Dr. Syed A. A. Rizvi
Associate Professor (Tenured),
Department of Pharmaceutical Sciences, Hampton University School of Pharmacy (HUSOP), Flemmie P. Kittrell Hall, 121 William R. Harvey Way, Hampton, VA 23668, USA.

ISBN 978-93-90888-31-3 (Print)
ISBN 978-93-90888-32-0 (eBook)
DOI: 10.9734/bpi/tipr/v4

This book covers key areas of pharmaceutical research. The contributions by the authors include gestational diabetes mellitus, pregnancy, complications, hyperglycaemia, DFT calculations, Kinetics,  acid-catalyzed hydrolysis,LLamotrigene formulations, gangliosides, signal transduction, mast cells, activation, newly formed mediators, newly synthesized mediators, antidotes, clinical assay, saliva-diagnostics, biomedical waste, environmental impact, pathological waste, potentially infectious waste, hazardous waste, medicinal plants, caffeine, phenolics, flavonoids, antioxidant activity, polycystic ovarian syndrome, hyperandrogenism, insulin resistance, metabolic syndrome, etiological factors, pathogenesis, clinical manifestations, prognosis, inhalation, euthanasia,  antioxidant parameters, reconstructive surgery, orthopaedic wounds, UV spectroscopy, microsponges, animal helminthoses, chemotherapy and prevention, anthelmintic substances, folk medicine, non-organic and organic anthelminthic substances, phloroglucines, phenothiazine, avermectin analogues, aminoacetonitril derivatives, monepantel, spiroindols, biological methods of helminthoses control. This book contains various materials suitable for students, researchers and academicians in the field of pharmaceutical research.


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A Brief Review on Gestational Diabetes Mellitus

Sachin B. Somwanshi, Kiran B. Kotade

Technological Innovation in Pharmaceutical Research Vol. 4, 29 May 2021, Page 1-9

GDM (gestational diabetes mellitus) is a common metabolic condition that manifests itself in varying degrees of severity before or during pregnancy. It has been linked to negative maternal and newborn outcomes. Globally, the prevalence of GDM is rising, along with the rise in the incidence of obesity and type 2 diabetes mellitus. It is critical to detect and treat GDM as soon as possible in order to minimise or eliminate difficulties for both the mother and the foetus. Globally, there is indeed a lack of consistency in evaluating and detecting GDM. This article discusses the most recent developments in the diagnosis and treatment of GDM. For the greatest outcomes, treatment must be tailored to the person, combining medical nutrition therapy, supplemental food, and exercise. If these strategies fail to regulate blood glucose levels, pharmacologic therapies, namely insulin and its analogues, should be implemented. The treatment with pharmacologic interventions has an important role on lowering the complications related to GDM. Other oral antihyperglycemic drugs like Metformin and Glyburide are also considered in light of emerging information about their safety and efficacy during pregnancy.

Design of Bitterless Atenolol Prodrugs for the Use in Aqueous Formulations for Pediatrics and Geriatrics

Rafik Karaman, Alaa Qtait

Technological Innovation in Pharmaceutical Research Vol. 4, 29 May 2021, Page 10-27

Based on DFT, MP2, and hybrid GGA: MPW1k calculations for an acid-catalyzed hydrolysis of nine Kirby’s N-alkylmaleamic acids, a number of atenolol prodrugs were designed. A linear correlation of the calculated and experimental rate values for the nine Kirby’s N-alkylmaleamic acids has established credible basis for designing atenolol prodrugs that are bitterless, are stable in neutral aqueous solutions, and have the potential to release the parent drug in a sustained release manner. For example, based on the calculated B3LYP/6-31 G (d,p) rates, the predicted t1/2 values for atenolol prodrugs ProD 1-ProD 2 at pH 2 were 65.3 hours and 11.8 minutes, respectively. In vitro kinetic study of atenolol prodrug ProD 1 revealed that the t1/2 was largely affected by the pH of the medium. The determined t1/2 values in 1N HCl, buffer pH 2, and buffer pH 5 were 2.53, 3.82, and 133 hours, respectively.

