Drug Invention Today最新文献

英文中文

Compressed glyceryl monostearate based biodegradable implant of Gentamicin using melt granulation technique: In vitro evaluation & biocompatibility in animals 基于熔融造粒技术的压缩单硬脂酸甘油可生物降解庆大霉素植入物:体外评价及动物生物相容性

Drug Invention Today

Pub Date : 2013-03-01 DOI: 10.1016/j.dit.2013.03.006

Ashish Y. Pawar , Kiran B. Erande , Deepak D. Sonawane , Vikas R. Asawale , Yogesh S. Harak , Deelip V. Derle

Objective

Osteomyelitis is a multibacterial bone infection which is still remains challenging and difficult to treat, despite of advances in antibiotics and new operative techniques. Present study aims at formulating Gentamicin implants in treatment of Osteomyelitis & other bone infections using glyceryl monostearate (GMS) matrices as a carrier.

Methods

Gentamicin implants were prepared by using combination of glyceryl monostearate and poly ethylene glycol as hydrophobic biodegradable sustained release matrices along with different percentage of Sorbitol and Tween80 as erosion enhancers. Several formulations were prepared (K1–K7) by melt granulation followed by compression to form disc shaped implants. The prepared formulations were evaluated for different in vitro parameters & optimized formulation was subjected to in vivo study.

Results & discussion

Formulation K4 shows excellent cumulative drug release profile and it does not completely lose its physical shape even after 28 days thus this formulation conclude to be optimum formulation among the all GMS based implant formulations. Also optimized GMS based implant does not show any severe signs of inflammation and other foreign body reactions in laboratory animals, thus it was concluded that GMS based implant have acceptable biological compatibility even after 28 days.

Conclusion

Therefore from this study it is proved that, the glyceryl monostearate based implants have potential to retard the drug release for more than five weeks in the treatment of osteomyelitis & bone infections.

目的骨髓炎是一种多细菌骨感染，尽管抗生素和新的手术技术取得了进展，但治疗仍然具有挑战性和难度。本研究旨在研制庆大霉素植入物治疗骨髓炎。以单硬脂酸甘油酯(GMS)基质为载体的其他骨感染。方法以单硬脂酸甘油酯和聚乙二醇为疏水可生物降解缓释基质，不同比例的山梨醇和吐温80为促蚀蚀剂，制备庆大霉素植入物。几种配方(K1-K7)通过熔融造粒，然后压缩形成圆盘状植入物。对制备的制剂进行了不同体外参数的评价;优化后的配方进行了体内实验。结果,制剂K4表现出优异的累积药物释放谱，即使在28天后也不会完全失去其物理形状，因此该制剂被认为是所有基于GMS的植入制剂中的最佳制剂。优化后的GMS植入物在实验动物中没有出现任何严重的炎症迹象和其他异物反应，因此GMS植入物在28天后仍具有可接受的生物相容性。结论单硬脂酸甘油酯植入体治疗骨髓炎有延缓药物释放5周以上的潜力;骨感染。

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引用次数: 1

RETRACTED: Nanosuspension of vasicine from Adhatoda vasica: Isolation and characterization 撤稿:从水蛭中提取水蛭疫苗的纳米悬浮液:分离和表征

Drug Invention Today

Pub Date : 2013-03-01 DOI: 10.1016/j.dit.2013.03.005

Jitender Kumar Malik , Akshat Sharma , Sanjiv Singh , Sourabh Jain

This article has been retracted: please see Elsevier Policy on Article Withdrawal (http://www.elsevier.com/locate/withdrawalpolicy).

This article has been retracted at the request of the Authors. The article was published with the omission of a legitimate author, Shailendra Singh, CSIR-Advanced Materials and Processes Research Institute (AMPRI).

本文已被撤回:请参阅爱思唯尔文章撤回政策(http://www.elsevier.com/locate/withdrawalpolicy).This)，应作者要求，文章已被撤回。这篇文章是在遗漏合法作者的情况下发表的，Shailendra Singh, csir -先进材料与工艺研究所(AMPRI)。

引用次数: 9

Fabrication of highly stable sonication assisted curcumin nanocrystals by nanoprecipitation method 用纳米沉淀法制备高稳定超声辅助姜黄素纳米晶体

Drug Invention Today

Pub Date : 2013-03-01 DOI: 10.1016/j.dit.2013.02.003

C. Moorthi, K. Kathiresan

Objectives

The present study was aimed to fabricate highly stable sonication assisted curcumin nanocrystals by nanoprecipitation method to overcome the poor aqueous solubility of curcumin.

Methods

Sodium lauryl sulfate coated curcumin nanocrystals and poloxamer 188 coated curcumin nanocrystals were prepared using nanoprecipitation method and characterized for particle size and related parameters.

Results

Poloxamer 188 coating has produced a significant size reduction in the distribution width (approximately 250 times in D 90) and in the average particle size (approximately 260 times in volume weight mean) with respect to pure curcumin. Similarly, sodium lauryl sulfate coating has produced a significant size reduction in the distribution width (approximately 1000 times in D 90) and in the average particle size (approximately 750 times in volume weight mean) with respect to pure curcumin. Sodium lauryl sulfate coated curcumin nanocrystals has shown a narrow distribution even after one week than the poloxamer coated curcumin nanocrystals.

