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Relevant bibliographies by topics / Pharmacokinetics. Drugs Chiral drugs

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Academic literature on the topic 'Pharmacokinetics. Drugs Chiral drugs'

Author: Grafiati

Published: 4 June 2021

Last updated: 4 February 2022

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Journal articles on the topic "Pharmacokinetics. Drugs Chiral drugs"

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Chen, Fuxin, Qiaoxiu Bai, Qingfeng Wang, Suying Chen, Xiaoxian Ma, Changlong Cai, Danni Wang, Ahsan Waqas, and Pin Gong. "Stereoselective Pharmacokinetics and Chiral Inversions of Some Chiral Hydroxy Group Drugs." Current Pharmaceutical Biotechnology 21, no. 15 (December 23, 2020): 1632–44. http://dx.doi.org/10.2174/1389201021666200727144053.

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Background: Chiral safety, especially chiral drug inversion in vivo, is the top priority of current scientific research. Medicine researchers and pharmacists often ignore that one enantiomer will be converted or partially converted to another enantiomer when it is ingested in vivo. So that, in the context that more than 50% of the listed drugs are chiral drugs, it is necessary and important to pay attention to the inversion of chiral drugs. Methods: The metabolic and stereoselective pharmacokinetic characteristics of seven chiral drugs with one chiral center in the hydroxy group were reviewed in vivo and in vitro including the possible chiral inversion of each drug enantiomer. These seven drugs include (S)-Mandelic acid, RS-8359, Tramadol, Venlafaxine, Carvedilol, Fluoxetine and Metoprolol. Results: The differences in stereoselective pharmacokinetics could be found for all the seven chiral drugs, since R and S isomers often exhibit different PK and PD properties. However, not every drug has shown the properties of one direction or two direction chiral inversion. For chiral hydroxyl group drugs, the redox enzyme system may be one of the key factors for chiral inversion in vivo. Conclusion: In vitro and in vivo chiral inversion is a very complex problem and may occur during every process of ADME. Nowadays, research on chiral metabolism in the liver has the most attention, while neglecting the chiral transformation of other processes. Our review may provide the basis for the drug R&D and the safety of drugs in clinical therapy.

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Vakily, Majid, Reza Mehvar, and Dion Brocks. "Stereoselective Pharmacokinetics and Pharmacodynamics of Anti-Asthma Agents." Annals of Pharmacotherapy 36, no. 4 (April 2002): 693–701. http://dx.doi.org/10.1345/aph.1a248.

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OBJECTIVE: To review the previously published studies on pharmacokinetics and pharmacodynamics of chiral drugs used in the treatment of asthma. DATA SOURCES: Primary and review articles were identified with a MEDLINE search (1980–May 2001) and through secondary sources. STUDY SELECTION AND DATA EXTRACTION: All English-language studies and reviews obtained from the MEDLINE search pertaining to stereoselective pharmacokinetics and pharmacodynamics of chiral anti-asthma drugs were assessed. DATA SYNTHESIS: Several anti-asthma drugs (e.g., β2-adrenergic agonists, leukotriene modifiers) are chiral and marketed as racemates, which consist of equal proportions of 2 enantiomers. Significant stereoselectivity has also been reported in pharmacodynamics and pharmacokinetics of the β2-agonists. The enantiomers of β2-agonists in the R configuration are primarily responsible for the bronchodilating effects of the racemate. The plasma concentrations of the enantiomers of anti-asthma drugs may differ as a reflection of stereoselectivity in clearance, volume of distribution, and route of administration. CONCLUSIONS: Stereoselectivity in the pharmacokinetics of anti-asthma drugs may complicate the relationship between dose and/or plasma concentration of racemic drug versus effect relationship. An appreciation of the stereoselective pharmacokinetics and pharmacodynamics of chiral anti-asthma drugs may optimize the use of these agents in asthmatic patients.

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Flockhart, David A., and Harold S. Nelson. "Single Isomer Versus Racemate: Is There a Difference? Clinical Comparisons in Allergy and Gastroenterology." CNS Spectrums 7, S1 (April 2002): 23–27. http://dx.doi.org/10.1017/s109285290002856x.

