A thermosensitive gel pharmaceutical preparation and preparation method thereof

A temperature-sensitive gel and pharmaceutical preparation technology, which is applied in the directions of drug combination, pharmaceutical formulation, aerosol delivery, etc., can solve the problem of not achieving the sustained release effect of the preparation, achieve good reference value and application significance, and improve medication compliance. Effect

Active Publication Date: 2016-12-21
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The technical problem to be solved by the present invention is to overcome the problem that the water-soluble drug in the water-soluble drug temperature-sensitive gel is easy to diffuse out through the water-soluble channel inside the gel, causing most of the drug to be released at the initial stage of the drug, and serious drug damage will occur for a period of time after the drug is taken. Burst release effect, not reaching the sustained release effect of preparations and other defects, but provides a temperature-sensitive gel pharmaceutical preparation that is particularly suitable for water-soluble drugs, reduces the burst release effect, and can slowly release drugs and its preparation method

Method used

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  • A thermosensitive gel pharmaceutical preparation and preparation method thereof
  • A thermosensitive gel pharmaceutical preparation and preparation method thereof
  • A thermosensitive gel pharmaceutical preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-2

[0083] Polymer A: hydrophilic PLGA-PEG-PLGA copolymer (polymer A, 1571-1500-1571, the molecular weight of the block is the number average molecular weight, the block molar ratio LA / GA=4, the molecular weight distribution coefficient is 1.15) ; Polymer B: appropriate amount of hydrophobic PLGA-PEG-PLAG copolymer (polymer B, 1255-1500-1255, the molecular weight of the block is the number average molecular weight, the block molar ratio LA / GA=4, the molecular weight distribution coefficient is 1.23 ).

[0084] Wherein, the synthesis process of polymers A and B refers to the synthesis methods in Examples 1 and 3 of the Chinese patent application with application number 200910049664.6.

[0085] Get polymer A and polymer B, add deionized water, dissolve under magnetic stirring, configure polymer, the weight ratio of polymer A / polymer B is 1 / 1, and the total polymer concentration is 25% (w / The aqueous solution of w) was passed through a 0.22 μm filter membrane for later use, and was...

Embodiment 3-4

[0090] Polymer A: hydrophilic PLGA-PEG-PLGA copolymer (polymer A, 1571-1500-1571, the molecular weight of the block is the number average molecular weight, the block molar ratio LA / GA=4, the molecular weight distribution coefficient is 1.15) ; Polymer B: appropriate amount of hydrophobic PLGA-PEG-PLAG copolymer (polymer B, 1255-1500-1255, the molecular weight of the block is the number average molecular weight, the block molar ratio LA / GA=4, the molecular weight distribution coefficient is 1.23 ).

[0091] Wherein, the synthesis process of polymers A and B refers to the synthesis methods in Examples 1 and 3 of the Chinese patent application with application number 200910049664.6.

[0092] Get polymer A and polymer B, add deionized water, dissolve under magnetic stirring, configure polymer, the weight ratio of polymer A / polymer B is respectively 1 / 1, and total polymer concentration is 25% (w / The aqueous solution of w) was passed through a 0.22 μm filter membrane for later use...

Embodiment 5-6

[0097] Polymer A: hydrophilic PLGA-PEG-PLGA copolymer (polymer A, 1571-1500-1571, the molecular weight of the block is the number average molecular weight, the block molar ratio LA / GA=4, the molecular weight distribution coefficient is 1.15) ; Polymer B: appropriate amount of hydrophobic PLGA-PEG-PLAG copolymer (polymer B, 1255-1500-1255, the molecular weight of the block is the number average molecular weight, the block molar ratio LA / GA=4, the molecular weight distribution coefficient is 1.23 ).

[0098] Wherein, the synthesis process of polymers A and B refers to the synthesis methods in Examples 1 and 3 of the Chinese patent application with application number 200910049664.6.

[0099] Get polymer A and polymer B, add deionized water, dissolve under magnetic stirring, configure polymer, the weight ratio of polymer A / polymer B is respectively 1 / 1, and total polymer concentration is 25% (w / The aqueous solution of w) was passed through a 0.22 μm filter membrane for later use...

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Abstract

The invention discloses a temperature-sensitive gel pharmaceutical preparation and a preparation method thereof. The raw material formula of the temperature-sensitive gel pharmaceutical preparation contains a drug, a temperature-sensitive gel composition, and an excipient C; the excipient C is one or more of metal salts, carbohydrates, and hydrophilic polymers for injection; The metal salt is a pharmaceutically acceptable metal salt that dissociates divalent metal cations in an aqueous solution; the drug is a substance A that exists in an anion form in an aqueous solution, and the substance A is a protein drug, a polypeptide One or more of class drugs and glycopeptide antibiotics. The preparation method comprises the following steps: according to the formula of raw materials, the drug is dissolved in the temperature-sensitive gel composition in the form of solution. The temperature-sensitive gel pharmaceutical preparation is especially suitable for water-soluble drugs, reduces the burst release effect, releases the drugs slowly, and achieves the purpose of sustained release.

Description

technical field [0001] The invention relates to a temperature-sensitive gel pharmaceutical preparation and a preparation method thereof. Background technique [0002] Exenatide (also known as exenatide or exendin-4) was first isolated from the saliva secretion of giant monster lizard (Heloderm suspectum), and it is a polypeptide containing 39 amino acids (Eng, J. et al., J.Biol.Chem ., 1990 (265): 20259-20262; or J.Biol.Chem., 1992 (267): 7402-7405), its amino acid sequence is similar to glucagon-like peptide-1 (GLP-1) There are about 53% identical components. Pharmacological studies have found that exenatide has a similar effect to GLP-1, that is, it can stimulate pancreatic β cells to secrete insulin. Exenatide can act on GLP-1 receptors on certain insulin-secreting cells in vitro, on interspersed acinar cells from the pancreas of guinea pigs, or on parietal cells from the stomach; it has also been reported that Exenatide The peptide stimulates somatostatin release and ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/17A61K9/06A61K47/34A61P3/10
Inventor 李坤陈庆华刘晓君包泳初潘峰韩蕾房超
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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