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In Vitro Release Kinetic Study of Ciprofloxacin HCl from Methocel K15M CR, Methocel K4M CR and Methocel K4M Premium Matrix Tablets 盐酸环丙沙星在Methocel K15M CR、Methocel K4M CR和Methocel K4M优质基质片中体外释放动力学研究
Pub Date : 2010-08-12 DOI: 10.3329/SJPS.V2I1.5814
Muhammad Shahidul Islam, T. Haque, R. Jahangir, K. Fatema, M. Vhuiyan, I. J. Biva
In the present study Ciprofloxacin HCl sustained release matrix tablet was prepared by utilizing different grades of hydroxypropyl methylcellulose (HPMC) polymers such as Methocel K4M CR, Methocel K4M Premium & Methocel K15M CR by direct compression method. Different amount of Methocel K15M CR was used to develop matrix builder in the three proposed formulations (F1-F3) for the study of release rate retardant effect at 5%, 6%, and 7% of total weight of tablet matrix respectively. The dissolution study of Methocel K15M CR based tablet matrices of those proposed formulations were carried out in the simulated gastric medium (pH 1.3) for 8 hours using USP dissolution apparatus II. Similarly Methocel K4M premium was used to develop matrix builder in another three proposed formulations (F4-F6). It was found that formulations F-4 (15%), F-5 (17%) and F-6 (18.3%) met the desired release rate of Ciprofloxacin HCl for 8hrs period. The release kinetics of formulation F-4, F-5 and F-6 followed Higuchi kinetic order. Again Methocel K4M premium was used for another three proposed formulations (F7-F9). It was found that formulations F-7 (6.7%), F-8 (12.3%) and F-9 (15.6%) met the desired release rate of Ciprofloxacin HCl for 8hrs period. The release kinetics of formulation F-7, F-8 and F-9 followed Higuchi kinetic order. Among these three polymers, Methocel K4M Premium showed better release retardant effect than Methocel K4M CR and Methocel K15M CR. Key Words: Ciprofloxacin HCl; Direct compression; Controlled release; Methocel K15M CR; Methocel K4M CR; Methocel K4M premium. DOI: 10.3329/sjps.v2i1.5814 Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 37-43
以不同等级的羟丙基甲基纤维素(HPMC)聚合物Methocel K4M CR、Methocel K4M Premium和Methocel K15M CR为原料,采用直接压缩法制备盐酸环丙沙星缓释基质片。以不同用量的Methocel K15M CR作为基质构建剂,分别在片剂总重量的5%、6%和7%时对缓释效果进行研究。采用USP溶出度仪II对上述处方的Methocel K15M CR片基质在模拟胃介质(pH 1.3)中溶出度进行了8小时的研究。同样,Methocel K4M premium也用于开发另外三种建议配方(F4-F6)中的基质构建剂。处方F-4(15%)、F-5(17%)和F-6(18.3%)满足环丙沙星8h的期望释放率。剂型F-4、F-5和F-6的释放动力学符合Higuchi动力学顺序。另外三种建议的配方(F7-F9)再次使用Methocel K4M溢价。处方F-7(6.7%)、F-8(12.3%)和F-9(15.6%)满足环丙沙星8h的期望释放率。制剂F-7、F-8和F-9的释放动力学符合Higuchi动力学顺序。三种聚合物中,Methocel K4M Premium的缓释效果优于Methocel K4M CR和Methocel K15M CR。关键词:环丙沙星HCl;直接压缩;控制释放;Methocel K15M CR;Methocel K4M CR;Methocel K4M premium。DOI: 10.3329/sjps.v2i1.5814斯坦福药物科学杂志Vol.2(1) 2009: 37-43
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引用次数: 5
Effect of raw materials on drug release from developed Ciprofloxacin tablets 原料对所制环丙沙星片药物释放的影响
Pub Date : 2010-08-12 DOI: 10.3329/SJPS.V2I2.5819
H. Ali, J. Aslam, Bazigah Rasool, S. Khan, Alaa Agondi
