Compound Levodopa Microcapsule Floating Tablets

A technology of levodopa microcapsules and floating tablets, which is applied in the field of medicine, can solve the problems of low bioavailability of ordinary tablets, complicated drug regimens, and many times of administration, etc., so as to prolong the residence time in the microcapsules and improve bioavailability The effect of high degree and flexible clinical application

Inactive Publication Date: 2017-06-23
XINJIANG MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The tablet has a very short residence time in the stomach and proximal small intestine, and the absorption time is limited, and once it passes through the absorption window, active absorption cannot occur effectively, resulting in low bioavailability of ordinary tablets
That is, the current compound levodopa benserazide ordinary tablets have the following disadvantages: 1. The number of administrations is high, the regimen is complicated, and it is difficult for patients to adhere to the medication; 2. The gastric residence time is short and the bioavailability is not ideal

Method used

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  • Compound Levodopa Microcapsule Floating Tablets
  • Compound Levodopa Microcapsule Floating Tablets
  • Compound Levodopa Microcapsule Floating Tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: The following methods are adopted to prepare compound levodopa microcapsule floating tablets:

[0026] The preparation of microcapsules includes the following steps:

[0027] 1) Levodopa is passed through a 400-mesh sieve for use.

[0028] 2) Weigh:

[0029] Levodopa-3g;

[0030] Ethyl cellulose with a viscosity of 10mPa·s——1.8g;

[0031] Ethyl cellulose with a viscosity of 20 mPa·s-7.2 g.

[0032] Ethyl cellulose of different viscosities was dissolved in 112.5 mL of methylene chloride, and the concentration of the capsule material after dissolution was 8%. After the ethyl cellulose is completely dissolved, add levodopa, stir at 400r / min for 30min in a 10℃ water bath, and add the resulting suspension to 1125mL aqueous solution containing 0.01~0.08g sodium lauryl sulfate at room temperature 400 / min. Min stirring for 1 hour, filtered under reduced pressure to obtain the microcapsule intermediate. The intermediate was washed with diluted hydrochloric acid at a ratio of 1...

Embodiment 2

[0048] Embodiment 2: The difference from embodiment 1 is:

[0049] Weigh in step A:

[0050] Levodopa-45.6g;

[0051] Ethyl cellulose with a viscosity of 10mPa·s——1.2g;

[0052] Ethyl cellulose with a viscosity of 20 mPa·s-1.2 g.

[0053] And ethyl cellulose of different viscosities was dissolved in 225 mL of methylene chloride, and the concentration of the capsule material after dissolution was 9%. In the end, 48 g of levodopa microcapsules were obtained.

[0054] Weigh in step B:

[0055] Benserazide hydrochloride-6.64g;

[0056] Vitamin C-1.36g.

[0057] Polyvinylpyrrolidone K30——3.6g;

[0058] Ethyl cellulose with a viscosity of 10 mPa·s-0.4 g.

[0059] Finally, 12 g of benserazide hydrochloride solid dispersion was obtained.

[0060] Weigh in step C:

[0061] Stearic acid-30g;

[0062] Acrylic resin IV-6.67g;

[0063] Hydroxypropyl methylcellulose K4M-3.33g.

[0064] Finally, 40g of auxiliary materials are obtained.

[0065] The levodopa microcapsules, benserazide hydrochloride solid dispersi...

Embodiment 3

[0066] Embodiment 3: The difference from embodiment 1 is:

[0067] Weigh in step A:

[0068] Levodopa-8g;

[0069] Ethyl cellulose with a viscosity of 10mPa·s——2g;

[0070] Ethyl cellulose with a viscosity of 20mPa·s-6g.

[0071] And ethyl cellulose of different viscosities was dissolved in 225 mL of methylene chloride, and the concentration of the capsule material after dissolution was 9%. In the end, a total of 16 g of levodopa microcapsules were obtained.

[0072] Weigh in step B:

[0073] Benserazide hydrochloride-2.14g;

[0074] Vitamin C-1.36g.

[0075] Polyvinylpyrrolidone K30——1.11g;

[0076] Ethyl cellulose with a viscosity of 10 mPa·s-0.22 g.

[0077] Finally, 4 g of benserazide hydrochloride solid dispersion was obtained.

[0078] Weigh in step C:

[0079] Stearic acid-20g;

[0080] Acrylic resin IV-40g;

[0081] Hydroxypropyl methylcellulose K4M-20g.

[0082] Finally, 80g of auxiliary materials are obtained.

[0083] The levodopa microcapsules, benserazide hydrochloride solid dispersio...

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Abstract

The invention discloses a compound levodopa microcapsule floating tablet, which comprises levodopa microcapsules, benserazide hydrochloride solid dispersion and pharmacologically acceptable auxiliary materials; and tablet hardness of the compound levodopa microcapsule floating tablet It is 4~6Kg / mm2. After optimization, the levodopa microcapsules include a capsule core and a capsule material, wherein the capsule core is composed of levodopa; the capsule material is composed of ethyl cellulose with a viscosity of 10 mPa s and ethyl cellulose with a viscosity of 20 mPa s . The invention has the advantages of reducing the times of use of the medicine and improving the drug compliance of patients; the clinical application of the preparation is more flexible; the medicine slowly passes through its specific absorption window to improve the bioavailability of the medicine.

Description

Technical field [0001] The invention relates to the technical field of medicine, in particular to a compound levodopa microcapsule floating tablet. Background technique [0002] As my country gradually enters an aging society, the incidence of Parkinson's disease is on the rise. Anti-Parkinson drugs can be divided into levodopa plus decarboxylase inhibitors (Roche's Medopa, Merck's Sinin), amantadine, MAO-B inhibitors (Sgining), dopamine receptor agonists (associated Liangxing, Tesuda), anticholinergic drugs (ankespa, antan), COMT inhibitor (tocapone). The American Neurological Association evaluated various anti-Parkinson's disease drugs, and the results showed that: dopamine agonists can control various symptoms of Parkinson's disease, but the effect is not as good as levodopa and the price is higher. MAO-B inhibitor (selegiline) may have certain therapeutic and protective effects, but its neurotrophic effect needs to be further confirmed. Compound levodopa preparations (Medo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/198A61K9/20A61K47/38A61P25/16A61K31/165
Inventor 滕亮马桂芝李文英
Owner XINJIANG MEDICAL UNIV
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