Development of drugs

As science and technology has developed, the manner by which drugs can be delivered has grown. Medicines may be taken orally, applied as topical pastes, creams or oils, patches or administered by direct injection to the body. This research explores an alternative method for the delivery of therapeutic compounds to the body. The basis of the study involves the application of traditional medicinal compounds used to cure minor neck and back pains through transdermal topical application, using a textile substrate as the carrier.

128p runthenight07 01-03-2023 10 3   Download

Developed a chemometric-photometric analysis process in combination with Kalman filter method to simultaneously analyze mixtures of 2 and 3 substances with molecular absorption spectra overlapping in pharmaceutical samples; apply the process has been built to simultanneously analyze mixtures 2 and 3 substances in some pharmaceuticals are on the market Vietnam.

26p nguathienthan12 23-05-2021 23 3   Download

Precision medicine promises to improve both the efficacy and safety of therapeutic products by better informing why some patients respond well to a drug, and some experience adverse reactions, while others do not. Pharmacogenomics is a key component of precision medicine and can be utilized to select optimal doses for patients, more precisely identify individuals who will respond to a treatment and avoid serious drug-related toxicities.

5p caothientrangnguyen 09-05-2020 11 2   Download

Development of optimized pediatric formulations for oral administration can be challenging, time consuming, and financially intensive process. Since its inception, the biopharmaceutical classification system (BCS) has facilitated the development of oral drug formulations destined for adults. At least theoretically, the BCS principles are applied also to pediatrics. A comprehensive age-appropriate BCS has not been fully developed.

9p caothientrangnguyen 09-05-2020 36 3   Download

AR-42, a new orally bioavailable, potent, hydroxamate-tethered phenylbutyrate class I/IIB histone deacetylase inhibitor currently is under evaluation in phase 1 and 2 clinical trials and has demonstrated activity in both hematologic and solid tumor malignancies. This report focuses on the preclinical characterization of the pharmacokinetics of AR-42 in mice and rats.

9p caothientrangnguyen 09-05-2020 18 3   Download

A Bayesian approach with frequentist validity has been developed to support inferences derived from a BLevel A^ in vivo-in vitro correlation (IVIVC). Irrespective of whether the in vivo data reflect in vivo dissolution or absorption, the IVIVC is typically assessed using a linear regression model. Confidence intervals are generally used to describe the uncertainty around the model. While the confidence intervals can describe population-level variability, it does not address the individual-level variability.

16p caothientrangnguyen 09-05-2020 35 2   Download

Schistosomiasis is an endemic disease in Egypt caused by the trematode Schistosoma which has different species. c the best known form of chronic disease with a wide range of clinical manifestations. The pathogenesis of schistosomiasis is related to the host cellular immune response. This leads to granuloma formation and neo angiogenesis with subsequent periportal fibrosis manifested as portal hypertension, splenomegaly and esophageal varices. Intestinal schistosomiasis is another well identified form of chronic schistosomal affection.

8p kethamoi1 17-11-2019 29 2   Download

The cytochrome P450 family of enzymes has long been known tometabolize a wide range of compounds, including many of today’s most common drugs. A novel nuclear receptor called PXR has been established as an activator of several of the cytochrome P450 genes, including CYP3A4. This enzyme is believed to account for the metabolism of more than 50% of all prescription drugs. PXR is therefore used as a negative selector target and discriminatory filter in preclinical drug development.

9p research12 29-04-2013 44 3   Download

Semi-synthetic cephalosporin antibiotics belong to the top 10 of most sold drugs, and are produced from 7-aminodes-acetoxycephalosporanic acid (7-ADCA). Recently new routes have been developed which allow for the production of adipyl-7-ADCA by a novel fermentation process. To complete the biosynthesis of 7-ADCAa highly active adipyl acylase is needed for deacylation of the adipyl derivative. Such an adipyl acylase can be generated from known glu-taryl acylases.

10p research12 23-04-2013 33 3   Download

The efficacy of antiretroviral agents approved for the treat-ment of HIV-1 infection is limited by the virus’s ability to develop resistance. As such there is an urgent need for new ways of thinking about anti-HIV drug development, and accordingly novel viral and cellular targets critical toHIV-1 replication need to be explored and exploited. The retroviral RNA genome encodes for three enzymes essential for viral replication: HIV-1 protease (PR), HIV-1 reverse transcrip-tase (RT) and HIV-1 integrase (IN). ...