The present study was undertaken to assess and evaluate the effect of two parameters on tablet formulation of Ciprofloxacin: a) particle size of raw material and b) storage conditions of both raw material and finished product. The raw materials were two commercial products, coarse (RM1) and fine (RM2) and locally produced granular form (RM3) prepared from RM2. Three tablet formulations were prepared from the raw materials and designated as F1, F2 and F3. The formulation F1 were prepared from RM1, F2 from RM2 by slugging and F3 from RM3 by direct compression. The raw materials and finished products were then subjected to assessment of the different parameters at the time of production and after storage for three month. The particle size distribution for the raw materials was found to be 250 μm for RM2, RM1 and RM3, respectively. The moisture uptake at 25°C and 4°C under 75% RH was found to be the highest for the fine powder raw material (RM2), however, the developed granular form RM3 showed the least uptake. Moreover, F2 did not attain 80% dissolution after storage of 3 month. The F1 and F3 formulation passed the dissolution test after storage of 3 month, hence, F3 showed the highest value of dissolution (82%) in 30 minutes. The physicochemical properties of raw materials, storage conditions, and manufacturing techniques were found to exert a great influence over the dissolution behavior of Ciprofloxacin tablet formulations. Key words: Ciprofloxacin tablets; dissolution behavior; physicochemical properties; storage conditions DOI: 10.3329/sjps.v2i2.5819 Stamford Journal of Pharmaceutical Sciences Vol.2(2) 2009: 8-15
本研究对环丙沙星片剂处方中两个参数的影响进行了评价:a)原料粒度和b)原料和成品的储存条件。原料是两种商业产品,粗(RM1)和细(RM2)和本地生产的颗粒状(RM3)由RM2制备。以该原料为原料制备3种片剂,分别命名为F1、F2和F3。配方F1由RM1、RM2经段塞法制备F2、RM3经直接压缩制备F3。然后在生产时和储存三个月后对原材料和成品进行不同参数的评估。RM2、RM1和RM3的粒径分布均为250 μm。在25°C和4°C 75% RH条件下,细粉状原料(RM2)的吸湿量最大,而发育的颗粒状原料RM3的吸湿量最少。贮藏3个月后,F2溶出度达不到80%。F1和F3在贮存3个月后通过了溶出度测试,其中F3在30分钟内溶出度最高(82%)。原料的理化性质、贮存条件和制备工艺对环丙沙星片剂的溶出行为有很大影响。关键词:环丙沙星片;溶解行为;物理化学性质;储存条件DOI: 10.3329/sjps.v2i2.5819斯坦福制药科学杂志Vol.2(2) 2009: 8-15
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引用次数: 1
Development of L-PLA based Intrascleral Implant for Sustained Intraocular Delivery of Dexamethasone Sodium Phosphate L-PLA基巩膜内植入体用于持续眼内给药地塞米松磷酸钠的研制
Pub Date : 2010-08-12 DOI: 10.3329/SJPS.V2I1.5817
Nazia Zaman, M. Talukder, T. Haque, K. Alam, K. Fatema
The present study was carried out to develop biodegradable intrascleral implants of Dexamethasone Sodium Phosphate and to evaluate the release pattern of the drug from the prepared implants. Intrascleral implants were prepared by using biodegradable polymer L-PLA (m.wt. 61,200 Da). Sodium chloride (NaCl), gelatin and glycerol monostearate (GMS) were used in various formulations to observe the effects of these additives on the release of Dexamethasone Sodium Phosphate from the prepared L-PLA based intrascleral implants. Five different formulations were prepared for this