Juan Candela, Gonzalez Vidal Noelia, Gallo Loreana
Departamento de Biología, Bioquímica y Farmacia, Universidad Nacional del Sur (UNS), San Juan 670, 8000, Bahía Blanca, Buenos Aires, Argentina.
Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET), Camino La Carrindanga Km 7, Bahía Blanca, Buenos Aires, Argentina.
AAPS PharmSciTech. 2025 Aug 13;26(7):212. doi: 10.1208/s12249-025-03208-2.
Several diseases that affect the pediatric population, e.g., heart diseases, cannot be efficiently treated because of the absence of a suitable dosage form. In this sense, orally disintegrating tablets (ODT) are solid dosage forms that are gaining acceptance. Losartan potassium (LP) is the drug of choice for managing pediatric arterial hypertension, although its bitter taste represents a major challenge to treatment compliance. To mitigate this drawback, this study aimed to develop palatable ODT, by the incorporation of spray-dried powders (SDP), composed of LP, Eudragit® polymers and adjuvants (i.e., colloidal silicon dioxide, mannitol, and PEG4000). The SDP were analyzed in terms of production yield and encapsulation efficiency. Selected SDP were incorporated into ODT by direct compression, and characterized in terms of mechanical and pharmaceutical properties, as well as palatability. Tablets with satisfactory disintegration time, hardness, and friability were obtained, though different performance during in vitro dissolution study. In the palatability study, the volunteer panel confirmed that the ODT-7SDP formulation, prepared by spray drying with Eudragit® E PO and colloidal silicon dioxide, showed a marked reduction in LP bitterness. In conclusion, the applied technologies successfully reduced the bitter taste of LP, enabling its oral administration in the form of ODT, particularly for pediatric patients.
几种影响儿童群体的疾病,例如心脏病,由于缺乏合适的剂型而无法得到有效治疗。从这个意义上讲,口腔崩解片(ODT)是一种正在获得认可的固体剂型。氯沙坦钾(LP)是治疗儿童动脉高血压的首选药物,但其苦味对治疗依从性构成了重大挑战。为了缓解这一缺点,本研究旨在通过加入由LP、丙烯酸树脂聚合物和辅料(即胶体二氧化硅、甘露醇和聚乙二醇4000)组成的喷雾干燥粉末(SDP)来开发可口的ODT。对SDP的产率和包封效率进行了分析。将选定的SDP通过直接压片法加入到ODT中,并对其机械性能、药学性能以及适口性进行了表征。获得了崩解时间、硬度和脆碎度令人满意的片剂,尽管在体外溶出研究中表现不同。在适口性研究中,志愿者小组证实,用丙烯酸树脂E PO和胶体二氧化硅喷雾干燥制备的ODT-7SDP制剂,LP的苦味明显降低。总之,所应用的技术成功降低了LP的苦味,使其能够以ODT的形式口服给药,特别是对于儿科患者。