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Journal of Applied Pharmaceutical Research
Published by Creative Pharma Assent
ISSN : -     EISSN : 23480335     DOI : 10.18231
Core Subject : Health,
Medicine & Pharmacology
Journal of Applied Pharmaceutical Research (JOAPR) is an official publication of Creative Pharma Assent (CPA). It is an open access, peer review online international journal. JOAPR is primarily focused on multiple discipline of pharmaceutical sciences (Pharmaceutics, Pharmaceutical Technology, Biopharmaceutics, Cosmetic Technology, Pharmacokinetics, Pharmaceutical/Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Pharmacognosy and Phytochemistry, Herbal drugs/ formulations, Pharmacology, Pharmaceutical Analysis, Pharmacy Practice, Clinical and Hospital Pharmacy, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics and Biotechnology of Pharmaceutical Interest) which publish quarterly. JOAPR also includes evaluation of pharmaceutical excipients & their practical application to research & industry based efforts. The aim of the scientific journal, JOAPR is to present a wide area for the current researchers to share their noble works and ideas in terms of the research papers, review articles and short communications. JOAPR only publish the original research works with a definite innovation and novelty after thorough reviewing. The paper must have a suitable and proper scientific background.
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Articles 14 Documents
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Search results for , issue "Vol. 12 No. 4 (2024)" : 14 Documents clear
Quantification of oteseconazole in rat plasma using LC-MS/MS and its application to pharmacokinetic study Susararla, Krishna Phani Chandra; Shelke, Om; Shorgar, Neetu
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.485

Abstract

Background: Oteseconazole is a new molecule launched for human treatment. However, the information is not available in the public domain for analyzing blood samples. This study describes the method development and validation using LC-MS/MS to measure the concentration of Oteseconazole in rat plasma. Methodology: The analysis method was developed using a phenyl column, which was utilized to accomplish separation. Furthermore, the mobile phase was a combination of acetonitrile and 0.1% formic acid in water, with a ratio of 30:70 (v/v). The sample was introduced into the system at a 1.0 mL/min flow rate, and the injection volume was 10 μLand analyzed for five minutes using mass spectrometer +ESI mode. Results and discussion: MRM is used to quantify Oteseconazole and Posaconazole by analyzing the transitions of their respective m/z values. The concentration ranges of Oteseconazole were 5-100 ng/mL. The correlation coefficient of Oteseconazole was found to be 0. 999. HQC, MQC, LQC, and LLQC precision and accuracy were determined to be 98.60%, 98.69%, 96.11%, and 94.48%, respectively. Respectively, the accuracy recovery of Oteseconazole was determined to be 97.48%. In pharmacokinetic studies, it was observed that Oteseconazole exhibited an average AUC0-t value of 1386 ng-hr/ml and a Cmax value of 44.864 ng/ml in rats. Conclusion: The validated approach has effectively demonstrated the determination of pharmacokinetic parameters after the oral administration of Oteseconazole in Wister rats.
Formulation and evaluation of ointment containing hydroalcoholic extract derived from the bark of Moringa oleifera for wound healing activity in rat model Sahu, Himanshu; Satapathy, Trilochan; Chandrakar, Shashikant; Gupta, Puahpa Prasad; Sahu, Poonam; Sahu, Akhilesh
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.556

Abstract

Background: This study aimed to assess the effectiveness of a hydroalcoholic extract derived from the bark of Moringa oleifera in facilitating the healing process of second-degree burns wounds. Moreover, a comprehensive assessment was carried out on standardized M. oleifera bark to ascertain its physiochemical characteristics, botanical compound layout, and antioxidant activity, all of which play a crucial role in its capacity to facilitate the healing process of burns. Methods: For 14 days, the efficacy of ointments containing a hydroalcoholic extract of M. oleifera bark at concentrations of 5% and 10% was evaluated for treating second-degree burns in rats. Additionally, histological analysis was conducted on skin tissue samples. Results: The M. oleifera bark extract exhibited TPC (52.56 mg/gm of dried extract) and TFC (84.33 mg/gm of dried extract) value along with antioxidant activity (IC50 value of 0.98 µg/ml) for radical scavenging, in the presence of several phytochemicals. The most favorable outcomes were achieved using a 10% ointment composition, demonstrating a wound closure and tissue repair rate of 83.04 ± 0.89%, along with a noteworthy decrease in tissue oxidative stress indicators. Histological investigations have verified the wound-healing properties of M. oleifera bark extract. Conclusion: Due to its significant antioxidant properties and its capacity to create a moist environment for wounds, M. oleifera has the potential to serve as a natural treatment for burns. Additional clinical trials are recommended to validate the efficacy of M. oleifera bark extract as a therapeutic agent for wound healing.
Treatment with Terminalia chebula (retz.): possible mechanism of inhibition of spermatogenesis and fertility in albino mice Gupta, Prakash Chandra; Yadav, Laxmi
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.570

