Development, Optimization and Evaluation of Mucoadhesive Microspheres of Amoxicillin for the Treatment of H.Pylori by Full Factorial Design.

Bhawna Sharma, Anand Chaurasia, Naveen Gupta, Dharmendra Singh Rajput
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Abstract

Objective: This work is aimed to formulate and evaluate Mucoadhesive Microspheres contain Amoxicillin for the effective use in the treatment of H.Pylori.

Methods: Microspheres were prepared using Emulsification-cross linking technique. To this guar gum (GG) and sodium alginate (SA) was dissolved in 200 ml of water and allowed to swell for 24 h at room temperature. And separately chitosan (CH) was dissolved in 2% (v/v) glacial acetic acid and this also kept for 24 h to swell or dissolve properly. After 24 h this swelled mixture was mixed under magnetic stirrer (Remi, India) at specific stirring rate for 1 h in order to find homogeneous mass of both the gum. Then slurry of chitosan also was homogenized for half an hour. The drug, Amoxicillin (1g) was then added to the chitosan solution and mixed homogeneously.

Results: The aim of the study was to formulate and evaluate microspheres, for SR of the chosen drug. The particle size of microspheres was in the range of 200-500 µ, maximum mucoadhesive property observed was 57.41% for Optimized formulation F-9, Drug release 68.52% till 8 h, and the maximum entrapment was 94.87% for F-9 formulation. The work also aims to study various parameters affecting the behavior of microspheres in oral dosage form.

Conclusion: Drugs with short half life that are absorbed from the gastrointestinal tract (GIT) are eliminated rapidly from the blood flow. To avoid this, the oral SR was developed as this formulation released the drug slowly into the GIT and maintained a stable drug concentration in the serum for a longer duration of time.

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通过全因子设计开发、优化和评估用于治疗幽门螺杆菌的阿莫西林黏胶微球
目的本研究旨在配制和评估含有阿莫西林的黏附性微球,以有效治疗幽门螺杆菌:方法:采用乳化-交联技术制备微球。将瓜尔胶(GG)和海藻酸钠(SA)溶于 200 毫升水中,在室温下放置 24 小时。另外,将壳聚糖(CH)溶于 2%(v/v)的冰醋酸中,同样放置 24 小时使其充分溶解或膨胀。24 小时后,在磁力搅拌器(Remi,印度)上以特定的搅拌速度混合这种膨胀的混合物 1 小时,以找到两种胶的均匀质量。然后,壳聚糖浆也被均质半小时。然后将药物阿莫西林(1 克)加入壳聚糖溶液并混合均匀:研究的目的是配制和评估微球,用于所选药物的 SR。微球的粒径在 200-500 µ 之间,优化配方 F-9 的粘附性最大为 57.41%,8 小时内的药物释放率为 68.52%,F-9 配方的最大夹持率为 94.87%。这项工作还旨在研究影响口服剂型微球行为的各种参数:半衰期短的药物从胃肠道(GIT)吸收后会迅速从血液中排出。为了避免这种情况,我们开发了口服 SR,因为这种制剂能缓慢地将药物释放到胃肠道,并在较长时间内保持血清中药物浓度的稳定。
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