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ABSTRACTMany commonly prescribed drugs exist as a mixture of two distinct chiral isomer forms (enantiomers), each with its own unique chemistry, receptor affinity, and pharmacokinetic profile. Much is unknown concerning the clinical utility of these single enantiomers. This review of the stereoisomers of two commonly used drugs—albuterol for asthma and omeprazole for gastroesophageal reflux disease (GERD) and peptic ulcers—examines the improved efficacy, pharmacokinetics, decreased adverse effects, and fewer drug-drug interactions associated with single enantiomers.

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Jamali, Fakhreddin. "Pharmacokinetics of enantiomers of chiral non-steroidal anti-inflammatory drugs." European Journal of Drug Metabolism and Pharmacokinetics 13, no. 1 (January 1988): 1–9. http://dx.doi.org/10.1007/bf03189920.

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Brocks, Dion R., and Reza Mehvar. "Stereoselectivity in the Pharmacodynamics and Pharmacokinetics of the Chiral Antimalarial Drugs." Clinical Pharmacokinetics 42, no. 15 (2003): 1359–82. http://dx.doi.org/10.2165/00003088-200342150-00004.

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Uwai, Yuichi. "Enantioselective Drug Recognition by Drug Transporters." Molecules 23, no. 12 (November 22, 2018): 3062. http://dx.doi.org/10.3390/molecules23123062.

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Drug transporters mediate the absorption, tissue distribution, and excretion of drugs. The cDNAs of P-glycoprotein, multidrug resistance proteins (MRPs/ABCC), breast cancer resistance protein (BCRP/ABCG2), peptide transporters (PEPTs/SLC15), proton-coupled folate transporters (PCFT/SLC46A1), organic anion transporting polypeptides (OATPs/SLCO), organic anion transporters (OATs/SLC22), organic cation transporters (OCTs/SLC22), and multidrug and toxin extrusions (MATEs/SLC47) have been isolated, and their functions have been elucidated. Enantioselectivity has been demonstrated in the pharmacokinetics and efficacy of drugs, and is important for elucidating the relationship with recognition of drugs by drug transporters from a chiral aspect. Enantioselectivity in the transport of drugs by drug transporters and the inhibitory effects of drugs on drug transporters has been summarized in this review.

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Gandhi, Karan, Umang Shah, and Sandip Patel. "Drug Stereochemistry: A Prodigy For Pharmacology and Drug Development." Current Drug Discovery Technologies 17, no. 5 (December 23, 2020): 565–73. http://dx.doi.org/10.2174/1570163816666190502101803.

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Stereochemistry has evinced the importance of many chiral drugs with respect to drug designing and development. A literature review was conducted for several chiral drugs involving pharmacokinetic and pharmacodynamic parameters of their enantiomers along with their uses in certain diseased conditions. This article mainly includes the pharmacological profile review of some chiral drugs and the aspects due to which the single enantiomer is of importance as compared to the racemic mixture of the drug. This was achieved by moderating the side effects or toxic effects; or by the potentiated activity of the single enantiomer. Resolution deals with the separation of racemic compounds which shows up the credibility to obtain the desired enantiomeric properties. As isomers vary in their pharmacokinetic and pharmacodynamic profiles, chiral drugs have showcased considerable importance in the drug development process. Both the enantiomers have a different pharmacological profile in the treatment of a disease, which differentiates them from drug racemates.

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Xiong, Fei, Bei-Bei Yang, Jie Zhang, and Li Li. "Enantioseparation, Stereochemical Assignment and Chiral Recognition Mechanism of Sulfoxide-Containing Drugs." Molecules 23, no. 10 (October 18, 2018): 2680. http://dx.doi.org/10.3390/molecules23102680.

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The distinct pharmacodynamic and pharmacokinetic properties of enantiopure sulfoxide drugs have stimulated us to systematically investigate their chiral separation, stereochemical assignment, and chiral recognition mechanism. Herein, four clinically widely-used sulfoxide drugs were chosen and optically resolved on various chiral stationary phases (CSPs). Theoretical simulations including electronic circular dichroism (ECD) calculation and molecular docking were adopted to assign the stereochemistry and reveal the underlying chiral recognition mechanism. Our results showed that the sequence of calculated mean binding energies between each pair of enantiomers and CSP matched exactly with experimentally observed enantiomeric elution order (EEO). It was also found that the length of hydrogen bond might contribute dominantly the interaction between two enantiomers and CSP. We hope our study could provide a fresh perspective to explore the stereochemistry and chiral recognition mechanism of chiral drugs.

