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Phytochemical Evaluation of Ficus Carica Seeds and their Cold Pressed Oil 无花果种子及其冷榨油的植物化学评价
Pub Date : 2021-12-15 DOI: 10.18579/jopcr/v20i4.2
Zeliha Ustun­-Argon, Z. Sarı, A. Gokyer, Sidika Buyukhelvacigil­-Ozturk
The use of plant materials as the source of oil and functional foods is becoming more important with the new trends and scientific research. In this study, fig (Ficus carica) seed, which is a rarely found, seed and its oil, have been studied to determine the phytochemical properties for possible applications. Fig seeds were obtained from Aydın, Turkey. The oil was extracted by the cold press method. The seeds were analyzed for oil yield, protein, ash, ash insoluble in hydrochloric acid and trace elements. The oil was evaluated for fatty acid, sterol compositions by GC and the volatiles were analyzed with GCMS, tocopherols analyzed by HPLC, total phenolic content and antioxidant activity were determined spectrophotometrically. The oil was also evaluated for free fatty acid (FFA), refractive index (RI), peroxide (PV) and p-anisidine value. The results showed that F. carica has 22.7% oil yield and was characterized by linolenic (41.27%), linoleic (30.06%), and oleic acids (18.10%). Total phenolics were 79.5 mg GAE/100 g, and nine different sterol components were analyzed and β-sitosterol was at the highest rate. Theα-β-γ-δ tocopherol content was 6.088, 0.18, 634, 18 mgkg-1, respectively. Antioxidant capacity was 52.54%. Fenchone, cymene, styrene d-limonene, linalool, camphor were found as important volatiles. Quality parameters were FFA (% oleic acid) 0.90, RI (40 oC) 1.4721, PV (meq O2/kg oil) 2.2, p-anisidine 2.22. As a result, F. carica oil can be an alternative oil source and a good option for functional foods with their rich contentof phytochemicals. For the future, more studies need to be done for both the seeds and the oil for further applications. Keywords Ficus carica seed, cold-pressed oil, fig seed, phytochemical properties
随着新的趋势和科学研究,利用植物材料作为油脂和功能食品的来源变得越来越重要。本研究对无花果(Ficus carica)这一罕见的植物种子及其油进行了研究,以确定其可能的应用价值。无花果种子来自Aydın,土耳其。用冷压法提取油。对种子进行了含油量、蛋白质、灰分、盐酸不溶灰分和微量元素分析。采用气相色谱法测定其脂肪酸、甾醇成分,气相色谱法测定挥发物,高效液相色谱法测定其生育酚,分光光度法测定其总酚含量和抗氧化活性。还对油进行了游离脂肪酸(FFA)、折射率(RI)、过氧化物(PV)和对茴香胺值的评价。结果表明,油麻的产油率为22.7%,主要成分为亚麻酸(41.27%)、亚油酸(30.06%)和油酸(18.10%)。总酚含量为79.5 mg GAE/100 g,分析了9种不同的甾醇成分,其中β-谷甾醇含量最高。α-β-γ-δ生育酚含量分别为6.088、0.18、634、18 mgkg-1。抗氧化能力为52.54%。凤耳酮、花香烃、苯乙烯d-柠檬烯、芳樟醇、樟脑是重要的挥发物。质量参数为:FFA(%油酸)0.90,RI(40℃)1.4721,PV (meq O2/kg油)2.2,对茴香胺2.22。因此,蓖麻油具有丰富的植物化学成分,可以作为一种替代油源和功能性食品的良好选择。为了进一步的应用,需要对其种子和油进行更多的研究。无花果籽;冷榨油;无花果籽
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引用次数: 1
Validation of Novel RP-HPLC Method for the Estimation of Naloxegol in Pharmaceutical Dosage Forms 新型反相高效液相色谱法测定药物剂型中纳洛格尔含量的验证
Pub Date : 2021-12-15 DOI: 10.18579/jopcr/v20i4.suneetha
A. Suneetha, G. Priyadarshini, V. Mounika, A. Ameen, K. Jyothi, A. Babitha
Background: Naloxegol is a peripherally acting µ-opioid antagonist. Purpose: The aim of the present research was to develop and validate a Reverse Phase High-Performance Liquid Chromatography for quantitative determination of Naloxegol in pharmaceutical dosage forms. Methodology: HPLC system used was Shimadzu coupled to a Photodiode Array Detector and was operated in an isocratic mode. Separation was achieved using Inertsil-C18 ODS column having dimensions 250 mm × 4.6 mm, 5 μm and the mobile phase composed of 90 volumes of methanol and 10 volumes