Rasagiline or medicinal salt sublingual film agent thereof as well as preparation method and application thereof

A technology for medicinal salts and film preparations, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve problems such as poor stability and increased content of oxidized impurities, and achieve good stability. , Rapid dissolution and good compliance

Pending Publication Date: 2022-05-13
SHANGHAI ZHONGXI PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The technical problem to be solved by the present invention is to overcome the defect of poor stability of rasagiline preparations in the prior art, and provide a kind of rasagiline or its medicinal salt sublingual film and its preparation method and application
The inventors found that a variety of excipients are prone to interact with rasagiline, resulting in a significant increase in the content of oxidized impurities, and the addition of antioxidants still cannot effectively solve the stability problem

Method used

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  • Rasagiline or medicinal salt sublingual film agent thereof as well as preparation method and application thereof
  • Rasagiline or medicinal salt sublingual film agent thereof as well as preparation method and application thereof
  • Rasagiline or medicinal salt sublingual film agent thereof as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] The compositions and dosages of prescriptions 1-5 and comparative prescriptions are shown in Table 1.

[0062] Table 1

[0063]

[0064] Preparation Process:

[0065] 1. Prepare the water slurry of the film-forming material: Dissolve HPMC and PVP in water according to the ratio of the prescription to prepare a water slurry with a mass concentration of 25%.

[0066] 2. Add rasagiline mesylate, hydroxypropyl-β-cyclodextrin, steviol glycoside, titanium dioxide and strawberry essence into the above water slurry, and stir evenly.

[0067] 3. Stand still for defoaming, and apply the film under the condition that the thickness of the film is 0.4mm and the drying temperature is 85°C. The speed of coating and film forming is 50cm / min.

[0068] 4. According to the specification of 0.5mg / tablet, it is cut and packaged.

[0069] It can be seen from Table 1 that (1) the physical properties of the film of prescription 1-3 of the present invention are better in strength and toug...

Embodiment 2

[0071] The prescription of embodiment 2 is as shown in table 2.

[0072] Table 2

[0073] Name of raw material Mass % Rasagiline mesylate 5 Hydroxypropyl Cellulose HPC 40 Sodium Carboxymethyl Cellulose CMC-Na 30 Maltodextrin 5 Glucosyl-β-cyclodextrin 5 Maltitol 10 Titanium dioxide 4 grape essence 1 total 100

[0074] Preparation Process:

[0075] 1. Prepare the water slurry of the film-forming material: 40g of HPC and 30g of CMC-Na are dissolved in water to prepare a water slurry with a mass concentration of about 20%.

[0076] 2. Add rasagiline mesylate, maltodextrin, glucosyl-β-cyclodextrin, maltitol, titanium dioxide, and grape essence into the above water slurry, and stir evenly.

[0077] 3. Stand still for defoaming, and apply the film under the condition that the thickness of the film is 0.4mm and the drying temperature is 85°C. The speed of coating and film forming is 50cm / min.

[0078] 4. Accordin...

Embodiment 3

[0080] The prescription of embodiment 3 is as shown in table 3.

[0081] table 3

[0082] Name of raw material Mass % Rasagiline mesylate 8 Polyvinyl alcohol PVA 30 corn starch 30 Maltodextrin 20 Aspartan 5 Titanium dioxide 4 Sweet Orange Flavor 3 total 100

[0083] Preparation Process:

[0084] 1. Prepare the water slurry of the film-forming material: 30g of PVA and 30g of cornstarch are dissolved in water to prepare a water slurry with a mass concentration of about 16%.

[0085] 2. Add rasagiline mesylate, maltodextrin, aspartame, titanium dioxide, and sweet orange essence into the above water slurry, and stir evenly.

[0086] 3. Stand still for defoaming, and apply the film under the condition that the thickness of the film is 0.4mm and the drying temperature is 85°C. The speed of coating and film forming is 50cm / min.

[0087] 4. According to the specification of 0.5mg / tablet, it is cut and packaged.

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Abstract

The invention discloses rasagiline or a medicinal salt sublingual film agent thereof as well as a preparation method and application of the rasagiline or the medicinal salt sublingual film agent. The sublingual film agent comprises the following prescription components: 0.5-15% of rasagiline or a pharmaceutical salt thereof, 30-85% of a polymer film-forming material, 5-40% of dextrin and 0-30% of other auxiliary materials (not 0), and the dextrin is one or more of maltodextrin, hydroxypropyl-beta-cyclodextrin, glucosyl-beta-cyclodextrin and sulfobutyl-beta-cyclodextrin; the percentage is the mass percentage of each component relative to the total components of the prescription of the sublingual film agent. The sublingual membrane disclosed by the invention can be adhered to an administration part and quickly dissolved without water, and a patient does not need to swallow, so that the sublingual membrane is good in compliance; through oral mucosa absorption, the first-pass effect of the liver is avoided, and the bioavailability is high; the stability is good, and the impurity content is still low after long-term storage; the pharmaceutical composition has a good dissolution characteristic, is rapid and complete in drug dissolution, is rapidly absorbed by sublingual mucosa and enters blood circulation, and takes effect rapidly.

Description

technical field [0001] The invention relates to a sublingual film of rasagiline or a medicinal salt thereof, a preparation method and application thereof. Background technique [0002] Parkinson's disease (PD), as the second largest neurodegenerative disease, mostly occurs in people over 40 years old, and 2-3% of people over 65 years old are afflicted by this disease. Symptoms are different for each Parkinson's patient, but the most common symptoms are movement disturbances and stiffness of skeletal muscles, tremors, slowness of movement, poor balance and gait disturbance. In addition, it is often accompanied by depression, sleep disturbance, dizziness, dementia, speech impairment, respiratory system disease and dysphagia, and the symptoms will increase year by year, and even cause death. [0003] Currently, the drugs for treating Parkinson's disease mainly include levodopa, DA receptor agonists, MAO-B inhibitors, COMT inhibitors, and anticholinergic agents. The most commo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/70A61K47/36A61K47/38A61K47/32A61K31/135A61P25/28A61P25/16
CPCA61K9/006A61K47/36A61K47/38A61K47/32A61K31/135A61P25/28A61P25/16A61K47/40
Inventor 陈芳丁祎馨王兵李德祥杨柳榴傅麟勇周敏丁云晖
Owner SHANGHAI ZHONGXI PHARMA
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