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Water soluble medicament sustained-release tablets and preparation method thereof

A technology of water-soluble drugs and sustained-release tablets, which is applied in pharmaceutical formulations, drug combinations, drug delivery, etc., can solve problems such as blockage, difficult release, and no sustained-release tablets, so as to reduce toxic and side effects, increase compliance, and treat good effect

Inactive Publication Date: 2010-09-15
XUZHOU PHOTOSYNTHETIC BIOLOGICAL NUTRIMENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In 2001, the U.S. FDA officially approved the drug for the treatment of AD, and it is now on the market in 25 countries. There are already sustained-release tablets, sustained-release capsules and other dosage forms, but the dosage forms listed in my country are only tablets, capsules and injections. No sustained-release tablets, sustained-release capsules and other dosage forms
Cap sustained-release capsules are already on the market in foreign countries. Since the water-soluble drug itself dissolves quickly, its release is difficult to be blocked. There is no sustained-release variety of Cap on the market in China.

Method used

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  • Water soluble medicament sustained-release tablets and preparation method thereof
  • Water soluble medicament sustained-release tablets and preparation method thereof
  • Water soluble medicament sustained-release tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1: Preparation of Galantamine Hydrobromide Sustained-release Tablets:

[0037] The formula is: each 1000 tablets is made of the following components:

[0038] Galantamine Hydrobromide 10.0g

[0039] Octadecanol 25.0g

[0040] Utechy L100-55 9.0g

[0041] Talc powder 10.0g

[0042] Lactose 8.0g

[0043] 60% ethanol 14ml

[0044] The above-mentioned galantamine hydrobromide refers to galantamine hydrobromide extracted from the plant Lycoris, which was purchased from Zhejiang Yixin Pharmaceutical Co., Ltd. Stearyl alcohol was purchased from Shanghai Sinopharm Group (imported repackaging); Utech L100-55 was purchased from Shanghai Texiang Pharmaceutical Technology Co., Ltd. (imported repackaging, Germany Rohm); talcum powder was purchased from Guangxi Long Bought from Sheng County Sanmen Talcum Powder Factory.

[0045] The preparation process is as follows:

[0046] (1) The raw materials and auxiliary materials are first passed through an 80-mesh sieve; ...

Embodiment 2

[0053] Embodiment 2: prepare captopril sustained-release tablet:

[0054] The formula is: each 1000 tablets is made of the following components:

[0055] Captopril 12.5g

[0056] Octadecanol 27.0g

[0057] Utech L100-55 10.5g

[0058] Talc powder 10.0g

[0059] Lactose 8.0g

[0060] 60% ethanol 15ml

[0061] The above-mentioned captopril was purchased from Wuhan Hezhong Biochemical Manufacturing Co., Ltd. Stearyl alcohol was purchased from Shanghai Sinopharm Group (imported repackaging); Utech L100-55 was purchased from Shanghai Texiang Pharmaceutical Technology Co., Ltd. (imported repackaging, Germany Rohm); talcum powder was purchased from Guangxi Long Bought from Sheng County Sanmen Talc Powder Factory.

[0062] The preparation process is as follows:

[0063] (1) The raw materials and auxiliary materials are first passed through an 80-mesh sieve;

[0064] (2) Pass 10.5g of Eutech L100-55, 27.0g of stearyl alcohol, 5.0g of talc and 8.0g of lactose through a 60-mesh ...

Embodiment 3

[0070] Embodiment 3: preparation metoprolol tartrate sustained-release tablet:

[0071] The formula is: each 1000 tablets is made of the following components:

[0072] Metoprolol Tartrate 100.0g

[0073] Octadecanol 80.0g

[0074] Utech L100-55 50.0g

[0075] Talc powder 20.0g

[0076] Lactose 10.0g

[0077] 3% carboxypropyl methylcellulose alcohol solution (80%, V / V) 32ml

[0078] The above-mentioned metoprolol tartrate was purchased from Wuhan Hezhong Biochemical Manufacturing Co., Ltd. Stearyl alcohol was purchased from Shanghai Sinopharm Group (imported repackaging); Utech L100-55 was purchased from Shanghai Texiang Pharmaceutical Technology Co., Ltd. (imported repackaging, Germany Rohm); talcum powder was purchased from Guangxi Long Bought from Sheng County Sanmen Talc Powder Factory.

[0079] The preparation process is as follows:

[0080] (1) The raw materials and auxiliary materials are first passed through an 80-mesh sieve;

[0081] (2) Pass 50.0g of Eutech L...

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Abstract

The invention discloses water soluble medicament sustained-release tablets, which comprise the following components in part by weight: water soluble medicament 1-30, octadecanol 5-70, Eudragite L 100-55 2-50, talcpowder 2-30 and lactose 2-30. The water soluble medicament may be galanthamine hydrobromide, captopril, metoprolol tartaric acid or pseudoephedrine hydrochloride. In the invention, the octadecanol serving as a hydrophobic auxiliary material and the Eudragite L 100-55 sreving as a water soluble polymer auxiliary are adopted, so the release speed of the medicament can be controlled properly. The Eudragite L 100-55 is insoluble in gastric juice, but dissolves in duodenal juice to make high-viscosity sticky liquid, and thus the release and diffusion speed of the medicament can be reduced. The talcpowder which is a hydrophilic matter insoluble in water plays a porogen role in the sustained-release tablets. In the invention, the release speed of the medicament is regulated by regulating the mixing ratio of the medicament to the auxiliary material. Thus, the release speed of an active medicament is controlled.

Description

technical field [0001] The invention relates to a water-soluble drug sustained-release tablet and a preparation method thereof. Background technique [0002] Alzheimer's disease, also known as Alzheimer's disease (AD), is a primary degenerative brain disease that occurs in old age and early old age, and refers to a persistent high-level neurological dysfunction, namely Impairments in memory, thinking, analysis and judgment, visuospatial recognition, emotion, etc., in the absence of disturbance of consciousness. The characteristic pathological changes are atrophy of the cerebral cortex, accompanied by β-amyloid deposition, neurofibrillary tangles, and a decrease in the number of large memory neurons. The course of the disease is long, about 3 to 20 years, and it is the "fourth killer" of the elderly's health after cardiovascular disease, cerebrovascular disease and cancer. In the United States, AD is the third most costly disease after heart disease and cancer. With the ac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K47/32A61K47/04A61K47/26A61K31/55A61K31/401A61K31/138A61K31/137A61P25/28
Inventor 屠锡德
Owner XUZHOU PHOTOSYNTHETIC BIOLOGICAL NUTRIMENT
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