Clonidine hydrochloride sustained-release micro-tablets as well as preparation method and application thereof

A clonidine hydrochloride, sustained-release technology, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problem that the treatment effect of eye diseases is not very satisfactory, and the drug release speed is not easy to obtain. control, systemic arterial pressure reduction and other issues, to achieve good practical application value, good controlled release effect, and the effect of improving compliance

Inactive Publication Date: 2020-12-08
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its long-term application is limited due to its influence on the central nervous system and the significant decrease in systemic arterial pressure.
[0004] In the treatment of glaucoma, eye drops are most commonly used in topical administration of the eye, but due to rapid clearance caused by blinking and tear drainage, the bioavailability is very low, so the amount entering the conjunctival blood vessels is very limited. With liquid administration, approximately 75% of the dose is drained almost immediately through the nasolacrimal duct, requiring more frequent dosing or higher doses to maintain therapeutic drug levels
Some macromolecule thickeners such as methyl

Method used

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  • Clonidine hydrochloride sustained-release micro-tablets as well as preparation method and application thereof
  • Clonidine hydrochloride sustained-release micro-tablets as well as preparation method and application thereof
  • Clonidine hydrochloride sustained-release micro-tablets as well as preparation method and application thereof

Examples

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[0033] In view of this, the present invention provides an ophthalmic clonidine hydrochloride sustained-release microtablet and its preparation method and application.

[0034] In one embodiment of the present invention, a kind of clonidine hydrochloride slow-release microtablet is provided, and by weight percentage, it is composed of:

[0035] Clonidine hydrochloride: 3-6%

[0036] Gel skeleton: 68-86%

[0037] Lubricant: 0.5~2%

[0038] Filling agent: 10-25%.

[0039] In a specific embodiment, the gel skeleton is selected from one or more of hypromellose, carbomer, ethyl cellulose, more preferably hypromellose and carbomer Further, the weight ratio of hypromellose and carbomer is: 65-80:3-6.

[0040] Hypromellose and carbomer are used as the hydrophilic gel skeleton, and the two cooperate with each other to play the role of slow-release medicine. After the inventor's experimental research, the amount of hypromellose and carbomer used in the embodiment of the present inven...

Embodiment 1

[0050] The prescription of clonidine hydrochloride sustained-release microtablets is:

[0051] Clonidine hydrochloride: 5%

[0052] Hypromellose RG4T: 75%

[0053] Carbomer 974P: 4%

[0054] Sodium stearyl fumarate: 1%

[0055] Mannitol: 15%

[0056] The above-mentioned raw materials were sterilized by γ-ray irradiation before use, and the following operations were all carried out in a sterile environment. The raw materials were mixed evenly with a mortar, pulverized, and pressed into small tablets with a diameter of 3 mm by using a direct compression method using a heterogeneous tablet press ((Korsch-EKO model, Berlin, Germany) with maximum pressure.

Embodiment 2

[0058] The prescription of clonidine hydrochloride sustained-release microtablets is:

[0059] Clonidine hydrochloride: 5%

[0060] Hypromellose RG4T: 65%

[0061] Carbomer 974P: 10%

[0062] Sodium stearyl fumarate: 1%

[0063] Mannitol: 17%.

[0064] The preparation method is the same as in Example 1.

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Abstract

The invention relates to the technical field of sustained-release drugs, in particular to clonidine hydrochloride sustained-release micro-tablets as well as a preparation method and application thereof. The clonidine hydrochloride sustained-release micro-tablets comprise the following components in percentage by weight of 3-6% of clonidine hydrochloride, 68-86% of a gel skeleton, 0.5-2% of a lubricant and 10-25% of a filler. The preparation method comprises the following steps of irradiating and sterilizing all the raw materials by gamma-rays before use, and performing the following operationsin a sterile environment: uniformly mixing and grinding all the raw materials by using a mortar, and performing pressing into small pieces with the diameter of 3mm through an anisotropic tabletting machine under the maximum pressure by a direct tabletting method. Compared with clonidine hydrochloride eye drops, the ophthalmic clonidine hydrochloride sustained-release micro-tablets disclosed by the invention have a good controlled-release effect, can prolong the residence time of drugs in eyes, reduce the administration times, improve the compliance of patients, improve the bioavailability ofthe drugs and reduce the toxic and side effects of a central nervous system, are simple in preparation process and have good practical application value.

Description

technical field [0001] The invention relates to the technical field of sustained-release medicines, in particular to a clonidine hydrochloride sustained-release microtablet and a preparation method and application thereof. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] Clonidine hydrochloride, whose chemical name is 2-[(2,6-dichloroaniline)-2imino]-imidazolidine hydrochloride, is an α-adrenoceptor agonist and is currently used as a second-line drug for hypertension In 2009, the FDA approved the clonidine hydrochloride sustained-release tablets developed by Addrenex Pharmaceuticals for the treatment of high blood pressure. In 2010, it was approved by the US FDA to add ind...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K31/4168A61K47/38A61K47/32A61P25/14A61P27/06
CPCA61K9/2027A61K9/2054A61K31/4168A61P25/14A61P27/06
Inventor 翟光喜王汝娟
Owner SHANDONG UNIV
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