study and were coded as FD-1 (10%drug+L-PLA), FD-2 (20%drug+L-PLA), FD-3 (10%drug+L-PLA+5%NaCl), FD-4 (10%drug+L-PLA +5%Gelatin) and FD-5 (10%drug+L-PLA+10% GMS). Discs were prepared and made into appropriate shape before submerging into the buffer solution of pH 7.4 in different vials. The in vitro release profile of Dexamethasone Sodium Phosphate from the implants showed a biphasic release pattern with an initial burst followed by a diffusive phase. It was observed that FD-1 and FD-2 showed 19.63% and 29.87% release on the first day and 24.22% and 38.5% release respectively at day 30. The drug loading of FD-1 and FD-2 was 10% and 20% respectively. Among FD-3, FD-4 and FD-5; FD-3 showed highest release (32.1%) at day 30 in which 5% NaCl was used. FD-4 showed 27.45% release at day 30 where gelatin, a hydrophilic agent was used and FD-5 containing GMS, a lipid material, was found to be most retarding (19.22% at day 30). The results of the dissolution study provide an idea that L-PLA may be successfully used for the preparation of biodegradable intrascleral implant of Dexamethasone Sodium Phosphate. Key words: Dexamethasone Sodium Phosphate; Bioidegradable polymer; Intrascleral implants. DOI: 10.3329/sjps.v2i1.5817 Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 56-60
本研究旨在制备可生物降解的地塞米松磷酸钠巩膜内植入物,并评价该药物在制备的植入物中的释放规律。采用可生物降解聚合物L-PLA (m.wt)制备巩膜内植入物。61200 Da)。采用氯化钠(NaCl)、明胶(明胶)和单硬脂酸甘油(GMS)配制不同配方,观察这些添加剂对制备的L-PLA基巩膜内植入物中地塞米松磷酸钠释放的影响。制备了5种不同的配方,分别编码为FD-1(10%药物+L-PLA)、FD-2(20%药物+L-PLA)、FD-3(10%药物+L-PLA+5%NaCl)、FD-4(10%药物+L-PLA+5%明胶)和FD-5(10%药物+L-PLA+10% GMS)。制备膜片,并将膜片制作成合适的形状,放入不同小瓶pH为7.4的缓冲液中浸泡。地塞米松磷酸钠的体外释放表现为两相释放模式,先是爆发期,然后是扩散期。观察发现,FD-1和FD-2在第1天的释放量分别为19.63%和29.87%,第30天的释放量分别为24.22%和38.5%。FD-1和FD-2的载药量分别为10%和20%。其中FD-3、FD-4、FD-5;在5% NaCl处理下,FD-3在第30天释放量最高,为32.1%。FD-4在第30天的释放率为27.45%,其中使用了亲水性明胶,而含有脂质材料GMS的FD-5在第30天的释放率为19.22%。溶出度研究结果为L-PLA可成功用于制备可生物降解的地塞米松磷酸钠巩膜内植入物提供了思路。关键词:地塞米松磷酸钠;Bioidegradable聚合物;Intrascleral植入物。DOI: 10.3329/sjps.v2i1.5817斯坦福药物科学杂志Vol.2(1) 2009: 56-60
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引用次数: 1
Comparative Dissolution Study of Different Brands of Amoxicillin Trihydrate Capsules Available in Bangladesh 孟加拉国不同品牌三水合阿莫西林胶囊溶出度比较研究
Pub Date : 2010-08-12 DOI: 10.3329/SJPS.V2I2.5827
N. Huda, Y. Jhanker, A. Shahid-ud-Daula, Most. Nazma Parvin, Shammy Sarwar
Commercially available twenty national and four multinational brands of Amoxicillin Trihydrate capsules were studied  in water  for 60 minutes using USP reference dissolution apparatus. All, except  two national brands (Code: NB-8 and NB-15); complied with  the USP  in vitro dissolution specification  for drug release (not  less than 80% of the labelled amount of amoxicillin trihydrate should be dissolved in 60 minutes). Drug releases from those two brands were 75% and 67% respectively within the specified time period. Key words: In vitro Dissolution; Market preparations; Amoxicillin Trihydrate; Capsule; National Brand; Multinational Brand. DOI: 10.3329/sjps.v2i2.5827 Stamford Journal of Pharmaceutical Sciences Vol.2(2) 2009: 72-75
