胰岛素口腔黏附片的制备及体外药学特性
Preparation and in vitro characteristics of insulin buccal adhesive tablets
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摘要: 优选胰岛素口腔黏附片处方组成，并探讨黏附材料对胰岛素口腔黏附片体外药学特性的影响。以苹果果胶、壳聚糖、卡波姆934P、羟丙基甲基纤维素和海藻酸钠为生物黏附材料，设计处方F1～F12，冻干法制备胰岛素口腔黏附双层片，以黏附片性状特点、体外黏附力、溶胀率、溶胀速率和体外释放度为指标，综合评价各处方的优劣。所制胰岛素口腔黏附片有多孔海绵状结构，利于胰岛素释放，具有疏水的保护层，可保证药物单向释放，避免药物损失；F5、F7和F12成形性差，未作进一步检测。F6和F8黏附力过大，F1和F11溶胀速率过快，均不理想。而F2、F9和F10具有优良的释药能力，适宜的体外黏附力[分别为（66.1±6.65)、(75.62±4.53)和（69.39±8.03） g/cm2]和溶胀率（2 h时溶胀率均小于4%）。因此F2、F9和F10处方制备的胰岛素口腔黏附双层片，体外药学特性优良，可进一步研究。Abstract: The objective of this study is to optimize the formulation of insulin buccal adhesive tablets and study the effects of adhesive excipients on in vitro characteristics of insulin buccal adhesive tablets.Twelve formulation (designated as F1-F12，80-mg tablet weight，and 2-mg insulin per tablet) were prepared using chitosan (CS)，apple pectin (AP)，carbomer-934P (CP)，hydroxypropyl methyl cellulose (HPMC)，sodium carboxymethyl cellulose (CMC-Na) and sodium alginate (SA) as adhesive excipient.Double-layer insulin buccal adhesive tablets were prepared by lyopyilization.Evaluation was performed on each formulation in the aspects of the appearance characteristics，the weight，in vitro adhesive strength，swelling percent and in vitro release of the tablets.The tablets have sponge-like porous structures，which might promote the release of insulin.The impermeable layer ensured directional release of insulin and attenuated drug loss.F5，F7 and F12 of poor compaction were aborted.In addition，the adhesive strength of F6 and F8 tablets and the swelling velocity of F1 and F11 tablets were unsatisfactory.Ultimately，tablets F2，F9 and F10，whose adhesive strengths were (66.1±6.65) g/cm2，(75.62±4.53) g/cm2 and (69.39±8.03) g/cm2，respectively，and swelling percents at 2 h lower than 4%，were acceptable.Therefore，tablets F2 using AP as primary adhesive excipient，and tablets F9 and F10 using CP have better overall pharmaceutical properties in vitro，which can be used for further studies.
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Keywords:
- insulin /
- buccal adhesive tablets /
- bioadhesive drug delivery
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