9p tumor12 22-04-2013 33 2   Download

Theb-amyloid peptide (Ab) is a major component of toxic amyloid plaques found in the brains of patients with Alzheimer’s disease.Abis liberated by sequential cleavage of amyloid precursor protein (APP) byb-andc-secre-tases.The level of Abdepends directly on the hydrolytic activity ofb-secretase.Therefore, b-secretase is an excel-lent target for drug design.An approach based on RNA-cleaving ribozymes was developed to control expression ofb-secretase.

9p tumor12 20-04-2013 37 4   Download

Thioredoxins are a group of small redox-active proteins involved in cellular redox regulatory processes as well as antioxidant defense. Thioredoxin, glutaredoxin, and try-paredoxin are members of the thioredoxin superfamily and share structural and functional characteristics. In the mal-arial parasite, Plasmodium falciparum, a functional thio-redoxin and glutathione system have been demonstrated and are considered to be attractive targets for antimalarial drug development.

8p tumor12 20-04-2013 42 3   Download

HIV-1 protease is an important target for treatment of AIDS, and efficient drugs have been developed. However, the resistance and negative side effects of the current drugs has necessitated the development of new compounds with different binding patterns. In this study, nine C-terminally duplicated HIV-1 protease inhibitors were cocrystallised with the enzyme, the crystal structures analysed at 1.8–2.3 A˚ resolution, and the inhibitory activity of the compounds characterized inorder toevaluate the effects of the individual modifications. ...

13p fptmusic 16-04-2013 44 3   Download

The Hsp90 molecular chaperone catalyses the final activa-tion step of many of themost important regulatory proteins of eukaryotic cells. The antibiotics geldanamycin and rad-icicol act as highly selective inhibitors of in vivo Hsp90 function through their ability to bindwithin the ADP/ATP binding pocket of the chaperone. Drugs based on these compounds are now being developed as anticancer agents, their administration having the potential to inactivate sim-ultaneously several of the targets critical for counteracting multistep carcinogenesis. ...

7p fptmusic 12-04-2013 42 3   Download

HIV-1 protease is a pivotal enzyme in the later stages of the viral life cycle which is responsible for the processing and maturation of the virus particle into an infectious virion. As such,HIV-1proteasehasbecomean important target for the treatment ofAIDS, and efficient drugs have beendeveloped. However, negative side effects and fast emerging resistance to the current drugs have necessitated the development of novel chemical entities in order to exploit different phar-macokinetic properties as well as new interaction patterns....

9p awards 05-04-2013 32 2   Download

Malaria remains a major health problem especially in trop-ical and subtropical regions of the world, and therefore developing new antimalarial drugs constitutes an urgent challenge. Lipid metabolism has been attracting a lot of attention as an application for malarial chemotherapeutic purposes in recent years. However, little is known about glycosphingolipid biosynthesis inPlasmodium falciparum. In this report we describe for the first time the presence of an active glucosylceramide synthase in the intraerythrocytic stages of the parasite....

11p dell39 03-04-2013 31 4   Download

Cyclic nucleotide specific phosphodiesterases (PDEs) are important components of all cAMP signalling networks. In humans, 11 different PDE families have been identified to date, all of which belong to the class I PDEs. Pharmaco-logically, theyhavebecome of great interest as targets for the development of drugs for a large variety of clinical condi-tions. PDEs in parasitic protozoa have not yet been exten-sively investigated, despite their potential as antiparasitic drug targets.

11p dell39 03-04-2013 40 4   Download

Polyamine oxidase (PAO) and spermine oxidase (SMO) are involved in the catabolism of polyamines – basic regulators of cell growth and prolifer-ation. The discovery of selective inhibitors of PAO and SMO represents an important tool in studying the involvement of these enzymes in polyamine homeostasis and a starting point for the development of novel antineoplas-tic drugs.

9p inspiron33 26-03-2013 41 5   Download

Streptococcus pneumoniaeis one of the major pathogens worldwide. The use of currently available antibiotics to treat pneumococcal diseases is ham-pered by increasing resistance levels; also, capsular polysaccharide-based vaccination is of limited efficacy. Therefore, it is desirable to find targets for the development of new antimicrobial drugs specifically designed to fight pneumococcal infections.

13p inspiron33 23-03-2013 44 3   Download

Recently published genomic investigations of the human pathogenMyco-bacterium tuberculosishave revealed that genes coding the proteins involved in riboflavin biosynthesis are essential for the growth of the organism. Because the enzymes involved in cofactor biosynthesis pathways are not present in humans, they appear to be promising candidates for the develop-ment of therapeutic drugs.

15p inspiron33 23-03-2013 36 4   Download