Method for preparing isosorbide mononitrate sustained-release capsules

A technology of isosorbide dinitrate and sustained-release capsules, applied in the directions of capsule delivery, microcapsules, pharmaceutical formulations, etc., can solve the problems of complex production process, inability to effectively prevent the migration of isosorbide mononitrate, poor drug stability, etc., and achieve stable Good properties, good drug safety, and the effect of avoiding easy agglomeration

Active Publication Date: 2016-11-23
广东隆信制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of this, the present invention provides a preparation method of isosorbide mononitrate slow-release capsules, which is used to solve the problem that in the prior art, the slow-re

Method used

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  • Method for preparing isosorbide mononitrate sustained-release capsules
  • Method for preparing isosorbide mononitrate sustained-release capsules
  • Method for preparing isosorbide mononitrate sustained-release capsules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] This example is a specific example of preparing Isosorbide Mononitrate Sustained Release Capsule Product 1.

[0048] Please refer to Table 1 for the formulation composition of Product 1.

[0049] Table 1: The prescription composition of product 1 (4000 capsules)

[0050]

[0051] The specific preparation method of product 1 is as follows.

[0052] Step 1. Fully mix the raw material drug of isosorbide mononitrate and microcrystalline cellulose according to the prescription ratio, and then carry out jet milling treatment to obtain a micronized mixed powder (D90: 10-20 microns), and weigh the above-mentioned micronized powder (wherein the mass ratio of isosorbide mononitrate to microcrystalline cellulose is 2:1) 300.0g is used for powder application; weigh 40.0g HPMC E30 and add 1000g of purified water at room temperature, stir and dissolve until clarification, to obtain Adhesive solution; Take by weighing 400.0g of lactose ball core and place it in the multifunctiona...

Embodiment 2

[0056] This example is a specific example of preparing Isosorbide Mononitrate Sustained Release Capsule Product 2.

[0057] Please refer to Table 2 for the formulation composition of Product 2.

[0058] Table 2: The prescription composition of product 2 (4000 capsules)

[0059]

[0060]

[0061] The specific preparation method of product 2 is as follows.

[0062] Step 1. Fully mix the raw material drug of isosorbide mononitrate and the prescribed amount of microcrystalline cellulose in proportion, then carry out jet milling treatment to obtain a micronized (D90: 10-20 microns) mixed powder, and weigh the above-mentioned micronized powder Powder (the mass ratio of isosorbide mononitrate and microcrystalline cellulose is 10:4) 280.0g, used for powder application; weigh 30.0g of HPMC E30, add 1000g of purified water at room temperature, stir and dissolve until clear , to get the binder solution; take 320.0g of sucrose ball core and place it in the multifunctional pellet c...

Embodiment 3

[0066] This example is a specific example of preparing Isosorbide Mononitrate Sustained Release Capsule Product 3.

[0067] Please refer to Table 3 for the formulation composition of Product 3.

[0068] Table 3: The prescription composition of product 3 (12000 capsules)

[0069]

[0070] The specific preparation method of product 3 is as follows.

[0071] Step 1. Fully mix the raw material drug of isosorbide mononitrate and the prescribed amount of microcrystalline cellulose in proportion, then carry out jet milling treatment to obtain a micronized (D90: 10-20 microns) mixed powder, and weigh the above-mentioned micronized powder Powder (the mass ratio of isosorbide mononitrate and microcrystalline cellulose is 10:3) 780.0g, used for powder application; weigh 60.0g HPMC E30, add 3000g of purified water at room temperature, stir and dissolve until clear, Promptly obtain adhesive solution; Take 800.0g of sucrose ball core and place it in the multi-functional pellet coating ...

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Abstract

The invention belongs to the field of medicine industry and particularly relates to a method for preparing isosorbide mononitrate sustained-release capsules. The method for preparing the isosorbide mononitrate sustained-release capsules, provided by the invention, comprises the steps: (1) preparing isosorbide mononitrate quick-release micropellets; (2) preparing isosorbide mononitrate sustained-release micropellets; (3) carrying out mixing: mixing the isosorbide mononitrate quick-release micropellets with the isosorbide mononitrate sustained-release micropellets, and carrying out encapsulation, thereby obtaining the product. Shown by experimental determination, the product prepared by the technical scheme provided by the invention is good in stability, the problem, i.e., crystallization of isosorbide mononitrate is solved, and the problems of the existing processes that principal drugs and adjuvants are prone to caking and heated softening, the removal of residual solvent is not facilitated, and the micropellets are adhered are also avoided. Shown by in-vitro dissolution and in-vivo biological equivalent experimental investigations, the isosorbide mononitrate sustained-release capsules provided by the invention have bioequivalence compared with original triturates.

Description

technical field [0001] The invention belongs to the field of pharmaceutical industry, in particular to a preparation method of isosorbide mononitrate sustained-release capsules. Background technique [0002] Isosorbide mononitrate, also known as 5-isosorbide mononitrate, is a long-acting nitrate ester antianginal drug. It is the main active metabolite of isosorbide dinitrate in the body. It is absorbed quickly after oral administration, and its absolute bioavailability can reach 100%. Individual differences are small, and the toxic and side effects are smaller than nitroglycerin and isosorbide dinitrate. The biological half-life is 4 to 5 hours. It can be used for long-term treatment of coronary heart disease, prevention of angina pectoris, and treatment of persistent angina pectoris after myocardial infarction. It is currently the most effective treatment for angina pectoris. One of the good medicines. At present, the clinical dosage forms of isosorbide mononitrate include...

Claims

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Application Information

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IPC IPC(8): A61K9/62A61K9/58A61K31/34A61P9/10
CPCA61K9/1635A61K9/1652A61K9/1682A61K9/5026A61K9/5042A61K9/5084A61K9/5089A61K31/34
Inventor 贾放许雅文黎秉富陈华兆刘海芹
Owner 广东隆信制药有限公司
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