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Ružena, Čižmáriková, Valentová Jindra, and Horáková Renáta. "Chirality of β2-agonists. An overview of pharmacological activity, stereoselective analysis, and synthesis." Open Chemistry 18, no. 1 (June 18, 2020): 628–47. http://dx.doi.org/10.1515/chem-2020-0056.

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Abstractβ2-Agonists (β2-adrenergic agonists, bronchodilatants, and sympathomimetic drugs) are a group of drugs that are mainly used in asthma and obstructive pulmonary diseases. In practice, the substances used to contain one or more stereogenic centers in their structure and their enantiomers exhibit different pharmacological properties. In terms of bronchodilatory activity, (R)-enantiomers showed higher activity. The investigation of stereoselectivity in action and disposition of chiral drugs together with the preparation of pure enantiomer drugs calls for efficient stereoselective analytical methods. The overview focuses on the stereoselectivity in pharmacodynamics and pharmacokinetics of β2-agonists and summarizes the stereoselective analytical methods for the enantioseparation of racemic beta-agonists (HPLC, LC-MS, GC, TLC, CE). Some methods of the stereoselective synthesis for β2-agonists preparation are also presented.

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Čižmáriková, Ružena, Jozef Čižmárik, Jindra Valentová, Ladislav Habala, and Mário Markuliak. "Chiral Aspects of Local Anesthetics." Molecules 25, no. 12 (June 12, 2020): 2738. http://dx.doi.org/10.3390/molecules25122738.

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Thanks to the progress made in chemical technology (particularly in the methodologies of stereoselective syntheses and analyses) along with regulatory measures, the number of new chiral drugs registered in the form of pure enantiomers has increased over the past decade. In addition, the pharmacological and pharmacokinetic properties of the individual enantiomers of already-introduced racemic drugs are being re-examined. The use of the pure enantiomer of a drug that has been used to date in the form of a racemate is called a “chiral switch”. A re-examination of the properties of the pure enantiomers of racemates has taken place for local anesthetics, which represent a group of drugs which have long been used. Differences in (R) and (S)-enantiomers were found in terms of pharmacodynamic and pharmacokinetic activity as well as in toxicity. Levobupivacaine and robivacaine were introduced into practice as pure (S)-(−)-enantiomers, exhibiting more favorable properties than their (R)-(+)-stereoisomers or racemates. This overview focuses on the influence of chirality on the pharmacological and toxicological activity of local anesthetics as well as on individual HPLC and capillary electrophoresis (CE) methods used for enantioseparation and the pharmacokinetic study of individual local anesthetics with a chiral center.

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Dissertations / Theses on the topic "Pharmacokinetics. Drugs Chiral drugs"

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Mashile, Tumelo Rameleko. "Enantioanalysis of pharmaceutical compounds." Pretoria : [s.n.], 2005. http://upetd.up.ac.za/thesis/available/etd-02222007-195248.

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Eriksson, Tommy. "Pharmacokinetics of the enantionmers of thalidomide." Malmö : Lund : Malmö University Hospital ; Lund University, 1997. http://catalog.hathitrust.org/api/volumes/oclc/68945032.html.

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Karlsson, Louise. "P-glycoprotein and chiral antidepressant drugs : Pharmacokinetic, pharmacogenetic and toxicological aspects." Doctoral thesis, Linköpings universitet, Klinisk farmakologi, 2012. http://urn.kb.se/resolve?urn=urn:nbn:se:liu:diva-76126.