of acetonitrile mixture. The flow rate of the mobile phase was 1 mL min−1. Detection wavelength was 250 nm and temperature was 25°C. Findings: The method was validated with regard to linearity, accuracy, precision, selectivity, and robustness in accordance with ICH guidelines. Conclusion: From this study it was concluded that the proposed method is accurate, reproducible and precise. Application: The method was applied successfully for the estimation of Naloxegol in marketed tablet dosage form. Keywords High-Performance Liquid Chromatography, Naloxegol
背景:纳洛戈洛是一种外周作用的微阿片拮抗剂。目的:建立并验证反相高效液相色谱法定量测定药物剂型中纳洛格尔的方法。方法:采用岛津耦合光电二极管阵列检测器的高效液相色谱系统,在等压模式下运行。采用尺寸为250 mm × 4.6 mm,尺寸为5 μm的Inertsil-C18 ODS色谱柱进行分离,流动相为90体积甲醇和10体积乙腈混合物。流动相流速为1 mL min - 1。检测波长为250 nm,温度为25℃。结果:该方法在线性、准确度、精密度、选择性和稳健性方面均符合ICH指南。结论:本方法准确、重现性好、精密度高。应用:该方法可用于市售纳洛格尔片剂的质量评价。高效液相色谱法;纳洛egol
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引用次数: 0
LC–MS/MS Determination of Prednisone, A Drug in Phase 4 of Multiple Sclerosis Therapy along with Teriflunomide and Pioglitazone in Rat Plasma LC–MS/MS法测定大鼠血浆中多发性硬化症4期药物泼尼松与特立氟胺和吡格列酮的浓度
Pub Date : 2021-12-15 DOI: 10.18579/jopcr/v20i4.ms21076
R. Rajeswari, A. Suneetha
Combination therapy or polytherapy is that uses more than one medication to treat a single disease and associated diseases. Pharmaceutical combination therapy may be achieved by prescribing separate drugs, or, where available, dosage forms that contain more than one active ingredient. A randomized efficacy phase 4 study is going on for prednisone in the treatment of multiple sclerosis, which is a neurodegenerative disease associated with many other disorders. A novel and accurate liquid chromatography tandem mass spectrometry method using electrospray ionization mode has been developed and validated for the simultaneous determination of prednisone (PDN), pioglitazone (PGZ) and teriflunomide (TFM) using imipramine (IMP) and ibuprofen (IBP) as internal standards (IS). The separation was carried on XTerra MS C18 (100 mm x 3.9 mm, 5 µm) reversed phase column using acetonitrile and 0.01M ammonium formate as the mobile phase in gradient mode at 1.0 mL/min. The method was validated in terms of specificity, linearity, accuracy and precision over the concentration range of 1–500 ng/mL. The intra and inter-day precision and accuracy, stability and extraction recoveries of all the analytes were found in the range of 97.2-102.2%. The lower limit of quantitation was 1.0 ng/mL for all the 3 analytes and the extraction recovery values were more than 65%. The method proved highly reproducible and sensitive and was successfully applied to pharmacokinetic study after single dose oral administration of PDN, PGZ and TFM to the rats. Keywords Polytherapy, Teriflunomide, Prednisone, Pioglitazone, Phase 4, Multiple Sclerosis, Pharmacokinetics
联合疗法或综合疗法是使用一种以上的药物来治疗一种疾病和相关疾病。药物联合治疗可以通过开出单独的药物,或在可用的情况下,含有一种以上活性成分的剂型来实现。一项针对强的松治疗多发性硬化症的随机疗效4期研究正在进行,多发性硬化症是一种与许多其他疾病相关的神经退行性疾病。建立了以丙咪嗪(IMP)和布洛芬(IBP)为内标(IS)同时测定强的松(PDN)、吡格列酮(PGZ)和特立氟米特(TFM)的电喷雾电离模式液相色谱串联质谱分析方法,并进行了验证。色谱柱为XTerra MS C18 (100 mm × 3.9 mm, 5µm)反相色谱柱,流动相为乙腈和0.01M甲酸铵,梯度分离速度为1.0 mL/min。在1 ~ 500 ng/mL的浓度范围内,对该方法的特异性、线性度、准确度和精密度进行了验证。所有分析物的日内、日间精密度、准确度、稳定性和提取回收率在97.2 ~ 102.2%范围内。3种分析物的定量下限均为1.0 ng/mL,提取回收率均大于65%。该方法重复性好,灵敏度高,成功应用于大鼠单次口服PDN、PGZ和TFM后的药代动力学研究。关键词综合疗法,特立氟米特,强的松,吡格列酮,4期,多发性硬化,药代动力学
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引用次数: 0
Solvent Extraction and Phytochemical Screening of Seeds, Coats, Pods and Leaves of Moringa Plant 辣木种子、皮、荚和叶的溶剂提取及植物化学筛选
