Current Aspects in Pharmaceutical Research and Development Vol. 8

The present study examine the antioxidant activity of the four dominant species and study the participation of other antioxidant compounds such as phenolics besides the well known Carotenoids. The antioxidant properties of four Trentepohlia species (T. abietina, T. arborum, T. diffracta, and T. umbrina) were evaluated in vitro, and all four species were shown to be rich in phenolic compounds, a surprising finding. T. abietina extract, on the other hand, had the highest total phenolic component and flavonoid content, as well as the strongest scavenging action and the lowest IC₅₀. The scavenging activity of the four Trentepohlia species extracts was observed to decrease in the following order T. abietina >T. arborum>T. diffracta>T. umbrina. Moreover, both DPPH radical scavenging activity and superoxide anion radi­cal scavenging activity varied significantly between the four species. In case of reducing power, extracts of all four species were concentration dependent where high reducing power was observed at higher concentration and gradually decreased with decrease in concentration of the extracts. Comparing amongst the species, T. abietina again showed highest reducing power at all the concentrations. The result of correlation showed a positive increase in scavenging activities with increase in flavonoids content. This present scenario the scavenging effect exhibited by the extract of four species of Trentepohlia mainly the DPPH scavenging activity could be attributed to the presence of mainly flavonoids constituent. This clearly indicated that in this case, the scavenging effect exhibited by the extract of all four species of Trentepohlia mainly the DPPH scavenging activity could be attributed to the presence of mainly flavonoids constituent.

Aryl naphthalene’s lignans are extracted by pet. ether from Cleistanthus collinus. Objective to study poisonous plant such as Cleistanthus collinus has contained biological potent Naphthalene. The bark, leaves, heartwood, fruits and other parts of this plant are rich in lignans cleistanone along with their lactones. Isolation of chemical constitutions by column chromatography, followed by TLC examination and Detection in iodine chamber with UV lamp or sprayer solution (CH₂Cl₂: CH₃OH). The isolated arylnaphthalide lignans are cleistanone, diphyllin, cleistanthins A, C and D and 4-O-(30-O-methyl-b -D- glucopyranosyl)-diphyl lin.

In this present study, the creation, and characterization of gold nanoparticles (AuNPs) for pharmacological applications like antimicrobial and anticancer exercises. The gold nanoparticles (GNPs) were arranged to utilize plant extracts in a basic natural approach. The Hygrophila spinosa watery leaf extract has been carried out within the show consider. The bioreduction of auric chloride (HAuCl4) for the blend of gold nanoparticles with the plant extract H. spinosa. The plant extract is blended with HAuCl₄, The decrease of auric chloride is driven by the arrangement of AuNPs inside 10 min at room temperature (28°C), The estimate, shape, and essential examination was carried out utilizing X-ray diffraction, SEM-EDAX, DLS, FT-IR, and UV-spectroscopy. The results showed that the leaf extract of H. spinosa could be an exceptionally great bioreductant for the union of gold nanoparticles. The synthesized gold nanoparticles have more dynamic against human pathogens additionally have great anti-cancer properties.

Background: The U.S. Food and Drug Administration Adverse Event Reporting System, FAERS, contains information on adverse events and medication error reports submitted to the FDA through the MedWatch program. Opioid use has been linked to a significant number of adverse events reported in the FAERS database. The focus of this research  was to determine the frequency counts and related deaths of opioid drug names in the FAERS database.

Methods: Drug information was obtained from the database's DRUG and OUTCOME files. Morphine, fentanyl, oxycodone, hydrocodone, tramadol, hydromorphone, methadone, codeine, oxymorphone, meperidine, propoxyphene, diphenoxylate, and heroin were among the drugs discovered. The MySQL database management system was used to determine the frequency counts and concomitant deaths of opioid drug names.

