Minocycline hydrochloride nano sustained-release gel as well as preparation method and application thereof

A technology of minocycline hydrochloride and sustained-release gel, which is applied in the direction of nanotechnology, nanotechnology, nanomedicine, etc., can solve the problem of low encapsulation efficiency of hydrophilic small molecule drugs, poor variability of size and shape, lesion site To achieve the effective concentration and other issues, to achieve the effects of strong drug loading capacity, enhanced distribution, and prolonged administration cycle

Pending Publication Date: 2021-12-17
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, the periodontal local sustained-release preparations that have been on the market are mainly the following: 1. Fiber type, the trade name is However, due to its non-biodegradable characteristics, it has been discontinued; 2. Film type, It is an absorbable film product, but its size and shape are poorly variable, easy to fall off after administration, and patient compliance is poor
3. Microsphere type, FDA approved minocycline microspheres in 2001 For the treatment of chronic periodontitis, because the powdery microspheres are difficult to stay in the periodontal disease for a long time, so its application is limited; 4. Gel/ointment type, doxycycline gel and minocycline hydrochloride ointment All of them have been approved by the FDA for the treatment

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  • Minocycline hydrochloride nano sustained-release gel as well as preparation method and application thereof
  • Minocycline hydrochloride nano sustained-release gel as well as preparation method and application thereof
  • Minocycline hydrochloride nano sustained-release gel as well as preparation method and application thereof

Examples

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Comparison scheme
Effect test

Embodiment 1

[0041] A preparation method of minocycline hydrochloride nano sustained release gel, according to the following steps:

[0042] 1) Preparation of minocycline hydrochloride double emulsion nanoparticles: 20 mg of minocycline hydrochloride was dissolved in 1 mL of distilled water, 8 mg of magnesium chloride and 15 mg of sodium sucrose octasulfate were dissolved in another 1 mL of distilled water to obtain two inner aqueous phases. Take 150mg of PLGA and dissolve it in 6mL of dichloromethane, and divide it equally into two oil phases. Drop the two inner water phases into the two oil phases respectively, prepare two W / O colostrums by ultrasonic probe, then mix the two colostrums and ultrasonic probe, and drop the obtained emulsion into 12mL Ultrasonic probe in the external water phase, the external water phase is 2% povidone solution, dichloromethane in the obtained W / O / W double emulsion is removed by vacuum distillation, and the emulsion is properly concentrated by dialysis, Tha...

Embodiment 2

[0045] A preparation method of minocycline hydrochloride nano sustained release gel, according to the following steps:

[0046] 1) Preparation of minocycline hydrochloride double-emulsion nanoparticles: 40 mg of minocycline hydrochloride was dissolved in 2 mL of distilled water, 18 mg of calcium chloride and 38 mg of dextran sulfate were dissolved in another 2 mL of distilled water to obtain two inner aqueous phases. Take 300mg of PCL and dissolve it in 5mL of dichloromethane, and divide it equally into two oil phases. Drop the two inner water phases into the two oil phases respectively, prepare two W / O colostrums by ultrasonic probe, then mix the two colostrums and ultrasonic probe, and drop the obtained emulsion into 25mL In the external water phase, the probe is ultrasonic, the external water phase is 0.5% sodium cholate solution, and the dichloromethane in the obtained W / O / W double emulsion is removed by vacuum distillation, and the minocycline hydrochloride double emulsio...

Embodiment 3

[0049] A preparation method of minocycline hydrochloride nano sustained release gel, according to the following steps:

[0050] 1) Preparation of minocycline hydrochloride double-emulsion nanoparticles: 80 mg of minocycline hydrochloride was dissolved in 4 mL of distilled water, 35 mg of calcium chloride and 100 mg of dextran sulfate were dissolved in another 4 mL of distilled water to obtain two inner aqueous phases . Dissolve 720mg of PLGA in 8mL of dichloromethane, and divide it into two oil phases. Drop the two parts of the inner water phase into the two parts of the oil phase respectively, prepare two W / O colostrums by ultrasonic probe, then mix the colostrum, ultrasonic probe, and drop the obtained emulsion into 40mL of external water In the phase, the probe is ultrasonicated, and the external water phase is 1% sodium cholate solution. The dichloromethane in the obtained W / O / W double emulsion is removed by vacuum distillation, and it is concentrated by lyophilization an...

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Abstract

The invention discloses minocycline hydrochloride nano sustained-release gel as well as a preparation method and application thereof, and belongs to the technical field of medicines. The problem of low encapsulation efficiency of small-molecule hydrophilic medicines is solved by introducing a form of a novel complex formed by chelating minocycline hydrochloride, metal ions and a compound with a plurality of sulfate, sulfonate or phosphate functional groups. Prepared minocycline hydrochloride multiple emulsion nanoparticles are smooth, round, high in encapsulation efficiency and strong in drug loading capacity. A prepared minocycline hydrochloride multiple emulsion nanoparticle is dispersed in a temperature-sensitive gel matrix to construct a double-layer delivery system which has certain biological adhesion, is good in periodontal retention and is convenient for administration. According to the minocycline hydrochloride nano sustained-release gel as well as the preparation method and application thereof, while the positioning advantage of the gel is exerted, burst release of a medicine can be remarkably reduced, the medicine administration period can be prolonged, possibility is created for further periodontal pocket local medicine administration treatment of periodontitis, the nanoparticles can penetrate through alveolar bone trabecula and bottom connective tissue, distribution of the medicine at a focus position is enhanced, and the antibacterial effect of the medicine is remarkably improved.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a minocycline hydrochloride nano sustained-release gel and a preparation method and application thereof. Background technique [0002] Periodontitis is a common chronic oral disease, clinically manifested as inflammation and bleeding of the gums, formation of periodontal pockets, loss of attachment, and destruction of alveolar bone resorption, which eventually leads to tooth loosening and loss, which is the main cause of tooth loss in adults. Among many pathogenic factors, bacterial infection is the main factor for inducing and maintaining inflammation. At the same time, due to the complex structure of periodontal pockets, it is difficult for mechanical scaling to effectively remove deep microorganisms and lead to recurrence of lesions. Therefore, basic mechanical scaling is supplemented with Local antibiotic treatment has become a trend in the treatment of periodon...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K31/65A61K47/52A61K47/54A61K47/61A61K47/34A61P1/02A61P29/00A61P31/02A61P31/04B82Y5/00B82Y40/00
CPCA61K9/06A61K9/0063A61K31/65A61K47/52A61K47/548A61K47/549A61K47/61A61K47/34A61P1/02A61P29/00A61P31/02A61P31/04B82Y5/00B82Y40/00
Inventor 张宇尹湉何海冰苟靖欣王艳娇唐星魏颖魏铭励
Owner SHENYANG PHARMA UNIVERSITY
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