Sawatdee Somchai, Atipairin Apichart, Sae Yoon Attawadee, Srichana Teerapol, Changsan Narumon, Suwandecha Tan
Drug and Cosmetics Excellence Center, Walailak University, Thasala, Nakhon Si Thammarat 80161, Thailand.
School of Pharmacy, Walailak University, Thasala, Nakhon Si Thammarat 80161, Thailand.
Pharmaceutics. 2019 Mar 20;11(3):134. doi: 10.3390/pharmaceutics11030134.
Albendazole is an anthelmintic agent with poor solubility and absorption. We developed a chewable tablet (200 mg drug equivalent), containing a self-microemulsifying drug delivery system (SMEDDS), with oral disintegrating properties. The emulsion was developed using sesame and soybean oils along with surfactant/co-surfactants, and the tablets were prepared by wet granulation using superdisintegrants and adsorbents. Infra-red (IR) spectral studies revealed no interaction between the drug and excipients, and all physical and chemical parameters were within acceptable limits. Stability studies for the formulation indicated no significant change over time. An in vitro release study indicated 100% drug release within 30 min, and in vivo plasma concentrations indicated that the area under the curve (AUC) of albendazole in rats administered SMEDDS chewable tablets was significantly higher than in those administered commercial tablets or powder (-value < 0.05). The systemic bioavailability of albendazole achieved through the SMEDDS tablets was 1.3 times higher than that achieved by the administration of comparable quantities of albendazole commercial tablets. This was due to the higher dissolution of albendazole SMEDDS in the chewable tablets. We conclude that the SMEDDS chewable formulation can be used to improve the dissolution and systemic availability of poorly water-soluble drugs.
阿苯达唑是一种溶解度和吸收率都较差的驱虫剂。我们研发了一种咀嚼片(相当于200毫克药物),其含有具有口腔崩解特性的自微乳化药物递送系统(SMEDDS)。该乳剂是使用芝麻油和大豆油以及表面活性剂/助表面活性剂研制而成的,而片剂则是通过使用超级崩解剂和吸附剂进行湿法制粒制备的。红外(IR)光谱研究表明药物与辅料之间没有相互作用,并且所有物理和化学参数均在可接受范围内。该制剂的稳定性研究表明,随着时间推移没有显著变化。体外释放研究表明,药物在30分钟内释放100%,体内血浆浓度表明,给予SMEDDS咀嚼片的大鼠体内阿苯达唑的曲线下面积(AUC)显著高于给予市售片剂或粉剂的大鼠(P值<0.05)。通过SMEDDS片剂实现的阿苯达唑全身生物利用度比给予等量阿苯达唑市售片剂时高出1.3倍。这是由于阿苯达唑SMEDDS在咀嚼片中的溶解度更高。我们得出结论,SMEDDS咀嚼片制剂可用于改善难溶性药物的溶解和全身可用性。