Recent Development and Validation of a Dissolution Method for Lamotrigine Tablets by UPLC

S. Sangeetha, S. Alexandar, J. Loganathan, B. Jaykar

Technological Innovation in Pharmaceutical Research Vol. 4, 29 May 2021, Page 28-34

The aim of the present work was to develop an accurate, precise, reproducible and economical development and validation of a dissolution method for lamotrigine tablets by UPLC. The UPLC method was carried out using buffer and acetonitrile 75:25%v/v. The flow rate 0.3 ml/min with UV detection at 310 nm. Column used was acquity UPLC BEH Shield RP18,2.1X50 mm. Assay percentage was found to be 100.8. The method was validated according to International Conference on Harmonization guidelines and successfully applied to marketed linearity was plotted from (100 µg/ml to 300 µg/ml) (r2 = 0.9979) Lamotrigene formulations. The method was found to be linear in the respectively. Satisfactory values of Percent relative standard deviation for the intra-day and inter-day precision studies indicated that method is precise. Literature review revealed enormous analytical methods were reported for the estimation of lamotrigene but there is no development and validation of a dissolution method for lamotrigine tablets by UPLC. The method was carefully assessed to guarantee the stability of the drug during the analysis time.

Cross-linking Mast Cell Specific Gangliosides Stimulates the Release of Newly Formed Lipid Mediators and Newly Synthesized Cytokines: An Advanced Study

Edismauro Garcia Freitas Filho, Elaine Zayas Marcelino da Silva, Camila Ziliotto Zanotto, Constance Oliver, Maria Célia Jamur

Technological Innovation in Pharmaceutical Research Vol. 4, 29 May 2021, Page 35-48

Mast cells are immunoregulatory cells that participate in inflammatory processes. Cross-linking mast cell specific GD1b derived gangliosides by mAbAA4 results in partial activation of mast cells without the release of preformed mediators. The present study examines the release of newly formed and newly synthesized mediators following ganglioside cross-linking. Cross-linking the gangliosides with mAbAA4 released the newly formed lipid mediators, prostaglandins D2 and E2, without release of leukotrienes B4 and C4. The effect of cross-linking these gangliosides on the activation of enzymes in the arachidonate cascade was then investigated. Ganglioside cross-linking resulted in phosphorylation of cytosolic phospholipase A2 and increased expression of cyclooxygenase-2. Translocation of 5-lypoxygenase from the cytosol to the nucleus was not induced by ganglioside cross-linking. Cross-linking of GD1b derived gangliosides also resulted in the release of the newly synthesized mediators, interleukin-4, interleukin-6 and TNF-?. The effect of cross-linking the gangliosides on the MAP kinase pathway was then investigated. Cross-linking the gangliosides induced the phosphorylation of ERK1/2, JNK1/2 and p38 as well as activating both NFkB and NFAT in a Syk-dependent manner. Therefore, cross-linking the mast cell-specific GD1b derived gangliosides results in the activation of signaling pathways that culminate with the release of newly formed and newly synthesized mediators. The present study helps to explain the extremely broad spectrum of potential mechanisms by which mast cells might act in suppressing, amplifying and modulating the non-FceRI mediated immune responses.

Poisoning; A Grave Public Health Concern

Shaib Muhammad, Jabbar Abbas

Technological Innovation in Pharmaceutical Research Vol. 4, 29 May 2021, Page 49-59

