A Novel Approach to Optimize and Formulate Fast Disintegrating Tablets for Nausea and Vomiting

The aim of this study was to optimize and formulate fast disintegrating tablets (FDTs) for nausea and vomiting using aminoacetic acid, carmellose and sodium alginate with enough mechanical strength. Ondansetron HCl (water soluble) or domperidone (water insoluble) drug were added to FDTs and their disintegration behaviour was evaluated. Plackett Burman Screening Design was used to screen the independent active process variables [concentration of aminoacetic acid (X ₁), concentration of carmellose (X ₂) and tablet crushing strength (X ₃)] which were found to actively influence the dependent variables [disintegration time in the mouth (DT), wetting time (WT), and water absorption ratio (WAR)] for both the drugs. Also, the coefficients of active variables (DT, WT and WAR) of FDTs containing domperidone was found to be significantly different (P < 0.05) from the coefficients of active factors (X ₁, X ₂ and X ₃) containing ondansetron HCl FDTs. Further, FDTs containing domperidone was prepared according to central composite design for estimating the effect of active factors (X ₁, X ₂, X ₃) in extended spherical domain. The regression analysis of quadratic fit revealed that DT, WT and WAR were 98% correlated with active factors (X ₁, X ₂ or X ₃). The optimized domperidone FDTs were further compared with superdisintegrants (croscarmellose sodium or crospovidone). The data revealed that optimized domperidone FDTs were better than domperidone FDTs containing croscarmellose or crospovidone. Hence, this novel excipients combination can be used for delivery of water insoluble drugs in place of superdisintegrants.     

Influence of Compression Force on The Behavior of Mucoadhesive Buccal Tablets

The purpose of this research was to study the compression force influence on polymers, tablet behavior and drug release rate. Several tablet batches were produced by varying the compression force and by using hydroxyethyl cellulose (HEC) and Carbopol 940 in the 1:1 ratio as matrix forming polymers. All batches were characterized by DSC and X-ray analyses and in terms of swelling, ex vivo and in vivo mucoadhesive time, ex vivo mucoadhesion force, and in vitro and in vivo release. No significant excipient–excipient or excipient–drug interactions were observed in any of the batches. All the tablets hydrated quickly and their high hydration percentage showed that the compression forces used did not remarkably affect the water penetration and the polymeric chain stretching. Mucoadhesion performances and drug release were mainly influenced by compression force; its increase produced higher ex vivo and in vivo mucoadhesion and the in vitro and in vivo drug releases were seen to decrease with the increase of the compression force. However tablets fabricated by using the lowest compression force showed the best in vivo mucoadhesive time and hydrated faster when compared to the others. Tablets 4 and 5, prepared with the highest forces, caused pain during in vivo application and gave rise to irritation needing to be detached by the volunteers while tablet 1, prepared with the lowest force, gave the best results because it was able to produce the highest drug salivary concentration and no pain. All tablets exhibited an anomalous release mechanism.     

Temporal characteristics of chlorophyll fluorescence quenching and dissolved oxygen concentration as indicators of photosynthetic activity in Chlorella emersonii

A simple chlorophyll fluorescence (CF) measuring system has been implemented to study temporal characteristics of chlorophyll fluorescence induction (CFI) in dark-adapted freshwater algal cultures of Chlorella emersonii. There were two different decay time constants describing the CF quenching: τ₀ (the faster) and τ₁ (the slower) with amplitudes A₀ and A₁, respectively. The relative amplitude of the faster quenching component decreased once the sample was subject to deprivation from dissolved oxygen (DO). The DO concentration of samples was monitored to validate the effects of deprivation from air contact for up to 7 d and to the effect of adding DCMU to the culture (herbicide for blocking electron transport of photosystem 2). CFI analysis and DO measurements showed that the relative amplitude of A₀ to (A₀ + A₁) and the DO concentration can be used as an indication of relative photosynthetic activity, thus allowing for the possibility to classify the physiological state of algal blooms into active and inactive states.     

