Journal of Pharmacy Research最新文献_第10页

In vitro determination of sun protection factor and chemical stability of Rosa kordesii extract gel 桃红提取物凝胶的防晒因子及化学稳定性的体外测定

Journal of Pharmacy Research

Pub Date : 2013-06-01 Epub Date: 2013-07-18 DOI: 10.1016/j.jopr.2013.05.021

Pratik P. Maske, Sachin G. Lokapure, Dhanashri Nimbalkar, Shobharaj Malavi, John I. D'souza

Aims

In the present study, to investigate its chemical stability and the in vitro sun protection factor (SPF) of Rosa kordesii petal extract in a gel formulation.

Methods

Due to its antioxidant and photoprotective properties, R. kordesii is a promising candidate for use in cosmetic and pharmaceutical formulations. A high performance liquid chromatography method was used to evaluate the chemical stability using R. kordesii extract as marker at 5, 25 and 45 °C for 3–4 months. The sun protection factors were analyzed by ultraviolet (UV) spectrophotometry using samples irradiated with UVB lamp.

Results

The chemical stability of the R. kordesii root extract gel was determined according to the concentration of R. kordesii extracts at different storage temperatures (5, 25 and 45 °C) for 3–4 months. It is screened for in vitro sun protection factor in the R. kordesii extract and of its gel formulation and determines Photostability of the isolated R. kordesii extract and SPF.

Conclusion

This study has shown that the R. kordesii petal extract gel is stable for at least 3–4 months when stored at 5 and 25 °C. It is essential for collection of similar data for different plants and their flowers, as well as other parts. This proved activity of plant showed its importance and prophylactic utility in anti-solar formulation. This will be a better, cheaper and safe alternative to harmful chemical sunscreens that used now a days in the industry.

目的研究玫瑰花瓣凝胶提取物的化学稳定性和体外防晒系数(SPF)。方法因其抗氧化和光防护的特性，在化妆品和药物制剂中具有广阔的应用前景。采用高效液相色谱法，在5℃、25℃和45℃条件下，以黄芩提取物为标记物，在3-4个月的时间内进行化学稳定性评价。用紫外分光光度法测定样品的防晒系数。结果在不同贮藏温度(5℃、25℃和45℃)下，以黄皮提取物的浓度测定黄皮提取物凝胶的化学稳定性。筛选黄芪提取物及其凝胶制剂的体外防晒因子，测定分离的黄芪提取物的光稳定性和SPF值。结论在5°C和25°C的低温条件下，冬青花瓣提取液凝胶的稳定性至少为3-4个月。这对于收集不同植物及其花以及其他部分的类似数据至关重要。这表明植物活性在抗太阳制剂中具有重要的预防作用。这将是一种更好、更便宜、更安全的替代品，可以替代目前行业中使用的有害化学防晒霜。

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引用次数: 29

Efficacy of Helicteres isora L. against free radicals, lipid peroxidation, protein oxidation and DNA damage 鸢尾抗自由基、脂质过氧化、蛋白质氧化和DNA损伤的功效

Journal of Pharmacy Research

Pub Date : 2013-06-01 Epub Date: 2013-06-27 DOI: 10.1016/j.jopr.2013.05.017

Vinay Kumar , Mansi Sharma , Melissa Lemos , Varsha Shriram

Background

Free radicals are implicated with cellular disorders through their detrimental actions on proteins, lipids and DNA and are causative factors for large number of degenerative diseases and aging process. Antioxidants of plant origin hold great significance and have therefore gained utmost importance in recent past. Present investigation was a step in this direction, with an objective to comprehensively evaluate the protective effects of Helicteres isora fruits against free radicals, protein oxidation and DNA damage.