Abstract

Background: There has been a continued effort to develop an effective male contraceptive of plant origin due to its ready availability, cost-effectiveness, and fewer side effects.  The present study has evaluated the mechanism of inhibitory action of Terminalia chebula Retz. (T. chebula; family: Combretaceae) on spermatogenesis and fertility in albino mice after oral administration of the aqueous bark extract (100, 300, and 500 mg/kg BW daily) of T. chebula for 35 d. Methodology: The effects of the Terminalia treatment on various reproductive endpoints such as sperm parameters, testis histology, activities of 3ß- and 17ß-HSDs, immunoblot expressions of StAR and AR proteins, immunostaining of AR, serum testosterone level, LPO level, activities of SOD and catalase, and fertility indices were investigated. Toxicological and recovery studies have also been performed. Results: Testes in Terminalia-treated mice showed nonuniform histologic alterations. Sperm parameters, activities of 3ß- and 17ß-HSDs, immunoblot expressions of StAR and AR proteins, immunostaining of AR, and serum testosterone level were adversely affected, though activities of SOD and catalase were unchanged. Libido remained unaffected, but fertility was inhibited markedly in treated males without signs of toxicity. By 42 d of treatment discontinuation, Terminalia-induced deviations in the reproductive endpoints recovered to control levels. Conclusion: The results of the present study indicate that T. chebula treatment reversibly inhibits spermatogenesis and fertility without signs of toxicity. Further, antifertility effects result from diminished production of testosterone due to Terminalia-mediated inhibition of testicular steroidogenesis.
Formulation and in-vitro anticancer activity of nilotinib immediate release and ibrutinib sustained release pellets Gupta, Vishal; Gupta, Jitendra
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.571

Abstract

Background: Blood cancer is a significant contributor to mortality rates worldwide, and its prevalence is projected to rise on a global scale. This trend places considerable strain on healthcare systems and necessitates the expedited development of innovative treatments by pharmaceutical firms to remain competitive. Conventional pellets produce rapid plasma drug levels, but they might cause side effects, decrease effectiveness, and lead to poor therapeutic management. Ibrutinib and Nilotinib are employed to treat leukemia patients. Methodology: The current research aims to formulate, characterize, and anticancer effect of Nilotinib immediate release (NIR) and Ibrutinib sustained release (ISR) seal sugar-coated pellets. Micrometric properties estimated the characterization of the drug pellets, and surface morphology was estimated using scanning electron microscopy. Drug excipient compatibility studies, stability studies, and in-vitro drug release were accessed. Result & Discussion: The results of pellet formulations FNI-1 to FNI-5 showed that FNI-5 formulations showed 100±6.0 µm size and possessed excellent mechanical strength for giving pellets a good self-life; also, due to the higher drug content up to 99%, FNI-5 was the best suited for pellet formulation and because NIR showed 99.18 ± 2.12 drug release at 2h and ISR 99.03±3.74% up to 12h so that anticancer concentration maintained for prolonged period. The standard dose for cytotoxicity against the THP-1 cell line of Nilotinib was found to be 200 mg, and the maintenance oral dose of Ibrutinib was 140mg, with four times the intake of the drug up to 560 mg.  In an in vitro study in FNI-5 (final formulation), the dose of Ibrutinib was reduced to 420 mg. Conclusion: A synergistic effect of Ibrutinib and nilotinib drugs was observed in the inhibition of cancer cell growth, with an IC50 value of 4.585 µg/mL
An update on phytoconstituents and pharmacological importance of Asparagus racemosus Meher, Deepak; Singh , Mithlesh; Meher , Bibekananda
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.588