Pub Date : 2021-11-10 DOI: 10.33140/jpr.06.02.06
The potency of six different solvents in extracting phytochemicals from the seeds, coats, pods and leaves of moringa plant was investigated. The seeds, coats, pods and leaves of the plant were cut into smaller pieces, air-dried, ground into powdery sample, sieved with 40 mm mesh size and properly labelled. Each sample was individually extracted using six different solvents (methanol, ethanol, chloroform, ethyl acetate, water and acetone) at ratio 1: 10 for 72 h. Each solvent extract was screened for twelve phytochemicals (alkaloid, flavonoid, saponin, cardiac glycoside, reducing sugar, tannin, quinone, volatile oil, phenol, terpenoid, phlobatannin and steroid). It was observed that the seeds and leaves of moringa plant were richest in phytochemicals followed by moringa pods and the least was in moringa coat. In all the six solvents used, thirty-four bioactive ingredients were detected in seeds and leaves of moringa plant while twenty-eight phytochemicals were obtained in moringa pods and twenty-one bioactive ingredients were gotten from moringa coats. In all the plant samples, twenty-three bioactive ingredient were detected in ethanol extract; twenty-one were obtained in each of acetone, ethyl acetate and methanol extracts; water extract had sixteen phytochemicals and chloroform extract had fifteen bioactive ingredients. Among the solvents used for extraction for all the plant samples, ethanol ranked first while acetone, ethyl acetate and methanol ranked second, water ranked third and chloroform was the least in ranking.
研究了6种不同溶剂对辣木种子、皮、荚和叶中植物化学物质的提取效果。将植物的种子、外皮、豆荚和叶子切成小块,风干,磨成粉状样品,用40毫米的筛孔筛过,并适当地贴上标签。每个样品分别使用6种不同的溶剂(甲醇、乙醇、氯仿、乙酸乙酯、水和丙酮)以1:10的比例提取72小时。每种溶剂提取物筛选12种植物化学物质(生物碱、类黄酮、皂苷、心糖苷、还原糖、单宁、醌、挥发油、苯酚、萜类、酞菁和类固醇)。结果表明,辣木种子和叶片中化学物质含量最高,豆荚次之,皮中化学物质含量最低。在6种溶剂中,从辣木种子和叶片中检出34种生物活性成分,从辣木豆荚中检出28种植物化学物质,从辣木皮中检出21种生物活性成分。在所有植物样品中,乙醇提取物检测到23种生物活性成分;丙酮提取液、乙酸乙酯提取液和甲醇提取液各提取21个;水提取物含有16种植物化学物质,氯仿提取物含有15种生物活性成分。在所有植物样品的提取溶剂中,乙醇排在第一位,丙酮、乙酸乙酯和甲醇排在第二位,水排在第三位,氯仿排在最后。
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引用次数: 2
Relationship of Amniotic Fluid Index (AFI) Between Maternal and Perinatal in Patients 羊水指数(AFI)与产妇及围产期的关系
Pub Date : 2021-09-20 DOI: 10.9734/JPRI/2021/V33I44A32638
Neranjana Manimekalai
Background : Alcohol amniotic, a protecting fluid that surround the embryo. It protects from concussion, pressure, desiccation, reminiscent of the aquatic origin of life. Adequate amount of amniotic fluid is essential requirement for the normal development and it acts like a cushion against trauma, agitation and accidental impulsions. It has also bacteriostatic properties and prevents the infection of many bacterial infections. Aim: To assess the maternal and fetal outcome in cases with normal and abnormal Amniotic Fluid Index levels. Results: The mode of delivery was spontaneous vaginal delivery followed by Assisted VD, Elective CS, Emergency CS respectively. It was affected by amount of liquor since, low AFI group 35 (75%) patients ended up in cesarean section for fetal distress. While in control group 63(18.3%) patients had caesarean section. Conclusion: Early neonatal death was seen in 0.2%, 4.5% and 70.5% newborns were born to pregnant women with normal AFI, oligohydramnios respectively. 70.5% neonates born to pregnant women with oligohydramnios had NICU admission. All cases were admitted in NICU because of respiratory distress.