Results: Fifteen different opioid drugs were linked to ADEs, including death, in the FAERS database, with three drugs (oxycodone, hydrocodone, and fentanyl) accounting for more than half of the reports. The highest frequency count value for oxycodone was 158,181, representing approximately 20.2 percent of the opioid frequency counts. Dextromethorphan had the lowest frequency count value of 2,161, accounting for approximately 0.3 percent of the total. The opioid with the highest proportion of deaths to drug count was heroin (71.8%), followed by dextromethorphan (55.6%), methadone (37.2%), morphine (26.8%), and propoxyphene (23.7%).

Conclusion: The FAERS database is an important source for detecting and reporting Adverse Drug Events (ADEs), particularly those involving opioids and related drugs. Estimating the true incidence of ADEs for this class of drugs in the general population remains challenging.

Plants have been used as a therapeutic agent since time immemorial and its mode of usages have been coevolved with human civilization. Man identified therapeutic potential of plants through trial and error method and passed the knowledge from generation to generation verbally and practice. Before 16^th century plant or plant parts have been used as such and in between 16^th and 18^th century mixture of plant or plant parts were used as medicine. Since in the beginning of 18^th century pure compounds have been isolated from plants and used as medicine. Today over 6,00,000 plant derived compounds are isolated from various plants and out of 252 drugs considered as basic and essential by the World Health Organization (WHO), 11% are exclusively of plant origin and a significant number are synthetic drugs obtained from natural precursors. The plant derived drugs are found to be more stable, induce fewer side effects and showed pleotropic druggability due to the unprecedented structural features and functional diversity. Moreover, plant derived molecules are synthesized within the living system and repeatedly tested and modified through long term evolutionary process. In addition to phytomolecules, plants are also the best synthesizer of nanoparticles with diverse therapeutic activities. The herbal medicines or the plant extracts contains a plethora of chemical constituents and numerous functional groups such as C=C – alkenyl, C=N – amide, O=H – phenolic and alcohol, N=H – amine, C-H and COO- carboxylic acid etc., these functional group may bind with metal ions and form nanoparticles. Biosynthesis of different metal nanoparticles such as Cu, Co, Ag, Au, Pd, Pt, Zn, Mn, Ti, Ni, Fe, etc. and alloy of Au, Al, Zn were successfully achieved. The versatility of plant derived drugs under various aspects such as historic background, plant derived drugs in modern medicine, importance of medicinal plants in drug discovery, plant derived drugs - advantages and disadvantages, characteristic features of plant derived drugs, major challenges in plant derived drug discovery, value and market potential, approaches of drug discovery from plants, importance of phytochemical and pharmacological screening, drug discovery from plants – Indian scenario, plant derived nano medicine are briefly reviewed.

In Egypt, Trifolium alexandrinum L. is an important green forage crop as well as an anti-diabetic medicinal plant. The overall forage phytomass was about 14.3 tons/fed/year. The current study assesses dry matter production, nutrient cycling and nutrient use efficiency (NTUE) in an agro ecosystem of T. alexandrinum under normal agricultural practices and rotational clipping by farmers. During the first and last three growth phases, the net above ground primary productivity was calculated to be around 0.066 and 0.093 g/g dry weight/day. Initially, the rate of nutrient accumulation in shoots was greater than the rate of biomass accumulation. There was a gradient of N and K concentration from roots to shoots, which is consistent with active translocation of these elements to the shoot. The amount translocated exceeds approximately 90% of the total N and K uptake. During the extensive growth period, the total organic constituents (TAC, CP, EE, and SOC) in the shoot reached their maximum content. Furthermore, T. alexandrinum was found to have different levels of NTUE during different growth periods. The primary controlling factor in changes in NTUE for the majority of elements was biomass allocation.

Introduction: Mitosis is a basic age–related process. Mitoses are found in various tissues and are controlled by mediators. Cytokines and hormones, for example, are used as drugs to treat cancer, graft–versus–host disease, and other diseases.

Objective: Our goal is to evaluate existing research on age–related mitoses, cytokines, and hormones in lymph (body fluid), specifically in thoracic duct lymph (TDL) in norm, and to use it in new drug design and development.

