OPTIMIZATION OF FAST-DISSOLVING TABLETS OF CARVEDILOL USING 23 FACTORIAL DESIGN

Q2 Pharmacology, Toxicology and Pharmaceutics

International Journal of Applied Pharmaceutics Pub Date : 2024-01-07 DOI:10.22159/ijap.2024v16i1.49535

Anusha Kusuma, S. KUMAR R.

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Abstract

Objective: Optimization of carvedilol fast-dissolving tablets through a 23 factorial design employing starch hyaluronate as a new superdisintegrating agent. Methods: The esterification method was used for producing starch hyaluronate. A direct compression process was used to develop carvedilol tablets utilizing a mix of starch hyaluronate (SH) as a novel superdisintegrant, crospovidone, and sodium starch glycolate. The prepared tablets are analyzed for physical characteristics, drug dissolution, in vivo pharmacokinetic, and stability studies. Results: New superdisintegrant synthesized was a fine, free-flowing crystalline powder. In the DSC study, starch hyaluronate had no interaction with the drug. NMR and FTIR investigations supported the ester connection between starch and hyaluronic acid. CF2, the optimized formulation, had the shortest disintegration time of 26±2 seconds. The percentage of drugs dissolved in ten minutes from the optimized composition was 93.4±1.32%. The optimized composition achieved peak plasma concentration in a short time and demonstrated higher relative bioavailability for the drug. Conclusion: A formula containing a 5% concentration of starch hyaluronate was optimized and has a proper potential for application in the formulation of rapidly disintegrating tablets, in addition to improving clinical obedience throughout the efficacious treatment of hypertension.

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采用 23 个因子设计优化卡维地洛速溶片剂

目的采用淀粉透明质酸盐作为新的超崩解剂，通过 23 个因子设计优化卡维地洛速溶片剂：方法：采用酯化法生产淀粉透明质酸盐。采用直接压片工艺，将淀粉透明质酸盐（SH）作为一种新型超微崩解剂、氯丙维酮和淀粉乙醇酸钠混合制成卡维地洛片剂。对制备的片剂进行了物理特性、药物溶解度、体内药代动力学和稳定性研究分析：结果：合成的新型超崩解剂是一种细小、自由流动的结晶粉末。在 DSC 研究中，淀粉透明质酸盐与药物没有相互作用。核磁共振和傅立叶变换红外光谱研究证实了淀粉和透明质酸之间的酯联系。优化配方 CF2 的崩解时间最短，为 26±2 秒。优化组合物在十分钟内溶解的药物百分比为 93.4±1.32%。优化后的组合物能在短时间内达到血浆峰值浓度，并显示出更高的药物相对生物利用度：结论：含有 5%浓度淀粉透明质酸盐的配方得到了优化，具有应用于快速崩解片剂配方的适当潜力，此外还能在有效治疗高血压的整个过程中提高临床顺应性。

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来源期刊

International Journal of Applied Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)

CiteScore

1.40

自引率

0.00%

发文量

219

期刊介绍： International Journal of Applied Pharmaceutics (Int J App Pharm) is a peer-reviewed, bimonthly (onward March 2017) open access journal devoted to the excellence and research in the pure pharmaceutics. This Journal publishes original research work that contributes significantly to further the scientific knowledge in conventional dosage forms, formulation development and characterization, controlled and novel drug delivery, biopharmaceutics, pharmacokinetics, molecular drug design, polymer-based drug delivery, nanotechnology, nanocarrier based drug delivery, novel routes and modes of delivery; responsive delivery systems, prodrug design, development and characterization of the targeted drug delivery systems, ligand carrier interactions etc. However, the other areas which are related to the pharmaceutics are also entertained includes physical pharmacy and API (active pharmaceutical ingredients) analysis. The Journal publishes original research work either as a Original Article or as a Short Communication. Review Articles on a current topic in the said fields are also considered for publication in the Journal.