Drug Designing & Intellectual Properties International Journal

Isak R Shaikh* and Alamgir A Shaikh

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Historical records show that scientific advancements accounted for substantial changes in our life-style and wellbeing. The Industrial Revolution took place in the western countries in the 1700s when people first appreciated the terms ‘science’ and ‘technology’ and valued the applications of ‘technological innovations’ for their commercialization......

François-Xavier Lacasse*

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The author of this short communication has been working in and teaching drug development for the last 20 years. He has been involved in more than 100 drug development projects, including drug delivery, medical device, biologics, innovators and generic drugs. He has also been involved in all the steps that are needed to file properly to different governmental agencies investigational new drug applications (IND), clinical trial applications (CTA), abbreviated and new drug applications/submissions (ANDAS; NDA/S), 505b2, 510k and biologics legal applications (BLA)......

Amit Gosar, Hussain Sayyed and Tabrez Shaikh*

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The present work is based on a assess analysis of the literature in order to define the genotoxic impurities present in the drug substances and drug products. Starting from the definition of genotoxic impurities, sources of genotoxic impurities, their generation and classification based on their toxicity. The article also explains the various regulatory guidelines to control the genotoxic impurities in drug substances. Isolation, qualification of impurity and its identification along with quantification by the various analytical methods is also described in this review article......

Benjamín Ruiz Loyola*

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In all animal species competition between individuals is presented to obtain mainly food and reproduction; When there are not enough satisfiers, there are disputes that usually stop when there is a winner, without individuals dying. The defeated one retires, and the winner is satisfied with the victory and, eventually, with the dominion over the rest of the group, which implies that he will eat and mate before the others. So far, animals do not have too much trouble. But the human is a very special animal, because he has a memory......

Amani Mohsen* and Rabih Chahine

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Once Antiphospholipid syndrome (APS) is diagnosed, risk profile of the patient will impact its management whether there was a previous thrombotic event or not, association with other autoimmune disorders, presence of other obstetrical complications as well as being currently pregnant. The current recommended regimen for preventing obstetrical complications. The current recommended regimen for preventing obstetrical complications includes low molecular weight Heparin and low dose aspirin. This regimen decreases the risk of miscarriage by only 54%. Here, we will review the studies that evaluated adding Hydroxychloroquine (HCQ) to the treatment of APS and how effective it would be......

A Krishna Sailaja*

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Splendid achievements have been made in management of disease through invention of drugs over past decade. The present conventional drug delivery systems often have side-effects and complications due to their wide distribution throughout the body fluids. The localization of drug action in injured tissue is a promising way to solve this problem. The objective of drug targeting is to achieve a desired pharmacological response at a selected site without undesirable interaction at other sites. This is especially important in cancer chemotherapy and rheumatoid arthritis treatment. Recently invention of drugs has been generated by various drug delivery systems like microspheres, liposomes, noisomes, nanocapsules and nanoparticles. Among all colloidal drug carriers’ nanoparticles are gaining more popularity b.....

Hossam Mohammed Gomaa* and Ahmed Hatim Hamdy EL-Dosokey

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Some of iron bismuth borate oxide glasses were prepared to form a series of glass samples contain a constant and a fixed amount of Fe2O3 whereas the B2O3 was replaced by Bi2O3, according to the formula 20 mol % Fe2O3–(15 + x) mol % Bi2O3–(65–x) mol % B2O3, where 0 ≤ x ≤ 20. The X-ray diffraction and FTIR Spectra showed formation of homogenous short-range order structures. The values of the refractive index were estimated using both FTIR date room temperature dialectic measurements are in a good agreement with each other. It is clear that the ε increased with the increasing of Bi2O3 content......

Isaac John Umaru*, Fasihuddin Badruddin Ahmed, Hauwa A Umaru, Kerenhappuch I Umaru and Benedict Samling

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A review of Barringtonia asiatica considered to be a mangrove associated species is made to update its Phytochemical and Pharmacological Properties which is claimed to be a broad-spectrum medicinal property. Barringtonia asiatica was commonly used in various country of the world for treatment of liver disorder, diarrheal disease, eye disease, as well as antifungal and antibacterial, as well as chest pains and heart troubles. It was also considered a fish killer; this has been identified as a source of Natural products with potentials as an antitumor. The aim of the present review is to provide detailed information regarding geographical distribution, phytochemicals and pharmacological properties of this plant......

