized state with an aqueous suspension composed of sinomenine hydrochloride micropowder and some fillers. The coating of the slow-release coating layer is preferably made of ethyl cellulose aqueous dispersion in the same fluidized device. conduct. The sinomenine micropills that this technology makes, respectively in water pH1.0 hydrochloric acid, in three kinds of media of aqueous solution and pH6.8 phosphate buffer solution, adopt Chinese Pharmacopoeia 2000 edition I method, carry out release test, the result shows that micropill releases Both pills last up to 12 hours. The process has the characteristics of good reproducibility, stable and reliable slow-release drug and the like.

Description

technical field [0001] The invention relates to an oral sustained-release pellet of sinomenine, an effective monomer of traditional Chinese medicine, in particular to a preparation method of an oral sustained-release pellet of sinomenine or a salt thereof. Background technique [0002] Sinomenine is an alkaloid monomer extracted from the traditional Chinese medicine Sinomenuim Scutum Retd.et et wils. Its hydrochloride is often used in medicinal preparations. Sinomenine has anti-inflammatory, immunosuppressive, analgesic, antihypertensive, antiarrhythmic and other pharmacological effects. It has been clinically proven to have good curative effect in the treatment of rheumatoid arthritis and other rheumatism and arrhythmia. (Liu Qiang et al., Chinese Herbal Medicine, 1997, 28(4): 247-249) (Yidandan et al., Chinese Journal of Hospital Pharmacy, 2002, 22(8): 465-467) Sinomenine was formally approved as a national medicine in 1996. The important protected varieties are recorded...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4748A61K9/28A61P29/00A61P9/12A61P9/06A61P37/06A61P19/02
Inventor 包泳初陈庆华潘峰瞿挺
Owner SHANGHAI INST OF PHARMA IND CO LTD