Sudhakar Yajaman, Bandyopadhyay A K
Buccal Adhesive Research Laboratory, Division of Pharmaceutics, Department of Pharmaceutical Technology, Jadavpur University, Kolkata 700032, India.
PDA J Pharm Sci Technol. 2008 Mar-Apr;62(2):97-110.
In the current investigation, white mustard mucilage from whole seeds of Sinapis alba was evaluated for its physical properties and compared with the other mucoadhesive polymers such as hydroxy propyl methylcellulose 5Cps and Carbopol 934P. Further, methanol precipitable solids from whole leaves of Aloe Vera L were used as permeation enhancer. To achieve improved bioavailability of diltiazem, novel buccal adhesive tablets (NBATs) in cup and core fashion designed to achieve unidirectional release towards mucosa were prepared in a three-stage process using specially fabricated punches. The adhesive cups were studied for its shear, tensile, and peel strengths by specially designed apparatus using excised ruminant and porcine buccal mucosa as model substrates. Ex vivo permeation studies in a Franz diffusion cell were conducted through porcine buccal mucosa. Fourier transform infrared spectroscopy studies and differential scanning calorimetry thermographs showed no remarkable interactions. Histopathological studies showed no remarkable damage of buccal mucosa by the NBATs. In vivo studies were conducted on anaesthetized male New Zealand albino rabbits, estimated by reversed-phase high-performance liquid chromatography, and the pharmacokinetics were compared with the oral and intravenous bolus injection. NBATs exhibited a Cmax 74.6 ng/mL, Tmax 3.5 h, t(1/2) 4.36 h. The NBATs prevented salivary scavenging effect and exhibited 82.1% bioavailability.
在当前的研究中,对白芥(Sinapis alba)全籽中的白芥子黏液质的物理性质进行了评估,并与其他黏附性聚合物(如羟丙基甲基纤维素5Cps和卡波姆934P)进行了比较。此外,将库拉索芦荟(Aloe Vera L)全叶中甲醇可沉淀固体用作渗透促进剂。为提高地尔硫䓬的生物利用度,采用特制冲头,分三个阶段制备了杯芯型新型口腔黏附片(NBATs),旨在实现向黏膜的单向释放。使用特制仪器,以切除的反刍动物和猪口腔黏膜为模型底物,研究了黏附杯的剪切强度、拉伸强度和剥离强度。在Franz扩散池中通过猪口腔黏膜进行了体外渗透研究。傅里叶变换红外光谱研究和差示扫描量热法热谱图显示没有明显的相互作用。组织病理学研究表明,NBATs对口腔黏膜没有明显损伤。在麻醉的雄性新西兰白化兔身上进行了体内研究,通过反相高效液相色谱法进行评估,并将药代动力学与口服和静脉推注进行了比较。NBATs的Cmax为74.6 ng/mL,Tmax为3.5小时,t(1/2)为4.36小时。NBATs防止了唾液清除作用,生物利用度为82.1%。