用USP标准溶出度仪对市售的20个国家品牌和4个跨国品牌的三水合阿莫西林胶囊进行了60分钟的水溶出度研究。除两个国家品牌(代码:NB-8和NB-15)外;符合USP体外释放度标准(不少于三水阿莫西林标记量的80%应在60分钟内溶出)。两个品牌在规定时间内的释药率分别为75%和67%。关键词:体外溶出度;市场准备工作;阿莫西林三水合物;胶囊;国家品牌;跨国品牌。DOI: 10.3329/sjps.v2i2.5827斯坦福制药科学杂志Vol.2(2) 2009: 72-75
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引用次数: 3
Comparative Evaluation of HPMC, PVA and Gelatin as Matrices for Controlled Release Drug Delivery HPMC、PVA和明胶作为控释给药基质的比较评价
Pub Date : 2010-08-12 DOI: 10.3329/SJPS.V2I1.5816
M. Basher, A. Kabir, M. M. Hussain, M. Mamun
The present study was undertaken to compare three different polymeric gums- HPMC, PVA and gelatin as controlled release matrices. Diclofenac sodium, a potent analgesic, was used as the model drug. Different ratio of HPMC, PVA and gelatin were incorporated into the lactose loaded Diclofenac tablet to explore their impact on drug release. Matrix tablets of Diclofenac were prepared by using individual polymer with magnesium stearate and aerosil by direct compression process at 5 ton pressure. The release of drug from these matrices was studied over 2 hrs in acidic media where insignificant release was observed. Then, the same formulations were studied over 8 hours in buffer media of pH 6.8 at a temperature of 37± 0.5°C. Statistically significant differences in drug release profile was found among the tablets prepared from different matrices. The study revealed that the average % release of drug from different types of polymer loaded matrix tablet varied with the ratio of different polymers. Among the three polymers, PVA showed best dissolution pattern. A comparison of Higuchi curve and bi-exponential curve was also performed. Key words: HPMC; PVA; Gelatin; Controlled release; Diclofenac DOI: 10.3329/sjps.v2i1.5816 Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 51-55
本研究比较了三种不同的聚合物胶- HPMC, PVA和明胶作为控释基质。双氯芬酸钠是一种强效镇痛药,被用作模型药物。将不同比例的HPMC、PVA和明胶掺入乳糖负载双氯芬酸片中,探讨其对药物释放的影响。在5吨压力下,采用硬脂酸镁和气相油为原料,采用单体聚合物直接压缩法制备双氯芬酸基质片。在酸性介质中研究药物在2小时内的释放,没有观察到药物的释放。然后,在pH为6.8的缓冲介质中,在37±0.5°C的温度下,研究相同的配方超过8小时。不同基质制备的片剂药物释放谱差异有统计学意义。研究表明,不同类型的聚合物负载型基质片的平均释药率随聚合物配比的不同而不同。在三种聚合物中,PVA表现出最好的溶解模式。并对Higuchi曲线和双指数曲线进行了比较。关键词:HPMC;PVA;明胶;控制释放;双氯芬酸DOI: 10.3329/sjps.v2i1.5816斯坦福德制药科学Vol.2(1) 2009: 51-55
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引用次数: 1
In vitro Evaluation of Antioxidant Potential of Leaves of Opuntia dillenii Haw. 山楂叶抗氧化能力的体外评价。
Pub Date : 2010-08-12 DOI: 10.3329/SJPS.V2I1.5811
R. Akter, S. Hasan, Mokarram Hossain, Taksim Ahmed, M. M. Majumder, Masuda Akter