Globally, due to various incidences of intentional and unintentional poisoning, more than half a million people experience death and low- and middle-income countries (LMIC) accounts for 84% of such cases. The clinical presentation of such cases varies from each other based upon age group, reason of poisoning, geographic region, substances involved and economic development of the country. This study was designed to estimate the number of poisoning cases in central district of Sindh province. The study was carried out in a tertiary care hospital (TCH) of Shaheed Benazirabad, Sindh, Pakistan, between July to December 2019. Subjects were the poisoned patients admitted in the TCH. Study instrument was designed based on the American Association of Poison Control Centers surveys. During the study period, total 263 poisoning cases were presented. Analysis of the study results showed that, the cases of poisoning are more in single (56.3%) males (58.9%) in the age group of 16-30 years (48.7%) having uneducated (55.1%) and jobless (54%) background. Suicide (intentional poisoning) was common reason (36.5%) of poisoning and pesticides (42.6%) were the most widely used substances for poisoning. About (17.5%) of such cases were admitted in Intensive Care Units during the study period and 5.3% of such cases did not survive through such condition. Through this study it was found that, by improving the regulatory controls for hazardous chemicals, establishment of poison control centers, minimization of reporting time and exposure of such substances would be beneficial for control of such cases.

Potential of Saliva-Based Diagnostics to Decrease Hazardous Waste Generation

Nivedita L. Rao, Greeshma B. Kotian, H. Prathapchandra Kedilaya

Technological Innovation in Pharmaceutical Research Vol. 4, 29 May 2021, Page 60-68

Green laboratories that reduce the impact on the environment by promoting sustainable best practices such as waste reduction, have gained importance in recent times. Researchers have developed new technologies and validated a wide range of salivary biomarkers that can soon make the use of saliva a clinical reality. Saliva, like blood, contains an abundance of biomarkers and has tremendous potential to become an alternative diagnostic fluid to blood. Saliva collection method is noninvasive, painless, and convenient to subjects compared to the conventional blood collection process. This chapter explores the potential advantages of using saliva as an alternative to blood, in terms of the volume and effect of the biomedical waste generated. Experimental evidence and theoretical explanation to how saliva-based diagnostics can substantially decrease the volume of potentially infectious, pathological hazardous waste generated by laboratories and impact global waste management strategies, are illustrated in this chapter.

Phytotherapeutic Activities of Six Plant Infusions: Chemical Constituents and Antioxidant Activity

Ana F. Vinha, Carla Sousa

Technological Innovation in Pharmaceutical Research Vol. 4, 29 May 2021, Page 69-84

The use of traditional medicine is attributable not only to cultural and poverty reasons but also to the ineffectiveness of many existing medicines. The lack of effective pharmaceutical formulas and the resistance created by current antibiotic pathogens, as well as oxidative stress new therapeutic agents from plants. In fact, several studies have shown that medicinal plants possess antioxidant properties due largely to their phytochemical profile. In addition, they can prevent oxidative modification by neutralizing free radicals, oxygen scavenging, or decomposing peroxides through their antioxidant activities. Endemic plants can be a source of new bioactive compounds able to prevent several diseases such as cancer, diabetes, hypertension, and Alzheimer’s disease by combating oxidative stress and its associated pathologies. The purpose of this study was to evaluate the contents of total phenolics, flavonoids, and caffeine in six medicinal plants used traditionally in phytotherapy, usually consumed as tea or infusion namely: Camellia sinensisMelissa officinalis, Lippia citriodora, Cymbopogon citratusMatricaria chamomilla, and Tilia cordata. Significant variations in total phenolics and flavonoids content were found among analyzed plants and depending on the nature of the extract. The concentration of caffeine was also very dissimilar and followed the sequence M. officinalis T. cordata C. citratus M. chamomilla L. citriodora C. sinensis. Also, the antioxidant activity of each plant was found to vary according to C. citratus (90.9%) > C. sinensis (87.8%) > M. officinalis (50.7%) > M. chamomilla (45.3%) > T. cordata (32.2%) > L. citriodora (28.0%).

