Department of Pharmaceutics, R.C. Patel Institute of Pharmaceutical Education & Research, Near Karwand Naka, Dhule, Shirpur, 425 405, Maharashtra, India.
Arch Pharm Res. 2013 Jul;36(7):846-53. doi: 10.1007/s12272-013-0097-3. Epub 2013 Apr 16.
Linseed is the crop that is used as a foodstuff in European and Asian countries. The objective of the present work was to extract mucilage from linseed, utilize it as mucoadhesive gelling agent along with synthetic polymers and administration of venlafaxine by buccal route in the gel form. Buccal administration of venlafaxine will avoid first pass metabolism, which will increase the bioavailability of the drug. Linseed mucilage based buccal mucoadhesive gel preparations in combination with chitosan, carbopol 934P, carboxy methylcellulose and polyvinyl pyrrolidone were formulated and the viscosity, gel strength, percentage mucoadhesion and in vitro diffusion of the formulation was evaluated. Formulation (F2) was subjected to in vivo analysis in rabbits. Formulation F2, which contained linseed mucilage (2 %) and chitosan (0.5 %), showed the highest percentage of mucoadhesion, gel strength and sustained drug diffusion. The bioavailability by the oral route and buccal route were compared with that of the intravenous route. The bioavailability of venlafaxine in the formulation F2 was 63.08 ± 1.28 % by buccal route, which was higher than by the oral route (39.21 ± 6.18 %). Based on these results, the combination of linseed mucilage and chitosan can be used to form a buccal mucoadhesive gel and increase the bioavailability of venlafaxine.
亚麻籽是一种在欧洲和亚洲国家被用作食品的作物。本工作的目的是从亚麻籽中提取粘胶，将其用作粘胶增稠剂，与合成聚合物一起，并以凝胶形式经口腔给予文拉法辛。经口腔给予文拉法辛可避免首过代谢，从而提高药物的生物利用度。将基于亚麻籽粘胶的口腔粘膜粘附凝胶制剂与壳聚糖、carbopol 934P、羧甲基纤维素和聚乙烯吡咯烷酮联合配制，并对制剂的粘度、凝胶强度、粘膜粘附百分比和体外扩散进行评估。将制剂（F2）进行兔体内分析。制剂 F2 含有 2%的亚麻籽粘胶和 0.5%的壳聚糖，显示出最高的粘膜粘附百分比、凝胶强度和持续的药物扩散。经口服和口腔途径与静脉途径进行了生物利用度比较。制剂 F2 经口腔途径的文拉法辛生物利用度为 63.08±1.28%，高于口服途径（39.21±6.18%）。基于这些结果，亚麻籽粘胶和壳聚糖的组合可用于形成口腔粘膜粘附凝胶并提高文拉法辛的生物利用度。