Antioxidant potential of the 80% methanol extract of the leaves of Opuntia dillenii was evaluated using 1, 1-diphenyl, 2-picryl hydrazyl (DPPH) and nitric oxide radical scavenging, reducing power, total phenol and total flavonoid content determination assays. Preliminary phytochemical screening of the extract was also carried out, which revealed that the extract possesses flavonoids, steroids, alkaloids and tannins. The extract showed significant antioxidant activities in all antioxidant assays compared to the reference antioxidant in a dose dependent manner. In DPPH radical scavenging activity, the IC 50 value of the crude extract was found to be 15.71μg/mL while the IC50 value for the reference ascorbic acid was 10.84 μg/mL. Again, the extract showed remarkable nitric oxide scavenging potential and good reducing power. Moreover, the methanol extract was found to contain high amount of phenols and flavonoids, expressed as gallic acid and rutin equivalents respectively. Based on the findings of the present study, we conclude that the methanol extract of the leaves of O. dillenii possesses remarkable antioxidant potential which may be attributed to the high amount of phenols and flavonoids present in the extract. Key Words: Opuntia dillenii ; Antioxidant; Reactive oxygen species; DPPH; Nitric oxide radical DOI: 10.3329/sjps.v2i1.5811 Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 22-26
采用1,1 -二苯基,2-苦味酰肼(DPPH)和一氧化氮自由基清除力、还原力、总酚和总黄酮含量测定法,对80%甲醇提取物的抗氧化能力进行了评价。对提取物进行了初步的植物化学筛选,发现提取物含有黄酮类化合物、甾类化合物、生物碱和单宁。与参比抗氧化剂相比,该提取物在所有抗氧化试验中均表现出显著的抗氧化活性,且呈剂量依赖性。粗提物对DPPH自由基的IC50值为15.71μg/mL,对参比抗坏血酸的IC50值为10.84 μg/mL。再次,提取物显示出显著的一氧化氮清除潜力和良好的还原力。此外,甲醇提取物含有大量的酚类和类黄酮,分别以没食子酸和芦丁当量表示。综上所述,黄酮和酚类化合物的含量较高,可能是黄酮和酚类化合物含量较高的主要原因。毕业论文关键词:冬青;抗氧化剂;活性氧;DPPH;一氧化氮自由基DOI: 10.3329/ spps .v2i1.5811斯坦福德药物科学杂志Vol.2(1) 2009: 22-26
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引用次数: 1
Formulation Development and Evaluation of Mouth Dissolving Tablets of Loratadine 氯雷他定口腔溶出片的处方研制与评价
Pub Date : 2010-08-12 DOI: 10.3329/SJPS.V2I2.5825
A. Kalam, Lutful Kabir, S. Rahman, Abu Shara, S. Rouf
Difficulty in swallowing (dysphagia) is common among all age groups, especially in elderly and pediatrics. Mouth dissolving tablets constitute an innovative dosage forms that overcome the problems of swallowing and provides a quick onset of action. The purpose of this study was to formulate and evaluate mouth dissolving tablet of loratadine using a special preparation technology (pharmaburst Technology) with a super disintegrating agent (Croscarmellose sodium). Tablets were prepared by direct compression technique. The granules were evaluated for angle of repose, bulk density, tapped density, bulkiness, compressibility index and hausners ratio. The tablets were evaluated for hardness, thickness, uniformity of weight, friability, wetting time, water absorption ratio, disintegration time and drug content. In vitro release studies were performed using USP-II (paddle method) in 900ml of pH 1.2 at 50rpm. The physical properties of the prepared tablets did not show any significant variations and were found to have good physical integrity. Tablets prepared with pharmaburst B2 and Croscarmellose sodium showed a lesser disintegration time and wetting time of 27±0.10 and 38±0.13 seconds respectively. The best formulations were subjected to stability studies at 40oC/75% RH for 60 days.
