International Journal of Pharmaceutical Investigation

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ISSN / EISSN : 2230-9713 / 2230-9713
Published by: EManuscript Services (10.5530)
Total articles ≅ 535
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Manjunath Pobbathi Nagaraj, Avinash Kumar Seth, Anand Kandkere Ravindra Kumar, Vivekanandan Sundaramurthy
International Journal of Pharmaceutical Investigation, Volume 12, pp 323-327; https://doi.org/10.5530/ijpi.2022.3.54

Abstract:
Background: Circadian rhythms is a natural process that regulates the sleep wake cycle which is associated with several physiological, biochemical, endocrine, behavioural processes in humans and entrainment to light-dark cycle. The activity of Ramelteon is believed to contribute to its sleep-promoting properties and thought to be involved in the maintenance of the circadian rhythm underlying the normal sleep-wake cycle. A tablet can be given before 2 hr of bed time, so the Ramelteon drug shows its effect throughout the night by releasing the active content with lag time followed by sustained action to promote the sleep. Materials and Methods: Chronotherapeutic drug delivery system were prepared by compression coating technology using pH independent, hydrophilic and hydrophobic polymers. Results: Drug excipient compatibility indicated that the Ramelteon Active pharmaceutical ingredient (API) is compatibility with the excipients proposed. The X-ray Diffraction (XRD) studies indicated that the crystalline form of the Ramelteon API existed in the finished formulation. Conclusion: The core tablets containing Eudragit RSPO 10mg/tablet and ratio of Ethyl cellulose: Hydroxy propyl methyl cellulose (HPMC) of 70:30 in the outer coating material yielded a desired lag time of 2 hr and drug release for a period of 4 hr to achieve a chronotherapeutic drug delivery system. Ramelteon is an excellent candidate in designing chronotherapeutic drug delivery systems and further in vivo studies can be explored in the treatment of circadian rhythm with sleep wake cycle disorders.
Utkarsh Ghate, Hema Kulkarni, Manasi Deshpande, Mandar Akkalkotkar
International Journal of Pharmaceutical Investigation, Volume 12, pp 250-254; https://doi.org/10.5530/ijpi.2022.3.45

Abstract:
Molecular docking studies are used to identify cultivated/ abundant herbs such as Coriander, Burmuda grass or Asparagus as potential replacement for Seeta Ashoka- Saraca asoca (Roxb.) De Wilde, syn. S. indica Linn. a rare Indian medicinal forest plant, threatened with extinction due to over harvest. Its bark is used to make the famous Ayurvedic medicine “Ashokarishta” to treat menorrhagia and as a uterine tonic like ergot but is mostly adulterated. We tested using molecular docking studies Quercetin and other polyphenols from Coriander as potent anti-inflammatory ingredients, similar to NSAID (Non-steroidal anti-inflammatory drugs)., Polyalthia longifolia, the common adulterant is also be noted to be effective as its bark contains 30-50% of tannin than Saraca asoca, so may help in thrombosis.
Ashish Yashwantrao Pawar, Ashvini Dhanraj Tapkir, Jyoti Bramhesh Rao, Rushikesh Pramod Dayama
International Journal of Pharmaceutical Investigation, Volume 12, pp 317-322; https://doi.org/10.5530/ijpi.2022.3.53