Polycystic Ovarian Syndrome: Insights into the Recent Trends

Ahmed M. Kabel

Technological Innovation in Pharmaceutical Research Vol. 4, 29 May 2021, Page 85-91

PCOS (polycystic ovarian syndrome) is a prevalent hormonal illness that affects women all over the world. Although the specific cause of PCOS is unknown, obesity, hyperandrogenism, and insulin resistance have all been considered as important triggering factors. Menstrual irregularities, acne, hirsutism, a predisposition toward central obesity, and insulin resistance symptoms are all signs of PCOS. Reduced body weight, androgen-lowering drugs, insulin-lowering drugs, and surgical treatments are all used to address the clinical symptoms and consequences of PCOS. The aim of this chapter is to shed light on PCOS regarding its prevalence, etiological factors, pathogenesis, clinical manifestations, methods of diagnosis, lines of management and prognosis in view of the recent trends.

Experimental Evaluation of the Effect of Chloroform Inhalation as a Method of Euthanasia on the Cerebellum and Hippocampus of Adult Wistar Rats

Aguwa Ugochukwu Samuel, Okeke Somadina Nnamdi, Ezejindu Darmian Nnabuihe, Eze Chinyere Elizabeth, Azurunwa Ogechi, Obinwa Benedict Nzube, Ovie Ogbo. Felix, Obi Kelvin Chukwuemeka, Onwuelingo Sopuru, Okonkwo David, Doris Ogbuokiri, Okeke Chijioke

Technological Innovation in Pharmaceutical Research Vol. 4, 29 May 2021, Page 92-104

Chloroform inhalation is a common method of rodent euthanasia in Nigeria for research purposes. This work is designed to evaluate the consequence of this method of sacrifice on the cerebellum and hippocampus of Wistar rats. Twenty male Wistar rats weighing between 160 and 180 were divided into 4 groups of 5 rats each. Group A served as control and was sacrificed using cervical dislocation (a widely acceptable non-inhalation method of sacrifice). Groups B, C and D were exposed to chloroform for 5 minutes once a day (group B), once a day for 2 days and once a day for 3 days. The brains were removed; four from each group was processed for antioxidant assay while one from each group was fixed in Bouin’s fluid for histological studies. Our results show that chloroform inhalation adversely affected the results of the antioxidant parameters studied in a dose-dependent fashion. That means that the adverse effect worsened as the number of days increased. This was also the case with the histology results as there was evidence of cell necrosis in the cerebellar and hippocampal tissues. This also showed dose dependence. We therefore conclude from our results that when studying the brain tissues or carrying out brain related researches, chloroform inhalation is not the method of choice for rat euthanasia. Therefore, chloroform sedation is not ideal for experimental purposes as a method of rat sacrifice, especially when studying rat brain.

Antiseptic Use in Wounds of the Lower Limb

Tiffanie-Marie Borg, Fahima A. Begum, Hamed Mazoochy, Nima Heidari

Technological Innovation in Pharmaceutical Research Vol. 4, 29 May 2021, Page 105-121

Objectives: The aim of this study is to review the available literature addressing the safety and efficacy of antiseptics in surgical wounds. The different antiseptic solutions, irrigation volumes, time scales and delivery methods have been compared so that evidence-based recommendations on antiseptic use in plastic, orthopaedic, foot and ankle surgical procedures can be proposed.

Methods: A literature search was performed using the online databases Medline and EMBase to identify in-vitro and in-vivo studies pertaining to antiseptic use in an orthopaedic context. Terms including antiseptic, irrigation fluid, bacitracin, hydrogen peroxide, povidone-iodine and chlorhexidine were searched. Literature published in English from inception to July 2020 in which the full text was accessible was considered for inclusion. Cellular and animal studies were included on the basis that authors analysed antiseptic efficacy and/or toxic effect of antiseptic on cells present in orthopaedic wounds. Clinical studies that met the criteria for inclusion in this review assessed antiseptic use in a surgical context, with a focus on foot and ankle procedures. These included case reports, case series, case control, prospective and retrospective studies as well as randomised controlled trials. Studies were categorised as in-vitro, animal and human studies. Twenty-three, eleven and forty-seven studies were identified as in-vitro, animal and human studies respectively. These have been summarised and presented herein in a narrative format.