Comparative in vitro and in vivo evaluation of matrix,osmotic matrix,and osmotic pump tablets for controlled delivery of diclofenac sodium

The aim of this investigation was preparation and comparative evaluation of fabricated matrix (FM), osmotic matrix (OM), and osmotic pump (OP) tablets for controlled delivery of diclofenac sodium (DS). All formulations were evaluated for various physical parameters, and in vitro studies were performed on USP 24 dissolution apparatus II in pH 7.4 buffer and distilled water. In vivo studies were performed in 6 healthy human volunteers; the drug was assayed in plasma using HPLC, and results were compared with the performance of 2 commercial tablets of DS. Various pharmacokinetic parameters (ie, C_max, T_max, area under the curve [AUC_0–24], and mean residence time) and relative bioavailability were compared. All fabricated formulations showed more prolonged and controlled DS release compared with commercial tablets studied. The OM and OP tablets, however, performed better than the matrix tablets. The rate and extent of drug release from FM1 matrix tablets (single polymer) was significantly different from that of FM2 (admixed polymers). Type of porosigenic agents and osmogens also influenced the drug release. Analysis of in vitro data by regression coefficient analysis revealed zero-order release kinetics for OM and OP tablets, while FM tablets exhibited Higuchi kinetics. In vivo results indicated prolonged blood levels with delayed peak and improved bioavailability for fabricated tablets compared to commercial tablets. It was concluded that the osmotic matrix and osmotic pump tablets could provide more prolonged, controlled, and gastrointestinal environmental-independent DS release that may result in an improved therapeutic efficacy and patient compliance.     

Effect of degree of esterification of pectin and calcium amount on drug release from pectin-based matrix tablets

The aim of this work was to assess the effect of 2 formulation variables, the pectin type (with different degrees of esterification [DEs]) and the amount of calcium, on drug release from pectin-based matrix tablets. Pectin matrix tablets were prepared by blending indomethacin (a model drug), pectin powder, and various amounts of calcium acetate and then tableting by automatic hydraulic press machine. Differential scanning calorimetry, powder x-ray diffraction, and Fourier transformed-infrared spectroscopy studies of the compressed tablets revealed no drug-polymer interaction and the existence of drug with low crystallinity. The in-vitro release studies in phosphate buffer (United States Pharmacopeia) and tris buffer indicated that the lower the DE, the greater the time for 50% of drug release (T₅₀). This finding is probably because of the increased binding capacity of pectin to calcium. However, when the calcium was excluded, the pectins with different DEs showed similar release pattern with insignificant difference of T₅₀. When the amount of calcium acetate was increased from 0 to 12 mg/tablet, the drug release was significantly slower. However, a large amount of added calcium (ie, 24 mg/tablet) produced greater drug release because of the partial disintegration of tablets. The results were more pronounced in phosphate buffer, where the phosphate ions induced the precipitation of calcium phosphate. In conclusion, both pectin type and added calcium affect the drug release from the pectin-based matrix tablets.     

参芍片联合酒石酸美托洛尔片对冠心病心绞痛患者氧化应激、血管内皮功能和心肌损伤标志物的影响

摘要 目的：探讨参芍片联合酒石酸美托洛尔片对冠心病心绞痛患者氧化应激、血管内皮功能和心肌损伤标志物的影响。方法：病例选取自我院2018年9月~2021年7月期间收治的110例冠心病心绞痛患者,按照入院的奇偶顺序将患者分为对照组（55例）和观察组（55例）,对照组患者接受酒石酸美托洛尔片治疗,观察组患者接受参芍片联合酒石酸美托洛尔片治疗,观察两组临床总有效率、心电图总有效率,对比两组临床症状、氧化应激[超氧化物歧化酶（SOD）、丙二醛（MDA）、谷胱甘肽过氧化物酶（GSH-PX）]、血管内皮功能[内皮素（ET）、血管内皮生长因子（VEGF）、一氧化氮（NO）]和心肌损伤标志物[心肌肌钙蛋白（cTn）、肌酸激酶同工酶（CK-MB）、脑钠肽（BNP）]水平变化,记录两组用药的不良反应发生率。结果：与对照组相比,观察组的临床总有效率、心电图总有效率进一步升高（P<0.05）。观察组治疗12周后心绞痛发作次数较对照组少,心绞痛持续时间较对照组短,6 min步行试验距离长于对照组（P<0.05）。治疗12周后,观察组VEGF、ET水平低于对照组,NO水平高于对照组（P<0.05）。治疗12周后,观察组CK-MB、cTn、BNP水平低于对照组（P<0.05）。治疗12周后,观察组MDA水平低于对照组,SOD、GSH-PX水平高于对照组（P<0.05）。两组不良反应发生率组间对比无差异（P>0.05）。结论：参芍片联合酒石酸美托洛尔片治疗冠心病心绞痛患者,可促进症状改善,减轻机体氧化应激和血管内皮损伤,发挥较好的心肌保护作用。     