背景:酒精羊水,一种保护胚胎的液体。它可以防止脑震荡、压力和干燥,让人想起生命的水生起源。充足的羊水是正常发育的必要条件,它就像一个缓冲垫,可以防止创伤、激动和意外冲动。它还具有抑菌特性,可以防止许多细菌感染。目的:评估羊水指数正常和异常病例的母婴结局。结果:分娩方式为自然阴道分娩,然后分别为辅助VD、选择性CS和急诊CS。它受到饮酒量的影响,因为低AFI组有35名(75%)患者因胎儿窘迫而剖宫产。对照组63例(18.3%)剖宫产。结论:AFI正常、羊水过少的孕妇所生新生儿早期死亡率分别为0.2%、4.5%和70.5%。70.5%的羊水过少孕妇所生新生儿进入新生儿重症监护室。所有病例均因呼吸窘迫而入住新生儿重症监护室。
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引用次数: 0
Simultaneous Estimation of Protein and Nucleic Acid Using Derivative Spectrophotometric Method 导数分光光度法同时测定蛋白质和核酸
Pub Date : 2021-09-15 DOI: 10.18579/jopcr/v20i3.ms21041
A. Agrawal, K. Kaur, Ra Sharma, Amit Goyal, A. Thakkar
Purpose: Simple and precise first derivative zero crossing spectrophotometric method has been developed for the simultaneous estimation of protein and nucleic acid without prior separation. Approach: The concentration ranges for protein and nucleic acid were taken in the range of 60-140 m g mL -1 and 20-100 m g mL -1 respectively in 0.1 M NaOH. Absorption spectra of the samples were recorded between 200 nm to 400 nm against a reagent blank. Zero-order spectra of protein and nucleic acid were stored individually within the above concentration ranges and were derivatized in first order using scaling factor 5 for both the substances. First derivative amplitudes were recorded at 261 nm and 289 nm for estimation of protein and RNA respectively for pure substances and binary mixture. Finding: Limit of detection was found to be 2.90 m g mL -1 and 0.36 m g mL -1 and limit of quantitation was 8.80 m g mL -1 and 1.02 m g mL -1 respectively for protein and nucleic acid respectively. Precision was found to be 1.38 % for protein and 1.25 % for RNA. Reproducibility was found to be 1.54 % for protein and 1.69 % for RNA. Conclusions: Thus, proposed method can be adapted for simultaneous determination of protein and nucleic acid and better alternate technique for immunoassays and electrophoretic methods.