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The blood-brain barrier (BBB) is formed by the capillary endothelial cells, joined together by tight junctions, with transporter proteins. BBB acts to regulate the brain concentrations of substances including many drugs. Transport across the cells is necessary for a drug to ensure that the drug reaches the site of action and transport proteins such as P-glycoprotein (P-gp; ABCB1) can limit the entrance into various tissues, including the brain. Molecules that are not superimposable on their mirror images and thus exist in two enantiomeric forms (enantiomers) are said to be chiral. A racemic compound is one composed of a 50:50 mixture of two enantiomers, S- and R-enantiomers. Two examples of frequently prescribed racemic drugs are the chiral antidepressants venlafaxine (VEN) and citalopram (CIT). The enantiomers of VEN possess different pharmacodynamic profiles where the R-enantiomer is a potent inhibitor of both serotonin and noradrenaline reuptake (SNRI), while the S-enantiomer is more selective in inhibiting serotonin reuptake (SSRI). The SSRI effect of CIT resides in the S-enantiomer, whereas the R-enantiomer is considered to be therapeutically inactive, or even that it counteracts the effects. The S-enantiomer of CIT is now available as a separate SSRI (escitalopram, EsCIT). VEN and CIT are also among the most commonly found drugs in forensic autopsy cases. Few previous studies have examined a possible enantioselective activity of P-gp. Thus, the general aim of this thesis was to study the enantiomeric distribution of chiral antidepressant drugs, focusing on the role of P-gp in the BBB. For this purpose, a mouse model disrupted of the genes coding for P-gp (abcb1ab (-/-) mice) was used. Brain and serum concentrations of the enantiomers of VEN and CIT, and their major metabolites, were compared to the corresponding wild-type mice (abcb1ab (+/+) mice). The open-field locomotor and rearing activities were examined after chronic VEN administration. In addition to the animal studies, genetic and toxicological aspects of P-gp were studied in a forensic autopsy material, where intoxication cases were compared with cases that were not related to intoxications. The brain to serum concentration ratios for VEN, CIT and EsCIT differed between knockout mice and wild-type mice, with 2-3 fold higher brain concentrations in mice with no expression of P-gp. Hence, all studied drugs, and their major metabolites, were substrates for P-gp. There was no evidence for a stereoselective P-gp mediated transport. The P-gp substrate properties were reflected in the open-field behavior test where the knockout mice displayed increased center activity compared with wild-type mice following chronic VEN exposure. The genotype distribution of ABCB1 SNPs C1236T, G2677T and C3435T in VEN positive cases was significantly (or borderline) different between the intoxication cases and the non-intoxication cases. This difference in genotype distribution was not observed for the CIT positive cases. To conclude, the present work has led to an increased knowledge about how the enantiomers of VEN and CIT are affected by the BBB transporter P-gp. Using an animal model, VEN and CIT have proved to be actively transported out of the brain by P-gp and no difference was observed for the enantiomers with regard to P-gp transport. Further, the ABCB1 genotype distribution was different in intoxication cases compared with non-intoxication cases. Taken together, these findings offer the possibility that the expression of P-gp in humans may be a contributing factor for limited treatment response and increased risk of side-effects following antidepressant drug treatment.

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Olsén, Lena. "Drugs in horses : pharmacokinetics and pharmacodynamics /." Uppsala : Dept. of Biomedical Sciences and Veterinary Public Health, Swedish University of Agricultural Sciences, 2007. http://epsilon.slu.se/200737.pdf.

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Song, Di. "Bladder tissue pharmacokinetics of anticancer drugs /." The Ohio State University, 1996. http://rave.ohiolink.edu/etdc/view?acc_num=osu1487940308433249.

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James, Devona Gwen. "The degradation of drugs in formaldehyde." Morgantown, W. Va. : [West Virginia University Libraries], 1999. http://etd.wvu.edu/templates/showETD.cfm?recnum=1149.

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Thesis (M.S.)--West Virginia University, 1999.
Title from document title page. Document formatted into pages; contains xvi, 100 p. : ill. Vita. Includes abstract. Includes bibliographical references (p. 98-99).

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Reis, Margareta. "Pharmacokinetics of antidepressant drugs : naturalistic and clinical trials /." Linköping : Univ, 2003. http://www.bibl.liu.se/liupubl/disp/disp2003/med783s.pdf.

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Hammann, Felix. "Prediction of transport, pharmacokinetics, and effect of drugs /." Basel : [s.n.], 2009. http://edoc.unibas.ch/diss/DissB_8905.

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Layton, Sherry E. "Comparison of various chiral stationary phases for the chromatographic separation of chiral pharmaceuticals /." Electronic version (PDF), 2005. http://dl.uncw.edu/etd/2005/laytons/sherrylayton.pdf.

