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Preparation method of dexamethasone implant for kidney

A technology of dexamethasone and dexamethasone acetate, which is applied to the composition of renal dexamethasone implants, the preparation of renal dexamethasone implants, the size, the drug release characteristics and the preparation process, and the shape field, which can solve the problem of thermal stability. It can solve the problems of poor performance, more degradation, and damage to the end face of the implant, so as to achieve the effect of high intensity of action, low blood drug concentration, and high kidney concentration.

Active Publication Date: 2016-05-11
ANHUI ZHONGREN TECH +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0023] 1. The prepared implant has poor thermal stability and is difficult to store and transport
Because PLGA is a material with poor thermal stability, and PLGA (50:50) is easier to degrade when heated, after secondary melt extrusion, it will degrade more and have poor thermal stability
[0024] 2. The end face of the prepared implant is damaged, which affects the success rate of drug release and puncture implant
When the filament is cut by a knife, the end surface is damaged, which affects both the drug release uniformity of the implant and the axial strength of the implant
When the implant is percutaneously punctured into the lesion with an implant needle, it is necessary to overcome the resistance of the tissue at the implant site. If the damaged end face cannot bear the thrust from the push rod, the implant will be broken Blocking the needle, resulting in drug administration failure

Method used

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  • Preparation method of dexamethasone implant for kidney
  • Preparation method of dexamethasone implant for kidney
  • Preparation method of dexamethasone implant for kidney

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0091] Example 1 Implant preparation

[0092] Component parts by weight

[0093] Dexamethasone 10

[0094] Polylactic-glycolic acid (75:25; molecular weight 9,000)87

[0095] Polyethylene glycol (molecular weight 6,000)3

[0096] The above-mentioned materials were crushed separately, passed through a 900-mesh sieve, weighed according to the prescription amount, 5 g in total, mixed evenly, and made into filaments with a micro-extruder. Crush filaments, sieve, make microspheres with a particle size of 30 microns or more, put them into a stainless steel mold with a pore size of 0.9 mm, put them in a ZR-Ⅱ medicine press (developed by Anhui Zhongren Technology Co., Ltd.), and place them under a pressure of 480 MPa Molding: demoulding to obtain dexamethasone implant A, and heat preservation at 56° C. for 15 minutes to obtain dexamethasone implant B, which is the dexamethasone implant of the present invention.

[0097] During the preparation process, the micro-extrusion machine...

Embodiment 2

[0098] Example 2 In vivo release test

[0099] Take 120 Wista rats and divide them into two groups: Ⅰ and Ⅱ, 60 rats in each group, and set 10 sampling time points, 6 rats in each point. Group Ⅰ was implanted with dexamethasone implant A, and group Ⅱ was implanted with dexamethasone implant A. For dexamethasone implant B, 1 piece of the corresponding implant after weighing was implanted into the inner muscle of the right hind leg of each rat, and the remaining implants were taken from 6 rats in each group at different time points after implantation , the remaining drug amount of dexamethasone in the residual implant was measured by high performance liquid chromatography, and the release rate was calculated according to the implanted drug amount and the remaining drug amount. Table 1 and figure 1 .

[0100]

[0101] Table 1 with figure 1 Show: the dexamethasone implant A (A) that embodiment 1 prepares, the difference of the release degree of dexamethasone implant B (B...

Embodiment 3

[0105] Embodiment 3 pharmacodynamics test

[0106] Replication of the nephrotic syndrome model: male SD rats weighing 180-220 g were injected with 4 mg / kg of doxorubicin hydrochloride through the tail vein on the 1st and 8th day after the start of the experiment (doxorubicin was dissolved in normal saline at 2 g / L) Medium, namely 2mL / kg), they were put into metabolic cages and fed and drank freely.

[0107]Grouping of animals: 10 male SD rats from the same batch without modeling were taken as the normal control group A. On day 14, 30 male SD rats successfully modeled by the above-mentioned tail vein injection of Adriamycin hydrochloride were taken and randomly divided into B, C, and D Three groups, 10 rats in each group, group B is the renal disease model group, group C is the renal disease model dexamethasone implant A treatment group, and group D is the renal disease model dexamethasone implant B treatment group.

[0108] Treatment: No treatment in groups A and B, weighin...

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Abstract

The present invention relates to a preparation method, uses and a use method of a dexamethasone implant for kidney, wherein the dexamethasone implant comprises dexamethasone or dexamethasone acetate, a degradable polymer material, and a water soluble auxiliary material. The preparation method comprises: crushing various materials, mixing, carrying out micro-spheroidization, carrying out mold pressing molding, and heating for a certain time at a proper temperature to prepare the cylindrical implant with a diameter of 0.2-0.9 mm and a length of 0.8-4 mm. According to the present invention, the implant has characteristics of smooth surface and uniform drug release in vivo, wherein the time for releasing 90% of the drug is 1 month to 1 year; and the implant can be implanted into the renal sac through a drug implanting needle so as to treat nephrotic syndrome, nephritis and other chronic kidney diseases.

Description

technical field [0001] The invention relates to a method for preparing a dexamethasone implant for kidney, in particular to the composition, shape, size, drug release characteristics and preparation process of a dexamethasone implant for kidney. [0002] The invention also relates to the application and application method of the dexamethasone implant. Background technique [0003] Dexamethasone is an adrenocortical hormone drug with anti-inflammatory, anti-allergic, anti-rheumatic, and immunosuppressive effects. It is mainly used for the treatment of severe bacterial infections and severe allergic diseases, various thrombocytopenic purpura, and neutropenia. disease, severe skin disease, immune rejection of organ transplantation, tumor treatment and inflammation sensitive to glucocorticoids, etc. [0004] Clinically, dexamethasone has three chemical forms used as drugs: dexamethasone, dexamethasone acetate and dexamethasone sodium phosphate, which are easily absorbed from th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/573A61K47/34A61P13/12
Inventor 王世亮尹情胜陈殿良谢传奇俞敏任翠丽周丽春邵娟周春霞
Owner ANHUI ZHONGREN TECH
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