Ma'ali Anwar, Naseef Hani, Qurt Moammal, Abukhalil Abdallah Damin, Rabba Abdullah K, Sabri Israr
Pharmacy Department, Faculty of Pharmacy, Nursing and Health Professions, Birzeit University, Ramallah P.O. Box 14, Palestine.
Pharmaceuticals (Basel). 2023 Oct 4;16(10):1412. doi: 10.3390/ph16101412.
Cobalamin (vitamin B), an essential vitamin with low oral bioavailability, plays a vital role in cellular functions. This research aimed to enhance the absorption of vitamin B using sublingual mucoadhesive tablets by increasing the residence time of the drug at the administration site. This research involved the preparation of different 50 mg placebo formulas using different methods. Formulas with disintegration times less than one minute and appropriate physical characteristics were incorporated into 1 mg of cyanocobalamin (S1-S20) using the direct compression method. The tablets obtained were evaluated ex vivo for residence time, and only those remaining for >15 min were included. The final formulas (S5, S8, S11, and S20) were evaluated in several ways, including pre- and post-compression, drug content, mucoadhesive strength, dissolution, and Permeapad permeation test employed in the Franz diffusion cell. After conducting the evaluation, formula S11 (Eudragit L100-55) emerged as the most favorable formulation. It exhibited a mucoadhesive residence time of 118.2 ± 2.89 min, required a detachment force of 26 ± 1 g, maintained a drug content of 99.124 ± 0.001699%, and achieved a 76.85% drug release over 22 h, fitting well with the Peppas-Sahlin kinetic model (R: 0.9949). This suggests that the drug release process encompasses the Fickian and non-Fickian kinetic mechanisms. Furthermore, Eudragit L100-55 demonstrated the highest permeability, boasting a flux value of 6.387 ± 1.860 µg/h/cm; over 6 h. These findings indicate that including this polymer in the formulation leads to an improved residence time, which positively impacts bioavailability.
钴胺素（维生素B）是一种口服生物利用度低的必需维生素，在细胞功能中起着至关重要的作用。本研究旨在通过增加药物在给药部位的停留时间，使用舌下黏膜黏附片来提高维生素B的吸收。本研究涉及使用不同方法制备不同的50毫克安慰剂配方。将崩解时间小于1分钟且具有适当物理特性的配方通过直接压片法与1毫克氰钴胺（S1 - S20）混合。对所得片剂进行体外停留时间评估，仅纳入停留时间大于15分钟的片剂。对最终配方（S5、S8、S11和S20）进行了多种评估，包括压片前后、药物含量、黏膜黏附强度、溶出度以及在Franz扩散池中进行的Permeapad渗透试验。评估后，配方S11（丙烯酸树脂L100 - 55）成为最有利的配方。它表现出118.2±2.89分钟的黏膜黏附停留时间，分离力为26±1克，药物含量维持在99.124±0.001699%，在22小时内药物释放率达到76.85%，与Peppas - Sahlin动力学模型拟合良好（R：0.9949）。这表明药物释放过程包括菲克和非菲克动力学机制。此外，丙烯酸树脂L100 - 55表现出最高的渗透性，在6小时内通量值为6.387±1.860微克/小时/平方厘米。这些发现表明，在配方中加入这种聚合物可改善停留时间，对生物利用度产生积极影响。