Conclusions

The study concludes that the anionic nature of sodium lauryl sulfate has provided higher zeta potential and offered high electrostatic force which overcomes the van der Waals force of attraction and gravitational force leading to prevention of nanocrystal aggregation resulting in narrow sized high stable curcumin nanocrystals.

目的利用纳米沉淀法制备高稳定性超声辅助姜黄素纳米晶体，克服姜黄素水溶性差的缺点。方法采用纳米沉淀法制备十二烷基硫酸钠包被姜黄素纳米晶体和poloxamer 188包被姜黄素纳米晶体，并对其粒径和相关参数进行表征。结果与纯姜黄素相比，spoloxam188涂层在分布宽度(d90中约250倍)和平均粒径(平均体积重量约260倍)上显著减小。同样，与纯姜黄素相比，十二烷基硫酸钠涂层在分布宽度(d90中约为1000倍)和平均粒径(平均体积重量约为750倍)上产生了显着的尺寸减小。十二烷基硫酸钠包被的姜黄素纳米晶体即使在一周后也比波洛沙姆包被的姜黄素纳米晶体分布窄。结论月桂醇硫酸钠的阴离子性质使其具有较高的zeta电位和较大的静电力，克服了范德华引力和万有引力的作用，阻止了纳米晶体的聚集，形成了窄尺寸、高稳定性的姜黄素纳米晶体。

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引用次数: 45

Preparation and evaluation of Bacopa–phospholipid complex for antiamnesic activity in rodents 假马齿苋-磷脂复合物的制备及对啮齿动物抗遗忘活性的评价

Drug Invention Today

Pub Date : 2013-03-01 DOI: 10.1016/j.dit.2013.02.004

Prasanna Habbu , Smita Madagundi , Ramesh Kulkarni , Sagar Jadav , Rashmi Vanakudri , Venkatrao Kulkarni

Objectives

Bacopa–phospholipid complex (BPC), a novel phytoformulation was prepared, characterized and evaluated for its possible enhancement of antiamnesic activity as compared to bacopa extract (BE) in natural aging induced amnesic mice.

Methods

BPC was characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and FTIR. Antiamnesic activity of BPC (40 mg/kg body weight) and BE (40 mg/kg body weight) was evaluated using elevated plus-maze (EPM), Morris water maze (MWM) and Passive shock avoidance (PSA) tests.

Results

SEM data showed that BPC has irregular size vesicles consisting of phoaphatidylcholine (PC) and BE was found to be intercalated in the lipid layer. BPC showed two endothermal peaks (80.90 °C and 171 °C) in DSC studies. Aged mice showed poor retention of memory in EPM, MWM and PSA models. Administration of BPC (40 mg/kg; p.o.) and BE (40 mg/kg; p.o.) significantly reversed cognitive deficits in aged mice. However, enhanced antiamnesic activity was observed with BPC as compared to BE in all the memory models tested. This is also supported by enhanced acetyl cholinesterase inhibitory activity of BPC. A higher serum concentration of bacopaside-I (12.21 μg/ml) and bacopaside-II (12.28 μg/ml) was observed for BPC in bioavailability studies as compared to BE. BPC maintained effective concentration of bacopasides for a longer period in rat serum.

Conclusion

Bacopa–phospholipid complex has shown improved antiamnesic activity as compared to bacopa extract at the dose studied. This might be due to better absorption of bacopasides from the complex.

目的制备一种新型植物制剂假马齿苋磷脂复合物(BPC)，与假马齿苋提取物(BE)相比，对其抗衰老性失忆症小鼠的抗遗忘活性进行了表征和评价。方法采用扫描电镜(SEM)、差示扫描量热法(DSC)和红外光谱(FTIR)对sbpc进行表征。采用升高+迷宫(EPM)、Morris水迷宫(MWM)和被动避震(PSA)试验评价BPC (40 mg/kg体重)和BE (40 mg/kg体重)的抗遗忘活性。结果扫描电镜显示，BPC具有由磷脂酰胆碱(PC)组成的不规则大小的囊泡，并在脂质层中嵌入BE。BPC在DSC研究中显示两个吸热峰(80.90°C和171°C)。老年小鼠在EPM、MWM和PSA模型中表现出较差的记忆保留。给药BPC (40 mg/kg;p.o.)和BE (40 mg/kg;p.o.)显著地逆转了老年小鼠的认知缺陷。然而，在所有测试的记忆模型中，与BE相比，BPC的抗遗忘活性都有所增强。BPC对乙酰胆碱酯酶抑制活性的增强也支持了这一点。在生物利用度研究中，与BE相比，BPC血清中bacopaside-I (12.21 μg/ml)和bacopaside-II (12.28 μg/ml)浓度较高。BPC能在较长时间内维持大鼠血清中假杆菌皂苷的有效浓度。结论与所研究剂量的假马齿苋提取物相比，假马齿苋磷脂复合物具有更强的抗遗忘活性。这可能是由于从复合体中更好地吸收了假马齿苋苷。

