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Formulation and Evaluation of Fast Dissolving Tablets of Taste-Masked Ondansetron Hydrochloride by Solid Dispersion 盐酸昂丹司琼味觉掩蔽快溶片的固体分散处方及评价
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2017-07-26 DOI: 10.1234/ijps.v26i1.685
Alaa A. Abdulqader, Eman B. H. Al-Khedairy
Ondansetron hydrochloride (ONH) is a very bitter, potent antiemetic drug used for the treatment and/or prophylaxis of chemotherapy or radiotherapy or postoperative induced emesis. The objective of this study is to formulate and evaluate of taste masked fast dissolving tablet (FDTs) of ONH to increase patient compliance.  ONH taste masked granules were prepared by solid dispersion technique using Eudragit E100 polymer as an inert carrier. Solvent evaporation and fusion melting methods were used for such preparation. Completely taste masking with zero release of drug in phosphate buffer pH 6.8was obtained from granules prepared by solvent evaporation method using drug: polymer ratio of 1:2, from which four formulas pass pre-compression evaluation and compressed to FDTs and evaluated for their drug content, in-vitro disintegration time, in-vivo disintegration time, wetting time and in vitro drug release profile. F7 which is prepared from solid dispersion product equivalent to the required dose of ONH  , Crosspovidone as superdisintegrant, Aspartame as sweetener ,Ross berry as flavor ,Polyvinylpyrolidone K30.3.as binder ,Avicil PH102 and , mannitol as diluents give best in- vitro, in-vivo disintegration time and best drug release profile. Key words: Ondansetron hydrochloride, taste masking, solid dispersion, Eudragit E100.
盐酸昂丹司琼(ONH)是一种非常苦、强效的止吐药物,用于治疗和/或预防化疗、放疗或术后诱发的呕吐。本研究的目的是配制和评价ONH的味觉掩蔽快溶片(FDTs),以提高患者的依从性。以Eudragit E100聚合物为惰性载体,采用固体分散技术制备了ONH味觉掩蔽颗粒。溶剂蒸发法和熔融法用于这种制备。从溶剂蒸发法制备的颗粒中,采用药物与聚合物的比例为1:2,在pH 6.8的磷酸盐缓冲液中获得药物零释放的完全味觉掩蔽,其中四个配方通过预压缩评估并压缩到FDTs中,评估其药物含量、体外崩解时间、体内崩解时间,润湿时间和体外药物释放曲线。F7是由相当于所需剂量的ONH的固体分散体产物制备的,交联聚维酮作为超级崩解剂,阿斯巴甜作为甜味剂,罗斯浆果作为香料,聚乙烯吡咯烷酮K30.3.a作为粘合剂,Avicil PH102和甘露醇作为稀释剂,提供了最佳的体外、体内崩解时间和最佳的药物释放特性。关键词:盐酸昂丹司琼,味觉掩蔽,固体分散体,优德拉吉E100。
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引用次数: 7
Formulation and Evaluation of Optimized Zaltoprofen Lyophilized Tablets by Zydis Technique Zydis技术优化Zaltoprofen冻干片的处方及评价
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2017-07-12 DOI: 10.1234/IJPS.V26I1.684
Suray A. Hazzaa, Shaimaa N. Abd-Alhameed
“Orodispersible Tablet” a tablet that is to be placed in oral cavity where it disperses rapidly by saliva with no need for water before swallowing. Zaltoprofen (ZLP) is one of NSAIDs which is used in the treatment of rheumatoid arthritis and osteoarthritis as well as to relieve inflammation and pain after surgery, injury and tooth extraction. The present study was aimed to prepare rapidly dissolved lyophilized Zaltoprofen tablet with different pharmaceutical excipients and studying the factors affecting pharmaceutical properties like (solubility, disintegration time DT, dissolution, etc.) of tablets. The lyophilized disintegrating tablets (LDTs) were prepared using Zydis technique by lyophilization an aqueous dispersion of Zaltoprofen with a matrix forming agent, gelatin, and a collapse protectant, glycine. In addition to many excipients like PVPK30 was used to improve the in vitro, in vivo disintegration time and dissolution rate, mannitol as bulk forming agent. Fourteen formulations were prepared to inspect the variables that affect the disintegration time and dissolution rate.  