Methods

Aqueous (AqE), aqueous-methanol (AqME), methanol (ME) and acetone (AE) extracts of mature pods (fruits) were obtained and concentrated in vacuo. Total phenols, flavonoids, ascorbic acid and carotenoids were estimated from extracts using standard methods. Antioxidant activities of extracts with varying concentrations (200–1000 μg/ml) were determined by total antioxidant activity (TAA), ferric reducing antioxidant power, DPPH, and OH radical scavenging assays besides lipid peroxidation inhibition. Extracts were assessed for protection against AAPH (2,2′-Azobis(2-methylpropionamidine) dihydrochloride) induced-protein oxidation using SDS-PAGE and Fenton's reagent induced-DNA damage using DNA nicking assay.

Results

The results postulated that the plant is a rich source of total phenols, flavonoids and ascorbic acid. Extracts showed concentration-dependent free radical scavenging activities and lipid peroxidation inhibition. Amongst all four extracts, AqME showed highest antioxidant potential in terms of reducing power (360 ± 5.9 gallic acid equivalent: GAE), TAA (150 ± 5.6 GAE), scavenging of free radicals including DPPH (75.6%) and OH (100%) besides maximal (97.4%) lipid peroxidation inhibition at 1000 μg/ml concentration. All the extracts barring ME effectively protected the DNA from hydroxyl radical-induced damage. Similarly, fruit extracts effectively protected the AAPH-induced-protein oxidation.

Conclusions

H. isora fruits exhibited broad-spectrum antioxidant potencies against free radicals and significantly ameliorated various impairments associated with free radical formation including lipid peroxidation, protein oxidation and DNA damage.

自由基通过对蛋白质、脂质和DNA的有害作用与细胞紊乱有关，并且是大量退行性疾病和衰老过程的致病因素。植物来源的抗氧化剂具有重要意义，因此近年来得到了极大的重视。本研究就是在这一方向上迈出的一步，目的是综合评价螺旋果对自由基、蛋白质氧化和DNA损伤的保护作用。方法提取成熟豆荚(果实)的水(AqE)、水-甲醇(AqME)、甲醇(ME)和丙酮(AE)提取物，并进行真空浓缩。用标准方法对提取物中总酚、类黄酮、抗坏血酸和类胡萝卜素进行了测定。通过总抗氧化活性(TAA)、铁还原抗氧化能力、DPPH、OH自由基清除能力及脂质过氧化抑制能力测定不同浓度(200 ~ 1000 μg/ml)提取物的抗氧化活性。采用SDS-PAGE和Fenton试剂对AAPH(2,2′-偶氮(2-甲基丙烯脒)二盐酸)诱导的蛋白质氧化和DNA损伤进行检测。结果该植物含有丰富的总酚、类黄酮和抗坏血酸。提取物具有浓度依赖性的自由基清除活性和脂质过氧化抑制作用。四种提取物中，AqME在还原能力(360±5.9没食子酸:GAE)、TAA(150±5.6 GAE)、清除自由基DPPH(75.6%)和OH(100%)方面表现出最高的抗氧化潜力，在1000 μg/ml浓度下，对脂质过氧化的抑制作用最大(97.4%)。所有抑制ME的提取物都能有效地保护DNA免受羟基自由基引起的损伤。同样，水果提取物对aaph诱导的蛋白氧化也有保护作用。异黄酮果实对自由基表现出广谱的抗氧化能力，并显著改善与自由基形成相关的各种损伤，包括脂质过氧化、蛋白质氧化和DNA损伤。

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引用次数: 20

Chiral separation of sitagliptin phosphate enantiomer by HPLC using amylose based chiral stationary phase 直链淀粉手性固定相高效液相色谱法拆分磷酸西格列汀对映体

Journal of Pharmacy Research

Pub Date : 2013-06-01 Epub Date: 2013-07-10 DOI: 10.1016/j.jopr.2013.06.014

Bhimireddy Venkata Rami Reddy , Nanduri Raman , Badam Sai Kumar , Chintala Rambabu

Background

Although a number of methods are available for evaluating sitagliptin phosphate (SGP), a common method for separation if its potential enantiomer and its possible impurities with good efficiency remains unavailable. With the objective of developing a method for rapid separation with shorter runtimes, a simple, precise, accurate stability indicating normal phase High-performance liquid chromatographic (NRP-HPLC) coupled with a photodiode array detector method was developed for the quantitative determination of (S)-enantiomer in API substance and as well as drug product.