吞咽困难(吞咽困难)在所有年龄组中都很常见,尤其是老年人和儿科。口腔溶解片剂构成了一种创新的剂型,克服了吞咽的问题,并提供了一个快速的行动。本研究采用一种特殊的制备工艺(pharmaburst technology)和一种超级崩解剂(交联蜜糖钠)制备氯雷他定口腔溶片,并对其进行了评价。采用直接压缩法制备片剂。对颗粒的休止角、容重、攻丝密度、体积、压缩性指数和hausners比进行了评价。考察其硬度、厚度、重量均匀性、脆性、润湿时间、吸水率、崩解时间和药物含量。体外释放研究采用USP-II(桨法),在900ml pH 1.2中,50rpm下进行。所制片剂的物理性质无明显变化,具有良好的物理完整性。以pharmurst B2和交联棉糖钠配制的片剂崩解时间和润湿时间较短,分别为27±0.10和38±0.13 s。最佳配方在40℃/75% RH条件下稳定性研究60天。
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引用次数: 2
Pattern of Antibiotics Use at the Primary Health Care Level of Bangladesh: Survey Report-1 孟加拉国初级卫生保健一级抗生素使用模式:调查报告1
Pub Date : 2010-08-12 DOI: 10.3329/SJPS.V2I1.5809
S. Hasan, Mokarram Hossain, R. Akter, Sm Hasibul Karim, S. Haque, Kamaluddin, Abdul Ghani
Although Bangladesh has made substantial progress in drug manufacturing since the introduction of its National Drug Policy (NDP) in 1982, irrational use of drugs, inappropriate prescribing, inadequate access to essential drugs and unjustified self medication are a few of a range of problems that are affecting the total health care system seriously. Taking this in view, a survey project has been designed to conduct nationwide to explore the pattern of antibiotics use at the primary health care level in Bangladesh using carefully constructed questionnaires containing questions covering both antibiotic prescription habit of the physicians and patients’ response to antibiotic use. In the first phase of this effort, 20 Upazila Health Complexes and the Union Health Centres thereunder each of Dhaka and Chittagong division were randomly surveyed. From physician survey it was evident that 55.57% of the doctors prescribe antibiotics in suspected infection while only 33.46% of them prescribe antibiotics in confirmed cases. 40.22% of doctors prescribe antibiotics in cold and fever before any diagnostic test. Moreover, 37.31% of doctors prescribe antibiotics for pleasing the patients whereas 62.44% denied such undue influence. Doctors seldom receive feedback of completion of course of antibiotic therapy by patients. Cephalosporin was found to be the most (26.9%) preferred antibiotic in case of empirical therapy. On the other hand, it was evident from patient survey that cold, fever and acute respiratory infection (ARI) were prevalent (39.78%) causes that brought the patients to physician. 60.1 % of the patients reported that they get essential antibiotics from hospital free of cost while 24.5% of them complained that they do not get antibiotics from hospital. 34.76% of the patients reported that they complete the course of antibiotic therapy by buying antibiotics from the market whereas 56.14% of them do not buy the full course and stop taking medicine (53.46%) as soon as symptoms subside. The results of the present survey indicate that antibiotics are widely and inappropriately used without following standard guidelines or based on any rationality. This is an alarming situation, which should be properly taken care of by the relevant authority to save the people from growing antibiotic resistance. Key words: Bangladesh; Rational use; Antibiotics; Primary health care. DOI: 10.3329/sjps.v2i1.5809 Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 1-7