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Zhang, Jing Lu. "Big data analysis of solid dispersion researches from 1980 to 2015." Thesis, University of Macau, 2018. http://umaclib3.umac.mo/record=b3952169.

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Books on the topic "Pharmacokinetics. Drugs Chiral drugs"

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Lin, Guo-Qiang, Qi-Dong You, and Jie-Fei Cheng, eds. Chiral Drugs. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2011. http://dx.doi.org/10.1002/9781118075647.

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Welling, Peter G., and Luc P. Balant, eds. Pharmacokinetics of Drugs. Berlin, Heidelberg: Springer Berlin Heidelberg, 1994. http://dx.doi.org/10.1007/978-3-642-78680-8.

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Sunjic, Vitomir, and Michael J. Parnham. Signposts to Chiral Drugs. Basel: Springer Basel, 2011. http://dx.doi.org/10.1007/978-3-0348-0125-6.

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Lin, Guo-Qiang. Chiral drugs: Chemistry and biological action. Hoboken, N.J: Wiley, 2011.

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Ahuja, Satinder. Chiral separation methods for pharmaceutical and biotechnological products. Hoboken, N.J: Wiley, 2010.

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1935-, Shader Richard I., ed. Pharmacokinetics in clinical practice. Philadelphia: Saunders, 1985.

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Sunjic, Vitomir. Signposts to Chiral Drugs: Organic Synthesis in Action. Basel: Springer Basel AG, 2011.

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Chirality and the biological activity of drugs. Boca Raton: CRC Press, 1995.

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Eeckhaut, Ann van. Chiral separations by capillary electrophoresis. Boca Raton: Taylor & Francis, 2009.

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Welling, Peter G. Pharmacokinetics of cardiovascular, central nervous system, and antimicrobial drugs. London: The Royal Society of Chemistry, 1985.

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Book chapters on the topic "Pharmacokinetics. Drugs Chiral drugs"

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Dong, Hanqing, Xiaochuan Guo, and Zengbiao Li. "Pharmacokinetics of Chiral Drugs." In Chiral Drugs, 347–79. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2011. http://dx.doi.org/10.1002/9781118075647.ch9.

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Wainer, Irving W. "Applicability of HPLC Chiral Stationary Phases to Pharmacokinetic and Disposition Studies on Enantiomeric Drugs." In BIOACTIVE ANALYTES, Including CNS Drugs, Peptides, and Enantiomers, 243–57. Boston, MA: Springer US, 1986. http://dx.doi.org/10.1007/978-1-4757-1892-8_20.

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Lin, Guo-Qiang, Jian-Ge Zhang, and Jie-Fei Cheng. "Overview of Chirality and Chiral Drugs." In Chiral Drugs, 3–28. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2011. http://dx.doi.org/10.1002/9781118075647.ch1.

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Yang, Guang, and Hai-Zhi Bu. "Toxicology of Chiral Drugs." In Chiral Drugs, 381–99. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2011. http://dx.doi.org/10.1002/9781118075647.ch10.

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Sun, Jiangqin, Dingguo Liu, and Zhimin Wang. "Representative Chiral Drugs." In Chiral Drugs, 401–48. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2011. http://dx.doi.org/10.1002/9781118075647.ch11.

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Lin, Guo-Qiang, and Xing-Wen Sun. "Chiral Drugs through Asymmetric Synthesis." In Chiral Drugs, 29–76. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2011. http://dx.doi.org/10.1002/9781118075647.ch2.

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Wang, Jianqiang, and Wenya Lu. "Chiral Drugs via Biocatalytical Approaches." In Chiral Drugs, 77–136. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2011. http://dx.doi.org/10.1002/9781118075647.ch3.

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You, Qi-Dong. "Resolution of Chiral Drugs." In Chiral Drugs, 137–94. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2011. http://dx.doi.org/10.1002/9781118075647.ch4.

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Qiu, Xiao-Long, Xuyi Yue, and Feng-Ling Qing. "Fluorine-Containing Chiral Drugs." In Chiral Drugs, 195–251. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2011. http://dx.doi.org/10.1002/9781118075647.ch5.