Results: There is strong evidence that skin preparation with antiseptics before plastic and orthopaedic procedures reduces the risk of post-operative infection.

Conclusion: Routine prophylactic intra-operative antiseptic use should be performed with caution as they increase the risk of local and systemic complications. However, there is strong evidence supporting the use of antiseptics pre-operatively when preparing the skin. Determining the best antiseptic preparation remains a matter of debate since a single agent or solution is not effective against all organisms. Further research is therefore needed to assess the efficacy of antiseptics in prevention and treatment of infections.

Development and Validation of UV-Spectrophotometric Method for the Determination of Lornoxicam in Microsponges

Ayya Rajendra Prasad, Bannaravuri Thireesha

Technological Innovation in Pharmaceutical Research Vol. 4, 29 May 2021, Page 122-130

Objective: To develop and validate a novel, specific, precise and simple UV-spectrophotometric method for the estimation of lornoxicam present in microsponges. Lornoxicam is  a non-steroidal  anti-inflammatory  drug(NSAID)  of  the oxicam class  with analgesic(pain  relieving), anti-inflammatory and antipyretic(fever reducing) properties.

Methods: UV-spectrophotometric determination was performed with Thermo Scientific Evolution 201 UV-Vis spectrophotometer using methanol as a medium. The spectrum of the standard solution was run from 200-400 nm range for the determination of absorption maximum (? max). ? max of lornoxicam was found at 353 nm. The absorbance of standard solutions of 3, 6, 9, 12 and 15, µg/ml of drug solution was measured at an absorption maximum at 353 nm against the blank. Then a graph was plotted by taking concentration on X-axis and absorbance on Y-axis which gave a straight line. Validation parameters such as linearity and range, selectivity and specificity, LOD and LOQ, accuracy, precision and robustness were evaluated as per ICH guidelines.

Results: Linearity for the UV-spectrophotometric method was noted over a concentration range of 3.0-15.0 µg/ml with a correlation coefficient of 0.9995. The limit of detection (LOD) and limit of quantification (LOQ) for lornoxicam was found at 1.26 ?g/ml and 3.82 ?g/ml respectively. Accuracy was in between 99.21 and 99.60%. % RSD for repeatability, intraday precision and interday precision were found to be 0.473, in between 0.478 and 0.619 and in between 0.855 and 1.818 respectively. The proposed UV method is found to be robust.

Conclusion: The proposed UV-Visible spectrophotometric method was validated according to the ICH guidelines and results and statistical parameters demonstrated that the developed method is sensitive, precise, reliable and simple for the estimation of lornoxicam present in microsponges.

Trends in Evolution of Anthelminthic Chemical Agents: Ecological, Physiological and Biochemical Adaptation in Helminth

M. Kh. Dzhafarov, F. I. Vasilevich

Technological Innovation in Pharmaceutical Research Vol. 4, 29 May 2021, Page 131-151

The major anthelminthic substances - alternative medicine components, distinct types of pluripotent synthetic and naturally occurring chemicals – are discussed in this study. Much attention is paid to the sections devoted to recent discoveries (Emodepside, Monepantel, Derquantel, Tribendimidine) and to some promising works. The overview further covers certain elements of anthelminthic substance molecular mechanisms of action, helminth adaptability to anthelminthic chemicals, and alternate worming therapy alternatives. Anthelminthic substances are synthetic non-organic and organic or natural compounds.  Based on the systemic analysis of particular features of the chemical structure of anthelminthic substances, the hypothesis on the viability of the targeted search for such compounds among the derivatives of  conditionally progenitor cyclic hydrocarbons – benzene,  indene, naphthalene,  1?-cyclopenth [a]-naphthalene and phenanthrene – by alternating absolutely unsaturated and saturated structures, including heterocyclic analogues containing nitrogen, oxygen and sulfur and different substitutes and functional groups, was voiced.