Robert Skopec*

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State Department evacuates a number of Americans from the U.S. consulate in Guangzhou, China after they experienced unexplained health issues. A group of U.S. diplomats stationed in China have been brought back to the states after being inflicted by a mystery illness that reportedly resembles the brain injuries previously suffered by staff in Cuba. Heather Nauert, a State Department spokeswoman, said in a statement that the individuals from the U.S. office in Guangzhou were returned home for further evaluation. It was unclear if there was any connection to last year’s situation in Cuba where 24 US government employees experienced a range of ailments after hearing an unusual sound......

Nahd Mohamed Elmaki, Inass A Al Sadawi, Anton Hermann and Abdul M Gbaj*

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Molecular modeling attempts to study the function, structure and inhibition of the acetylcholinesterase enzyme due to the fact that the inhibition of this enzyme is importance to medical conditions such as Alzheimer’s disease, myasthenia gravis and Parkinson’s disease, and it is also important in eminent toxicological susceptibility to nerve agents. In this study we present an approach for forecasting the inhibitory activity of acetylcholinesterase (AChE) inhibitors by using docking studies. The docking studies were done on acetylcholinesterase to attain the conformation of the enzyme in water surroundings. The obtained conformation of the enzyme was used for docking with four inhibitors (physostigmine, neostigmine, pyridostigmine and rivastigmine). Docking analysis showed that hydrogen bonds and hydrophobic interactio.....

Kapoor D*, Vyas RB and Dadrwal D

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Ionic liquids considered to be a reasonably current magical chemical due their unique properties, have a large variety of applications in all areas of the chemical and pharmaceutical industries. The areas of application consist electrolyte in batteries, lubricants, plasticizers, solvents and catalysis in synthesis, matrices for mass spectroscopy, solvents to manufacture nano-materials, extraction, gas absorption agents, etc. Non-volatility and nonflammability are their widespread characteristics giving them a beneficial edge in a variety of applications. Ionic liquids can be considered as green solvents due to their very low vapor pressure and wide range of applications with unique physical and chemical properties. Ionic liquids use for clean and efficient energy, through the development of a broad swath of energ.....

Cauê Benito Scarim and Chung Man Chin*

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Chagas disease is a protozoan infection which was first identified more than one hundred years ago. But even now, drugs to treat the latent and chronic phases of the disease are not available. The success of a drug design is highly dependent on activity and toxicity. In the case of Chagas disease, questions remain as to identifying the best treatment (mainly for the chronic phase), and how new drugs and drug combinations compare to current therapy. The principal priority of this mini-review is to report the enormous difficulty that pharmaceutical chemists encounter in the development of new drugs for neglected tropical infectious diseases, in this case Chagas disease......

Kholmuradova Mushtariy*

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Name of drugs are analyzed in the represented article “Kutadgu bilig”. Lexical units of medical concepts are widely investigated by the works of Yusuf Khos Khojib including human body part, health, temper, and eating habits. The importance of medical terms, and medical viewpoints are enlightened of our nowadays medicine......

Debarshi Kar Mahapatra*, Mohamad Taleuzzaman, Santosh S Chhajed

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The irrational use of antimicrobial agents for several decades has led to the drug-resistance among the patient population. Overcoming the present drug-resistance is a major challenge for modern day scientists. In order to counter this problem, several approaches have been utilized, one of which involve drug design and discovery, where new classes or unexplored chemical moieties are explored for a particular activity, either serendipitously or quite rationally. Learning lessons from the previously synthesized four compounds (Part-I of Research), we have now (Part-II of Research) designed two compounds (3 and 5) by incorporating an additional 4-(2-aminoethyl) aniline group in the fabricated isoindoline-1,3-dione scaffold by successive synthetic step utilizing similar protocol and screened th.....