目的:建立一阶导数零交叉分光光度法同时测定蛋白质和核酸的简便、精确方法。方法:测定0.1 m NaOH溶液中蛋白质和核酸的浓度范围分别为60 ~ 140 m g mL -1和20 ~ 100 m g mL -1。在试剂空白条件下,在200 ~ 400 nm范围内记录样品的吸收光谱。蛋白质和核酸的零级光谱分别在上述浓度范围内存储,并对这两种物质使用比例因子5进行一阶衍生。在261 nm和289 nm处记录一阶导数振幅,分别用于估计纯物质和二元混合物中的蛋白质和RNA。发现:蛋白质和核酸的检出限分别为2.90 m g mL -1和0.36 m g mL -1,定量限分别为8.80 m g mL -1和1.02 m g mL -1。结果表明,蛋白质的精密度为1.38%,RNA的精密度为1.25%。蛋白质和RNA的重复性分别为1.54%和1.69%。结论:该方法适用于蛋白质和核酸的同时测定,是免疫测定和电泳测定的更好替代技术。
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引用次数: 1
Development and Validation of RP-HPLC Method for the Estimation of Dolutegravir and Rilpivirine in Bulk and its Tablet Dosage form RP-HPLC法测定多卢替拉韦和利匹韦林的含量及片剂剂型的建立与验证
Pub Date : 2021-09-15 DOI: 10.18579/jopcr/v20i3.ms21040c
P. Pravalika, G. T. Rani, P. T. Sree, Y. Saritha
S T A C T An accurate and precise method was developed and validated for the simultaneous estimation of the Dolutegravir and Rilpivirine in Tablet dosage form. Chromatogram was run using Agilent C 18 column (4.6x150mm, 5 m m) with mobile phase containing KH 2 PO 4 buffer of pH 3.5 and Acetonitrile in the ratio of 45:55 v/v was pumped through column at a flow rate of 1mL/min. Temperature was maintained at 30 ◦ C. Selected wavelength was 240.0 nm. Retention time of Dolutegravir and Rilpivirine was found to be 2.239 min and 2.899 min respectively. %RSD of the Dolutegravir and Rilpivirine for system precision was found to be 0.9 and 0.6 respectively. Accuracy was performed in triplicate and the % Recovery was obtained as 99.33% and 100.5% for Dolutegravir and Rilpivirine respectively. LOD, LOQ values for Dolutegravir was 0.2 m g/mL, 0.6 m g/mL and for Rilpivirine was 0.02, 0.06 m g/mL respectively. So, the method developed was simple,accurateandreproduciblecanbeadoptedinregularQualitycontroltestinpharmaceuticalIndustry.
S T A C T开发并验证了一种准确、精确的方法,用于同时测定片剂剂型中的多卢替格拉韦和利匹韦林。色谱图使用安捷伦C18柱(4.6x150mm,5 m m),流动相含有pH3.5的KH2 PO4缓冲液,乙腈以45:55 v/v的比例以1mL/min的流速泵送通过柱。温度保持在30◦ C.选择波长为240.0nm。多卢替格拉韦和利匹韦林的保留时间分别为2.239分钟和2.899分钟多洛替格拉韦和利匹韦林的系统精密度RSD分别为0.9和0.6。准确度一式三份,多卢替格拉韦和利匹韦林的回收率分别为99.33%和100.5%。多洛替格拉韦的LOD和LOQ值分别为0.2 m g/mL、0.6 m g/mL和利匹韦林的为0.02、0.06 m g/mL。因此,所开发的方法简单、准确,可在制药工业质量控制中重复使用。
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引用次数: 0
Comparative In Vitro Quality Evaluation of Brands of Propranolol Tablet Marketed in Okada, Edo State, Nigeria. 尼日利亚江户州Okada市售品牌心得安片体外质量比较评价
Pub Date : 2021-09-15 DOI: 10.18579/jopcr/v20i3.ms21055
Oluwatobi O Olakojo, Precious Okpara, Stephanie Ikebiagbo
Propranolol, a beta-blocker is used in the management of cardiovascular conditions such as irregular heart rate and high blood pressure.The study was carried out to examine the in vitro quality control tests for seven brands of propranolol hydrochloride 40mg tablet formulation, sold in retail pharmacies in Okada, EdoState, Nigeria. The parameters determined were identification, weight variation, friability, hardness, disintegration, dissolution rate, and assay of the tablets. The tablets were evaluated for conformity with British Pharmacopoeia (BP) standards. Results obtained showed tablet weight in the range of 155.6±3.2mg to 348.2±2.0mg, hardness ranged from 1.03±0.17to 10.70±0.90 kg/cm2, friability of < 1 % except for one brand, disintegration time of 1.37±0.15 to 18.05±2.88 min whereby two brands are uncoated tablets and assay of 90.07 ±1.15 to 102±1.62% with one brand deviating from the specified limit. The seven batches also released more than 80% of their drug content within 30min. Analysis of similarity factor revealed that all brands but PN-7 can be interchangeable with PN-1 in terms of dissolution profile. The study showed that propranolol samples examined passed all the Pharmacopoeial tests for satisfactory quality exceptPN-6 which did not comply with most of the Pharmacopoeial specifications. Thus, not all brands can be used interchangeably in clinical practice.