Abstract:
Background: The pharmaceutical industries are keen in development of new herbal bioactive molecules with an improved effect and less toxicity in order to replace synthetic drugs. Constipation is the most prevalent medical concerns. It’s estimated that one in five adults worldwide suffers from constipation. Hence, the demand of herbal laxatives is increasing worldwide. The purpose of this research work was to develop Senna nanoparticles with the help of Eudragit L100 an enteric coating polymer to provide site specific activity and to prevent degradation of Senna in acidic environment. Materials and Methods: Senna loaded nanoparticles were prepared by using emulsion solvent evaporation method. Different formulation has been formulated with varying concentration of Eudragit L-100 and constant aqueous and organic phase ratio (1:9). Drug and polymer compatibility study was analysed by FTIR. The prepared formulation was characterized by melting point, particle size, zeta potential, polydispersity index, vesical morphology and in-vitro drug release. Results: All the formulation batches shows particle size between 380.61 - 1061.71nm. The zeta of optimized batch (F5) was found to be -23.75mV. Entrapment efficiency of the entire prepared formulation batch in between 3.16±0.31- 55.18±0.35%. The in-vitro drug release shows maximum drug release i.e. 61.03% in 8 hrs which shows that release of drug prolonged and site specific due to use of enteric coated polymer Eudragit L100. Conclusion: The developed Senna loaded nanoparticles can provide site specific drug delivery. The polymer used in Senna Nanoparticles formulations shows efficient and targeted drug release as well as reduction in dose, dosing frequency and side effects
Snigdha Bhardwaj, Pushpraj S Gupta
International Journal of Pharmaceutical Investigation, Volume 12, pp 260-271; https://doi.org/10.5530/ijpi.2022.3.47

Abstract:
Background: Pseudomonas aeruginosa (P. aeruginosa) is considered as one of the most opportunistic pathogens that may infect humans and led to increase in bacterial virulence or pathogenicity. P. aeruginosa exhibits variety of virulence factors and their rate of expression are associated with cell-to-cell communication process also known as quorum sensing (QS). LasR, a transcriptional factor which regulates the process of QS in P. aeruginosa is known as attractive drug target. Materials and Methods: The research work involves identification of putative inhibitors of LasR by molecular docking approach. Total 60 compounds were docked in the active site of LasR and CviR protein, followed by subsequent screening based on Lipinski’s rule of five, Veber rule and molar refractivity. Results: Out of 60 compounds, total seven novel compounds were selected on the basis of binding energies (docking score> 10). Structures of LasRinhibitor complexes were analyzed to have vital insights from the binding between LasR and inhibitor molecules. The selected compounds were analyzed for physico-chemical properties and drug likeness to establish correlation between oral bioavailability and pharmacokinetics of compound. Conclusion: The study revealed the potential of thiazole derivative as novel QSI and expedite the possibility to combat virulence of multi-drug resistant P. aeruginosa in more effective manner.
Patricia Gaitan-Hahn, Anita Ricablanca, Ami Abbott, Jessica Chadwick, Alicia Thomas, Nathalia Cruz, Alice Deng, Leah Ordinanza, Mudassar Iqbal Arain, Eduardo Fricovsky
International Journal of Pharmaceutical Investigation, Volume 12, pp 334-339; https://doi.org/10.5530/ijpi.2022.3.56

Abstract:
Background: Previous studies suggested that glycogen storage was facilitated by ascorbate inhibition of phosphofructokinase-1 (PFK-1) in resting mammalian muscle; these studies showed that purified PFK-1 from fish or chicken muscle has properties similar to PFK-1 from mammalian muscles. Materials and Methods: The enzymes utilized in the assay systems came from Sigma-Aldrich Co. Rabbit (Oryctolagus cuniculus) muscle G-actin (A 2522) was free of aldolase, LDH (EC 1.1.1.28) or AK (EC 2.7.4.3) activity and rabbit muscle aldolase (EC 4.1.2.13) was free of AK (EC 2.7.4.3) and LDH activity. Rabbit muscle PFK-1 (RPFK-1), chicken (Gallus gallus) muscle PFK- 1 (CPFK-1) and Pacific red snapper (Lutjanus peru) muscle PFK-1 (FPFK-1) used in these tests were prepared from frozen tissues with modifications of a method. AK, LDH, and aldolase activity were absent in purified FPFK- 1 and CPFK-1 preparations. Results: It can be shown that the following enzymes associated with glycolysis are not inhibited by 0.1 M ascorbate under our conditions: rabbit muscle aldolase (EC 4.1.2.13); rabbit muscle glyceraldehyde 3-phosphate dehydrogenase (EC 1.2.1.12); rabbit muscle phosphoglucose isomerase (EC 5.3.1.9); rabbit muscle pyruvate kinase (EC 2.7.1.40); yeast hexokinase (EC 2,7.1.1); and yeast 3-phosphoglyceric phosphokinase (EC 2.7.2.3). Rabbit muscle enolase (EC4.2.1.11) is inhibited under our conditions. Conclusion: In summary, FPFK-1 and CPFK-1, possess characteristics and behaviors similar to RPFK-1, e.g., losses of activities due to dilutions and protections of some of these activity losses by rabbit muscle aldolase. These interactions of a mammalian aldolase with fish and a bird PFK-1’s suggests a conservative evolutionary relationship among aldolases and PFK-1’s.
Raseema Raheema Sharafudeen, Annie Abraham, Reshma Usha Soman
International Journal of Pharmaceutical Investigation, Volume 12, pp 255-259; https://doi.org/10.5530/ijpi.2022.3.46

