Quality by Design Approach for Optimization of Microbial and pH-Triggered Colon-Targeted Tablet Formulation Using Carboxymethyl Tamarind Gum.

IF 1.6 4区 医学 Q4 BIOCHEMICAL RESEARCH METHODS
Jaymin Patel, Kaushika Patel, Shreeraj Shah
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Abstract

ABSTRACT The purpose of this study was to apply the quality by design (QbD) approach in the development of a microbial and pH-triggered colon-targeted budesonide tablet. A retrospective research strategy was used to select various polysaccharide-based natural gums such as tamarind gum, gellan gum, karaya gum, gum ghutti, and khaya gum, which were then evaluated for their effectiveness in microbial degradation and targeting the colon. Viscosity profiles were generated in the presence of a prebiotic culture medium prepared by using the Velgut capsule that mimicked the impact of 4% rat cecal content and helpful in screening of natural polymer. Based on the cumulative drug release data of preliminary batches, carboxymethyl (CM) tamarind gum was identified as a superior and an excellent polymer over the tamarind gum for formulation development. The presence of water as a bridging agent in wet granulation also played an important role in the retardation of drug release. Tablets were supercoated with the enteric polymer, Eudragit S100. The Box-Behnken design was utilized, where the selected independent variables were the proportion of CM tamarind gum, % water proportion, and % weight gain of Eudragit S 100 to optimize the formulation. The optimized design space was generated with the criteria that a drug release should be of less than 5% within the first 2 h, less than 10% within the first 5 h, and more than 70% within the first 8 h, to achieve colon targeting. The optimized batch F3 was found stable as per International Council for Harmonisation guidelines. The roentgenography study for optimized formulation demonstrated that it remained intact for 5 h and, at 7 h, was disseminated completely. CM tamarind gum is efficient for colon targeting, and its proportion in 100 mg along with an enteric coating of 6% led to the optimized formulation.

采用羧甲基罗望子胶优化微生物和pH触发结肠靶向片剂配方的设计质量方法。
摘要本研究的目的是将设计质量(QbD)方法应用于微生物和pH触发结肠靶向布地奈德片剂的开发。采用回顾性研究策略选择了各种基于多糖的天然胶,如罗望子胶、结兰胶、卡拉亚胶、ghutti胶和khaya胶,然后评估它们在微生物降解和靶向结肠方面的有效性。在使用Velgut胶囊制备的益生元培养基存在的情况下产生粘度曲线,该胶囊模拟了4%大鼠盲肠含量的影响,有助于筛选天然聚合物。根据初步批次的累积药物释放数据,羧甲基罗望子胶被确定为一种优于罗望子树胶的优良聚合物,可用于配方开发。在湿法制粒中,水作为桥接剂的存在也在延缓药物释放方面发挥了重要作用。片剂用肠溶性聚合物Eudragit S100进行过冷却。采用Box-Behnken设计,其中选择的自变量为CM罗望子胶的比例、水分比例%和Eudragit S100的增重%,以优化配方。优化设计空间是根据前2个月内药物释放应小于5%的标准生成的 h、 前5年内低于10% h、 前8个月内超过70% h、 以实现结肠靶向。根据国际协调理事会的指导方针,优化的F3批次是稳定的。优化配方的X射线照相研究表明,它在5年内保持不变 h和,在7 h、 完全传播。CM罗望子胶对结肠靶向有效,其在100 mg以及6%的肠溶包衣得到了优化的制剂。
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来源期刊
Assay and drug development technologies
Assay and drug development technologies 医学-生化研究方法
CiteScore
3.60
自引率
0.00%
发文量
33
审稿时长
>12 weeks
期刊介绍: ASSAY and Drug Development Technologies provides access to novel techniques and robust tools that enable critical advances in early-stage screening. This research published in the Journal leads to important therapeutics and platforms for drug discovery and development. This reputable peer-reviewed journal features original papers application-oriented technology reviews, topical issues on novel and burgeoning areas of research, and reports in methodology and technology application. ASSAY and Drug Development Technologies coverage includes: -Assay design, target development, and high-throughput technologies- Hit to Lead optimization and medicinal chemistry through preclinical candidate selection- Lab automation, sample management, bioinformatics, data mining, virtual screening, and data analysis- Approaches to assays configured for gene families, inherited, and infectious diseases- Assays and strategies for adapting model organisms to drug discovery- The use of stem cells as models of disease- Translation of phenotypic outputs to target identification- Exploration and mechanistic studies of the technical basis for assay and screening artifacts
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