Isaac John Umaru*, Chinedu Imo, Kayode Arowora, Silas Verwiyah Tatah and Hauwa A Umaru

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Essential oils are liquid mixture of volatile compound obtained from aromatic plants. It was observed that many essential oils have antioxidant properties and can present antimicrobial activities. The Aim of the present study were: a) to determine the cytotoxicity lethality of the leafs and stem-bark of Barringtonia asiatica using brine shrimp (Artimia salina). b) to evaluate the antioxidant potential of composition of the leaf and stem-bark essential oil using the DPPH (2,2-diphenyl-1-picrylhydrazyl) free radical scavenging assay. The essential oil exhibited a mild toxicity and significant IC50 of 36.55μg/mL and 22.10μg/mL value of antioxidant potential leaf and stem-bark of Barringtonia asiatica respectively......

Loai Aljerf * and Nuha AlMasri

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Alcohol use disorders (AUD) involving hazardous, harmful and addictive misuse of alcohol are widespread in most parts of the world. The aim of this study was to review the effect of the common inhibitors in the treatment of patients with AUD, taking into consideration, the short- and long- terms abstinence. An extensive literature search conducted in MEDLINE, PubMed, Scopus and CINAHL databases identified 776 articles, which were then evaluated for pre‐specified criteria for relevance and quality assurance. A total of 38 articles, including 36 human studies and 2 animal studies, were selected for this review. Many inhibitors used in the treatment of alcoholism and some were considered of effective medication when their intakes are supervised by an expert. However, their therapeutic efficacies vary widely; for instance, disulfiram is a.....

Robert Skopec*

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State Department evacuates a number of Americans from the US consulate in Guangzhou, China after they experienced unexplained health issues. A group of US diplomats stationed in China have been brought back to the states after being inflicted by a mystery illness that reportedly resembles the brain injuries previously suffered by staff in Cuba. Heather Nauert, a State Department spokeswoman, said in a statement that the individuals from the US office in Guangzhou were returned home for further evaluation. It was unclear if there was any connection to last year’s situation in Cuba where 24 US government employees experienced a range of ailments after hearing an unusual sound......

Amani Mohsen*

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Globally, mental health disorders are increasingly prevalent worldwide with depression particularly contributed to the largest percentage of global disability (7.5% of all years lived with disability in 2015). It is more common in females than males affecting 4 -7% of women in reproductive age group [1]. Women with mild depression are treated with cognitive based therapy and antidepressants are used depending on the severity of the symptoms [2]......

Rahul Hajare*

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We report here doggy style sex inter subtype alcohol dependent recombinants from India. One among those is recombinant penile fracture is reported for the first time from India......

Rahul Hajare*

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An Extra-marital affair relationship can break heart. Extra-marital affair women, according to a study, have a higher risk for heart disease. Turns out, for women, being extra-marital affair can be injurious to health. According to a study conducted by the New York University, extra-marital affair women have a higher risk for heart disease compared with non-extra-marital affair women across several modifiable risk factors [1-3]. “Our findings highlight the impact of sexual orientation, specifically sexual identity, on the cardiovascular health of women and suggest clinicians and public health practitioners should develop tailored screening and prevention to reduce heart disease risk in extra-marital affair women,” Little is known about the impact of sexual orie.....

Mahmoud Kamal, Mohamed Maher, Amr Ibrahim and Dina Louis*

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Niosome are non-ionic surfactant vesicles acquired on hydration of synthetic nonionic surfactants, with or without consolidation of cholesterol or their lipids. They are vesicular systems like liposome’s that can be utilized as transporters of amphiphilic and lipophilic medications. Niosomes are promising vehicle for drug delivery and being non-ionic; and Niosomes are biodegradable, biocompatible non mmunogenic and show adaptability and flexibility in their structural characterization. Niosomes have been generally assessed for controlled discharge and targeted delivery for the treatment of tumor, viral infections and other microbial illnesses. Niosomes can entangle both hydrophilic and lipophilic medications and can prolong the circulation of the entrapped medication in body. Encapsul.....