Abstract:
Background: The coconut palm is so much more than just a tree; because all of this is essential with medicinal benefits. Coconut inflorescence sap (CIS) is the sweet, oyster-white colored, non-fermented juice tapped from the immature coconut spadix. Coconut products are widely used in Indian folk medicine for their effects on hemorrhaging, bronchitis, antimicrobial, radical scavenging, analgesics, anti-inflammation, anthelmintics, and immunotherapies. Many studies reported the fantastic health benefit of the coconut palm tree. The coconut inflorescence has cytoprotective and antihyperglycemic properties [Renjith, R.S. et al., 2013]. But not many systematic studies have been conducted on Coconut Inflorescence Sap. The objective of the present study is to analyze the nutritional components, detect the mineral composition, perform preliminary phytochemical screening, and find out biologically active compounds using FTIR Spectrum analysis and LCMS analysis. Materials andMethods: CIS’s nutritional components and mineral content analysis were done following the standard procedures. The phytochemical screening, FTIR Spectrum analysis, and LCMS analysis are also done to confirm the health benefits of CIS. Results: CIS exhibited a significant amount of micro and macronutrients. The Phytochemical analysis also showed the presence of flavonoids, alkaloids, terpenes, steroids, phenols, and glycosides. The LCMS Spectrum analysis of CIS shows the presence of biologically significant compounds, namely 4-HydroxyCoumarin, P-Coumaric acid, Mellein, Leucopelargonidin, Coumarin, 3 Caffeoylquinic acid, Ferulic acid 4-O-Glucosidase and also three essential aminoacids L-Phenylalanine, L-isoleucine and D-Tryptophan. Conclusion: The nutritional composition, active phytochemical constituents, and polyphenolic compounds of CIS showed that CIS has a significant beneficial effect in upgrading the antioxidant status. CIS is a natural drink with effective antioxidant potential. Concerning the nutrient composition, mineral and amino acid composition, and scavenging assays, it would be possible to exploit this natural drink in clinical therapy.
Kk Mueen Ahmed
International Journal of Pharmaceutical Investigation, Volume 12, pp 399-399; https://doi.org/10.5530/ijpi.2022.3.68

Abstract:
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Rajeshwari Pasupula, S. Bhanu Uday Sankar, Sreya Kosanam, Ch Naga Priya, Ch Varudhini Devi, Bhimavarapu Sai Deepika
International Journal of Pharmaceutical Investigation, Volume 12, pp 396-398; https://doi.org/10.5530/ijpi.2022.3.67

Abstract:
Congenital Hydrocephalus is due to buildup of excess cerebrospinal fluid in the brain at birth. Fluid buildup leads to neurological and psychological damages to the child. Aqueductal stenosis means a narrowing the passageway between the third and fourth ventricles. In this case report, Ventriculoperitoneal shunt is placed to relieve the pressure, but was removed due to Meningitis. As per review of literature, incidence of shunt failure in infants below 2 years is 5-12% and with more than 60% mortality rate.
Sai Latha K, Abhinaya P, Parimala G, Lakshmi Pk
International Journal of Pharmaceutical Investigation, Volume 12, pp 391-395; https://doi.org/10.5530/ijpi.2022.3.66