尽管孟加拉国自1982年实行国家药物政策以来在药品生产方面取得了重大进展,但药物的不合理使用、不适当的处方、基本药物的获取不足和不合理的自我药疗是严重影响整个卫生保健系统的一系列问题中的几个。考虑到这一点,已经设计了一个调查项目,在全国范围内开展,以探索孟加拉国初级保健一级抗生素使用的模式,使用精心设计的问卷,其中的问题包括医生的抗生素处方习惯和患者对抗生素使用的反应。在这项工作的第一阶段,随机调查了达卡和吉大港各区的20个Upazila保健中心及其下属的联盟保健中心。医师调查显示,55.57%的医生对疑似感染患者开抗生素,而对确诊病例开抗生素的比例仅为33.46%。40.22%的医生在感冒和发烧的诊断检查前开抗生素。37.31%的医生开抗生素是为了取悦患者,62.44%的医生否认存在不当影响。医生很少收到患者关于抗生素疗程完成情况的反馈。在经验性治疗中,头孢菌素是首选抗生素(26.9%)。另一方面,从患者调查中可以看出,感冒、发烧和急性呼吸道感染(ARI)是导致患者就诊的常见原因(39.78%)。60.1%的患者反映从医院免费获得必要的抗生素,24.5%的患者抱怨没有从医院获得抗生素。34.76%的患者通过从市场购买抗生素完成了抗生素治疗疗程,56.14%的患者没有购买完整疗程,症状消退后立即停药(53.46%)。本调查结果表明,抗生素的广泛和不适当使用没有遵循标准指南或基于任何合理性。这是一个令人担忧的情况,有关当局应该妥善处理,以拯救人们免受日益增长的抗生素耐药性。关键词:孟加拉国;合理使用;抗生素;初级保健。DOI: 10.3329/sjps.v2i1.5809斯坦福药物科学杂志Vol.2(1) 2009: 1-7
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引用次数: 11
In Vitro Release Kinetics Study of Different Brands of Esomeprazole Sustained Release Tablets Available in Bangladesh 孟加拉国不同品牌埃索美拉唑缓释片体外释放动力学研究
Pub Date : 2010-08-12 DOI: 10.3329/SJPS.V2I1.5812
A. Kabir, Tasbira Jesmeen, M. Talukder, Abu Taher Md Rajib, D. M. Rahman
Commercially available four national and four international brands of esomeprazole magnesium sustained release matrix tablets were studied in simulated gastric medium (pH 1.2) for 2 hours and simulated intestinal medium (pH 6.8) for 8 hours time period using USP reference dissolution apparatus. All the national and international brands complied with the USP in-vitro dissolution specifications for drug release in simulated gastric medium. However, one of the national brands (Code: MP-1) and one of the international brands (MP-7) failed to fulfill the official requirement of 80% drug release within 8th hour in simulated intestinal medium. Drug release of that national and international brand were 70.49% and 67.05% respectively within the specified time period, however one national brand (Code: MP-4) released 103.46 % drug within 8th hour in intestinal medium. Drug release profiles were analyzed for zero order, first order and Higuchi equation to reveal the release kinetics perspective of esomeprazole magnesium sustained release matrix tablets. It was found that zero order release kinetics was the predominant release mechanism than first order and Higuchi release kinetics for those brands (Code: MP-2, MP-3, MP-4, MP-5, MP-6 and MP-8) which complied with the USP in vitro dissolution specification for drug releases. On the other hand, first order release kinetics was predominant for one national and also one international non compliant brands (Code: MP-1 and MP-6). Key Words: In vitro dissolution; Sustained release; Market preparations; Kinetic analysis; Esomeprazole; National brand; International brand. DOI: 10.3329/sjps.v2i1.5812 Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 27-31
采用USP标准溶出度仪对市售4个国产、4个国际品牌的埃索美拉唑镁缓释片在模拟胃介质(pH 1.2)中2小时、模拟肠道介质(pH 6.8)中8小时的时间进行研究。所有国内、国际品牌均符合美国药典模拟胃介质药物体外释放度标准。然而,其中一个国家品牌(代码:MP-1)和一个国际品牌(MP-7)在模拟肠道介质中8小时内药物释放率达80%,均未达到官方要求。该国产品牌与国际品牌在规定时间内的释药率分别为70.49%和67.05%,而某国产品牌(代码:MP-4) 8 h内在肠道介质中的释药率为103.46%。通过零级、一级和Higuchi方程分析药物释放曲线,揭示埃索美拉唑镁缓释片的释放动力学视角。结果表明,符合美国药典体外释放度标准的品牌(药典代号:MP-2、MP-3、MP-4、MP-5、MP-6、MP-8)的释放机制以零级释放动力学为主,一级和通口释放动力学次之。另一方面,一级释放动力学在一个国家和一个国际不合规品牌(代码:MP-1和MP-6)中占主导地位。关键词:体外溶出度;持续释放;市场准备工作;动力学分析;拉唑;国家品牌;国际品牌。DOI: 10.3329/sjps.v2i1.5812斯坦福药物科学杂志Vol.2(1) 2009: 27-31