All the formulations were evaluated for their physical appearance, mechanical strength, X-ray diffraction, FTIR, DT, and in vitro drug release. The prepared tablets were optimized and formula was subjected to different measured parameters such as disintegration time, Drug content, and in-vitro drug release. Results obtained from dissolution studies and DT showed that lyophilized disintegrating tablets (LDTs) (F8,F10,F12,F13 was 45,37,21 and 17 Sec.) respectively ,while(F14) displayed considerably faster in vitro dissolution rate of (Zaltoprofen) 3 min. and DT 9 sec. The (lyophilized disintegrating tablets) were also evaluated showing the transformation into amorphous state and absence of interaction of Zaltoprofen with the components of the tablets. From visual inspection ,physical strength ,DT and release behavior obtained ,one can conclude that the formulas(F14) which contains Zaltoprofen 3.2% ,gelatin3%, mannitol 3%, glycine 1.5%, PVP K30 1.5% was the most suitable one. Keywords : Zaltoprofen, lyophilization, PVPK30 .
“口服分散片”是一种放置在口腔中的片剂,在吞咽前通过唾液快速分散,不需要水。Zaltoprofen(ZLP)是一种非甾体抗炎药,用于治疗类风湿性关节炎和骨关节炎,以及缓解手术、损伤和拔牙后的炎症和疼痛。本研究旨在用不同的药用辅料制备快速溶解的冻干Zaltoprofen片剂,并研究影响片剂药物性质的因素,如溶解度、崩解时间DT、溶出度等。使用Zydis技术,通过将Zaltoprofen的水分散体与基质形成剂明胶和崩解保护剂甘氨酸冷冻干燥,制备冻干崩解片(LDTs)。除了使用许多赋形剂如PVPK30来改善体外、体内崩解时间和溶解速率外,甘露醇作为本体形成剂。制备了14种制剂,以检查影响崩解时间和溶解速率的变量。对所有制剂的物理外观、机械强度、X射线衍射、FTIR、DT和体外药物释放进行了评估。对制备的片剂进行了优化,并对配方进行了不同的测定参数,如崩解时间、药物含量和体外药物释放。从溶出度研究和DT获得的结果表明,冻干崩解片(LDTs)(F8,F10,F12,F13分别为45,37,21和17秒),而(F14)显示出明显更快的体外溶出速率(Zaltoprofen)3分钟和DT 9秒。还对(冻干崩解片)进行了评价,显示其转变为无定形状态,并且Zaltoprofen与片剂成分没有相互作用。从外观检查、物理强度、DT和释放行为可以得出结论,含有3.2%Zaltoprofen、3%明胶、3%甘露醇、1.5%甘氨酸、1.5%PVP K30的配方(F14)是最合适的配方。关键词:Zaltoprofen,冷冻干燥,PVPK30。
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引用次数: 2
Formulation and Evaluation of Sustained and Raft Forming Antacid Tablet 缓释成筏抗酸片的处方及评价
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2017-07-08 DOI: 10.1234/IJPS.V26I1.679
M. Al-lami
Antacids have been widely used in the treatment of various gastric and duodenal disorders such as heartburn, reflux esophagitis, gastritis, irritable stomach, gastric and duodenal ulcers. A pH-responsive of bi-polymer of sodium alginate and pectin have been studied as raft-forming polymers using sodium bicarbonate and calcium carbonate as gas-generating and calcium ion sources. The aim of study was to formulate and evaluate mono and bilayer tablets of floating and sustained release antacid delivery systems using sodium carboxy methyl cellulose as a gel forming substance, calcium and magnesium carbonate as sources of acid neutralizing and carbon dioxide gas generators agents upon contact with acidic solution. The effect of the formulation contents on the buoyancy has been investigated. In addition to, the antacid activities of intact and pulverized tablets have been studied. The result obtained showed that the buoyance is remarkably affected by the percentages of sodium carboxy methyl cellulose and carbonates salts. All formulas of mono and bilayer tablets revealed sustained action of acid neutralization and raft formation. Besides, bilayer tablets showed a significant and higher level of acid neutralizing capacity than monolayer tablets. Moreover, the pulverized of bilayer tablets exhibited significant and higher acid neutralizing capacity at raft than that at bulk of artificial gastric juice medium. Keywords: Raft forming agent, Antacid, floating drug delivery, Acid neutralizing capacity, Sodium carboxy methyl cellulose.