Joydeep Dhar*

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Inability to early diagnosis is a major concern for the treatment of fatal disease like cancer. Early diagnosis and treatment enhances the scope of disease curability. The accurate identification, real-time monitoring and targeting the cancerous tissues in a precise manner hold the key for longer progression free survival of a patient. Among different diagnostic techniques, fluorescence based minimally invasive bio-imaging techniques are considered to be ideal to have clear understanding about the physiological processes of the infected tissues as well as to reduce physical and mental stress of a patient. Super-resolution luorescence microscopy has improved the spatial optical resolution of biological molecules, living cells and tissues with the use of highly fluorescent inorganic semiconductor nanocrystal.....

Suresh Kumar*

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Intrinsically disordered proteins (IDPs) are proteins that usually do not adopt well-defined native structures when isolated in solution under physiological conditions. Numerous IDPs have close relationships with human diseases such as Parkinson disease, Alzheimer disease, diabetes, and so on. Recently IDPs are getting importance as desirable drug targets for major diseases. This review introduces IDP’s in drug discovery by experimental and by computational approach......

Isaac John Umaru*, Fasihuddin A Badruddin and Hauwa A Umaru

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Leptadenia hastata extracts were evaluated for antibacterial activity and antioxidant properties. The leaf of the plant was extracted with n-hexane, dichloromethane, ethyl acetate, chloroform and ethanol to give respective extracts. The Antibacterial activity against staphylococcus aureus, was determined by disc diffusion method. Antioxidant activity was assayed by the DPPH radical scavenging activity mechanism. The results showed that of n-hexane, ethyl acetate, dichloromethane, chloroform and methanol extracts of Leptadenia hastata , methanol extract and chloroform extracts displayed more activity with 1.10 ± 0.10ab and 0.97 ± 0.06ab than others at 25-1000ppm/desk of the extracts tested. The most antioxidant activities against DPPH were displayed by the hexane.....

Chang Rok Jeong*

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In the US, more than 400,000 medical treatments are carried out each year to eliminate intestinal adhesion. The economic loss from these medical treatments is estimated to be about $1.2 billion. This economic loss has been significant, and the search results from pub med under keyword Intestinal Obstruction have been decreasing since 2015. It is difficult to research and prevent a disease caused by small intestine, which is one of the emergency diseases. Because emergency diseases have structural problems that are very difficult to collect and analyze data for research. Emergency care measures, especially drug development, require a platform that allows public funding and sharing of clinical data. Emergency diseases have scattered clinical data. The research into this emergency disease requires a method of receiving clinical data.....

Ayoub Ainane *, Fatima khammour, M’hamed Elkouali, Mohammed Talbi , El Hassan Abba, Sanaa Cherroud, Adnane Elyaacoubi, Khadija Oumaskour, Nabila Boujaber, Said Benhar and Tarik Ainane

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This work aims to evaluate the composition of the essential oils of certain mints grown in the region of Settat Morocco and to determine their chemical compositions. The essential oils obtained by hydrodistillation have an average yield of: 2.93% for Mentha pulegium , 1.23% for Mentha piperita and 0.91% for Mentha spicata . Analyzes of oils by GC-MS, showed the presence of several components including Menthone (42.97%) and Menthol (27.64%) are the major components of Mentha iperita , piperitone (31.27%) and piperitenone (22.98%) were obtained as the major compounds of Mentha pulegium , and so the main essential oil compounds of Mentha spicata are carvone (33.14%) and trans-Carveol (20.06%)......

M Garofano, MM Ascoli, M Ciriello, M Aliberti and M Calabrese*

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The present work is based on a careful analysis of the literature in order to find out what the right type of exercise can be recommended to the patient with COPD. Starting from the basic assumption that exercise is itself a biological therapy, we have looked to molecules that are critically altered in these patients so as to constitute potential molecular markers. We have also seen if, how, and how much the exercise is able to determine a modulation of the levels of these molecules in a functional sense to improve the clinical condition of the patients......

