Khan Shujaat A, Ahmad Mahmood, Murtaza Ghulam, Aamir Muhammad N, Akhtar Naveed, Kousar Rozina
Department of Pharmacy, Faculty of Pharmacy and Alternative Medicines, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
Acta Pol Pharm. 2010 May-Jun;67(3):299-306.
The objective of this study was to formulate stable and controlled release microparticles for simultaneous delivery and UV spectrophotometric detection in combined dosage of an non-steroidal anti-inflammatory drug (NSAID) (nimesulide, NMS) and a spasmolytic agent (tizanidine, TZN) to maintain plasma concentration that may increase patients compliance, improved therapeutic efficacy, The aim was also to reduce severity of upper GI side effects of NMS because of alteration in delivery pattern via slow release of drug from microparticles and to increase the benefits of spasticity and disability for spastic patients by administering TZN in a modified release formulation as these two drugs are often prescribed in combination for the management of pain associated with muscles spasm. Ethyl cellulose was used as a retardant polymer. Drug-polymer and drug-drug compatibility study were conducted by different analytical tests. Microparticles were prepared by coacervation thermal change method. The prepared microparticles were characterized for their micromeritics and drug loading. The prepared microparticles were light yellow, free flowing and spherical in shape. The drug-loaded microparticles showed 87% and 91% entrapment efficiency of NMS and TZN, respectively, and release was extended up to 10 h. The infrared spectra, differential scanning calorimetry thermograms and XRD spectra showed the stable character of both the drugs in the drug-loaded microparticles. The in vitro release study of microparticles was performed in phosphate buffer pH 6.8. Linearity was observed in the concentration range of 5.0-30.0 microg/mL of NMS and 0.5-3.0 microg/mL of TZN. The microparticles have a potential for the prolongation and simultaneous delivery of the NIM and TIZ. The proposed UV method for simultaneous detection can be used for routine analysis of combined dosage form.
本研究的目的是制备稳定的控释微粒，用于同时递送非甾体抗炎药（NSAID）（尼美舒利，NMS）和解痉药（替扎尼定，TZN）的联合剂型，并进行紫外分光光度法检测，以维持血浆浓度，从而提高患者的依从性，改善治疗效果。其目的还包括通过微粒缓慢释放药物来改变给药方式，降低NMS上消化道副作用的严重程度；通过以控释制剂形式给药TZN，增加痉挛患者缓解痉挛和残疾的益处，因为这两种药物经常联合使用以治疗与肌肉痉挛相关的疼痛。乙基纤维素用作阻滞剂聚合物。通过不同的分析测试进行药物 - 聚合物和药物 - 药物相容性研究。通过凝聚热变法制备微粒。对制备的微粒进行了微观特性和载药量表征。制备的微粒呈浅黄色，自由流动且形状为球形。载药微粒对NMS和TZN的包封率分别为87%和91%，释放时间延长至10小时。红外光谱、差示扫描量热法热谱图和XRD光谱显示了载药微粒中两种药物的稳定性。在pH 6.8的磷酸盐缓冲液中进行微粒的体外释放研究。在5.0 - 30.0μg/mL的NMS浓度范围和0.5 - 3.0μg/mL的TZN浓度范围内观察到线性关系。这些微粒具有延长和同时递送NIM和TIZ的潜力。所提出的同时检测紫外方法可用于联合剂型的常规分析。