普萘洛尔是一种β受体阻滞剂,用于治疗心律失常和高血压等心血管疾病。开展这项研究是为了检查在尼日利亚埃多州冈田市零售药店销售的7个品牌盐酸心得安40mg片剂制剂的体外质量控制测试。测定了其鉴别、重量变化、脆度、硬度、崩解度、溶出度、含量测定等参数。按照英国药典(BP)标准对其进行了符合性评价。结果表明:片重为155.6±3.2mg ~ 348.2±2.0mg,硬度为1.03±0.17 ~ 10.70±0.90 kg/cm2,除1个品牌外,脆碎度< 1%,崩解时间为1.37±0.15 ~ 18.05±2.88 min,其中2个品牌为无包衣片,崩解时间为90.07±1.15 ~ 102±1.62%,其中1个品牌偏离规定限量。7个批次在30min内释放出80%以上的药物含量。相似因子分析表明,除PN-7外,所有品牌均可与PN-1在溶出度方面互换。研究表明,除tpn -6不符合大部分药典标准外,经检验的普萘洛尔样品均通过药典检验,质量满意。因此,不是所有的品牌都可以在临床实践中互换使用。
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引用次数: 0
Chemical Profiling and Antihyperglycaemic Study on Butanol Fraction of Chlorophytum alismifolium Baker (Liliaceae) 百合科吊兰丁醇组分的化学谱分析及降糖作用研究
Pub Date : 2021-09-15 DOI: 10.18579/jopcr/v20i3.cp
Abubakar Abdulhakim, Omogbai E K Inanemo, Nazifi A Balarabe, Sania Bashir
Purpose: Diabetes mellitus is a disorder associated with debilitating complications. This study was aimed at evaluating the chemical profile and antihyperglycaemic effect of butanol fraction of Chlorophytum alismifolium. Methodology: The powdered plant was extracted sequentially using soxhlet apparatus with solvents of varying polarities until butanol fraction was obtained. GC-MS analysis, phytochemical screening and acute toxicity studies were carried out. Antihyperglycaemic study was carried out using alloxaninduced hyperglycaemia in rats. Male Wistar rats were injected with 120 mg/kg of alloxan intraperitoneally, the rats with fasting blood glucose levels between 200 and 350 mg/dL were considered hyperglycaemic. Experimental groups were set up using normal rats in group I and hyperglycaemic rats in five groups of six rats each. Group II was the hyperglycaemic control while groups III, IV and V received the butanol fraction of C. alismifolium at 250, 500 and 1000 mg/kg respectively. Group VI received glimepiride 1 mg/kg. Blood glucose levels were monitored before treatment at 0 hour and 1, 2, 3 and 5 hours after treatment. Findings: Phytochemical screening revealed the presence of alkaloids, saponins, flavonoids, glycosides and triterpenes while GC-MS analysis revealed the presence of thirteen compounds some of which include; isoxazolidine, isothiazole and acetamide. Oral median lethal dose of the extract in rats was estimated to be >5,000 mg/kg. The butanol fraction of C. alismifolium at all the doses tested showed significant (p<0.05) blood glucose lowering effect when compared over time.Conclusion: Thefindings from this research showed that butanol fraction of Chlorophytum alismifolium possesses important compounds with antihyperglycaemic activity.