Abstract

Background: Asparagus racemosus (family: Liliaceae), is a well-researched traditional or ancient medicine in the Siddha, Ayurveda, and Unani systems. It is commonly known as Satawar, Satamuli, Satavari, and found at low altitudes throughout India. It contains bioactive metabolites such as fructo-oligosaccharides, polysaccharides, asparosides, shatavarins, sapogenins, racemosols, isoflavones, glycosides, mucilage, and fatty acids, while saponin is one of the main active constituents of asparagus. Objective: Across the globe, Asparagus racemosus gained importance for its ethano-pharmacological value in curing various ailments. This review will outline the medicinal properties, uses, and value addition of Asparagus racemosus. Methods: We have reviewed and retrieved the relevant information by probing the main keywords in online databases (PubMed, Scopus, Science Direct and Web of Science, etc.). Screening of relevant abstracts/ title and full papers were done to pick the suitable content based on the pharmacological profile of Asparagus racemosus. Conclusion: The whole plant possesses pleiotropic therapeutic activity, antioxidant, anti-inflammatory, immunomodulatory, neuroprotective, nootropic, antidepressant, etc., without showing any remarkable side effects. It also treats stomach ulcers, diabetes, kidney disorders, and Alzheimer's disease, etc.
Formulation and development of bilayer tablet containing irbesartan and metformin hydrochloride for diabetic hypertensive patients Gorde, V D; Rachh, Punit R; Mankar, Someshwar; Amin, Saurin; Gorde, Prasad L
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.589

Abstract

Background: Hypertension is a common complication of type II diabetes. The present research work aimed to develop bilayer tablets that would manage type II diabetes patients with hypertension. The prepared bilayer tablet has an immediate-release layer of anti-hypertensive irbesartan and a sustained-release (SR) layer of anti-diabetic metformin hydrochloride. The purpose of these bilayer tablets was to increase patient compliance by converting two separate monotherapy to single combination therapy. Methodology: Several ratios of polymers, including HPMC K100M, EC, Eudragit, and Guar gum, were employed to prolong the drug release for twelve hours. An immediate-release layer of irbesartan was prepared by spherical agglomeration. The physical properties, drug content, solubility profiles, release kinetics, and stability of prepared bilayer tablets were assessed. Results and Discussion: The examination of SR granules and bilayer tablets revealed outstanding packing qualities and excellent flow properties, with bulk and tapped densities ranging from 0.39-0.46 g/cm³ and 0.42-0.55 g/cm³, respectively. In vitro dissolution tests revealed that the immediate-release layer gave an initial burst of Irbesartan. Still, the sustained-release layer of metformin showed controlled drug release over 12 hours at greater polymer concentrations. According to stability testing, the bilayer tablets' physical properties, drug content, and dissolving profiles did not change significantly. Conclusion: The bilayer tablet combination of Irbesartan and Metformin exhibited desired physical features, controlled drug release, and stability. This formulation represents a viable treatment option for diabetic hypertensive patients, offering effective and consistent management of both disorders while improving patient compliance.
Optimization and evaluation of nebivolol hydrochloride loaded transferosomes using Box-Behnken experimental design Shelke, P V; Rachh, Punit R; Mankar, Someshwar; Amin, Saurin; Jain, Deepak
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.590

Abstract

Background: This study optimizes and evaluates transferosomes containing Nebivolol Hydrochloride to enhance the drug's bioavailability and therapeutic efficacy. Ultra-deformable vesicles called transferosomes help to increase drug administration via the skin. Methodology: Using a thin-film hydration technique, beta-blocker Nebivolol Hydrochloride, which has antihypertensive properties, was added to transferosomes. To attain the ideal vesicle size (between 200 to 300 nm), entrapment efficiency, and deformability, the formulation was adjusted by adjusting the amounts of phosphatidylcholine, Span 80, and hydration time using a Box-Behnken experimental design. Particle size analysis, zeta potential measurement, and in vitro drug release tests were performed to characterize the transferosomes. Results and discussion: The optimized formulation demonstrated notable deformability, an entrapment effectiveness of 50%, and a vesicle size of 265 nm. The Box-Behnken design made it easier to evaluate the interactions between variables systematically. In vitro drug release studies showed a drug diffusion that persisted for a whole day, suggesting that transferosomes may have long-lasting therapeutic effects. Stability studies at room temperature and accelerated conditions over six months confirmed the formulation's robustness. Conclusion: The results imply that Nebivolol Hydrochloride transferosome-based delivery may be a viable strategy for improving the drug's bioavailability and effectiveness, as nearly 100% of drugs diffuse within 24 hr, perhaps leading to a breakthrough in the management of hypertension.
Pharmaceutical development of etodolac transfersomal gel for topical drug delivery system in rheumatoid arthritis Bachhav, Ashwini; Pingale, Prashant L; Upasani, Chandrashekhar D
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.597