Methods: We investigated the data banks of PubMed/Medline, World Cat, Google and Index Copernicus searching for articles published in the past four decades.

Results: Three articles characterised some morphological properties and quantitative changes in age-related mitoses in normal TDL. One study looked at the quantitative and morphological characteristics of TDL lymphocytes in healthy and thyroxin-treated people. Several studies on the physiology of angiotensins, insulin, and steroid hormones were conducted. Many recent publications have focused on proliferation and mitosis mediators. Interleukins are being studied in lymph for their antigen–stimulation and other effects. The effect of age on the immune system, particularly mitoses, was discovered. Despite advances in the field of drug design, there is a perception of failed attempts to solve some problems using reductionist methods. To develop a drug, several complex multistep schemes must be completed, cytotoxicities must be controlled, and the results must be compared.

Conclusion: The data presented above show that the immune system changes with age, both in norm and in impact. The differences and changes in TDL mitosis mediators in mature and immature organisms have not been studied. New drug components must be developed. It is proposed that the differences in TDL mitosis mediators between healthy newborns (neonatal, immature) and adults (mature) can be used to develop new drugs for cancer, graft–versus–host disease, and other diseases.

Background: Recognizing population management as a critical step toward global health encourages more research into male contraception. Despite the fact that there are numerous synthetic contraceptives on the market, they all have a variety of side effects. Different possible male contraceptive options, including hormonal, pharmacological, and immunological therapies, were studied over a lengthy period of time, and these methods demonstrated good antifertility effects with low failure rates when compared to condoms.

Main Text: This chapter is focused on the idea of herbal contraceptives, which are an efficient way to restrict animal and human fertility. This review has focused on herbal medicinal plants and plant extracts that have been shown to have antifertility effects in males. The review considers plants that have been traditionally used for their spermicidal and antispermatogenic activities, as well as plants with reported animal studies and some with human studies for antifertility effects, as well as their doses, chemical constituents, and mechanism of action for the antifertility effect of the plants. The stages of sperm development, hormone production, and the mechanism of male contraceptives are also explained in this chapter.

Conclusion: In terms of the current review's relevance, it could be very valuable in producing plant monographs and suggestions for their use. Many of the plant species listed here could be useful as alternative oral fertility-regulating agents in males. As a result, more research into the chemical and biological features of these less-explored plants is needed to determine their contraceptive efficacy as well as to possibly identify their harmful effects, so that these substances can be used confidently to manage male fertility. In this field, new inventions are required to focus on modern, more potent drugs with less harmful content that are self-administerable, less expensive, and completely reversible.

Citrus maxima (pomelo) proved to exhibit anti-microbial activity toward several microorganism strains although the negative result shown in this research conducted. There are several factors which can affect their antimicrobial activity such as resistance of tested bacterial strains, variation of temperature of preparation condition and low concentration of phytochemical present in the plant extract. Malaysia is popular for growth of “Citrus maxima” with the local name of pomelo. Pomelo is helpful in boosting body immune system, prevent weight gain and as anti-aging agent. Pomelo is also useful in preventing constipation as to promote digestion and peristalsis. Pomelo contains a huge amount of potassium (an effective vasodilator) and vitamin C (an antioxidant). Maceration and Soxhlet extraction of peel of Citrus maxima were carried out with n-hexane. Anti-microbial activity of Citrus maxima was followed by “Well Diffusion” method and comparing the clear inhibition zone of standard antibiotic and the extracts on “Mullen-Hinton agar”. Anti-oxidant activity of Citrus maxima was carried out by using DPPH radical-scavenging activity of total phenol assay. The qualitative test for alkaloids confirmed in all the extracts. The presence of terpenoids observed in filtrate and residue after maceration while terpenoids were absent in the Soxhlet sample. Presences of Flavonoids were found only in residue. Total phenolic compounds present in the hexane extract and found that higher the sample concentration, the higher the GAE value obtained.