Methods

The proposed novel method uses the mixture of n-heptane-ethanol-diethylamine (DEA) 35:65:0.1 (v/v/v) as a mobile phase. The enantiomer of sitagliptin phosphate was baseline resolved on a Chiralpak AD-H (250 mm×4.6 mm, 5 μm) column. The flow rate of the mobile phase is 1.0 mL/min and the detector wavelength monitored at 265 nm. The developed method was extensively validated.

Result

In these conditions, linearity over the concentration range 400-2250 ng/ml for (S)- enantiomer was obtained. The limit of detection and quantification were 150 and 400 ng/ml, respectively. The intra and inter-day precision was less than 1.5%. The recovery of (S)- enantiomer was within 107% in bulk drug.

Conclusion

The proposed method was found to be suitable, precise, and accurate for the quantitative determination of (S)-enantiomer in bulk drugs as well as in pharmaceutical formulations.

虽然有许多方法可用于评价磷酸西格列汀(SGP)，但目前还没有一种有效分离其潜在对映体及其可能杂质的常用方法。为建立一种运行时间短、简便、精确、准确、稳定的正相色谱方法，建立了高效液相色谱-光电二极管阵列检测器联用技术定量测定原料药和制剂中(S)-对映体的方法。方法以正庚烷-乙醇-二乙胺(DEA) 35:65:0.1 (v/v/v)为流动相。在Chiralpak AD-H (250 mm×4.6 mm, 5 μm)柱上基线分离西格列汀磷酸对映体。流动相流速为1.0 mL/min，检测器波长为265 nm。所开发的方法得到了广泛的验证。结果(S)-对映体在400 ~ 2250 ng/ml范围内呈良好的线性关系。检测限为150 ng/ml，定量限为400 ng/ml。日内、日间精度均小于1.5%。原料药中(S)-对映体的回收率在107%以内。结论该方法适用于原料药和制剂中(S)-对映体的定量测定，精密度高，准确度高。

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引用次数: 15

Formulation and in-vitro evaluation of moxifloxacin loaded crosslinked chitosan films for the treatment of periodontitis 莫西沙星载交联壳聚糖膜治疗牙周炎的制备及体外评价

Journal of Pharmacy Research

Pub Date : 2013-06-01 Epub Date: 2013-07-18 DOI: 10.1016/j.jopr.2013.06.019

Durga Praveena Chinta, Prakash Katakam, Varanasi Satya Narayana Murthy, Maria John Newton

Aim

The purpose of the present work was to develop a local drug delivery system of moxifloxacin loaded crosslinked chitosan films using sodium citrate as a crosslinking agent with different concentrations and crosslinking time.

Methods

The films were prepared using solvent casting technique. The formulated films were evaluated for physicochemical parameters like FT-IR, DSC, thickness, weight variation, content uniformity, surface pH and release kinetics.

Results

IR and DSC studies indicated that there is no interaction between the drug and excipients. The drug loaded chitosan films were flexible, possessed good tensile strength and demonstrated satisfactory physicochemical characteristics. Although the films showed an initial burst release of drug, the release was sustained for up to 15 days. From the obtained results F6 formulation is optimized one among all the formulations.

Conclusion

The present work suggests that the controlled release Moxifloxacin loaded Chitosan films crosslinked with sodium citrate have a remarkable role in the local therapy of periodontitis.