目的:糖尿病是一种伴有衰弱性并发症的疾病。本研究旨在评价吊兰丁醇组分的化学性质及其降血糖作用。方法:采用索氏提取装置,用不同极性的溶剂依次提取,得到丁醇馏分。进行了GC-MS分析、植物化学筛选和急性毒性研究。采用四氧嘧啶诱导大鼠高血糖进行降糖研究。雄性Wistar大鼠腹腔注射四氧嘧啶120 mg/kg,空腹血糖200 ~ 350 mg/dL为高血糖大鼠。实验组设正常大鼠为1组,高血糖大鼠为5组,每组6只。II组为高血糖对照组,III、IV、V组分别给予茜草丁醇部位250、500、1000 mg/kg。VI组给予格列美脲1mg /kg。分别于治疗前0小时和治疗后1、2、3、5小时监测血糖水平。结果:经植物化学筛选,发现含有生物碱、皂苷、黄酮类化合物、苷类化合物和三萜,GC-MS分析发现含有13种化合物,其中包括;异恶唑烷,异噻唑和乙酰胺。大鼠口服中位致死剂量估计为50 000 mg/kg。各剂量川芎丁醇部位的降血糖作用随时间的变化均有显著性(p<0.05)。结论:吊兰丁醇部位具有一定的抗高血糖活性。
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引用次数: 0
Design and Characterization of Buccal Films of Benzocaine for Mouth Ulcer 苯佐卡因口腔溃疡膜的设计与表征
Pub Date : 2021-09-15 DOI: 10.18579/jopcr/v20i3.ms21062
J. Jose, M. V. Sisira, M. Prasanth, C. Prasanth, P. Pradeep
Mouth ulcer is very common in recent years, which occurs due to the damage of epithelial tissue and/or lamina propria that finally leads to tissue necrosis. Benzocaine has been used to treat the mouth ulcers due to its excellent local anaesthetic effect that relieves the pain associated with mouth ulcer. Hence an attempt was made to develop and characterize the buccal films of Benzocaine to treat mouth ulcers with an aim of prolonging the drug release and improving the patient convenience. The films were fabricated using the mucoadhesivepolymerblendofchitosanandHPMCbysolventcastingmethodandthephysico-mechanical, in vitro drug release and ex vivo buccal mucosal permeation characteristics of the films were studied. All fabricated film formulations prepared were smooth and almost opaque, with good flexibility. The weight and thickness of all the formulations were found to be uniform. Drug content in the films ranged from 97–99%, indicating favorable drug loading and uniformity. The inclusion of HPMC, significantly reduced the bioadhesive strength and in vitro mucoadhesion time of chitosan films, although the degree of swelling increased. In vitro drug release and permeation studies in simulated saliva showed a prolonged release for a period of 6 h for all formulations. The formulation with Chitosan: HPMC ratio 1:1, 10% w/w polysorbate 80 and 10% w/w propylene glycol as plasticizers showed the best results which exhibited the cumulative percentagedrugreleaseof87.9%andthecumulativeamountofdrugpermeationof7.62mg/cm 2 acrossgoat buccal mucosa in 6 h. Drug-excipient interaction studies were carried out using DSC and FT-IR technique; films indicated no chemical interaction between drug and polymers used.
口腔溃疡是近年来非常常见的疾病,它是由于上皮组织和/或固有层的损伤而最终导致组织坏死。苯佐卡因具有良好的局部麻醉效果,可减轻口腔溃疡引起的疼痛,已被用于治疗口腔溃疡。因此,本研究试图研制苯佐卡因治疗口腔溃疡的口腔膜,并对其进行表征,以期延长药物释放时间,提高患者使用的方便性。采用壳聚糖黏附聚合物和hpmc溶剂铸造法制备膜,研究膜的物理力学特性、体外药物释放特性和体外口腔粘膜渗透特性。制备的薄膜配方光滑,几乎不透明,柔韧性好。所有配方的重量和厚度都是均匀的。膜中药物含量在97 ~ 99%之间,具有良好的载药量和均匀性。HPMC包合显著降低壳聚糖膜的生物黏附强度和体外黏附时间,但肿胀程度增加。体外药物释放和在模拟唾液中的渗透研究表明,所有制剂的释放时间都延长了6小时。以壳聚糖:HPMC比例为1:1、10% w/w聚山梨酯80和10% w/w丙二醇为增塑剂的配方效果最佳,6 h的累积释药率为87.9%,累计释药量为7.62mg/ cm2。采用DSC和FT-IR技术对药物与辅料的相互作用进行了研究;薄膜显示药物和聚合物之间没有化学相互作用。
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引用次数: 0
期刊
Journal of Pharmaceutical Research
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