This survey article covers the Fluidized bed processing as a novel methodology of solubility enhancement for inadequately water-soluble medications. The main objective of this work was to study the solubility and dissolution kinetics of poorly water-soluble drugs simvastatin from its solid dispersion with different carriers by using fluidized bed processing technique. One of the significant boundaries to accomplish wanted convergence of medication in blood is drug solubility. Among all recently and existing medication up-and-comer around 40% drugs are lipophilic in nature and neglects to arrive at helpful reach because of poor solubility and at last it shows slow dissolution and low bioavailability. Choice of solubility upgrade procedure relies upon drug properties, site of ingestion and required dose structure attributes. Simvastatin is BCS class- II i. e. low soluble and high permeable, which reduces its bioavailability, to overcome this problem, a solid dispersion is formed using various techniques with polymeric carrier to potentially enhance the solubility and dissolution rate such as fluidized bed processing, it will extend drug absorption, therefore the objectives were to make a comparative evaluation among different solid dispersions and to assess the effect of various carriers in solid dispersions on the drug release profile and solubility behaviours. For solid dispersion, Gelucire® 44/14, PVP- K30 and Poloxamer utilized as carrier for poorly water-soluble drugs in order to improve their bioavailability. The dissolution profiles were correlated using various mathematical models such as Zero order, first order, Higuchi and Hixon Crowell model and the Zero order kinetics model gave better correlation results than the other models. Dissolution profile of SIM was significantly improved via complexation with Gelucire 44/14 as compared with the pure drug and other carriers. The binary system which was prepared using FBP showed the highest dissolution rate and solubility profile. It is also concluded that all SDs of SIM showed considerable enhancement in dissolution rate and solubility compared to both PMs and the dissolution rate of both PMs was higher compared to the pure simvastatin.

Background: Ranitidine is a histamine-2 (H2) blocker, which decreases the amount of acid created by the stomach. In September 2019, the drug was recalled due to impurities N-nitrosodimethylamine (NDMA) by the Food and Drug Administration (FDA), European Medicines Agency (EMA), and Health Canada. NDMA is a carcinogen based on results from laboratory tests.

Aim: The objective of the study is to assess the awareness among the physicians and pharmacists in and around Chennai about the ranitidine recall notification and its related issues.

Materials and Methods: A descriptive, cross-sectional study was carried out where a questionnaire was administered on 198 physicians and 113 pharmacists who were enrolled in the study. Awareness, knowledge, and issues related to recall notification were recorded from the participants.

Results: Results showed that only 75% of the study participants were aware of the notification and the issues related, with significantly more participants from the urban area compared with the rural area. When the notification was known by many, the reasons pertaining to the notification were not known. The findings indicate that the majority of participants who were not familiar with the ranitidine recall notification and the related issues were from the rural area.

Conclusion: Overall, the awareness assessed among physicians and pharmacists was not satisfactory. Physicians and pharmacists are the most responsible healthcare providers and to be updated with every notification on medication published by regulatory bodies.

Aims: Linagliptin and Empagliflozin is a new drug combination for the treatment of Diabetes Mellitus which is one of the oldest and lethal diseases of the mankind. Aim of the research work was to develop and validate novel, rapid, sensitive, specific, robust stability indicating analytical method for the simultaneous estimation of Linagliptin and Empagliflozin in the pharmaceutical dosage form as fixed dose formulation.

Study Design: Method development and validation was performed as recommended in ICH guideline “Validation of analytical procedures: Test and Methodology Q2(R1)”.

Methodology: Method develop with chromatographic parameters as Phenyl column (150mm×4.6 mm, 3.5 mm particle size), Column temperature was 30°C, HPLC system with PDA detector and mobile phase contained a degassed mixture 0.1% Perchloric Acid: Acetonitrile (75:25 v/v). The flow rate was set to 1.2 ml/min with responses measured at 226 nm, injection volume was 20 µl, and run time of 22 mins.