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引用次数: 1
Fasting and Post Prandial Monitoring of Dipeptidyl Peptidase-IV (DPP-IV) - A Biomarker to Assess Incretin Response in Type-2 Diabetes 空腹和餐后监测二肽基肽酶- iv (DPP-IV) -一种评估2型糖尿病肠促胰岛素反应的生物标志物
Pub Date : 2010-08-12 DOI: 10.3329/SJPS.V2I2.1698
Venkatesham Allenki, R. Devarakonda, R. N. R. Anreddy, N. Pantam, N. Yellu
Dipeptidyl peptidase-IV (DPP-IV) could serve as a potential biomarker in monitoring the disease progression and improvement on treatment. To investigate fasting & post prandial response of DPP-IV enzyme as indirect marker of incretin response failure after chronic treatment with metformin in type 2 diabetes. The study included twelve nondiabetic subjects, ten patients with glycosylated hemoglobin values (6-8%) and fifteen patients with glycosylated hemoglobin greater than 8 % of type-2 diabetes patients of either sex with metformin treatment above 3 years were recruited. Fasting and post prandial DPP-IV levels were calculated. HbA1c was used to assess diabetes status. DPP-IV activity (fasting) in type 2 diabetic subjects with HbA1c > 8 % was significantly higher DPP-IV (44.67 ± 2.19 U/l) than in non diabetic subjects (24.39 ± 3.97 U/l). A significant correlation between DPP-IV (fasting / post prandial) and HbA1c (r = 0.821 & r = 0.732, P< 0.01) was observed in both diabetic (HbA1c 6-8, HbA1c < 8) patients. Hyperglycemia induces significant increase in serum DPP-IV activity in fasting condition and might contribute to the reduction in active glucagon like peptide-1(GLP-1) in type 2 diabetic subjects. In normal subjects during post prandial condition, there is sudden increase followed by decrease of GLP-1 due to cleavage of GLP-1 to as substrate of DPP-IV is seen as upsurge of DPP-IV. This response was lacking in diabetic patients with high HbA1c indicates indirectly metformin failure to secrete GLP-1. High fasting level and decreased post prandial of DPP-IV may indicate drug failure in type-2 diabetes mellitus. Key words: Type 2 diabetes; metformin; DPP-IV; HbA1c; GLP-1. DOI: 10.3329/sjps.v2i2.1698 Stamford Journal of Pharmaceutical Sciences Vol.2(2) 2009: 81-85
二肽基肽酶- iv (DPP-IV)可作为监测疾病进展和治疗改善的潜在生物标志物。探讨DPP-IV酶作为2型糖尿病慢性二甲双胍治疗后肠促胰岛素反应失败的间接标志的空腹和餐后反应。本研究纳入了12名非糖尿病受试者、10名糖化血红蛋白值(6-8%)的患者和15名糖化血红蛋白值大于8%的2型糖尿病患者,这些患者不分性别,接受二甲双胍治疗3年以上。计算空腹和餐后DPP-IV水平。HbA1c用于评估糖尿病状态。2型糖尿病HbA1c患者空腹DPP-IV活性(44.67±2.19 U/l)明显高于非糖尿病患者(24.39±3.97 U/l)。两组糖尿病患者(HbA1c 6 ~ 8, HbA1c < 8) DPP-IV(空腹/餐后)与HbA1c均有显著相关性(r = 0.821 & r = 0.732, P< 0.01)。高血糖导致空腹状态下血清DPP-IV活性显著升高,并可能导致2型糖尿病患者胰高血糖素样肽-1(GLP-1)活性降低。正常受试者在餐后状态下,由于GLP-1裂解为DPP-IV的底物,导致GLP-1突然升高后又下降,视为DPP-IV的高涨。高HbA1c的糖尿病患者缺乏这种反应,间接表明二甲双胍不能分泌GLP-1。2型糖尿病患者空腹DPP-IV水平高,餐后DPP-IV水平低可能提示用药失败。关键词:2型糖尿病;二甲双胍;DPP-IV;糖化血红蛋白;GLP-1。DOI: 10.3329/sjps.v2i2.1698斯坦福制药科学杂志Vol.2(2) 2009: 81-85
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引用次数: 1
期刊
Stamford Journal of Pharmaceutical Sciences
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