Benzion Amoyav and Ofra Benny*

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We are currently facing a global health challenge regarding the way we discover and develop new drugs. Small biotech companies, as well as large pharmaceutical corporations, spend increasingly more money on the classical route of drug development, and it fails more often than it succeeds. Consequently, some diseases are not being treated and patients who are in dire need of new therapies are not receiving them. The classic tools available for testing whether a drug will work efficiently and safely or fail before we reach advanced stages of human clinical trials and spend millions of dollars, do not predict in a robust way......

Veronika Benson* and Eva Neuhӧferová

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Micro RNAs are short non-coding RNA molecules, which are important regulators of cell functions. Deregulation of certain micro RNA level is contributing factor to tumor formation and progression. Possible gene therapy by modulation of the micro RNA level is currently considered. Recently it has been proved that nano diamonds coated with PEI serve as efficient transfection and monitoring system. The aim of our work was to deliver micro RNA inhibitor and micro RNA mimic sequences into specialized mammalian cells using fluorescent nano diamond particles and to test the nano complex uptake and cell compatibility during primary in vivo application. Short RNA molecules were bound to the PEI coated nano diamonds, transported into the colon cancer cell line in vitro and observed in a confocal microscope. The miRNA mimic coated nano diamond.....

Carmen Gruber Traub* and Jenny Ullrich

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Within the EU funded project »N2B-patch« eleven partners from eight countries aim to develop an innovative technology for the nose-to-brain delivery of an active pharmaceutical ingredient via the olfactory region for the regenerative treatment of multiple sclerosis using novel multi-functional biomaterials combined with a medical device. The four year EU-funded research involves an innovative method of bypassing the blood-brain barrier by delivering a potential multiple sclerosis drug with a special medical device via the nose directly to the brain. The World Health Organisation (WHO) estimates that more than one billion people worldwide are suffering from neurological disorders [1]. The therapy of central nervous system (CNS) diseases like multiple sclerosis (.....

Rahul Hajare*

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Single mother cannot produce benefit properly which is required to children, playing, and other food source into energy. Researcher has been looking for simple and effective ways to deliver benefit into the children who have a single mother to child by their choices as well as single mother has to her choice. The most common one is taking orally that has financial support from organization which is privately manage and ruled out by under the surveillances of Pharmacy council of India. However research shows that is easily broken down by the system. This problem has solved by using intervention by secretarial level department of health research (DHR) government of India. These can be done by binding pharmacy council of India by department of health research with government of India. The encouragement is protected with.....

Maximiliano A Iramain and Silvia A Brandán*

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The structural and vibrational properties of acid species, hexa-hydrated and anhydrous trisodic salts of antiviral drug foscarnet in gas phase and in aqueous solution have been studied in this work by using the hybrid B3LYP method with the 6-31G* and 6-311++G** basis sets. The properties in solution were carried out with the self consistent reaction force (SCRF) method by using the integral equation formalism variant polarised continuum (IEFPCM) and SD models while the complete vibrational assignments for those three species were performed in both media by using the experimental available infrared spectrum of hexa-hydrated trisodic salt and the scaled quantum mechanical force field (SQMFF) methodology. The natural bond orbital (NBO) studies suggest that the hexa-hydrated salt in solution is most stable than the anhydrous one in the same m.....

Robert Skopec*

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Thanks to their influence on the owner’s gut micro biome, dogs may be beneficial in reducing cardiovascular, diabetes, multiple sclerosis and cancer risk by providing a non-human form of social support and increasing physical activity. Ownership of hunting dog breeds was associated with a decreased risk of CVD, and ownership of all purebred breeds was associated with lower risk of all-cause mortality. Dog ownership has also been associated with elevated parasympathetic and diminished sympathetic nervous system activity, lower reactivity to stress, and faster recovery of blood pressure following stressful activity. We provide evidence that supports epsilon toxin’s ability to cause BBB permeability and show that epsilon toxin kills the brain’s myelin producing cells, oligodendrocytes; the same cells die in multiple s.....

