A kind of preparation method of dexamethasone implant for kidney
A technology of dexamethasone and dexamethasone acetate, which is applied in the composition, drug release characteristics and preparation process, size, preparation and shape of dexamethasone implants for kidneys, and can solve thermal stability problems Poor drug resistance, high degradation, and damage to the end surface of the implant, etc., to achieve the effect of high action strength, low blood drug concentration, and high kidney concentration
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Embodiment 1
[0090] Example 1 Implant preparation
[0091] Component Parts by weight
[0092] Dexamethasone 10
[0093] Polylactic-glycolic acid (75:25; molecular weight 9,000) 87
[0094] Polyethylene glycol (molecular weight 6,000) 3
[0095] 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.
[0096] During the preparation process, the micro-extrusion machine...
Embodiment 2
[0097] Example 2 In vivo release test
[0098] 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 .
[0099]
[0100] 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) in...
Embodiment 3
[0104] Embodiment 3 Pharmacodynamics test
[0105] Replication of the nephrotic syndrome model: Male SD rats with a body weight of 180-220 g were injected with 4 mg / kg of doxorubicin hydrochloride through the tail vein on the 1st day and the 8th day after the experiment started (2 g / L for doxorubicin) Dissolved in normal saline (ie 2 mL / kg), put them in metabolic cages for feeding, free to eat and drink.
[0106]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.
[0107] Treatment: No treatment was given to groups A ...
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