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Liu, Rui, Carl Behrens, and Chao-Ying Ni. "Industrial Application of Chiral Technologies." In Chiral Drugs, 253–96. Hoboken, NJ, USA: John Wiley & Sons, Inc., 2011. http://dx.doi.org/10.1002/9781118075647.ch6.

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Conference papers on the topic "Pharmacokinetics. Drugs Chiral drugs"

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Liu, Chunye, Yanqing Miao, Yihui Guo, Yinjuan An, Yunfang Li, Huanhuan Liu, Jia Chen, Jiarui Liu, and Huibin Dai. "Chiral drugs separation by a new antibiotics-based chiral stationary phase." In International Conference on Medical Engineering and Bioinformatics. Southampton, UK: WIT Press, 2014. http://dx.doi.org/10.2495/meb140641.

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Scherf-Clavel, M., L. Samanski, R. Burger, J. Deckert, A. Menke, and S. Unterecker. "Differences in the pharmacokinetics of psychopharmacological drugs between smokers and nonsmokers." In XIIIth Symposium of the Task Force Therapeutic Drug Monitoring of the AGNP. Georg Thieme Verlag KG, 2018. http://dx.doi.org/10.1055/s-0038-1649541.

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Caron, Whitney P., Harvey Clewell, Robert Dedrick, Ramesh K. Ramanathan, Ning Yu, Jan H. Schellens, Jos H. Beijnen, and William C. Zamboni. "Abstract 373: Allometric scaling of the pharmacokinetics of pegylated liposomal anticancer drugs." In Proceedings: AACR 102nd Annual Meeting 2011‐‐ Apr 2‐6, 2011; Orlando, FL. American Association for Cancer Research, 2011. http://dx.doi.org/10.1158/1538-7445.am2011-373.

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Du, Yong, Jianjun Liu, and Zhi Hong. "Characteristics of chiral and racemic ketoprofen drugs using terahertz time-domain spectroscopy." In ISPDI 2013 - Fifth International Symposium on Photoelectronic Detection and Imaging, edited by Marco Rahm, Konstantin Vodopyanov, Wei Shi, and Cunlin Zhang. SPIE, 2013. http://dx.doi.org/10.1117/12.2033147.

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Shimada, Takashi, Noriko Iwamoto, Sho Saeki, Ji-ichiro Sasaki, Taka-Aki Sato, and Akinobu Hamada. "Abstract 2962: Development of the LCMS bioanalysis for clinical pharmacokinetics of antibody drugs using Fab-selective limited proteolysis (nSMOL)." In Proceedings: AACR 107th Annual Meeting 2016; April 16-20, 2016; New Orleans, LA. American Association for Cancer Research, 2016. http://dx.doi.org/10.1158/1538-7445.am2016-2962.

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Lee, Jae-Hwan, and Ramana M. Pidaparti. "An Implantable Device Design Concept for Ocular Drug Delivery." In ASME 2012 Summer Bioengineering Conference. American Society of Mechanical Engineers, 2012. http://dx.doi.org/10.1115/sbc2012-80176.

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New drugs for curing eye diseases have been developing for a decade and are very unique for each eye diseases such as glaucoma, cataracts, and age-related macular degeneration (AMD). It is estimated that 1.6 million adults in the US over the age of 50 and above suffer from age-related macular degeneration and about 200,000 cases are diagnosed annually. Worldwide, about 500,000 cases are diagnosed annually [1]. Drugs currently utilized for AMD are delivered via repeated intravitreal injections of the drug into the eye. Risks of repeated intravitreal injections can include intraocular infections (endophthalmitis), intraocular hemorrhage, and retinal detachment. Also, reducing the frequency of dosing will clearly benefit the patient by reducing the need for risky intravitreal injections and improving the pharmacokinetics of the drug in the eye. The eye disease of posterior segment (Dry and Wet) has limits to deliver the drug to retina region using typical eye drop. The drug injection using a needle with syringe can deliver but it barely provide right amount of doses, or over doses that may cause more severe problem such as swelling, fatigue, and damaging photoreceptor molecules. Furthermore, most drugs run away in a month so that repeated injection is necessary. Developing an implantable drug delivery device will help reduce the costs and risks associated with frequent injections and facilitate delivering the drug in a controlled manner and in the required amounts, and improve therapeutic efficacy and safety of drugs. This study focuses on the design, simulation and development of the implantable ocular drug delivery device.

