Background and Introduction

Piroxicam is an NSAID (non-steroidal anti-inflammatory drug) persisting antipyretic and analgesic effects and being usually implied in managing and treating osteoarthritis, rheumatoid arthritis, soft tissue disorders, ankylosing spondylitis, and acute gout and also in post-operative pain management.

Aim

The present research was undertaken aiming to formulate Piroxicam encompassing floating oral in situ gels, in order to augment its anti-inflammatory activity and to alleviate its gastric ulceration potential.

Materials and Methods

In the present work, a three-factor at two-level (2³) factorial design was adopted to inspect the effects of three factors viz. sodium alginate [A], sodium bicarbonate [B], and sodium citrate [C] on the dependent variables like in vitro gelation, in vitro floating, percentage water uptake, and percentage drug release.

Results

All the formulations have exhibited pH ranging from 6.7 ± 0.25 to 7.4 ± 0.24. Percentage drug content was noted in the range of 96.3 ± 0.27 to 99.5 ± 0.28%. In vitro gelation was instantaneous post administration of the system, which remained intact for an extended time period. Percentage water uptake was in the range 9.01 ± 0.15 to 31.01 ± 0.25%; floating lag time was estimated around 7 ± 0.39 to 57 ± 0.36 s. Formulations F4 and F5 reflected floating even past 12 h. All the formulations have exhibited drug release of around 90% within 8 h. It was experiential that the chosen independent variables had significant effect on the dependent variables, justifying the robustness and aptness of design implied for optimization.

Conclusions

The developed system may be a promising and alternative strategy to augment gastric retention of Piroxicam, thereby increasing its therapeutic efficacy. It even offers additional benefit of reducing the gastric irritation, tissue damage, and ulceration, by avoiding direct contact of drug with mucosa of stomach.

中文翻译：

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2 3吡罗昔康浮动口腔原位凝胶系统的配方设计和评估的全因子设计

背景与介绍

吡罗昔康是一种NSAID（非甾体类抗炎药），具有解热镇痛作用，通常隐含在治疗和治疗骨关节炎，类风湿性关节炎，软组织疾病，强直性脊柱炎和急性痛风中，以及在术后疼痛处理中。

目标

进行本研究的目的是配制包含浮动口服原位凝胶的吡罗昔康，以增强其抗炎活性并减轻其胃溃疡的可能性。

材料和方法

在当前的工作中，采用了三因素两级（2 ³）析因设计来检查三个因素的影响。海藻酸钠[A]，碳酸氢钠[B]和柠檬酸钠[C]与因变量有关，例如体外凝胶化，体外漂浮，吸水百分比和药物释放百分比。

结果

所有制剂的pH均在6.7±0.25至7.4±0.24的范围内。药物含量百分比范围为96.3±0.27至99.5±0.28％。体外凝胶化是在系统给药后立即进行的，其在较长时间内保持完整。吸水百分比在9.01±0.15至31.01±0.25％的范围内；浮动滞后时间估计约为7±0.39到57±0.36 s。配方F4和F5甚至在12小时后仍反映出漂浮状态。所有制剂在8小时内均显示出约90％的药物释放。经验表明，选择的自变量对因变量有显着影响，证明了优化所隐含的设计的鲁棒性和适用性。

结论

开发的系统可能是增加吡罗昔康在胃中滞留从而提高其治疗功效的有前途的替代策略。通过避免药物与胃粘膜直接接触，它甚至还具有减少胃部刺激，组织损伤和溃疡的额外好处。