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Dezocine in-situ gel composition and application thereof

A composition and technology of dezocine are applied in the field of pharmaceutical preparations to achieve the effects of excellent biocompatibility and maintaining analgesic effect

Active Publication Date: 2021-11-23
YANGTZE RIVER PHARM GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Whether the drug can form a gel dosage form with expected physical and chemical properties during application, and whether the formed gel can achieve good pharmacokinetics and pharmacokinetic properties in vivo, and whether it has biocompatibility and safety after administration, etc. A lot of research and experimental verification, there is no research related to the gel preparation of dezocine

Method used

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  • Dezocine in-situ gel composition and application thereof
  • Dezocine in-situ gel composition and application thereof
  • Dezocine in-situ gel composition and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0046] Embodiment 1 Dezocine Solubility Experiment

[0047] The approximate solubility of dezocine was investigated with reference to the approximate solubility test method in the second volume of the "Chinese Pharmacopoeia" 2015 edition, and the results are shown in Table 1-1.

[0048] Table 1-1 Approximate solubility of dezocine

[0049] solvent Solubility of DX (mg / ml) NMP ＞400 DMSO ＞400 DMA ＞400 PEG400 ＞40

Embodiment 2

[0050] Embodiment 2 Polymer carrier material, solvent system research experiment

[0051] The blank preparation of dezocine was prepared, the carrier material and solvent system were studied, and the solubility of the carrier material in the solvent and the gelling properties of the blank preparation were investigated. For specific experimental results, refer to the following table 2-1 (corresponding figure 1 , 2 ), Table 2-2 (corresponding image 3 ), Table 2-3 (corresponding Figure 4 ).

[0052] Table 2-1 Effect of PLGA and solvent-gel properties on experiments

[0053]

[0054] Table 2-2 Effect of PLGA and solvent-gel properties on experiments

[0055]

[0056] Table 2-3 Effect of PLGA and solvent-gel properties on experiments

[0057]

[0058]

[0059] According to the results of the above table 2-1, it can be known that the four types of PLGA investigated can be dissolved in NMP, DMSO, and DMA, and PEG400 can swell PLGA, but cannot fully dissolve, which...

Embodiment 3

[0059] According to the results of the above table 2-1, it can be known that the four types of PLGA investigated can be dissolved in NMP, DMSO, and DMA, and PEG400 can swell PLGA, but cannot fully dissolve, which may be related to the low solubility and high viscosity of PLGA in PEG400 . However, PEG400 can be used as an adjusting solvent in the in situ gel system. On the one hand, it can adjust the solubility and release of the drug, and on the other hand, it can reduce the amount of organic solvent used. For details, see the experiment below. According to the results of the above table 2-2, it can be seen that the three PLGAs investigated can be dissolved in the solvents NMP, DMSO, and DMA, and have gelation; but as the molecular weight of PLGA increases, the viscosity of the solution also increases; The three kinds of PLGA investigated can be dissolved in twice the amount of mixed solvent NMP:PEG 400 (1:1), and have gelation effect to form colloids; but the solution is too ...

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Abstract

The invention discloses a dezocine in-situ gel composition and a preparation thereof, the composition comprises the following components: dezocine, a biodegradable carrier and a non-aqueous solvent, and the dezocine in-situ gel composition has proper viscosity, can be used for injection, and is gelatinized at a medication site to form a semi-solid drug reservoir. The composition and the preparation disclosed by the invention not only can continuously deliver drugs and is beneficial to maintaining an analgesic effect, but also have excellent biocompatibility and safety.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a dezocine in-situ gel composition and its preparation, preparation method and application. Background technique [0002] Dezocine is a mixed opioid receptor agonist-antagonist with a structure similar to pentazocine. It was developed by Wyeth-Ayerst Laboratories in the United States in the 1970s and was approved by the FDA in 1989. Dalgan is marketed by Astrazeneca for the treatment of postoperative pain. Since it was launched in China in 2009, it has been widely used in general anesthesia induction, postoperative analgesia and preemptive analgesia, and for the treatment of visceral pain and cancer pain. Its chemical name is: (-)-[5R-(5α,11α,13S*)]-13-amino-5,6,7,8,9,10,11,12-octahydro-5-methyl- 5,11-methylenebenzocyclodecen-3-ol, the structural formula is as follows: [0003] [0004] In situ gel, also known as instant gel, can undergo a phase transi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/06A61K47/34A61K31/135A61P29/00
CPCA61K9/06A61K9/0019A61K47/34A61K31/135A61P29/00
Inventor 胡涛陈航平徐浩宇蔡伟王亚龙董志奎李峰董达文刘景龙李浩冬
Owner YANGTZE RIVER PHARM GRP CO LTD
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