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Sadiq, Muhammad Waqas, Olaf Holz, Birthe Ellinghusen, Cornelia Faulenbach, Meike Müller, Philipp Badorrek, Ulf G. Eriksson, et al. "Late Breaking Abstract - Spatial pharmacokinetics of inhaled drugs in human lung – evaluation of regional lung targeting by direct sampling of epithelial lining fluid." In ERS International Congress 2019 abstracts. European Respiratory Society, 2019. http://dx.doi.org/10.1183/13993003.congress-2019.oa2103.

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Bhushan, Indu. "Efficient media for high production of microbial lipase from Bacillus subtilis (BSK-L) using response surface methodology for enantiopure synthesis of drug molecules." In 2nd International Scientific Conference "Plants and Microbes: the Future of Biotechnology". PLAMIC2020 Organizing committee, 2020. http://dx.doi.org/10.28983/plamic2020.044.

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Lipases are a multipurpose enzyme that holds a significant position in industrial applications due to its ability to catalyse a large number of reactions such as hydrolysis, esterification, interesterification, transesterification which makes it a potential candidate. It is also used for the separation of chiral drugs from the racemic mixture and this property of lipase is considered very important in pharmaceutical industries for the synthesis of enantiopure bioactive molecules. Assuming the tremendous importance of lipases, as stereoselective biocatalysts, in pharmaceuticals and various other commercial applications, industrial enzymologists have been forced to search for those microorganisms which are able to produce novel biocatalysts at reasonably high yield. In the present study microbial lipase was isolated from the water sample of pond at Katra, Jammu and Kashmir (India). This enzyme has shown wide specificity and higher enantioselectivity, which make it pharmaceutical important enzyme. To make it economical for industrial application, it was produced on cheap nutrient media using Response Surface Methodology and got maximum production. It was used for resolution of chiral drugs and the significant results obtained during the course of work shall have potential towards pharmaceutical industries.

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Shafahi, Maryam, and Parham Piroozan. "Model of Drug Delivery to the Eye." In ASME 2014 International Mechanical Engineering Congress and Exposition. American Society of Mechanical Engineers, 2014. http://dx.doi.org/10.1115/imece2014-39438.

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Ocular diseases cause vision deficiency and blindness in a substantial number of people in the world every day. Therefore, a controlled and sustained system of drug delivery to a specific spot within the eye is of interest for the ophthalmology community. The unique and complicated anatomy, physiology, and biochemistry of the eye make this organ highly resistant to drug delivery systems. The major challenge is to improve the efficiency of each treatment method along with avoiding the invasive techniques which damage the eye’s protective barrier tissues. In this work we make a computer model for the drug delivery to the anterior sections of the eye and provide a summary of transport characteristics of the eye, pharmacokinetics and efficacy of the utilized drugs. A two dimensional finite element model is utilized to solve the conservation of mass and momentum equations within different eye sub-domains such as cornea, anterior chamber, iris and sclera. The commercial software Comsol Multiphysics was utilized to obtain the profile of concentration in the eye and the grid independency of the numerical results has been checked. The results are being shown in terms of transient drug concentration profile in the eye subdomains. The influence of the modeling parameters on the efficiency of the drug delivery system is studied. The effect of physical variables such as drug molecular size and its bioavailability are investigated. The results are compared with the available literature data which are based on the drug diffusion within the domain.

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10

Tourlomousis, Filippos, and Robert C. Chang. "2D and 3D Multiscale Computational Modeling of Dynamic Microorgan Devices as Drug Screening Platforms." In ASME 2015 International Mechanical Engineering Congress and Exposition. American Society of Mechanical Engineers, 2015. http://dx.doi.org/10.1115/imece2015-52734.

