Andrographolide ground suspending liquid, preparation method thereof, and application of pharmaceutical preparation

A technology of andrographolide and pharmaceutical preparations, which is applied in the direction of drug combination, antibacterial drugs, pharmaceutical formulations, etc., can solve the problems of low oral bioavailability, achieve superior stability, fast dissolution speed, convenient operation and time-saving effect

Inactive Publication Date: 2012-08-01
SHENYANG PHARMA UNIVERSITY
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

Andrographolide compound is a terpenoid compound composed of a five-membered lactone ring and its basic structure of diterpene bicyclic mother core. It is almost insoluble in water and aqueous media, and i

Method used

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  • Andrographolide ground suspending liquid, preparation method thereof, and application of pharmaceutical preparation
  • Andrographolide ground suspending liquid, preparation method thereof, and application of pharmaceutical preparation
  • Andrographolide ground suspending liquid, preparation method thereof, and application of pharmaceutical preparation

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preparation example Construction

[0031] (1) Preparation method of andrographolide grinding suspension:

[0032] Weigh andrographolide raw material drug, respectively prepare a certain concentration (w / v) of hydrophilic excipient aqueous solution, put andrographolide and the above-mentioned hydrophilic excipient aqueous solution of different concentrations in the grinding cup, the grinding frequency is 35Hz high speed Grinding for 1-5 hours in a running basket mill, the model of the mill is the SMA-0.75 Basket Mill SMA-0.75 for laboratory use produced by Shanghai Sower Electromechanical Equipment Co., Ltd.

[0033] (2) Preparation method of andrographolide immediate-release pellets:

[0034]Select one or a mixture of sucrose, microcrystalline cellulose, and lactose, and use 5% hydroxypropyl methylcellulose as a binder to prepare blank pellet cores. The particle diameter range of blank pellet cores is 16-24, 24- One of 32 or 32-40 mesh, the particle size range is preferably 32-40 mesh blank pellet core. The ...

Embodiment 1

[0040] (1) Andrographolide Grinding Suspension is prepared from the following raw materials:

[0041] Andrographolide 120g, polyvinylpyrrolidone (PVP-K30) hydrophilic carrier aqueous solution concentrations are 5% (w / v), 10% (w / v), 15% (w / v), 500ml distilled water;

[0042] Mix the said amount of andrographolide raw material drug with the above-mentioned PVP-K30 hydrophilic auxiliary material aqueous solution of different concentrations, place it in a basket grinding cup, and mix evenly. The grinding frequency was set to 35Hz, and the grinding time was 3h to obtain the corresponding andrographolide grinding suspension;

[0043] (2) Preparation of Andrographis paniculata immediate-release pellets:

[0044] The andrographolide suspensions prepared by the above 5%, 10% and 15% PVP-K30 aqueous solutions were layered on the surface of 32-40 mesh blank pellet cores, and the drug loading was controlled at 10-15%. Fluidized bed granulation parameters: blast flow rate is 45...

Embodiment 2

[0050] (1) Andrographolide Grinding Suspension is prepared from the following raw materials:

[0051] Andrographolide 120g, polyethylene glycol hydrophilic carrier aqueous solution concentrations are respectively 10% (w / v), 15% (w / v), 20% (w / v), 500ml distilled water;

[0052] Mix the above-mentioned amount of andrographolide bulk drug with the above-mentioned polyethylene glycol hydrophilic carrier aqueous solution of different concentrations, place in a basket grinding cup, and mix evenly. The grinding frequency was set to 35Hz, and the grinding time was 3h to obtain the corresponding andrographolide grinding suspension;

[0053] (2) Preparation of Andrographis paniculata immediate-release pellets:

[0054] The above-mentioned 10%, 15% and 20% polyethylene glycol hydrophilic carrier aqueous solution prepared andrographolide suspensions were layered on the surface of 32-40 mesh blank cores, and the drug loading was controlled at 10-15%. Fluidized bed granulation p...

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Abstract

The invention relates to andrographolide ground suspending liquid, a preparation method thereof, and the application of pharmaceutical preparation, which belongs to the field of pharmaceutical preparation. The preparation method comprises the steps of adding andrographolide into hydrophilic accessory solution with certain concentration, and grinding the andrographolide in a basket grinder to prepare suspending liquid with particle sizes smaller than 3000 nm. Liquid layers of pharmaceutical suspending liquid are laminated onto blank pellet cores with certain particle size range, to prepare andrographolide immediate-release pellets. After grinding, by reducing pharmaceutical particle sizes, increasing particle surface areas and improving the wettability of pharmaceutical particles, the dissolution in vitro of the drug is improved, and hydrophilic carriers are adopted to effectively prevent the aggregation of pharmaceutical particles so as to improve the stability of the pharmaceutical preparation. The preparation method is simple and easy for industrialized production, and the dissolving-out speed of the prepared andrographolide immediate-release pellets is high, so that the bioavailability is obviously improved.

Description

technical field [0001] The invention relates to andrographolide grinding suspension, a preparation method thereof and application of pharmaceutical preparations, belonging to the field of pharmaceutical preparations. Background technique [0002] Andrographolide is a diterpene lactone compound extracted from Andrographis paniculata, a plant of the Acanthaceae family. It is one of the main active ingredients of Andrographis paniculata, a traditional Chinese medicine. Clinically, it is widely used in the treatment of upper respiratory tract infection, bacillary dysentery and other diseases. As a traditional Chinese medicine antibacterial drug, it has definite curative effect, less adverse reactions and side effects, and less tolerance. Andrographolide compound is a terpenoid compound composed of a five-membered lactone ring and its basic structure of diterpene bicyclic mother core. It is almost insoluble in water and aqueous media, and its oral bioavailability is low. Yang Ji...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/365A61K47/42A61K47/38A61K47/36A61K47/34A61K47/32A61P31/04A61P11/00A61P1/12
CPCY02A50/30
Inventor 唐星何海冰张宇
Owner SHENYANG PHARMA UNIVERSITY
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