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[林可霉素与超高度分散羟基磷灰石联合用药时的药代动力学]

[The pharmacokinetics of lincomycin when used as a component of a drug combination with ultrahighly dispersed hydroxyapatite].

作者信息

Zuev V P, Pankratov A S, Sergeev P V, Bolotova E N, Semeĭkin A V

出版信息

Stomatologiia (Mosk). 1998;77(6):19-22.

Abstract

A drug composition LINCOGAP is assessed, consisting of lincomycin hydrochloride (33%), ultrahighly dispersed hydroxyapatite (HA) (33%), gelatin (7%), and water (27%). Distribution of tritium-labeled lincomycin in organs and tissues of experimental animals was studied by the radiometric method after implantation of the composition into a standard rat mandibular defect. Lincomycin concentration surpassing by orders of magnitude the minimal inhibitory concentration for the main lincomycin-sensitive microorganisms persisted at the site of implantation of the composition for at least 7 days, while the concentration in internal organs and tissues was the minimum. Microbiological findings indicate active diffusion of lincomycin from the site of injection into the adjacent bone. Thus, LINCOGAP exerts an antibacterial effect in the pathological focus while its general toxic effect is low and, therefore, side effects are minimized. Combination of the antibiotic with ultrahighly dispersed HA helps regulate the process of bone repair, stimulating the proliferative and functional activity of osteoblasts. Hence, combined drug LINCOGAP is a promising agent for the treatment of inflammatory destructive diseases of osseous tissue.

摘要

对一种名为LINCOGAP的药物组合物进行了评估,其由盐酸林可霉素(33%)、超高度分散的羟基磷灰石(HA)(33%)、明胶(7%)和水(27%)组成。在将该组合物植入标准大鼠下颌骨缺损处后,采用放射性测量法研究了氚标记林可霉素在实验动物器官和组织中的分布情况。在组合物植入部位,林可霉素浓度比主要对林可霉素敏感的微生物的最低抑菌浓度高出几个数量级,且至少持续7天,而在内脏器官和组织中的浓度则最低。微生物学研究结果表明,林可霉素从注射部位向相邻骨骼有活跃的扩散。因此,LINCOGAP在病理病灶处发挥抗菌作用,同时其总体毒性作用较低,从而使副作用降至最低。抗生素与超高度分散的HA相结合有助于调节骨修复过程,刺激成骨细胞的增殖和功能活性。因此,复方药物LINCOGAP是治疗骨组织炎性破坏性疾病的一种有前景的药物。

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