Results: The retention time of Linagliptin and Empagliflozin was 10.2 min and 15.7 min respectively. Linearity was established in the range of 10-30 µg/ml for Linagliptin and 20-60 µg/ml for Empagliflozin with correlation coefficients more than 0.999. The percentage recoveries were between (98.4-100.5%) and (99.2-100.4%) for Linagliptin and Empagliflozin respectively. Validation parameters were evaluated according to the International Conference on Harmonization (ICH) Q2 R1 guidelines. The forced degradation studies were performed by using HCl, NaOH, H2O2, thermal and UV radiation. The developed method was successfully applied for the quantification and hyphenated instrumental analysis.

Conclusion: Significance of developed method is that it can be utilize for routine or unknown sample analysis of assay of Linagliptin and Empagliflozin in pharmaceutical dosage form developed by various Pharmaceutical Industry.

Objective: The present study was intended to evaluate the hepatoprotective activity of ethanolic extract of leaves of Vitex negundo Linn. The Vitex negundo Linn. is a medicinal plant found throughout India. It is a short plant of mediterranian region and used as herbal remedy of folklore usage.

Methods: The ethanolic extract of Vitex. Negundo Linn. (300 mg/kg) was administered orally by suspending in tween-20 solution to the animals with hepatotoxicity induced by paracetamol (3 gm/kg). Silymarin (25 mg/kg) was given as reference standard. The hepatoprotective activity was also supported by histopathological studies of liver tissue. An effective significant alteration in all biochemical parameters and histopathological sections were observed

Results: Since results of biochemical studies of blood samples of paracetamol treated rats showed significant increase in the levels of serum enzyme activities, reflected the liver injury caused by paracetamol and blood samples from the animals treated with the oral administration of ethanol extract produced a significant reduction in serum enzymes alanine aminotransferase (ALT), aspartate aminotransferase, (AST), alkaline phosphatase (ALP) to the acute hepatotoxic induced rats. They exhibited a significant inhibition of hepatic toxicity by using various marker enzymes and the histopathological analysis.

Conclusion: From these results, it is concluded that the Vitex negundo Linn. is effective in protecting the liver against the injury induced by paracetamol in rats at the dose of 300 mg/kg/body weight. These results suggest that leaves of Vitex negundo Linn. may supports the hepatic cells protection.

Henna (Lawsonia inermis) has been found to have both medicinal and commercial uses. The pigment lawsone derived from this plant is the source of Mehendi. The henna plant represents a vast repertoire of secondary metabolites, giving the plant important medicinal properties, like anticarcinogenic, antidiabetic, analgesic, immunostimulatory, and many more. This creates a huge demand pressure, which can’t be met by traditional farming due to the low propagation rate. So, the main objectives of this study involve, the establishment of the plant from lab to land, analysis of the secondary metabolite content of the plant by various assays, to see if in vitro plants have more secondary metabolic accumulation as compared to in vivo plants. To further validate the results, HPLC analysis and comparative transcriptome analysis were done, followed by KEGG analysis of the pathways. Out of the various solvents used for the study, methanol responded best to the secondary metabolic assays. It was also interesting to see that in vitro plants showed a higher accumulation of secondary metabolites than in vivo plants. Comparative transcriptome analysis through the TRAPID platform showed a significant difference between the plant’s transcript sets, showing gene families and enzymes contributing to secondary metabolites being more enriched in vitro plants. KEGG analysis of the pathways showed a large number of pathways related to secondary metabolites for tissue culture grown plants, like terpenoids, phenols, and flavonoid biosynthesis, which can be held responsible for the plant’s wide medicinal and commercial properties. Hence, this work shows that in vitro henna plants have higher secondary metabolite accumulation, with a better propagation rate than traditional farming. These enriched secondary metabolic pathways can make the in vitro plants more efficient for the commercial and medicinal industry, being propagated, in a stable and controlled environment, without exposing the plant to stress, saving the plant from overexploitation.