同型半胱氨酸与H型高血压左室肥厚的相关性及马来酸依那普利叶酸片的干预效果

目的:探讨同型半胱氨酸(Hcy)与H型高血压左室肥厚的相关性及马来酸依那普利叶酸片的干预效果。方法:选取达州市中心医院于2015年8月-2017年7月收治的450例原发性高血压患者,根据血浆Hcy水平将患者分为Hcy正常组(n=134)和H型高血压组(n=316),比较Hcy正常组、H型高血压组患者超声心动图检测指标的差异,并对Hcy水平与左心室结构改变进行相关性分析。同时将316例H型高血压患者随机分为观察组(n=158)和对照组(n=158),其中对照组患者给予马来酸依那普利片治疗,观察组给予马来酸依那普利叶酸片治疗。两组均连续治疗24个月。分别于治疗前、治疗后6个月、12个月、24个月检测血压、血浆Hcy和左心室质量指数(LVMI)水平,观察脑卒中及药物不良反应发生情况。结果:H型高血压组左室收缩末内径(LVESD)、左室舒张末内径(LVEDD)、左室后壁厚度(LVPWT)、室间隔厚度(IVST)、左心室质量(LVM)、LVMI均较Hcy正常组增大(P0.01)。血浆Hcy与LVPWT、IVST、LVM及LVMI呈正相关(r=0.652、0.526、0.736、0.786,均P0.05);治疗后6个月、12个月、24个月,观察组与对照组的H型高血压患者收缩压(SBP)、舒张压(DBP)水平及观察组Hcy、LVMI均较治疗前降低(P0.05),且观察组SBP、DBP、Hcy及LVMI均低于同时间点的对照组(P0.05)。两组均未见严重药物不良反应发生,观察组脑卒中发生4例(2.53%)较对照组12例(7.59%)明显减少,差异有统计学意义(P0.05)。结论:血浆Hcy水平是影响原发性高血压患者左心室肥厚的危险因素;马来酸依那普利叶酸片干预H型高血压患者后可显著降低血压、血浆Hcy水平,改善患者左心室肥厚程度,降低脑卒中发生率。     

左旋氨氯地平联合心理干预治疗高血压伴更年期综合征患者的疗效观察

目的:探讨左旋氨氯地平联合心理干预治疗高血压伴更年期综合征的疗效;方法:将100例高血压伴更年期综合征患者随机分为两组,对照组给予左旋氨氯地平+常规更年期综合征治疗,联合组给予左旋氨氯地平+心理干预+常规更年期综合征治疗,采用汉密尔顿焦虑量表(HAMA)和抑郁量表(HAMD)评分评估患者主要症状改善情况,对比两组临床疗效及卵巢功能。结果:治疗1个月后,两组患者血压均降低,联合组降压总有效率为92.0%,优于对照组的52.0%,比较有显著性差异(P0.05);与对照组相比,联合组血清促卵泡成熟激素(FSH)和促黄体生成素(LH)下降明显,雌激素(E2)水平显著上升,两组比较有显著性差异(P0.01);联合组症状积分改善较为显著,明显优于对照组(P0.01)。结论:左旋氨氯地平联合心理干预对治疗高血压伴更年期综合征具有显著的疗效,可有效降低患者血压,改善负性情绪。     

高效液相色谱法测定氟伐他汀钠缓释片的含量

建立高效液相色谱法测定含量和含量均匀度的方法。采用SHIMADZU CLC-ODS色谱柱,以乙睛-水-冰醋酸(380∶120∶0.2)为流动相,234nm波长处检测。氟伐他汀钠在41μg/mL~328μg/mL浓度范围内线性关系良好(r=0.9998),平均回收率为100.5%,相对标准偏差(relative standaral deviation,RSD)0.5%(n=9)。本方法具有简单,柱效高,经济等优点。