目的以柠檬酸钠为交联剂，研究不同浓度、不同交联时间的莫西沙星负载壳聚糖交联膜的局部给药体系。方法采用溶剂铸造法制备膜。对配制的薄膜进行了理化参数评价，如FT-IR、DSC、厚度、重量变化、含量均匀性、表面pH和释放动力学。结果sir和DSC研究表明，该药物与辅料无相互作用。壳聚糖载药膜柔韧性好，抗拉强度高，具有良好的理化性能。虽然影片显示了药物最初的突然释放，但释放持续了长达15天。从所得结果来看，F6配方是所有配方中最优的配方。结论柠檬酸钠交联莫西沙星壳聚糖控释膜在牙周炎的局部治疗中具有重要作用。

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引用次数: 9

Zea mays leaf extracts protects primary chick embryo fibroblast cells from apoptosis induced by hydrogen peroxide in vitro 玉米叶提取物对过氧化氢诱导鸡胚成纤维细胞凋亡的保护作用

Journal of Pharmacy Research

Pub Date : 2013-06-01 Epub Date: 2013-06-27 DOI: 10.1016/j.jopr.2013.06.009

Balasubramanian Kiruthika , Sudha Devi Manickam , Palghat Raghunathan Padma

Background

It is known that excessive oxidative damage, when unchecked, can result in cell death. Therefore, in the present study, the extent of cell death induced by H₂O₂-induced oxidative stress in primary cultured chick embryo fibroblasts and its protection by Zea mays leaf extracts was followed.

Methods

Various apoptosis related parameters like cell viability, morphological changes, nuclear changes and apoptotic index were characterized. SRB and MTT assays were used to quantify the extent of cell death in the group exposed to H₂O₂, plant extracts and their combination.

Results and discussion

The treatment with hydrogen peroxide exhibited cytotoxicity in the primary chick embryo fibroblasts cells. The number of apoptotic cells increased in the oxidant treated groups. When administered along with H₂O₂, the leaf extracts resulted in a significantly decreased number of apoptotic cells. The maximum inhibition of H₂O₂-induced apoptosis was exhibited by the methanolic extract followed by the aqueous and chloroform extracts.

Conclusion

These results indicate that the Zea mays leaves can render protection to chick embryo fibroblasts against H₂O₂-induced cell death.

众所周知，过度的氧化损伤，如果不加以控制，会导致细胞死亡。因此，本研究对原代培养的鸡胚成纤维细胞在h2o2氧化应激诱导下的细胞死亡程度及玉米叶提取物对成纤维细胞的保护作用进行了研究。方法观察细胞活力、形态学变化、细胞核变化及凋亡指数等凋亡相关参数。使用SRB和MTT测定暴露于H2O2、植物提取物及其组合的组的细胞死亡程度。结果与讨论双氧水处理对鸡胚成纤维细胞具有细胞毒性。氧化处理组凋亡细胞数量增加。当与H2O2一起施用时，叶提取物导致凋亡细胞数量显著减少。甲醇提取物对h2o2诱导的细胞凋亡的抑制作用最大，其次是水提取物和氯仿提取物。结论玉米叶对h2o2诱导的鸡胚成纤维细胞死亡具有保护作用。

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引用次数: 2

Development and in-vivo characterization of novel trans buccal formulations of Amiloride hydrochloride 新型盐酸阿米洛利经口腔剂型的研制及体内表征

Journal of Pharmacy Research

Pub Date : 2013-06-01 Epub Date: 2013-06-21 DOI: 10.1016/j.jopr.2013.04.051

J. Ravi Kumar Reddy , Y. Indira Muzib , K.P.R. Chowdary

Objectives

Formulation development and characterization of novel trans-buccoadhesive patches and bilayer tablets of Amiloride hydrochloride (AMHCL) with the objectives to avoid the first-pass effect, incomplete absorption from GIT, improve the bioavailability, minimize the dose, improve the duration of action and hence produce controlled drug delivery.

Methods

AMHCL patches were prepared by solvent casting method, using hydroxy propyl methyl cellulose (HPMC), Carbopol, Chitosan, and polyvinylpyrrolidone-K30 (PVP). Tablets were prepared by direct compression method, using sodium carboxy methyl cellulose (SCMC), HPMC K100, sodium alginate, Carbopol 934 P, Eudragit RL 100, PVP and ethyl cellulose (EC) as a backing layer. The both formulations were evaluated for their thickness uniformity, folding endurance, weight uniformity, content uniformity, swelling behavior, tensile strength, buccoadhesive strength, surface pH and in vitro release studies.