Subhajit Ghosh*, Dr PN Murthy and Dr H Joshi

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In this study was to evaluate the effect of Draksharishta-T and Draksharishta -M prepared by traditional and modern methods respectively and Dabur Draksharishta and comparison between them on fasting blood glucose and serum lipid profile in alloxan induced diabetic rats. Oral administration of Draksharishta-T, Draksharishta-M and Dabur Draksharishta (2ml/kg p.o.) for 21 days caused a significant decrease in fasting blood glucose (FBG) and showed significant rise in blood glutathione level (GSH) in diabetic rats. Glibenclamide was used as a standard anti diabetic drug (10 mg/kg, p.o). These preparations also caused significant reduction in serum cholesterol, LDL and triglycerides and showed significant rise in serum HDL level in diabetic albino rats. Thus all these preparations were able to maintain the tested parameters near to the normal.....

François Xavier Lacasse*

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During the last decade, and exponentially over the last three years, numerous pharmaceutical manufacturing plants have closed their doors following current Good Manufacturing Practices (cGMP) audits from various agencies, such as FDA, EMA and Health Canada. Regulatory affairs have been evolving and so should be the audits, auditors and regulations. However, the density and interpretations of regulatory requirements have become increasingly stringent, especially with respect to sterile products, making them more difficult to develop and manufacture within reasonable time and cost. A quick search on Google shows numerous press releases from various pharmaceutical organizations reporting critical/ major deficiencies, leading to temporary or permanent closures of manufacturing plants. Furthermore, it seems that this evolving situation has not.....

Samell Keo*, Sonita Leang, Chanseiha Ny, Sokhany Lim, KosalvorlakChean, Huykhim Ung, Juthamart Maneenet, Yaowared Chulikhit and Sin Chea

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Cambodian medicinal plants have been used to treat different diseases such as cardiovascular diseases, inflammation, cancers, diabetes and AIDS. This study aimed at conducting the Phytochemical analysis and in vitro antioxidant activities of whole plant of Bryophyllumpinnatum (Lam.) Kurz, barks of Dillenia ovata Wall. ex Hook. f. & Thomson, rhizomes of Drynariafortunei (Kunzeex Mett.) J. Sm. and barks of Lophopetalumwallichii Kurz. native to Cambodia. All the plants were extracted with ethanolby maceration extraction method. The Phytochemical analysis for alkaloids, phenolic compounds, tannins, flavonoids, coumarins, steroids, terpenoids, cardiac glycosides, essential oils, saponins and resins by using the standard methods. The in vitro antioxidant property was evaluated by assessing the DPPH ̇ radical.....

Zaid A Abdulmonaim and Athir M Haddad*

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The semi interpenetrating network hydrogels (Z1-Z15) were prepared from different ratio of sodium alginate and linear poly (acrylamide-co-diallyl dimethyl ammonium chloride) then they mixed with the acrylamide and bisacrylamide as cross linking agent and polymerized via redox polymerization to form the semi-IPNs. All prepared semi-IPNs were loaded with three different amounts from Gabapentin as drug model. The swelling characteristics were studied for all semi- IPN hydrogels by determining the swelling ratio (Q).The release of Gabapentin was followed by using U.V. spectroscopy at (202 , 201 and 204) nm at constant temperature (37ºC) in distilled water , simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) respectly. The results of Gabapentin released indicated that all semi-IPNs have the ability to re.....

Kapoor D*, Vyas RB and Dadarwal D

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The top priority in any health system is delivering of medicine as a strategic product. In the present context of a health-conscious society, management of pharmaceutical supply chains has become more complex because it involves the life-saving interest of human being and requires the participation of different stakeholders such as pharmaceutical manufacturers, wholesalers, distributors, customers, information service providers and regulatory agencies. Limited research is available in the area of pharmaceutical supply chains. Pharmaceutical companies, a most important player of the drug supply chain, are subject to many risks. These risks interrupt the quantity and quality of supply of medicine and their delivery to the accurate place and customers and at the correct time......

Eric Lattmann* and Pornthip Lattmann

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Early anti-cancer research was dominated by the development of alkylating agents, followed by the discovery of a variety of anti-metabolites, which were useful anti-viral agents at the same time. Current anti-cancer drugs are designed towards molecular targets in order to reduce their toxicity and to enhance the selectivity on the cancer cells. Within an increasingly growing number of molecular targets, the cholecystokinin, as a neuro modulator, became an important anti-cancer target, especially when it was shown that cholecystokinin regulates the invasiveness of human pancreatic cancer cell lines via the protein kinase C pathway. The low potency and the lack of subtype receptor selectivity of those early non-peptide CCK-antagonists, was improved in the following generations of CCK antagonists. These potent and selective antagonists have .....

