Gil Eddy Castellanos, Colarte Antonio Iraizoz, El Ghzaoui Abdelsam, Durand Denis, Delarbre Jean Louis, Bataille Bernard
Center of Pharmaceutical Chemistry (CQF), Havana, Cuba.
Eur J Pharm Biopharm. 2008 Feb;68(2):319-29. doi: 10.1016/j.ejpb.2007.04.015. Epub 2007 Apr 29.
We reported the physical chemical characterization of a new series of native dextran (B110-1-2). The chemical structure of the polymer was characterized by IR, (1)H and (13)C NMR spectroscopy and compared with that of a commercial native dextran B512-F obtained from Sigma Company. Molecular weights of the product and different commercial dextran fractions of Leuconostoc mesenteroides from 43000 to 170000 average molecular weight (M(w)) were established by the analysis of intrinsic viscosity in aqueous solutions and compared with those obtained by gel permeation chromatography (GPC). The critical overlap concentration around 9g/L was obtained. No interactions of powder mixtures with different commercial excipients (lactose, cetyl alcohol, HPMC) and drugs (propranolol hydrochloride, acetyl salicyclic acid, isosorbide dinitrate, lobenzarit disodium, and nifedipine) were demonstrated by differential scanning calorimetry (DSC) analysis. Tablets obtained by direct compression showed good physical-mechanical and technological properties. Dextran B110-1-2 has similar physical chemical properties as commercial Sigma B512-F. Water uptake, erosion and dissolution profile studies for dextran tablets established that glucose polymer with molecular weight M(w) > or = 2x10(6) is suitable for the development of controlled release solid dosage forms (soluble drugs). Fraction of dextran (M(w) 40000-170000) could be more useful for immediate release tablets.
我们报道了一系列新型天然葡聚糖（B110 - 1 - 2）的物理化学特性。通过红外光谱、氢核磁共振（¹H NMR）和碳核磁共振（¹³C NMR）光谱对该聚合物的化学结构进行了表征，并与从西格玛公司获得的商业天然葡聚糖B512 - F的结构进行了比较。通过分析水溶液中的特性粘度确定了产品以及来自肠系膜明串珠菌的不同商业葡聚糖级分的分子量，其平均分子量（M(w)）在43000至170000之间，并与通过凝胶渗透色谱法（GPC）获得的分子量进行了比较。得到了约9g/L的临界重叠浓度。通过差示扫描量热法（DSC）分析表明，粉末混合物与不同的商业辅料（乳糖、十六醇、羟丙甲纤维素）和药物（盐酸普萘洛尔、乙酰水杨酸、硝酸异山梨酯、苯并噻嗪二钠和硝苯地平）之间没有相互作用。通过直接压片获得的片剂显示出良好的物理机械性能和工艺性能。葡聚糖B110 - 1 - 2具有与商业西格玛B512 - F相似的物理化学性质。对葡聚糖片剂的吸水、侵蚀和溶出曲线研究表明，分子量M(w)≥2×10⁶的葡萄糖聚合物适用于开发控释固体剂型（可溶性药物）。葡聚糖级分（M(w) 40000 - 170000）可能对速释片剂更有用。