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The ability to incorporate three-dimensional (3D) hepatocyte-laden hydrogel constructs using layered fabrication approaches into devices that can be perfused with drugs enables the creation of dynamic microorgan devices (DMDs) that offer an optimal analog of the in vivo liver metabolism scenario. The dynamic nature of such in vitro metabolism models demands reliable numerical tools to determine the optimum process, material, and geometric parameters for the most effective metabolic conversion of the perfused drug into the liver microenvironment. However, there is a current lack of literature that integrates computational approaches to guide the optimum design of such devices. The groundwork of the present numerical study has been laid by our previous study [1], where the authors modeled in 2D an in vitro DMD of arbitrary dimensions and identified the modeling challenges towards meaningful results. These constructs are hosted in the chamber of the microfluidic device serving as walls of the microfluidic array of channels through which a fluorescent drug substrate is perfused into the microfluidic printed channel walls at a specified volumetric flow rate assuring Stokes flow conditions (Re<<1). Due to the porous nature of the hydrogel walls, a metabolized drug product is collected at the outlet port. A rigorous FEM based modeling approach is presented for a single channel parallel model geometry (1 free flow channel with 2 porous walls), where the hydrodynamics, mass transfer and pharmacokinetics equations are solved numerically in order to yield the drug metabolite concentration profile at the DMD outlet. The fluid induces shear stresses are assessed both in 3D, with only 27 cells modeled as single compartment voids, where all of the enzymatic reactions are assumed to take place. In this way, the mechanotransduction effect that alters the hepatocyte metabolic activity is assessed for a small scale model. This approach overcomes the numerical limitations imposed by the cell density (∼1012 cells/m3) of the large scale DMD device. In addition, a compartmentalization technique is proposed in order to assess the metabolism process at the subcellular level. The numerical results are validated with experiments to reveal the robustness of the proposed modeling approach and the necessity of scaling the numerical results by preserving dynamic and biochemical similarity between the small and large scale model.

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Reports on the topic "Pharmacokinetics. Drugs Chiral drugs"

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Johnson, Corey, Colton James, Sarah Traughber, and Charles Walker. Postoperative Nausea and Vomiting Implications in Neostigmine versus Sugammadex. University of Tennessee Health Science Center, July 2021. http://dx.doi.org/10.21007/con.dnp.2021.0005.

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Purpose/Background: Postoperative nausea and vomiting (PONV) is a frequent complaint in the postoperative period, which can delay discharge, result in readmission, and increase cost for patients and facilities. Inducing paralysis is common in anesthesia, as is utilizing the drugs neostigmine and sugammadex as reversal agents for non-depolarizing neuromuscular blockers. Many studies are available that compare these two drugs to determine if neostigmine increases the risk of PONV over sugammadex. Sugammadex has a more favorable pharmacologic profile and may improve patient outcomes by reducing PONV. Methods: This review included screening a total of 39 studies and peer-reviewed articles that looked at patients undergoing general anesthesia who received non-depolarizing neuromuscular blockers requiring either neostigmine or sugammadex for reversal, along with their respective PONV rates. 8 articles were included, while 31 articles were removed based on our exclusion criteria. These were published between 2014 and 2020 exclusively. The key words used were “neostigmine”, “sugammadex”, “PONV”, along with combinations “paralytic reversal agents and PONV”. This search was performed on the scholarly database MEDLINE. The data items were PONV rates in neostigmine group, PONV rates in sugammadex group, incidence of postoperative analgesic consumption in neostigmine group, and incidence of postoperative analgesic consumption in sugammadex group. Results: Despite numerical differences being noted in the incidence of PONV with sugammadex over reversal with neostigmine, there did not appear to be any statistically significant data in the multiple peer-reviewed trials included in our review, for not one of the 8 studies concluded that there was a higher incidence of PONV in one drug or the other of an y clinical relevance. Although the side-effect profile tended to be better in the sugammadex group than neostigmine in areas other than PONV, there was not sufficient evidence to conclude that one drug was superior to the other in causing a direct reduction of PONV. Implications for Nursing Practice: There were variable but slight differences noted between both drug groups in PONV rates, but it remained that none of the studies determined it was statically significant or clinically conclusive. This review did, however, note other advantages to sugammadex over neostigmine, including its pharmacologic profile of more efficiently reversing non-depolarizing neuromuscular blocking drugs and its more favorable pharmacokinetics. This lack of statistically significant evidence found within these studies consequentially does not support pharmacologic decision-making of one drug in favor of the other for reducing PONV; therefore, PONV alone is not a sufficient rationale for a provider to justify using one reversal over another at the current time until further research proves otherwise.

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