Results

Data of in vitro release from both patches and tablets were fit to different equations and kinetic models to explain release profiles. In vivo drug release studies in rabbits showed 91.65% of drug release from HPMC-Chitosan patch, while it was 82.63–90.21% release from sodium alginate-SCMC buccal tablets. Good correlation among in vitro release and in vivo release of AMHCL was observed in both formulations.

Conclusion

The satisfactory results were obtained in all prepared formulations and based on the results, it can be concluded, Amiloride hydrochloride oral mucoadhesive buccal formulations which can be used mainly in minimizing dose and mainly help to improve the patient compliance and Amiloride hydrochloride is a drug of choice for delivery through the control release via buccal route.

目的研制新型盐酸阿米洛利(AMHCL)反式胶粘片和双层片的处方及表征，以避免药物的首过效应、GIT的不完全吸收、提高生物利用度、减少剂量、延长作用时间，从而实现药物的可控给药。方法以羟丙基甲基纤维素(HPMC)、卡波醇、壳聚糖、聚乙烯吡罗烷酮- k30 (PVP)为原料，采用溶剂铸造法制备samhcl贴片。以羧甲基纤维素钠(SCMC)、HPMC K100、海藻酸钠、卡波波934p、乌龙茶RL 100、PVP和乙基纤维素(EC)为底层，采用直接压缩法制备片剂。对两种配方的厚度均匀性、折叠耐久性、重量均匀性、含量均匀性、膨胀性、拉伸强度、抗拉强度、表面pH和体外释放研究进行了评价。结果贴片和片剂的体外释放数据符合不同的方程和动力学模型来解释释放曲线。兔体内释药实验表明，壳聚糖贴片释药率为91.65%，海藻酸钠- scmc口腔片释药率为82.63-90.21%。两种制剂的体内和体外释放量均呈良好的相关性。结论所有制剂均获得满意的效果，结论盐酸阿米洛利口腔黏合剂制剂可主要用于减少剂量和提高患者依从性，是口腔途径控释给药的首选药物。

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引用次数: 15

Study of physico–chemical properties of various concentrations of self developed root canal lubricant 自行研制的不同浓度根管润滑剂的理化性质研究

Journal of Pharmacy Research

Pub Date : 2013-06-01 Epub Date: 2013-07-16 DOI: 10.1016/j.jopr.2013.05.018

Satish D. Ingale , Rajendra Kankariya

Background and aim

The major aim of this work is to study the physico–chemical properties of different concentrations of self developed root canal lubricant gel in order to standardize the formulations and to observe its effect on the performance.

Materials and methods

The different concentrations of self developed root canal lubricant gel such as 10%, 24% & 31% was prepared and their physico–chemical properties such as appearance, Solid content, 5% aqueous solution pH, Moisture content, B. F. Viscosity and 5% aqueous solution stability etc. are studied.

Results

From the experimental study, it was observed that there is no remarkable difference in the physical appearance of the root canal lubricant gel. Solid content goes on increasing and moisture content goes on decreasing as concentration of EDTA increases.

Conclusion

The chelating efficiency, cleaning & shaping of root canal goes on increasing as percentage of EDTA increases i.e. solid content increases. Efficiency of lubrication was also found to be better in highly concentrated formulation. B. F. Viscosity of the formulations is always kept similar by adjusting quantity of rheology modifier in order to get good handling characteristics. From 5% aqueous solution stability, it is observed that gel is highly stable.

