用于花生诱发的过敏性哮喘的快速崩解草药提取物舌下免疫治疗片剂的配方与表征
Formulation and characterization of fast-disintegrating herbal extract sublingual immunotherapy tablet for peanut-induced allergic asthma.
作者信息
Aswathy K N, Asdaq Syed Mohammed Basheeruddin, Saritha C K, Thomas Litha, Haridas Nithya, Viswanad Vidya, Sahu Ram Kumar, Fattepur Santosh, Alamri Abdulhakeem S, Alsanie Walaa F, Alhomrani Majid, Sreeharsha Nagaraja, Khalid Anwer Md
机构信息
Department of Pharmaceutics, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham, AIMS Health Sciences Campus, Kochi 682041, Kerala, India.
Department of Pharmacy Practice, College of Pharmacy, AlMaarefa University, Dariyah 13713, Riyadh, Saudi Arabia.
出版信息
Saudi J Biol Sci. 2022 Mar;29(3):1283-1297. doi: 10.1016/j.sjbs.2021.12.031. Epub 2021 Dec 22.
BACKGROUND
Allergen immunotherapy (AIT) involves the regimen of gradually incrementing doses of the allergen, thereby inducing desensitization and tolerance. Sublingual Immunotherapy tablets (SLIT-tablets) have been formulated for several allergies and had manifested efficacy for allergic rhinitis and allergic asthma. SLIT promises an alternative method to other routes of AIT enabling patients to self-administer AIT.
OBJECTIVE
The study aimed to formulate fast disintegrating SLIT containing crude peanut extract for peanut-induced allergic asthma.
METHODS
The crude peanut extract was prepared by a simple extraction method and was subjected to quantitative and qualitative analysis. The extract was also characterised for its physical properties. The preformulation study for the extract and excipients of the tablet was performed using FT-IR spectroscopy and Differential scanning calorimetry. The tablet powder blends were characterised for pre-compression properties. The SLIT tablets were developed by direct compression and the post-compression evaluation was performed.
RESULTS
The results of the quantitative and qualitative analysis of extract confirmed the presence of peanut proteins in the extract. The preformulation studies using FT-IR spectroscopy and Differential Scanning Calorimetry revealed that there is no significant interaction between the CPE and excipients. The pre-compression characterisation showed that the powder blends had good flowproperties. Three doses of SLIT tablets were formulated with each dose containing four batches and the tablet of each dose was optimized by studying the effect of varying concentrations of super disintegrants on disintegration time and dissolution rate. The post compression characterization of the tablets was performed and the optimized batch of the three doses with the concentration of 5% crospovidone and 2% croscarmellose sodium showed less wetting time and high-water absorption ratio, shorter disintegration time of 14secs and maximum drug release of >90% within 2-3 min.
CONCLUSION
The results indicated the suitability of formulated SLIT tablets for peanut induced allergic asthma.
背景
变应原免疫疗法（AIT）包括逐渐增加变应原剂量的方案，从而诱导脱敏和耐受。舌下免疫疗法片剂（SLIT片剂）已针对多种过敏症配制而成，并已证明对过敏性鼻炎和过敏性哮喘有效。SLIT为AIT的其他给药途径提供了一种替代方法，使患者能够自行进行AIT。
目的
本研究旨在制备含花生粗提物的快速崩解型SLIT片剂，用于治疗花生诱发的过敏性哮喘。
方法
采用简单的提取方法制备花生粗提物，并进行定量和定性分析。还对提取物的物理性质进行了表征。使用傅里叶变换红外光谱（FT-IR）和差示扫描量热法对片剂提取物和辅料进行了处方前研究。对片剂粉末混合物的压片前性质进行了表征。通过直接压片法制备SLIT片剂，并进行压片后评价。
结果
提取物的定量和定性分析结果证实了提取物中存在花生蛋白。使用FT-IR光谱和差示扫描量热法进行的处方前研究表明，CPE与辅料之间没有显著相互作用。压片前表征表明，粉末混合物具有良好的流动性。制备了三剂量的SLIT片剂，每剂量包含四批，通过研究不同浓度的超级崩解剂对崩解时间和溶出速率的影响，对每剂量的片剂进行了优化。对片剂进行了压片后表征，优化后的三剂量批次，交联聚维酮浓度为5%，交联羧甲基纤维素钠浓度为2%，其润湿时间较短，吸水率较高，崩解时间为14秒，在2-3分钟内药物最大释放率>90%。
结论
结果表明所制备的SLIT片剂适用于花生诱发的过敏性哮喘。
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