Diclofenac sodium hydrogel microballoon with pH sensitivity, preparation method and application thereof

A technology of diclofenac sodium and hydrogel microspheres, which is applied in the direction of non-central analgesics, bone diseases, antipyretics, etc., and can solve problems such as the listing of diclofenac sodium preparations

Inactive Publication Date: 2011-04-20
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no diclofenac sodium preparation that releases drugs according to the physiological and pathological characteristics of this type of disease.

Method used

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  • Diclofenac sodium hydrogel microballoon with pH sensitivity, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] 1. Preparation of diclofenac sodium hydrogel microspheres

[0021] (1) Preparation of various reagents

[0022] The four main raw materials used are shown in Table 1 below:

[0023] Table 1 Proportion of four main raw materials

[0024] Diclofenac Sodium (Ds)

Chitosan (Cs)

Sodium Alginate (SA)

CaCl 2

10g

50g

50g

75g

[0025] ① Preparation of sodium alginate solution

[0026] Dissolve 50g of sodium alginate in 5L of distilled water, stir well with a mixer, the concentration of sodium alginate is 1% (w / v);

[0027] ② Preparation of chitosan acetic acid solution

[0028] Dissolve 50g of N-succinyl chitosan in 5L of 0.05mol / L acetic acid solution, stir evenly with a mixer, and the concentration of N-succinyl chitosan is 1% (w / v);

[0029] ③ Preparation of CaCl 2 the solution

[0030] 75g CaCl 2 Dissolve in 5L distilled water, stir evenly, CaCl 2 The concentration is 1.5% (w / v).

[0031] (2) Drug solution preparation

...

Embodiment 2

[0038] 1. Preparation of diclofenac sodium hydrogel microspheres

[0039] (1) Preparation of various reagents

[0040] The four main raw materials used are shown in Table 2 below:

[0041] Table 2 Proportion table of four main raw materials

[0042] Diclofenac Sodium (Ds)

Chitosan (Cs)

Sodium Alginate (SA)

CaCl 2

15g

25g

25g

45g

[0043] ① Preparation of sodium alginate solution

[0044] Dissolve 25g of sodium alginate in 2.5L of distilled water, stir well with a mixer, the concentration of sodium alginate is 1% (w / v);

[0045] ② Preparation of chitosan acetic acid solution

[0046] Dissolve 25g of N-succinyl chitosan in 2.5L of 0.05mol / L acetic acid solution, stir well with a mixer, and the concentration of N-succinyl chitosan is 1% (w / v);

[0047] ③ Preparation of CaCl 2 the solution

[0048] 45g CaCl 2 Dissolve in 3L distilled water, stir evenly, CaCl 2 The concentration is 1.5% (w / v).

[0049] (2) Drug solution prepara...

Embodiment 3

[0056] 1. Preparation of diclofenac sodium hydrogel microspheres

[0057] (1) Preparation of various reagents

[0058] The four main raw materials used are shown in Table 3 below:

[0059] Table 3 Proportion table of four main raw materials

[0060] Diclofenac Sodium (Ds)

Chitosan (Cs)

Sodium Alginate (SA)

CaCl 2

18g

30g

42g

60g

[0061] ① Preparation of sodium alginate solution

[0062] Dissolve 35g of sodium alginate in 3.5L of distilled water, stir well with a mixer, the concentration of sodium alginate is 1% (w / v);

[0063] ② Preparation of chitosan acetic acid solution

[0064] Dissolve 30g of N-succinyl chitosan in 3L of 0.05mol / L acetic acid solution, stir well with a mixer, and the concentration of N-succinyl chitosan is 1% (w / v);

[0065] ③ Preparation of CaCl 2 the solution

[0066] 60g CaCl 2 Dissolve in 4L distilled water, stir evenly, CaCl 2 The concentration is 1.5% (w / v).

[0067] (2) Drug solution preparati...

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Abstract

The invention relates to a diclofenac sodium hydrogel microballoon with pH sensitivity, a preparation method and application thereof. In the invention, chitosan and sodium alginate are used as drug carriers to prepare a diclofenac sodium hydrogel microballoon slow release preparation; the mass ratio of a used diclofenac sodium drug to the chitosan to the sodium alginate is (1-3):(5-8):(5-8); and the chitosan is N-succinyl-chitosan. The microballoon preparation can durably develop the drug effect to ensure that diclofenac sodium can be regularly and quantitatively released for a long time; after the microballoon preparation is taken, the blood concentration is stable, the fluctuation is small, and the duration time is long; the microballoon preparation has pH sensitivity, thereby irritations and toxic hazards to the stomach mucous membrane, which are caused by directly and orally taking diclofenac sodium tablets, are reduced; and the microballoon preparation has good effects of cooling down and easing pains and is suitable for various rheumatisms, rheumatoid arthritis, lupus erythematosus, ankylosing spondylitis, various pains caused after operations, fevers caused by various reasons, and the like.

Description

technical field [0001] The invention relates to a diclofenac sodium hydrogel microsphere with pH sensitivity, a preparation method and an application. Background technique [0002] Diclofenac Sodium (Diclofenac Sodium, also known as Diclofenac Sodium, referred to as DS), is a new type of non-steroidal anti-inflammatory analgesic, has good antipyretic and analgesic effects, and its indications are various rheumatism, rheumatoid arthritis, Lupus erythematosus, ankylosing spondylitis, pain after various operations and fever caused by various reasons, etc. Since Giba-Geigy, a Swiss company, was launched for the first time in 1974, it has relieved countless patients from pain and suffering, and has become one of the top ten best-selling drugs in the world. In 1986, diclofenac sodium was industrialized in my country. Through continuous technological innovation, my country has gained certain advantages in terms of price, quality and production technology, and has become the main p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/196A61K47/36A61P19/02A61P19/04A61P29/00
Inventor 任天斌雷雪黄超刘秋明侠文娟
Owner TONGJI UNIV
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