背景与目的研究自行研制的不同浓度根管润滑凝胶的理化性质，以规范其配方并观察其对根管润滑性能的影响。材料与方法:自行研制的根管润滑凝胶浓度为10%、24%、amp;并对其外观、固含量、5%水溶液pH、水分含量、b.f.粘度、5%水溶液稳定性等理化性能进行了研究。结果从实验研究中观察到，根管润滑凝胶的物理外观没有显著差异。随着EDTA浓度的增加，固含量增加，水分含量降低。结论螯合效果好，清洗效果好;随着EDTA含量的增加，即固形物含量的增加，根管的成形也随之增加。高浓缩配方的润滑效果也较好。通过调节流变改性剂的用量，使配方的粘度保持一致，以获得良好的处理特性。从5%的水溶液稳定性来看，凝胶具有很高的稳定性。

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引用次数: 0

Design and evaluation of glipizide CR tablets employing starch acetate as rate controlling matrix former 以醋酸淀粉为控速基质的格列吡嗪CR片的设计与评价

Journal of Pharmacy Research

Pub Date : 2013-06-01 Epub Date: 2013-07-03 DOI: 10.1016/j.jopr.2013.06.013

P. Seenivasan , K.P.R. Chowdary , C. Uma Maheswara Reddy , J.S.N. Murthy

Background/Objectives

In the present work, starch acetate was synthesized, characterized and evaluated as effective release retarding matrix materials.

Methods

Matrix tablets of glipizide were formulated employing starch acetate in different proportions of drug and polymer and the tablets were evaluated for drug release kinetics and mechanism.

Results

Starch acetate (SA) was prepared by acetylation of potato starch with acetic anhydride in alkaline medium. The percent acetylation was 42.38% and the degree of substitution was 2.75. Glipizide (10 mg) matrix tablets prepared using starch acetate as matrix former in different concentrations gave slow and controlled release more than 24 h. Glipizide release from the tablets formulated was slow and depends on the concentration (%) of starch acetate in the matrix tablets and nature/type of diluent. A linear relationship was found out between percent of polymer, starch acetate and release rate (K₀) of the tablets. The controlled release characteristics of the starch acetate matrix tablets of the drug remained unaltered during short time accelerated stability study.

Conclusions

Starch acetate was found suitable as matrix former for controlled release and the matrix tablets of glipizide formulated employing starch acetate gave controlled release of glipizide over 24 h.

背景/目的合成醋酸淀粉为缓释基质材料，对其进行表征和评价。方法以醋酸淀粉为原料，以不同的药物和聚合物比例配制格列吡嗪基质片，并对其释放动力学和释药机理进行评价。结果马铃薯淀粉与乙酸酐在碱性介质中乙酰化制备淀粉醋酸酯(SA)。乙酰化率为42.38%，取代度为2.75。以不同浓度醋酸淀粉为基质制备的格列吡嗪(10 mg)基质片缓释和控释均大于24 h。格列吡嗪的缓释与基质片中醋酸淀粉的浓度(%)和稀释剂的性质/类型有关。聚合物、醋酸淀粉含量与片剂的释放度(K0)呈线性关系。在短期加速稳定性研究中，醋酸淀粉基质片的控释特性保持不变。结论醋酸淀粉可作为格列吡嗪基质片的缓释基质，醋酸淀粉配制的格列吡嗪基质片在24 h内具有良好的缓释效果。

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引用次数: 3

In vitro antioxidant activity and in vivo alpha glucosidase activity of endophytic actinomycetes isolated from Catharanthus roseus (l.) G. Don 长春花内生放线菌体外抗氧化活性和体内α -葡萄糖苷酶活性的研究g .不

Journal of Pharmacy Research

Pub Date : 2013-06-01 Epub Date: 2013-06-21 DOI: 10.1016/j.jopr.2013.06.007

D. Jacintha Jasmine, P. Agastian

Aim

Antioxidant compounds in food play an important role as a health protecting factor. Scientific evidence suggests that antioxidants reduce the risk for chronic diseases including cancer and heart disease. The present study was to evaluate the free radical scavenging activity and alpha glucosidase activity of Ethyl acetate extracts of endophytic actinomycetes (EEA) isolated from the roots of Catharanthus roseus (l.) G. Don.