抗酸剂已广泛用于治疗各种胃和十二指肠疾病,如胃灼热、反流性食管炎、胃炎、胃易激综合征、胃和十二指肠溃疡。以碳酸氢钠和碳酸钙为气体生成源和钙离子源,研究了海藻酸钠和果胶双聚合物作为筏形聚合物的pH响应性。本研究的目的是使用羧甲基纤维素钠作为凝胶形成物质,碳酸钙和碳酸镁作为酸中和剂和二氧化碳气体发生器剂的来源,在与酸性溶液接触时,制备和评估漂浮和缓释抗酸剂递送系统的单层和双层片剂。研究了配方含量对浮力的影响。此外,还对完整片剂和粉碎片剂的抗酸活性进行了研究。结果表明,羧甲基纤维素钠和碳酸盐的含量对浮力有显著影响。单层和双层片剂的所有配方都显示出酸中和和筏形形成的持续作用。此外,双层片比单层片显示出显著且更高水平的酸中和能力。此外,与人工胃液培养基相比,双层粉碎片在筏板上表现出显著且更高的酸中和能力。关键词:漂流剂;抗酸剂;漂浮给药;酸中和能力;羧甲基纤维素钠。
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引用次数: 0
Estimation of Superoxide Dismutase, Matrix-metalloprotinase-9, and Interleukin -18 in Patients with Type Two Diabetes Mellitus 2型糖尿病患者超氧化物歧化酶、基质金属蛋白酶-9和白细胞介素-18的测定
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2017-07-08 DOI: 10.1234/IJPS.V26I1.682
S. Moustafa, S. Omar
Antioxidant status imbalance and inflammatory process are cooperative events involved in type 2 diabetes mellitus. This study aimed to investigate     superoxide dismutase as a potential biomarkers of antioxidant imbalance, matrix-metaloprotinase-9,   and interleukin -18  as biomarkers of inflammation in serum and to estimate  the effects of other confounding factors  gender, age and finally measuring the relation among the interested biomarkers. This case - control study included 50 patients,   and   45 of  healthy subjects matched age –gender were also enrolled  in this study as a control group.    The   focused   parameters    were        measured   using      ELISA technique. There was  significant   reduction   in   the   serum   superoxide dismutase level and significant elevation in serum matrix- metaloptotinase-9 and interleukin -18 levels which have been   associated with diabetes.  This finding may explain the role of the defect in antioxidants status   leading to significant reduction in serum superoxide  dismutase  levels  associated with increased inflammatory process leading to significant elevations of a  matrix- metaloptotinase-9 and interleukin -18. These parameters  added a diagnostic information  and evaluated as potential tools for disease risk prediction.  Keywords: Type 2 diabetes mellitus, Superoxide dismutase,   Matrix metaloptotinase-9 and Interleukin -18.
