曲马多HCL果胶包被壳聚糖LDH生物纳米复合微球结肠给药系统的制备与评价

A. Pawar, Komal Ahire, K. Naikwade, S. Talele, Pritesh Gaikwad
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摘要

盐酸曲马多(TH)是一种中枢镇痛药,用于治疗中度至重度疼痛性肠道疾病。为了研制用于结肠靶向的果胶包被壳聚糖LDH生物纳米复合微球,采用沉淀反应法将LDH-TH嵌入制备了生物纳米复合TH微球。对制备的微球进行了堆积密度、轻叩密度、休止角、HR、CI、粒度、SEM、溶胀研究、载药和EE等表征。ph1.2 HCl缓冲液的体外释放研究pH为6.8缓冲液和pH为7.4缓冲液。相容性研究采用FTIR和DSC研究。优化后的配方(F8)呈球形,光滑。在543µm至888µm的粒径范围内,所有其他微观特性均在可接受范围内。包覆过程中所使用的果胶浓度对溶胀量有很大影响。F1 ~ F8批的载药量为52.37% ~ 90.25%。F1 ~ F8批次的EE %在71.92% ~ 88.78之间。FTIR和DSC研究显示药物与所用辅料之间没有物理不相容性。批次(F8)在果胶最高包覆浓度(1.5%)时表现出较好的控释模式。稳定性研究还表明,药物释放谱没有变化。开发的微珠可用于靶向结肠,以获得长效释放特性。
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Formulation and evaluation of Tramadol HCL pectin coated chitosan LDH bionanocomposite beads for colon drug delivery system
Tramadol HCl (TH) is a centrally acting analgesic that is used to treat moderate to severe pain intestinal disorders. Its use is limited orally due to instability To develop e TH Pectin-coated chitosan LDH bionanocomposite beads for colon targeting LDH-TH intercalation was done by precipitation reaction and it was used to prepare bionanocomposite beads of TH. The developed beads were characterized for bulk density, tap density, angle of repose, HR, CI, particle size, SEM, swelling study, drug loading, and EE. In vitro release study in pH 1.2 HCl buffer; pH 6.8 buffer & pH 7.4 buffer was performed. The compatibility study was performed using FTIR and DSC studies. he optimised formulation (F8) was found to be spherical and smooth. All other micromeritics properties were found within the acceptable range with the particle size of 543µm to 888 µm. The amount of swelling is greatly influenced by the pectin concentration employed in the coating process. Drug loading of batches F1 to F8 was in the range from 52.37% to 90.25%. % EE of batches F1 to F8 was in the range from 71.92% to 88.78. FTIR and DSC studies showed no physical incompatibility between the drug and used excipients. Batch (F8) showed a more controlled release pattern at the highest coating concentration of pectin (1.5%). The stability study also revealed that there was no change in the drug release profile. The developed beads can be used to target the colon to prolonged-release characteristics.
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