Scopolamine hydrobromide orally disintegrating microencapsule tablets based on NIMS system

A technology of scopolamine and oral rapid disintegration, which is applied in the field of medicine, can solve the problems of large drug side effects, no visible drug absorption, and abnormally high drug absorption, and achieve the effects of taking convenience, reducing drug side effects, and reducing local irritation

Inactive Publication Date: 2010-03-17
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Scopolamine hydrobromide is odorless and tasteless, and is easily soluble in water. At present, the clinically used dosage forms are mainly oral tablets and injection injections. A lot of inconvenience, and oral tablets or injections often cause abnormally high blood levels of drug absorption, and the side effects of drugs are large
[0003] The NiMS system is a new technology used for drug entrapment in recent years. After the drug is made into nanoparticles, it is spray-dried and microencapsulated to form a dru

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1: Preparation of orally rapidly disintegrating microcapsule tablets of scopolamine hydrobromide based on the "NiMS" system

[0047] 1. Preparation of scopolamine hydrobromide "NiMS" system (referred to as drug-loaded "NiMS" system):

[0048] 1) prepare the chitosan solution containing scopolamine hydrobromide:

[0049] Take 150 mg of chitosan and 90 mg of hypromellose, dissolve them in 300 ml of 0.3% dilute acetic acid to obtain a 0.5% chitosan solution, and after swelling overnight, add 80 mg of scopolamine hydrobromide powder to it to make a hydrobromide-containing solution. Chitosan solution of scopolamine acid;

[0050] 2) Preparation of tripolyphosphate solution:

[0051] Prepare a 0.5% tripolyphosphate solution with distilled water;

[0052] 3) Preparation of scopolamine hydrobromide "NiMS" system:

[0053] At 40°C, with continuous stirring at 600 rev / min, the above 0.5% tripolyphosphate solution was slowly added dropwise to the chitosan solution cont...

Embodiment 2

[0066] Example 2. Preparation of Oral Rapidly Disintegrating Microcapsules of Scopolamine Hydrobromide Based on the "NiMS" System

[0067]Get chitosan 150mg, hypromellose 150mg, dissolve in the dilute acetic acid of 300ml 0.3%, swell overnight, all the other are the same as embodiment 1. The encapsulation efficiency of the obtained "NiMS" system was 94%, and the average particle size was 1.5 μm.

Embodiment 3

[0069] Prepare scopolamine hydrobromide orally rapidly disintegrating microcapsules according to the following ratio (w / w):

[0070] Drug-loaded "NiMS" system (same as Example 1) 2.5%

[0071] Microcrystalline Cellulose 40%

[0072] Sodium Starch Carboxymethyl 10%

[0073] Mannitol 40%

[0074] Lactose 5%

[0075] Xylitol 1%

[0076] Magnesium Stearate 0.5%

[0077] Micronized silica gel 0.2%

[0078] Vinylpyrrolidone 1.5%

[0079] The rest are the same as in Example 1, the disintegration time of the obtained scopolamine hydrobromide orally disintegrating microcapsules is 48 s, and the cumulative release rate in 37° C. water for 30 min is 17%.

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PUM

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Abstract

The invention relates to the technical field of medicines, particularly to scopolamine hydrobromide orally disintegrating microencapsule tablets based on a NiMS system and a preparation method thereof. The orally disintegrating microencapsule tablet provided by the invention is prepared by the NiMS system containing scopolamine hydrobromide and auxiliary materials. The auxiliary materials comprise microcrystalline cellulose, sodium carboxymethyl starch, mannitol, lactose, xylitol, magnesium stearate, superfine silica powder, etc. The copolamine hydrobromide orally disintegrating microencapsule tablet provided by the invention can be taken conveniently, and disintegrated rapidly in mouth by solvent of saliva without needing to drink water. The NiMS system further has a slow release effect,thereby not causing abnormal high blood drug concentration, reducing drug side effects, reducing local stimulation, and meeting requirements for special conditions and special groups, particularly the aged, children and patients who swallow difficultly.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to an orally rapidly disintegrating microcapsule tablet of scopolamine hydrobromide based on a "NiMS" system and a preparation method thereof. Background technique [0002] Motion sickness is a series of nervous system dysfunction syndromes caused by abnormal exercise stimulation. Its pathogenesis is not yet clear, but it is generally believed that it is closely related to the vestibular system cholinergic hyperfunction. Scopolamine hydrobromide can block M-choline receptors, inhibit the central function, and is mainly used to prevent and treat motion sickness. Scopolamine hydrobromide is odorless and tasteless, and is easily soluble in water. At present, the clinically used dosage forms are mainly oral tablets and injection injections. Many inconveniences, and oral tablets or injections often cause abnormally high blood levels of drug absorption, and the side effects of the drug ar...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/46A61K47/38A61P1/08
Inventor 胡晋红吕维玲李凤前朱全刚
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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