Combined medicine used for treating pain, and preparations and preparation method thereof

A drug and preparation technology, applied in the direction of medical preparations containing active ingredients, drug combinations, pharmaceutical formulas, etc.

Active Publication Date: 2016-02-10
GUIZHOU YIBAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there are many drugs for treating pain, but due to problems such as adverse reactions and addiction, there are many defects and deficiencies in clinical application, and they have not been well developed. Good to meet the clinical needs; the present invention aims at the clinical pharmacological performance of cobotide and atropine, adopts a large number of tests to screen the prescription, and explores a fast onset, strong and long-lasting analgesic effect, avoiding or reducing addiction, Combination drugs and preparations with adverse reactions such as dependence

Method used

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  • Combined medicine used for treating pain, and preparations and preparation method thereof
  • Combined medicine used for treating pain, and preparations and preparation method thereof
  • Combined medicine used for treating pain, and preparations and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example

[0032] Experiment 1 Analgesic study of combined drugs

[0033] 1.1 Normal mouse hot plate experiment:

[0034] Put healthy mice (20±2g) with basically the same physical signs on a metal plate heated to 56±1°C, thermally stimulate the feet of the mice to produce pain and licking reactions. The latency of hind paw licking reaction in mice was used as the pain response index, which was the pain threshold. Mice with hind paw licking latency 30s and jumping were excluded. Before administration, the pain threshold of each mouse was measured three times and the average value was taken as its basic pain threshold.

[0035] Administration method:

[0036] Experimental group 1-4: mice were given intraperitoneal injection of 0.5 μg atropine, tail vein injection of 0.15 μg naloxone, tail vein injection of 0.01 μg tropicamide (M4 muscarinic receptor antagonist), tail vein injection of 0.1 μg Methyllycaconitine (MLA, α7 nicotinic receptor antagonist), the administration volume is 0.1m...

Embodiment 1

[0083] Example 1 Preparation of injection microemulsion containing cobotide and atropine (injection microemulsion A1)

[0084] Dissolve 40 mg of active ingredient cobotide and 20 mg of atropine in 300 ml of water for injection, add 6 g of poloxamer, and stir evenly to obtain an aqueous phase solution; heat 600 ml of soybean oil for injection at 100-110°C, add 5 g of poloxamer Magnesium monostearate, stir until the oil is clear and transparent, keep it warm at 105°C for 30 minutes, place it at room temperature to cool to obtain an oil phase solution; then pour the prepared water phase solution into the prepared oil phase solution, and make up the oil for injection to 1000ml, stir (2000 rpm) for 30 minutes, after homogenization, water-in-oil oil emulsion is obtained, which is divided into ampoules, sterilized, and injection microemulsion is obtained, each 2.5ml, containing the effective amount of cobotide 100μg, atropine 50μg.

Embodiment 2

[0085] Example 2 Preparation of injection microemulsion containing cobotide and atropine (injection microemulsion A2)

[0086]Dissolve 20 mg of kobotide and 8 mg of atropine in 280 ml of water for injection, add 2 g of Span-60, and stir well to obtain an aqueous phase solution; take 600 ml of soybean oil for injection and heat it at 100-110 ° C, add 2 g of Span-60 Magnesium monostearate, stir until the oil is clear and transparent, keep it warm at 105°C for 30 minutes, place it at room temperature to cool to obtain an oil phase solution; then pour the prepared water phase solution into the prepared oil phase solution, and make up the oil for injection to 1000ml, stir (2000 rpm) for 30 minutes, after homogenization, water-in-oil oil emulsion is obtained, which is divided into ampoules, sterilized, and injection microemulsion is obtained, each 2.5ml, containing the effective amount of cobotide 50μg, atropine 20μg.

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Abstract

The invention provides a combined medicine used for treating pain, and preparations and a preparation method thereof. The combined medicine is prepared from active ingredients cobratoxin and atropine, and pharmaceutic adjuvants; excellent synergistic effects are achieved; and effect is treating pain is excellent. The invention also discloses a controlled-release injection microemulsion used for treating pain. According to the controlled-release injection microemulsion, oil for injection is taken as a menstruum, medicine active ingredients are uniformly dispersed in the oil menstruum via emulsion process so as to obtain a water-in-oil emulsion, slow and stable release of the controlled-release injection microemulsion is realized, pain treatment effect is better, and toxic and side effect is avoided. A preparation of the controlled-release injection microemulsion is simple; cost is low; and the preparation method is suitable for industrialized production.

Description

Technical field: [0001] The invention belongs to the technical field of medicines, and relates to a combined drug for treating pain, in particular to a combined drug made of medicinal active ingredients cobotide and atropine and a preparation thereof. Background technique: [0002] Pain is an unpleasant feeling and emotional experience that occurs when the body is damaged. It is a clinical manifestation of a group of complex pathological and physiological changes. Pain can be local or a reflection of systemic diseases. The above diseases with "pain" as the main symptom are collectively referred to as "pain". At present, opioid analgesics and non-steroidal anti-inflammatory drugs are classic clinical analgesics, and have a long history of being used in pain treatment. However, there are also many defects and deficiencies in its clinical application, and the adverse reactions are also daunting. For example, some strong opioid analgesics that are clinically used for severe ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/17A61K9/107A61P29/00A61P35/00A61P25/02A61P25/00A61K31/46
Inventor 窦啟玲苏凯
Owner GUIZHOU YIBAI PHARMA CO LTD
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