Eric Lattmann*, JintanaSattayasai, Ramesh Narayanan, Julian Benyamen, PN Balaram and Pornthip Lattmann

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Arylated 5-hydroxy–pyrrol-2-ones were prepared in 2 synthetic steps from muco-chloric acid and were optimised as CCK1 / CCK2 selective ligands using radio labelled binding assays. A potent CCK1 selective ligand was identified (PNB-081: CCK1=20nM) as well as a potent CCK2 ligand (PNB-001, IC50= 22nM) during a systematic SAR optimisation. The antagonism was confirmed for both ligands by using isolated tissue preparations with CCK5 and CCK8S. Subsequent in vivo evaluation revealed analgesic activity for the gastrin CCK2 antagonist PNB-001, in the hotplate and tail immersion test at 0.5mg /kg by IP administration in mice. The cholecystokinin antagonist PNB-081 potentiated the analgesic effect of morphine and reversed opiate tolerance in mice from doses >1 mg/kg by oral administration......

VK Singh*, Peeyush Bharadwaj and Poonam Rishishwar

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1,2,3-Benzotriazole (BTA) is a heterocyclic compound with three nitrogen atoms. It is a polar and colourless compound which can be used for its great versatility. The enormous investigations on derivatives of benzotriazole reveal wide applicability of this molecule for tagging and delivering huge number of heterocyclic nuclei. In the present work synthesis of several derivatives of 2-(substituted)-5-[(n-benzotriazolomethyl)-1,3,4-thiadiazolyl]-4-thiazolidinone has been synthesized and are evaluated for their anxiolytic activity. The antianxiety activities of the synthesized derivatives were evaluated using EPM test and Bright and dark box test experimental models of anxiety. All results were expressed as mean± standard error mean (SEM) and analysed by one-way ANOVA. Post-hoc comparisons were performed by applying Dunnet’s test. P <0.05.....

P Veera Lakshmi, KPR Chowdary*, A Prameela Rani S and VUM Prasad

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Recently much emphasis is being laid on the development of micro particulate DDS in preference to single unit systems because of their potential benefits such as increased bioavailability, reduced risk of systemic toxicity, reduced risk of local irritation and predictable gastric emptying. The objective of the present study is to prepare and evaluate micro particulate drug delivery systems of Gliclazide using starch acetate, a new modified starch for oral controlled release. The starch acetate (DS 2.75) was freely soluble in chloroform and insoluble in several aqueous fluids and organic solvents. Chloroform could be used as solvent for starch acetate in the preparation of micro particles, microcapsules and in film coating Spherical starch acetate- Gliclazide micro particles could be prepared by the emulsification-solvent evaporation metho.....

Y Y Gao, S Ediz, M R Farahani* and M Imran

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Topological indices which are graph invariants derived from molecular graphs of molecules are used in QSPR researches for modeling physicochemical properties of molecules. Topological indices are important tools for determining the underlying topology of a molecule in view of theoretical chemistry. The second harmonic index has been defined recently. In this study we compute the second harmonic index of Titania nanotubes......

François Xavier Lacasse* and France Guay

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During the last decades, life science startup companies have relatively rapidly increased their presence in the pharmaceutical landscape. Pharmaceutical development has evolved because technology (analytical and process development) and clinical development (hybrid design in phase 1, including patients in phase 1B) have evolved in parallel allowing in certain cases to decrease the time to regulatory filings (IND, CTA, NDA, NDA 505 (b)(2),..), which seemed attractive for startup companies. However, new molecular entities have become more complex since polypeptides, proteins, and monoclonal antibodies drug products take more and more place in many therapeutic areas (more than 50% in the 50 best seller drugs) along with the more conventional small molecules. But it is not the end of small molecules; research institutes, startup companies are.....