<br>用于配制左旋肉碱微胶囊以提高其可制造性的一次一个因素和析因实验设计,Heliyon

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用于配制左旋肉碱微胶囊以提高其可制造性的一次一个因素和析因实验设计
Heliyon ( IF 3.4 ) Pub Date : 2023-12-13 , DOI: 10.1016/j.heliyon.2023.e23637
Mahmoud M Hegazy ₁ , Alia A Badawi ₂ , Mohamed A El-Nabarawi ₂ , Mohammed A Eldegwy ₃ , Dina Louis _{2,

4}

Affiliation

左旋肉碱是一种具有生理重要性的必需膳食补充剂。由于左旋肉碱具有吸湿性，因此难以处理和生产，从而影响其流动特性以及固体剂型的稳定性。该研究旨在通过将其封装在疏水性、对 pH 值不敏感的聚合物中来降低左旋肉碱的吸湿性。采用油包油固体（s/o/o）乳液溶剂蒸发技术进行微胶囊化，以排除吸水的可能性。使用的聚合物是两种具有不同粘度的乙基纤维素（EC）等级。聚合物选择的溶剂是丙酮，液体石蜡是药物和聚合物不溶的分散介质。开发了 16 种配方，并对其进行了评估，以研究抗聚结型、混合速度、表面活性剂类型和聚合物比例以及粘度等级等配方参数。使用了 “One Factor at A Time” （OFAT）实验设计和因子设计。研究结果表明，使用 Aerosil 200 （0.1%）作为抗聚结剂，混合速度为 1000 rpm，使用 Ethocel Std 20 以 3：1 的药物与聚合物比例成功实现微胶囊化。含有左旋肉碱的微胶囊制剂成功压缩成片剂，显示出可接受的含水量、崩解时间、硬度和溶解度。此外，与湿法制粒制备的左旋肉碱片剂相比，它在 40 °C、75 % RH 下储存 6 个月后显示出可接受的稳定性。

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One Factor at a Time and factorial experimental design for formulation of l-carnitine microcapsules to improve its manufacturability

l-carnitine is an essential dietary supplement of physiological importance. Handling and manufacture of l-carnitine is difficult due to its hygroscopic nature, resulting in impairing its flow properties, as well as solid dosage form stability. The study aimed at reducing l-carnitine hygroscopicity through its encapsulation within a hydrophobic, pH-insensitive polymer. A solid in oil in oil (s/o/o) emulsion solvent evaporation technique for microencapsulation was adopted to exclude the possibility of water uptake. The polymers used were two ethyl cellulose (EC) grades with different viscosities. The chosen solvent for the polymer was acetone, and liquid paraffin was the dispersion medium in which both the drug and polymer were insoluble. Sixteen formulations were developed, and evaluated to study the formulation parameters as anti-coalescent type, mixing speed, surfactant type and polymer ratio, and viscosity grade. A “One Factor at A Time” (OFAT) design of experiment, and a factorial design were utilized. Study results revealed that successful microencapsulation occurred by using Aerosil 200 (0.1 %) as anti-coalescent, a mixing speed of 1000 rpm, and Ethocel Std 20 at a 3:1 drug-to-polymer ratio. Microcapsule formulation containing l-carnitine base, successfully compressed into tablets, showed acceptable water content, disintegration time, hardness, and dissolution. Moreover, it showed acceptable stability upon storage at 40 °C at 75 % RH for six months compared to l-carnitine tablets prepared by wet granulation.

更新日期：2023-12-13

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