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Low-water-activity amoxicillin trihydrate pharmaceutical composition and preparation method thereof

A technology of amoxicillin trihydrate and amoxicillin water, which is applied in the antibacterial field and can solve the problems of cumbersome operation and long preparation work

Active Publication Date: 2020-07-07
JIANGSU SIMCERE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the preliminary preparation work of this technical solution is relatively long, and the raw materials need to be further processed, and the operation is relatively cumbersome.

Method used

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  • Low-water-activity amoxicillin trihydrate pharmaceutical composition and preparation method thereof
  • Low-water-activity amoxicillin trihydrate pharmaceutical composition and preparation method thereof
  • Low-water-activity amoxicillin trihydrate pharmaceutical composition and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Prescription composition:

[0039] Element Feeding amount Amoxicillin Trihydrate 150g (calculated as amoxicillin)

[0040] Preparation Process:

[0041] 称取处方量的阿莫西林,使用马西姆丁J-40气流粉碎机(0.5g-100g / h),加料速度设定为 50%,进料压力设定为0.7MPa,粉碎压力设定为0.6MPa,将物料粉碎1次,收集粉碎后阿莫 西林。

[0042] 粉碎前水活度为0.174aw,粒径d(0.9)μm=49.365

[0043] 粉碎后水活度为0.064aw,粒径d(0.9)μm=25.657

Embodiment 2

[0045] Prescription composition:

[0046] Element Feeding amount Amoxicillin Trihydrate 150g (calculated as amoxicillin)

[0047] Preparation Process:

[0048] 称取处方量的阿莫西林,使用马西姆丁J-40气流粉碎机(0.5g-100g / h)加料速度设定为 50%,进料压力设定为0.7MPa,粉碎压力设定为0.3MPa,将物料粉碎2次,收集粉碎后阿莫 西林。

[0049] 粉碎前水活度为0.174aw,粒径d(0.9)μm=49.365

[0050] 粉碎后水活度为0.062aw,粒径d(0.9)μm=19.759

Embodiment 3

[0052] Prescription composition:

[0053] Element Feeding amount Amoxicillin Trihydrate 350g (calculated as amoxicillin)

[0054] Preparation Process:

[0055] 称取处方量的阿莫西林,使用马西姆丁J-40气流粉碎机(0.5g-100g / h)加料速度设定为 50%,进料压力设定为0.2MPa,粉碎压力设定为0.3MPa,将物料粉碎3次,收集粉碎后阿莫 西林。

[0056] 粉碎前水活度为0.174aw,粒径d(0.9)μm=48.380

[0057] 粉碎后水活度为0.082aw,粒径d(0.9)μm=24.779

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Abstract

The invention discloses a method for controlling the water activity of amoxicillin, which comprises the step of controlling the water activity of amoxicillin trihydrate in a jet milling mode to obtainthe amoxicillin trihydrate with the water activity value lower than 0.1 aw. The invention also discloses a low-water-activity amoxicillin trihydrate pharmaceutical composition and a preparation method thereof; the pharmaceutical composition comprises amoxicillin trihydrate and pharmaceutically acceptable auxiliary materials, and the amoxicillin trihydrate is crushed in a jet milling mode before use to control the water activity value to be lower than 0.1 aw. Compared with the prior art, the stability of the low-water-activity amoxicillin trihydrate obtained through airflow crushing treatmentis obviously improved, and the jet milling method is short in consumed time, simple in process and low in cost.

Description

technical field [0001] 本发明属于抗菌技术领域,具体涉及一种低水活度阿莫西林三水合物药物组合物及其制备 方法。 Background technique [0002] 阿莫西林,其化学名称为:(2S,5R,6R)-3,3-二甲基-6-[(R)-(-)-2-氨基-2-(4-羟基苯基)乙酰氨 基]-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-甲酸三水合物。分子式为:C 16 h 19 N 3 o 5 S·3H 2 O. [0003] Its chemical structural formula is: [0004] [0005] 阿莫西林为青霉素类抗生素,对肺炎链球菌、溶血性链球菌等链球菌属、不产青霉素酶葡 萄球菌、粪肠球菌等需氧革兰阳性球菌、大肠埃希菌、气易变形杆菌、沙门菌属、流感嗜血杆 菌、淋病奈瑟菌等需氧革兰阴性菌的不产β内酰胺酶菌株及幽门螺杆菌具有良好的抗菌活性。 体外抗菌实验表明,阿莫西林与氨苄青霉素相比,在体外抗菌作用及抗菌谱方面,两者十分类 似,阿莫西林对细菌细胞壁的穿透能力较强,与细胞壁作用时,能够使细胞壁的合成受阻,所 以阿莫西林的杀菌作用更强,更迅速,特别是对肠球菌及沙门氏菌具有更强的作用。阿莫西林 的β-酰胺环是作为其基本结构而发挥抗菌活性作用,患者口服后其内酰胺基即刻水解成肽键, 迅速同菌中的转肽酶相结合,抑制细菌黏肽合成酶的活性,切断了菌体依靠转肽酶合成糖肽用 来建造细胞壁的唯一途径,造成细菌细胞壁损坏或破坏,促使细菌细胞迅速成为球形体破裂溶 解。哺乳动物的细胞没有细胞壁,所以阿莫西林对于人体的毒性比较小,但还是可以产生恶心、 呕吐、腹泻等不良反应。 [0006] 阿莫西林在临床医学中得到了极为广泛的应用,在多个领域发挥着积极的作用。在具体的 治疗中,基本可以全部治愈慢性支气管炎、皮肤和软组织感染以及由肺炎球菌、溶血性款球菌、 青霉素酶金黄葡萄球菌等细菌引起的鼻窦炎、支气管炎、扁桃体炎、咽炎、中耳炎和肺炎等。 同时,阿莫西林与庆大霉素合用对心脏内膜炎也有一定的功效,还可以治疗伤寒杆菌引起的伤 寒,并且可以用于因骨髓抑制而不能使用氯霉素的患者相关炎症的治疗。但是目前很多阿莫西 林制剂的日剂量较频繁,患者的适从性较差,因此亟需制备一个能够维持长效生物利用...

Claims

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Application Information

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IPC IPC(8): C07D499/68C07D499/18A61K31/43A61K31/424A61P31/04A61K9/20A61K47/38
CPCC07D499/68C07D499/18A61K31/43A61K31/424A61P31/04A61K9/2054A61K2300/00Y02A50/30
Inventor 张庆珍黄琦任晋生
Owner JIANGSU SIMCERE PHARMA