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Novel diclofenac injection and preparation method thereof

A technology of diclofenac and diclofenac sodium, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., which can solve problems such as difficulty in ensuring effective gelation, difficulty in rapid drug absorption, and inability to detect drugs , achieve the effect of shortening the gelation time, excellent sustained release effect and good animal compliance

Active Publication Date: 2021-03-19
ZHENGZHOU BARY ANIMAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are deficiencies: 1) The gelation temperature is high, and it is difficult to ensure effective gelation when the external environment is cold and the body surface temperature is low; 2) The gelation time is as long as 18 seconds to 24 seconds, and it cannot be quickly achieved at the injection site. Some drugs will inevitably be absorbed quickly, and the longer gelation time indicates insufficient gelation strength; 3) Diclofenac exists in the system in the form of easily soluble sodium salt, and the absorption is faster; its pharmacokinetic data also show that although blood The peak concentration of the drug is lower than that of conventional preparations, but the drug cannot be detected in the blood after 48 hours of administration

Method used

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  • Novel diclofenac injection and preparation method thereof
  • Novel diclofenac injection and preparation method thereof
  • Novel diclofenac injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The prescription is as follows:

[0033]

[0034] Preparation:

[0035] Step 1: take each component according to the above-mentioned prescription quantity;

[0036] Step 2: Take the prescribed amount of benzyl alcohol, sodium alginate, polyethylene glycol, poloxamer 188 and diclofenac sodium, add them into water accounting for about 80% of the prescribed amount, and stir until completely dissolved to obtain a mixed solution;

[0037] Step 3: Take the prescription amount of diclofenac, poloxamer 407, and hydroxypropyl methylcellulose, mix evenly, add to the mixture in step 2, stir until a lump-free, uniformly dispersed medicinal solution is obtained, add water to volume , that is.

[0038] The in vitro performance evaluation of Diclofenac Sodium Injection was carried out, including the determination of properties, needle passability, gelation temperature, gelation time, thermal reversibility, and release rate. The in vitro release profile is as figure 1 shown. Th...

Embodiment 2

[0045] The prescription is as follows:

[0046]

[0047] Preparation:

[0048] Step 1: take each component according to the above-mentioned prescription quantity;

[0049] Step 2: Add the prescribed amount of ethyl p-hydroxybenzoate, sodium alginate, polyethylene glycol, poloxamer 188 and diclofenac sodium into water accounting for about 80% of the prescribed amount, and stir until completely dissolved to obtain a mixed solution;

[0050] Step 3: Take the prescribed amount of diclofenac, poloxamer 407, and povidone K30, mix evenly, add to (2), stir until a lump-free, uniformly dispersed medicinal solution is obtained, add water to volume, and the product is ready.

[0051] The in vitro performance evaluation was carried out, including the determination of properties, penetrability, gelation temperature, gelation time, thermal reversibility, and release rate. The in vitro performance evaluation method is the same as in the examples. The in vitro release profile is as fig...

Embodiment 3

[0053] The prescription is as follows:

[0054]

[0055] Preparation:

[0056] Step 1: take each component according to the above-mentioned prescription quantity;

[0057] Step 2: Take the prescribed amount of benzoic acid, sodium alginate, polyethylene glycol, poloxamer 188 and diclofenac sodium, add them into water accounting for about 80% of the prescribed amount, and stir until completely dissolved to obtain a mixed solution;

[0058] Step 3: Take the prescribed amount of diclofenac, poloxamer 407, and sodium carboxymethylcellulose, mix evenly, add to the mixed solution in step 2, stir until a lump-free and evenly dispersed medicinal solution is obtained, add water to volume, Instantly.

[0059] The in vitro performance evaluation was carried out, including the determination of properties, penetrability, gelation temperature, gelation time, thermal reversibility, and release rate. The in vitro performance evaluation method is the same as that in Example 1. The in vi...

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Abstract

The invention belongs to the technical field of pharmaceutical preparations for animals, and discloses a novel diclofenac injection and a preparation method thereof. The diclofenac injection comprisesdiclofenac existing in a dispersed form, diclofenac sodium dissolved in a system, a temperature-sensitive in-situ gel matrix, polyethylene glycol, sodium alginate, a polymer retardant and water for injection, wherein the temperature-sensitive in-situ gel matrix consists of poloxamer 407 and poloxamer 188. The diclofenac injection specifically comprises the following components in percentage by mass of 2-18 percent of the diclofenac, 0-8 percent of the diclofenac sodium, 10-25 percent of the poloxamer 407, 0.1-16 percent of the poloxamer 188, 0.1-7 percent of polyethylene glycol, 0.02-5 percent of sodium alginate, 0.01-5 percent of the polymer retardant, 0.001-2 percent of a bacteriostatic agent and the balance of the water for injection. According to the diclofenac injection disclosed bythe invention, the gelling temperature is 31-35 DEG C, the gelling time is within 15 seconds, the diclofenac injection exists in a liquid state at room temperature, and a gel storage can be quickly formed at an injection part during intramuscular injection or subcutaneous injection administration.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations for animals, and relates to a novel diclofenac injection and a preparation method thereof. Background technique [0002] Diclofenac is a non-steroidal antipyretic analgesic anti-inflammatory drug belonging to the fenamic acid class. It is insoluble in water and its sodium salt is commonly used. Diclofenac sodium is a white to off-white crystalline powder, soluble in water and ethanol, insoluble in chloroform. [0003] Diclofenac can effectively relieve symptoms of fever, pain and inflammation, and has been widely used to control infection or non-infectious inflammation and pain. The mechanism of action is to inhibit the activity of cyclooxygenase, thereby blocking the conversion of arachidonic acid to prostaglandins; at the same time, it can also promote the combination of arachidonic acid and triglyceride, reduce the concentration of free arachidonic acid in cells, and indire...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K47/10A61K47/36A61K31/196A61P29/00
CPCA61K9/08A61K9/0019A61K47/10A61K47/36A61K31/196A61P29/00A61K2300/00
Inventor 余祖功周衡崔小七申金燕张艳丽丁佳丽李春艳
Owner ZHENGZHOU BARY ANIMAL PHARMA
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