Method

The EEA was screened for its capability in lowering blood sugar level and radical scavenging activity against Hydroxyl (HO^-), Hydrogen peroxide (H₂O₂), Nitric oxide (NO) and scavenging of stable radical 2,2-diphenyl-1-picrylhydrazyl or DPPH and using standard procedures.

Result

Significant free radical scavenging activity and marked alpha glucosidase activity were exhibited by EEA isolated from the roots of Catharanthus roseus (l.) G. Don.

Conclusion

The extract used in the study possesses significant antioxidant activity as well as an alpha glucosidase inhibition and have the potential for application in pharmaceuticals.

目的食品中的抗氧化化合物是一种重要的健康保护因子。科学证据表明，抗氧化剂可以降低患慢性疾病的风险，包括癌症和心脏病。本研究对玫瑰花(Catharanthus roseus)根内生放线菌(endoophytic放线菌，EEA)乙酸乙酯提取物的自由基清除活性和α葡萄糖苷酶活性进行了研究。g .堂。方法采用标准方法筛选EEA降血糖、清除羟基(HO-)、过氧化氢(H2O2)、一氧化氮(NO)自由基和清除稳定自由基2,2-二苯基-1-picrylhydrazyl或DPPH的能力。结果从长春花根中分离得到的EEA具有明显的自由基清除活性和α -葡萄糖苷酶活性。g .堂。结论该提取物具有明显的抗氧化活性和α -葡萄糖苷酶抑制作用，具有广阔的药物应用前景。

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引用次数: 14

Tab-in-tab formulation of ramipril and nifedipine for effective anti-hypertensive activity 雷米普利与硝苯地平片内联合处方有效降压

Journal of Pharmacy Research

Pub Date : 2013-06-01 Epub Date: 2013-06-27 DOI: 10.1016/j.jopr.2013.06.008

Pravin K. Shende , Vedraj V. Vellody , R.S. Gaud

Background

The aims of this work were to enhance the solubility of nifedipine in acidic medium; to formulate and characterize tab-in-tab dosage form for immediate release of nifedipine and controlled release of ramipril and to avoid the mutual interactions of drugs. This combination appreciably intended to reduce the incidence of peripheral edema and reflex tachycardia.

Methods

Ramipril was firstly wet granulated with a HPMC polymer to form stable granules and then was directly compressed to form a core tablet. Enteric coating was given with a water insoluble polymer to withstand the acidic pH of stomach. Initially, nifedipine microcapsules were prepared, granulated with excipients and then compressed, keeping the inner tablet in between the granules.

Results and discussion

This novel tab-in-tab dosage form allowed the nifedipine to release for stomach-specific absorption and ramipril to the intestine-specific absorption. Distinctive release profiles were obtained for immediate- and controlled-release tab-in-tab formulations, giving better bioavailability with no metabolic side-effects.

Conclusion

Tab-in-tab drug delivery system used to formulate combination drugs with different pharmacokinetic profiles provide reduction in dosage, dosing frequency, reduction in side effects, additive effects and single pill convenience.

背景:提高硝苯地平在酸性介质中的溶解度;制定硝苯地平即刻释放和雷米普利控释的片内剂型，并对其进行表征，避免药物相互作用。这种组合明显旨在减少周围水肿和反射性心动过速的发生率。方法先用HPMC聚合物湿法制粒，使雷米普利形成稳定的颗粒，然后直接压缩制成芯片。肠包衣用不溶于水的聚合物来抵抗胃的酸性pH。首先制备硝苯地平微胶囊，用辅料制成颗粒，然后压缩，使内片保持在颗粒之间。结果与讨论这种新型片剂使硝苯地平释放为胃特异性吸收，雷米普利释放为肠特异性吸收。不同的释放曲线获得即时和控释片剂制剂，提供更好的生物利用度，没有代谢副作用。结论采用片内给药系统制备不同药动学特征的联合用药，可减少给药剂量、给药频次、减少毒副作用和加性效应，且单粒方便。

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引用次数: 3