Scholarlink

<p>Gastrointestinal and genitourinary infections caused by mixed bacterial and protozoal pathogens remain a significant therapeutic challenge, particularly in paediatric populations where palatability and dosage form suitability are critical. The present study aimed to formulate, optimize, and evaluate a taste-masked dry suspension of Secnidazole (750 mg/5 mL) and Ofloxacin (150 mg/5 mL) using drug–polymer complexation and statistical optimization to achieve a stable, palatable, and patient-compliant oral antimicrobial formulation. Taste masking was achieved by complexing Secnidazole with Amberlite IRP-69 ion-exchange resin (1:2 ratio) and Ofloxacin with β-Cyclodextrin (1:1 ratio). A three-factor, three-level Box–Behnken Design (17 runs) was employed using Design-Expert® software to optimize xanthan gum, aspartame, and pineapple flavour concentrations. Five critical quality attributes pH, viscosity, sedimentation volume ratio, redispersibility, and drug release were evaluated as dependent responses. Stability studies were conducted per ICH Q1A(R2) guidelines. Both DPCs demonstrated effective taste masking with drug release below 1% in simulated salivary conditions (pH 6.8). In vivo bitterness evaluation confirmed scores ≤ 0.5 for all volunteers. The Box–Behnken models showed excellent predictability (R² = 0.9268–0.9838). DS-13 was identified as the optimized formulation based on desirability value of 1.000, exhibiting pH 7.00, viscosity 275 cP, sedimentation volume ratio 89%, redispersibility 97%, and drug release 94% within 45 min. Stability studies confirmed negligible physicochemical changes under long-term (25 °C/60% RH) conditions and acceptable variations under accelerated (40 °C/75% RH) conditions over three months. The optimized formulation DS-13 demonstrated superior physicochemical stability, effective taste masking, and rapid drug release, confirming its suitability as a patient-compliant oral antimicrobial dry suspension. The clinical significance of this formulation lies in its potential to improve therapeutic adherence in paediatric and geriatric populations managing mixed infections. Future in vivo pharmacokinetic and clinical palatability studies are warranted to support its translational development.</p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Box–Behnken Design-Assisted Formulation Engineering and Multivariate Optimization of a Taste-Masked Secnidazole–Ofloxacin Dry Suspension System

  • 期刊论文

  • 发表日期：

    2026年6月25日

查看全文
  • Shubham N. Kanawade,
  • Santosh B. Dighe,
  • Ravindra B. Laware,
  • Salim G. Patel,
  • Vishwas B. Patare,
  • Rahul R. Kunkulol

摘要

Gastrointestinal and genitourinary infections caused by mixed bacterial and protozoal pathogens remain a significant therapeutic challenge, particularly in paediatric populations where palatability and dosage form suitability are critical. The present study aimed to formulate, optimize, and evaluate a taste-masked dry suspension of Secnidazole (750 mg/5 mL) and Ofloxacin (150 mg/5 mL) using drug–polymer complexation and statistical optimization to achieve a stable, palatable, and patient-compliant oral antimicrobial formulation. Taste masking was achieved by complexing Secnidazole with Amberlite IRP-69 ion-exchange resin (1:2 ratio) and Ofloxacin with β-Cyclodextrin (1:1 ratio). A three-factor, three-level Box–Behnken Design (17 runs) was employed using Design-Expert® software to optimize xanthan gum, aspartame, and pineapple flavour concentrations. Five critical quality attributes pH, viscosity, sedimentation volume ratio, redispersibility, and drug release were evaluated as dependent responses. Stability studies were conducted per ICH Q1A(R2) guidelines. Both DPCs demonstrated effective taste masking with drug release below 1% in simulated salivary conditions (pH 6.8). In vivo bitterness evaluation confirmed scores ≤ 0.5 for all volunteers. The Box–Behnken models showed excellent predictability (R² = 0.9268–0.9838). DS-13 was identified as the optimized formulation based on desirability value of 1.000, exhibiting pH 7.00, viscosity 275 cP, sedimentation volume ratio 89%, redispersibility 97%, and drug release 94% within 45 min. Stability studies confirmed negligible physicochemical changes under long-term (25 °C/60% RH) conditions and acceptable variations under accelerated (40 °C/75% RH) conditions over three months. The optimized formulation DS-13 demonstrated superior physicochemical stability, effective taste masking, and rapid drug release, confirming its suitability as a patient-compliant oral antimicrobial dry suspension. The clinical significance of this formulation lies in its potential to improve therapeutic adherence in paediatric and geriatric populations managing mixed infections. Future in vivo pharmacokinetic and clinical palatability studies are warranted to support its translational development.