抗氧化状态失衡和炎症过程是参与2型糖尿病的协同事件。本研究旨在研究超氧化物歧化酶作为抗氧化失衡的潜在生物标志物,基质金属蛋白酶-9和白细胞介素-18作为血清炎症的生物标记物,并评估其他混杂因素的影响——性别、年龄,最后测量感兴趣的生物标志物之间的关系。本病例对照研究包括50例患者,45名健康受试者与年龄相匹配“性别也被纳入本研究作为对照组。使用ELISA技术测量重点参数。血清超氧化物歧化酶水平显著降低,血清基质金属视黄酶-9和白细胞介素-18水平显著升高,这与糖尿病有关这一发现可能解释了抗氧化剂状态缺陷的作用,该缺陷导致血清超氧化物歧化酶水平显著降低,而炎症过程增加导致基质金属视黄酶-9和白细胞介素-18显著升高。这些参数增加了诊断信息,并被评估为疾病风险预测的潜在工具。关键词:2型糖尿病,超氧化物歧化酶,基质金属蛋白酶-9和白细胞介素-18。
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引用次数: 1
A Highly Sensitive Kinetic-Spectrophotometric Method for the Assay of Carbamazepine in Pure and Commercial Tablet 高灵敏动力学分光光度法测定纯片和市售片中卡马西平的含量
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2017-07-08 DOI: 10.1234/ijps.v26i1.680
S. B. Dikran, F. Zankanah
The study aimed to recommend a new spectrophotometric-kinetic method for determination of carbamazepine (CABZ) in its pure form and pharmaceutical forms. The proposed procedure based on the coupling of CABZ with diazotized sulfanilic acid in basic medium to yield a colored azo dye. Factors affecting the reaction yield were studied and the conditions were optimized. The colored product was followed spectrophotometrically via monitoring its absorbance at 396 nm. Under the optimized conditions, two method (the initial rate and fixed time (10 minute)) were applied for constructing the calibration graphs. The graphs were linear in concentration ranges 2.0 to 18.0 µg.mL-1 for both methods. The proposed was applied successfully in the determination of CABZ in its commercial formulations. Keywords: Kinetic, Spectrophotometry, Carbamazepine, Pharmaceutical formulations
本研究旨在推荐一种新的动力学分光光度法测定卡马西平(CABZ)的纯形式和药物形式。提出了一种基于CABZ与重氮化氨基苯胺酸在碱性介质中偶联产生有色偶氮染料的方法。研究了影响反应收率的因素,并对反应条件进行了优化。通过监测其在396nm处的吸光度,用分光光度法跟踪着色产物。在优化条件下,采用两种方法(初始速率和固定时间(10分钟))构建校准图。两种方法的曲线图在2.0至18.0µg.mL-1的浓度范围内呈线性。该方法已成功应用于商业制剂中CABZ的测定。关键词:动力学,分光光度法,卡马西平,药物制剂
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引用次数: 0
Serum Trace Elements (Zinc, Copper and Magnesium) Status in Iraqi Patients with Acne Vulgaris :( Case- Controlled Study) 伊拉克寻常痤疮患者血清微量元素(锌、铜、镁)状况(病例对照研究)
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2017-03-29 DOI: 10.31351/vol20iss2pp44-49
Basil OM Saleh, Zainab N. H. Anbar, Ali Y. Majid
Recently on the dermatological fields, the serum levels and the roles of Zn, Cu and Mg have been studied especially in acne vulgaris, but the results were controversial. The aim of the present study is to investigate  a relationship between the severity of acne and the serum levels of zinc (Zn), copper (Cu) and magnesium (Mg) and to demonstrate the status of serum levels of zinc, copper, and magnesium in Iraqi male patients with acne vulgaris and to compare it with those of healthy controls.This case controlled study was conducted in the Department of Dermatology and Venerology and in the Poisoning Consultation Center of Baghdad Teaching Hospital between May 2009 to January 2010. Forty- five male patients with acne vulgaris, their ages ranged from 18-30 (21.82±3.77) years and 45 healthy male subjects as controls, their ages ranged from 18-30 (22.18±3.85) years were included in this study. Patients were subdivided into three groups according to the severity of their acne; mild acne group (n=15), moderate (n=15) and severe acne group (n=15). Investigations included serum estimation of Zn, Cu and Mg in both patient and control groups.The data obtained from this study showed that the (mean±SD) values of serum levels of Zn was significantly decreased in severe acne group compared with controls, mild and moderate type of acne group (P< 0.05). Serum Mg concentration was significantly lower in severe acne group compared with mild and moderate acne group (P< 0.05). With regard to serum Cu, there were no significant differences  among groups of patients with acne vulgaris.This study revealed a significant association between serum levels of either Zn or Mg with the severity of acne. Key words: Acne vulgaris, zinc, copper, magnesium. 
