DEVELOPMENT, PHARMACEUTICAL EVALUATION, AND ASSESSMENT OF THE BACTERICIDAL ACTIVITY OF THE KC-250 TABLET FORMULATION AGAINST CLINICALLY SIGNIFICANT MICROORGANISMS

Received: 28 July 2026

Accepted: 31 July 2026

Published online: 21 August 2026

UDC: 615.453.64; 615.281

DOI: 10.53511/pharmkaz.2026.4.19

 

DEVELOPMENT, PHARMACEUTICAL EVALUATION, AND ASSESSMENT OF THE BACTERICIDAL ACTIVITY OF THE KC-250 TABLET FORMULATION AGAINST CLINICALLY SIGNIFICANT MICROORGANISMS

 

Shepilov D.A.^1,*, Taganov Zh.I.¹, Jumagaziyeva A.B.¹, Kenesheva S.T.¹, Jumabayeva S.M.¹, Zhanturiyev B.M.², Bukeyeva T.A.¹, Turganbay S.^3,4, Seisembekova A.B.¹

¹JSC “Scientific center for anti-infectious drugs”, Almaty, 050060, Kazakhstan

²Biological Testing Laboratory of the Testing Center (Almaty Territorial Branch), National Center for Expertise of Drugs and Medical Devices (NCED), Almaty, 050000, Kazakhstan

³Faculty of Natural Sciences, Kazakh National Women’s Teacher Training University, Almaty, 050000, Kazakhstan

⁴Kazakh-British Technical University, School of Petroleum Engineering, “One Belt, One Road” Research Center, Almaty, 050000, Kazakhstan

*Corresponding author: shepilov2002@gmail.com

 

Introduction: Conversion of iodine-containing complexes into solid dosage forms requires adequate tablet strength while preserving disintegration, release, and antimicrobial activity. This study aimed to develop a directly compressed KC-250 tablet formulation, evaluate its pharmaceutical quality, and determine its bactericidal activity against clinically significant bacteria.

Methods: Tablets containing 60 mg of KC-250 at a target mass of 500 mg were prepared using MicroceLac® 100, povidone K30, and magnesium stearate. Compression forces of 3.24 and 6.96 kN were compared by friability and disintegration testing. The selected formulation was evaluated for pharmacopoeial quality attributes. Bactericidal activity against eight reference, resistant, and clinical bacterial strains was determined in triplicate by broth serial dilution followed by agar subculture.

Results: Increasing compression force from 3.24 to 6.96 kN reduced friability from 0.81% to 0.21%, while disintegration increased from 1.62 to 4.62 min. Tablets produced at 6.96 kN had friability of 0.20%, a disintegration time of 4 min 54 s, a KC-250 content of 63.05 mg/tablet, and dissolution of 102.95% within 45 min. All evaluated attributes complied with the predefined acceptance criteria. Minimum bactericidal concentrations were 60 mg/mL for the tested Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa strains and 30 mg/mL for Enterococcus faecalis and Enterococcus faecium.

Discussion: Compression at 6.96 kN provided the most appropriate balance between mechanical resistance and rapid disintegration without restricting KC-250 release. The retained bactericidal activity indicates that tablet formulation did not eliminate the antimicrobial function of KC-250 and supports further development of the selected MicroceLac® 100–povidone K30 matrix.

Keywords: pharmaceutical formulation; solid dosage forms; tablets; antimicrobial agents; active pharmaceutical substances; iodine-containing compounds

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