Abstract:
Objectives: Access to health care is a basic right of population. Essential medicines are those which satisfy the priority of health care needs and intended to be available at all times. Hence prices and availability need to assess periodically. The objective of the study was to measure the variation in prices of selected medicines, to measure the availability of some selected medicines used for treating common diseases/ailments and to compare the prices and availability of medicines among the sectors. The present survey is conducted for 20 essential medicines in Hyderabad, Telangana. Methods: Medicines were selected based on the criteria of WHO/HAI methodology. Data was collected during October 2019 to March 2020 for originator brands and lowest priced generics in 60 medicine outlets. Prices were compared to international reference prices and expressed as median price ratio. Percent availability computed only on the day of data collection. Results: Median MPRs for originator brands and lowest priced generics were 2.20 and 1.53 in independent outlets, 2.20 and 1.61 in chain pharmacies respectively. Median MPR for generics in Jan Aushadhi Kendra was 0.38 i.e., all available medicines were priced less than international reference prices. Availability was 95.8%, 95.4% and 67.5% for generics and 12% and 13.3% for originator brands respectively. Conclusion: The survey revealed reasonable prices and high availability in private sectors but in JanAushadhi Kendra, prices are flattened with good availability. The maximum applicable Goods and Services Tax rate is 12% for medicines under price control and life-saving drugs resulted in 2.3% increase in tax rate ultimately causing burden to patients. Government should ensure certain policies about importance of generic drugs and their availability in Jan Aushadhi Kendra.
Rajasekhar Pinnamaneni, Udaya Sri Puttagunta
International Journal of Pharmaceutical Investigation, Volume 12, pp 280-287; https://doi.org/10.5530/ijpi.2022.3.49

Abstract:
Background: Herbicides are classified either by toxicity or by mechanism of action, based on the chemical nature of the compound. Herbicides fall into two categories. Contact the herbicide and the transferred herbicide. Herbicides have been selected because they are highly toxic to plants and less toxic to animals and humans, but the main concern is the direct toxic effects of herbicides on animals. Since ketol acid reductoisomerase (KARI) is considered an acceptable target for most amide herbicides, this study conducted an in-silico analysis of KARI from Staphylococcus aureus against eight amide herbicides, obsessed with investigating by performing virtual molgro molecule docking. Materials and Methods: The ilvC gene encoding KARI from Staphylococcus aureus was amplified and its sequence and chimera were checked using the GenBank project`s CHIMERA CHECK program. It uses the BLAST algorithm and the GenBank database to compare the environment sequence with the GenBank sequence to find evolutionary relatives. Homology modeling of Staphylococcus aureus ketol acid reductoisomerase (KARI) was performed because its threedimensional structure revealed by either X-ray crystallography or NMR studies was not available. The generated model was used to repeat the energy minimization cycle many times using SPDBV software, and the final model was also used to perform docking analysis against the amide herbicide used in the inhibitor study. Results: The amplified DNA fragment containing 1005 base sequence BLAST hit, shows an absolute open reading frame encoding the Staphylococcus aureus protein KARI. PROSITE method shows active site residues Gln28, Leu79, Leu80, Asp82, Ala106, His107, Pro129, Lys130, Gly131, Pro132, Glu186, Asp190, Glu194, Cys199. The alignment of the protein sequence Ketol acid reductoisomerase (KARI) from Staphylococcus aureus and template >1NP3A had a chain length of 327. The three-dimensional structure of Staphylococcus aureus ketol acid reductoisomerase (KARI) was predicted using SPDBV. The generated model used SPDBV software to repeatedly repeat the energy minimization cycle, so the final model received a stereochemical evaluation. After energy minimization, the energy of the protein model is 1.10 KJ / mol, which fits the Ramachandran diagram. Docking studies of Staphylococcus aureus ketol acid reductoisomerase (KARI) were initiated using the inhibitors reported in the literature. This model was then used to dock to various ligands, amides that act as herbicides. In silico models have demonstrated that this enzyme is effective against amide herbicides. Conclusion: On the idea of the docking scores, these ligands (amide herbicides) were assigned the results of favorable interactions between the compounds, and therefore the situation of KARI to search out more impregnable candidates out of the screened ligands, optimization of those amides should be extended further.
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