近年来,皮肤病学对锌、铜、镁在寻常痤疮中的作用及其血清水平进行了研究,但结果存在争议。本研究的目的是调查痤疮严重程度与血清锌(Zn)、铜(Cu)和镁(Mg)水平之间的关系,并证明伊拉克男性寻常痤疮患者血清锌、铜和镁水平的状况,并将其与健康对照组进行比较。本病例对照研究于2009年5月至2010年1月在巴格达教学医院皮肤病和性病科以及中毒咨询中心进行。选取年龄18-30岁(21.82±3.77)岁的男性寻常性痤疮患者45例和年龄18-30岁(22.18±3.85)岁的健康男性45例作为对照。根据痤疮的严重程度将患者分为三组;轻度痤疮组(n=15)、中度痤疮组(n=15)、重度痤疮组(n=15)。调查包括患者和对照组血清锌、铜和镁的测定。本研究数据显示,重度痤疮组血清锌水平(mean±SD)值较对照组、轻度和中度痤疮组显著降低(P< 0.05)。重度痤疮组血清Mg浓度显著低于轻度、中度痤疮组(P< 0.05)。寻常痤疮患者血清铜含量在不同组间差异无统计学意义。这项研究揭示了血清锌或镁水平与痤疮严重程度之间的显著关联。关键词:寻常痤疮,锌,铜,镁。
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引用次数: 0
Pharmaceutical quality system 药品质量体系
Q3 Pharmacology, Toxicology and Pharmaceutics Pub Date : 2014-10-27 DOI: 10.4172/2329-6631.S1.009
Lothar Hartmann
Purpose: The concept of quality is embedded in every process that takes place in an organization. There is a general perception that while increasing quality cost also increases. This perception was challenged by Dr. Genichi Taguchi. Taguchi states that quality can be increased without increasing cost and cost can also be reduced by increasing quality (Campanella 1999). Measuring quality-related costs has been advocated as an important component of quality improvement (Moen 1998). Gryna (1988) states that quality related costs range from 10-30 percent of sales and 25-40 percent of operating expenses. Researchers have proposed several methods of quality cost estimation. Commonly used methods areQuality Costing Approach, Process Cost Approach and Quality Loss Approach (Campanella, 1999). Tsiakals (1983) used Quality Costing Approach (PAF Approach) to collect Cost of Quality in a Pharmaceutical Industry and Malchi and McGurk (2001) used alternative cost model (Schiffauerova et al, 2006).The present paper aimed atcollecting and measuring Cost of Poor Quality in a Pharmaceutical Industry on the basis of Process Cost Approach.
目的:质量的概念嵌入在组织中发生的每一个过程中。人们普遍认为,在提高质量的同时,成本也在增加。田口元一博士对这种看法提出了挑战。田口指出,质量可以在不增加成本的情况下提高,成本也可以通过提高质量来降低(Campanella 1999)。测量与质量有关的成本一直被提倡作为质量改进的一个重要组成部分(Moen 1998)。Gryna(1988)指出,质量相关成本占销售额的10- 30%,占运营费用的25- 40%。研究人员提出了几种质量成本估算方法。常用的方法有质量成本法、过程成本法和质量损失法(Campanella, 1999)。Tsiakals(1983)使用质量成本法(PAF法)收集制药行业的质量成本,Malchi和McGurk(2001)使用替代成本模型(Schiffauerova et al ., 2006)。本文以过程成本法为基础,对制药企业的不良质量成本进行了收集和计量。
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引用次数: 36
期刊
Iraqi Journal of Pharmaceutical Sciences
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