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引用次数: 50

In silico validation of human N-myc downstream-regulated gene 2 protein against Alzheimer's disease using molecular modeling, docking and dynamics studies 基于分子模型、对接和动力学研究的人类N-myc下游调控基因2蛋白抗阿尔茨海默病的计算机验证

Drug Invention Today

Pub Date : 2013-03-01 DOI: 10.1016/j.dit.2013.02.002

Aathi Muthusankar, Piramanayagam Shanmughavel

Objectives

The human N-myc downstream-regulated gene 2 (hNDRG2) protein is mainly responsible for Alzheimer's disease (AD). It has 371 amino acid residues in their sequence. The 3dimensional (3D) structure of the complete sequence of this protein is still unknown. The present research computationally emphases to predict the 3D structure for the complete sequence of hNDRG2 protein and efficiency of this protein against AD was evaluated with synthetic and natural compounds using docking studies. Molecular dynamics (MD) study was performed to find the stability of the best interacted molecule.

Methods

The hNDRG2 protein was modeled using Modeller9v10. The lead compounds were retrieved from PubChem database. Docking studies were performed using AutoDock4.2. MD study was done by Macro model.

Results

The modeled hNDRG2 protein was validated using Ramachandran plot and it showed the value of 90.8% in the most favored regions. From the results of docking studies, the interaction of modeled protein with synthetic tacrine showed the binding energy value of −4.44 kcal/mol and the interactions with 15 phytocompounds of Rosmarinus officinalis, a natural compound (+)-borneol showed the best binding energy value of −4.64 kcal/mol. The result of MD study determined that, the complex of modeled protein with (+)-borneol was stable at 2.2 ns.

Conclusions

In the above study, when the interaction of phytocompounds compared with synthetic tacrine, the natural compound (+)-borneol have showed good interaction with modeled protein and it is suggested to treat AD for avoiding the side effects of synthetic drugs.

目的人类N-myc下游调控基因2 (hNDRG2)蛋白是阿尔茨海默病(AD)的主要致病因子。它的序列有371个氨基酸残基。该蛋白完整序列的三维结构尚不清楚。本研究的计算重点是预测hNDRG2蛋白全序列的三维结构，并通过对接研究，对该蛋白与合成和天然化合物的抗AD效率进行了评价。通过分子动力学(MD)研究确定了最佳相互作用分子的稳定性。方法采用modeler9v10对hNDRG2蛋白进行建模。先导化合物从PubChem数据库中检索。对接研究使用AutoDock4.2进行。MD研究采用宏观模型。结果构建的hNDRG2蛋白经Ramachandran图验证，在最有利区域的表达率为90.8%。从对接研究结果看，模型蛋白与合成龙脑碱的相互作用结合能值为−4.44 kcal/mol，与15种迷迭香植物化合物的相互作用结合能值最高，其中天然化合物(+)-冰片的结合能值为−4.64 kcal/mol。MD研究结果表明，模型蛋白与(+)-冰片的复合物在2.2 ns时稳定。结论在上述研究中，当植物化合物与合成冰片碱的相互作用比较时，天然化合物(+)-冰片与模型蛋白的相互作用良好，建议用于治疗AD以避免合成药物的副作用。

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引用次数: 3

Review on Prosopis cineraria: A potential herb of Thar desert 塔里木沙漠潜在草本植物棘豆的研究进展

Drug Invention Today

Pub Date : 2013-03-01 DOI: 10.1016/j.dit.2013.03.002

Akash Garg , Sanjeev K. Mittal

Prosopis cineraria (L.) Druce is an important herbal plant as mentioned in ancient literature. It is used traditionally for treatment of various ailments like leprosy, dysentery, asthma, leucoderma, dyspepsia and earache etc. Various phytoconstituents like tannins (gallic acid), steroids (Stigmasterol, campesterol, sitosterol etc), Flavone derivatives (Prosogerin A, B, C, D, and E), alkaloids (Spicigerine, Prosophylline) etc has been isolated from the plant. Pharmacological activities like analgesic, antipyretic, antihyperglycemic, antioxidant, antihypercholesterolemic, antitumor, nootropic have been reported from different plant extracts. The present paper deals with review of phytoconstituents and pharmacological action of plant P. cineraria.

灰藜(L.)德鲁斯是古代文献中提到的一种重要的草本植物。传统上用于治疗各种疾病，如麻风病、痢疾、哮喘、白癜风、消化不良和耳痛等。从该植物中分离出多种植物成分，如单宁(没食子酸)、类固醇(豆甾醇、油菜甾醇、谷甾醇等)、黄酮类衍生物(Prosogerin A、B、C、D和E)、生物碱(Spicigerine、prosophyline)等。不同植物提取物具有镇痛、解热、降血糖、抗氧化、降胆固醇、抗肿瘤、促智等药理作用。本文综述了金针菇的植物成分及其药理作用的研究进展。

引用次数: 36

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