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Polymer, nanosphere, lubricant and preparation methods thereof

A technology of nano-microspheres and polymers, applied in pharmaceutical formulations, microcapsules, drug combinations, etc., can solve the problems of loss of lubrication function, shear thinning, etc., and achieve good lubrication and maintain the effect of lubrication

Active Publication Date: 2019-01-04
TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, HA has a certain lubricating effect only when the viscosity is high. If under the shear action of the sliding articular cartilage surface, the viscosity of HA is roughly the same as that of water, showing shear thinning, thus losing the lubricating function.

Method used

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  • Polymer, nanosphere, lubricant and preparation methods thereof
  • Polymer, nanosphere, lubricant and preparation methods thereof
  • Polymer, nanosphere, lubricant and preparation methods thereof

Examples

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preparation example Construction

[0055] Embodiments of the present invention also provide a method for preparing the polymer, comprising the following steps:

[0056] S1, providing hyaluronic acid and a first compound, the general formula of the first compound is NH 2 -R1-SH, making the amino group of the first compound react with the carboxyl group of the hyaluronic acid to undergo an amidation reaction to obtain a polymer including the third repeating unit; or

[0057] Hyaluronic acid, a second compound having the general formula NH 2 -R1-S-S-R5, making the amino group of the second compound and the carboxyl group of the hyaluronic acid undergo an amidation reaction to form a polymer including the fourth repeating unit represented by general formula (IV), and make the The fourth repeating unit undergoes a reduction reaction with the reducing agent to form a polymer comprising the third repeating unit:

[0058]

[0059] as well as

[0060] S2, providing a phospholipid molecule, the phospholipid molecul...

Embodiment 1

[0091] The preparation of embodiment 1 polymer

[0092] (1) Hyaluronic acid 0.2g, initiator EDC (1-(3-dimethylaminopropyl)-3-ethylcarbodiimide) 0.15g, catalyst HOBT (1-hydroxybenzotriazole) 0.01 g and 0.33 g of cystamine dihydrochloride were added to deionized water, the pH was adjusted to 6.8, and stirred at room temperature for 14 h.

[0093] (2) Dithiothreitol (DTT) 0.23 g was added to the resulting solution after dialysis, stirred overnight, adjusted to acidic pH, precipitated by ethanol and dried in a vacuum oven.

[0094] (3) The product of step (2) was dissolved in deionized water, after adding hydrochloric acid to make it acidic, 0.5 ml of tetrabutylammonium hydroxide was added dropwise, stirred at room temperature, dialyzed and freeze-dried.

[0095] (4) Dissolve 0.2 g of the product of step (3) in an organic solution, add 10 μl of methanesulfonic acid (MSA), 7 mg of carbonyldiimidazole (CDI) and 0.08 g of hexadecylamine, react at 42 ° C for 16 h, and dissolve the so...

Embodiment 2

[0097] The preparation of embodiment 2 nanometer microspheres

[0098] The polymer and the drug prepared in Example 1 were dissolved in an organic solution, added dropwise to deionized water, stirred for 24 hours, dialyzed and then stored dry to obtain self-assembled nanospheres.

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Abstract

The invention discloses a polymer. The polymer comprises a first repeating unit which has a structural unit as shown in the general formula (I), wherein the formula is defined in the description. Theinvention further discloses a nanosphere. The nanosphere comprises a shell which comprises the polymer. The invention further discloses a lubricant. The lubricant includes the nanophere and an aqueoussolution, and the nanosphere is dispersed into the aqueous solution. The embodiment of the invention further discloses a preparation method of the polymer.

Description

technical field [0001] The invention relates to the field of biopharmaceuticals, in particular to a polymer, a nanometer microsphere, a lubricating liquid and a preparation method thereof. Background technique [0002] Hyaluronic acid (HA) is the main component in joint synovial fluid and articular cartilage, and is an essential physiological component. As a linear polysaccharide, HA is biocompatible and biodegradable, and has a good high water adsorption and retention capacity. Clinically, HA is commonly used as a mucus supplement for intra-articular injection to relieve the symptoms of osteoarthritis. However, HA has a certain lubricating effect only when the viscosity is high. If under the shear action of the sliding articular cartilage surface, the viscosity of HA is roughly the same as that of water, showing shear thinning, thus losing the lubricating function. Contents of the invention [0003] Based on this, it is necessary to provide a polymer with good lubricati...

Claims

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Application Information

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IPC IPC(8): C08B37/08A61L31/04A61L31/14A61K9/50A61K47/36A61K47/24A61P19/02
CPCA61K9/5015A61K9/5036A61L31/042A61L31/14A61L31/148A61L2300/602A61L2400/12A61P19/02C08B37/0072C08L5/08
Inventor 张洪玉郑意为
Owner TSINGHUA UNIV
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