Abstract

Background: Transferosomes provide delivery of the drug into systemic circulation via the skin as a topical delivery system. So, this study started with the objective of formulating Etodolac transfersomal gel to enhance its skin permeation. Methodology: A total of nine transferosomes (ET-1 to ET-9) containing lecithin, different grades of span and tween, were successfully prepared using a rotary film evaporator. Results and Discussion: After primary evaluation, results were as particle sizes ranged from 222 to 421 nm, zeta potential shows results from –18.50 to –62.53 mV with PDI values 0.254 to 0.303, and the entrapment efficiency (EE%) of Etodolac in the transferosomes ranged from 54.15% to 80.25%. Additionally, the transfersomes formulations were included in carbopol 940 gels (ETC-1 to ETC-9 and EC-0 without transferosomes) and assessed for various characteristics like color, pH, homogeneity, spreadability, viscosity, and in vitro drug release study. Optimized formulation (ET4 and ETC4) underwent further analysis using SEM, TEM, DSC, FTIR, XRD, ex vivo skin permeation, skin irritation and in vivo studies. The in vivo results were compared. % edema inhibition maximum was observed with optimized transfersomal gel formulation (ETC4) as compared to the marketed formulation and plain Carbopol gel when the study was completed after 8 hrs. Conclusion: After this research, it is suggested that Etodolac Transfersomal gel (ETC4) can be considered as an alternate drug carriers system for topical delivery and it could be used to treat Rheumatoid Arthritis
Solubility enhancement of etoricoxib using inclusion complexation with cyclodextrins: formulation of oro dispersible tablets by QbD approach Mahapatra, Anjan Kumar; Dora, Siddharth; Parida, Sanatan; Bal, Usharani; Jena, Bandana Rani; Lenka, Madhusmita
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.603

Abstract

Background: The work was intended to enhance etoricoxib's solubility and dissolution rate and then develop oro-dispersible tablets for faster onset of action. Methodology: Inclusion complexes (ICs) of the drug were obtained with β-cyclodextrin (β-CD) and hydroxypropyl β-cyclodextrin (HP β-CD) at ratios of 1:0.125, 1:0.25, 1:0.5, 1:1, and 1:2 (w/w). The selected cyclodextrin at appropriate drug carrier proportion was used to develop oro-dispersible tablets (ODTs) by direct compression, adding crospovidone as a super disintegrant. Phase solubility studies of etoricoxib were carried out by using multiple concentrations of β-cyclodextrin and hydroxypropyl β-cyclodextrin, i.e., 1 %, 2 %, 3 % w/v in distilled water at 37±2°C. Spectroscopic (FT-IR) and thermal analysis (DSC) techniques were employed to identify the drug-carrier interactions. Result: It showed that etoricoxib solubility improves with increasing hydrophilic carrier concentration. The Gibbs free energy values (ΔG˚tr) are consistently negative, showing the solubility of etoricoxib. Significant drug carrier interaction in spectroscopic or thermal analysis was not found. Discussion: The ICs of drugs with β-CD and HP β-CD have successfully addressed the challenges of solubility enhancement and taste masking for etoricoxib. Conclusions: It is observed that the inclusion complexes formed by the kneading method using β-cyclodextrin (β-CD) at a 1:1 ratio and hydroxypropyl β-cyclodextrin (HP β-CD) at a 1:2 ratio can be used to improve dissolution. Hence β-CD (at a 1:1 ratio) is selected for the formulation of oro-dispersible tablets. ODTs offer more patient compliance and an alternative to available conventional tablets.
Bioanalytical method for the simultaneous estimation of atoltivimab, maftivimab and odesivimab in rat plasma by LCMS/MS and its application to a pharmacokinetic study Syed, Ibrahim Baje; Nannapaneni, Madhavi
Journal of Applied Pharmaceutical Research Vol. 12 No. 4 (2024)
Publisher : Creative Pharma Assent

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.69857/joapr.v12i4.607

Abstract

Background: A quick, accurate, reproducible, and straightforward liquid chromatography-tandem mass spectrometry(LC-MS/MS) system employing Atoltavimab, Maftivimab, and Odesivimab as an internal standard for Zanamivir quantification was achieved. Zanamivir is a neuraminidase inhibitor that effectively treats influenza caused by influenza A and B viruses. Methodology: Whenever we use the Kinetex C-18 column, all HPLC parameters and conditions are obeyed, so we use this column. Separation was performed on a Kinetex C18 column (100 mm x 4.6 mm, 2.6µm) using isocratic elution with a buffer containing 1mL of formic acid in 1Lit of water and a mobile step consisting of a 40:60 v/v mixture of two elements, buffer and acetonitrile, with a flow rate of 1mL/min at 300C temperature was used. Results & Discussion: We used different stationary phases in the optimization process, such as C18, C8, and CN-propyl. Using a kinetex C18 column with dimensions of (100 mm x 4.6 mm, 2.6 µm) connected to a PDA detector, we obtain strong peak shapes of Atoltivimab, Maftivimab, and Odesivimab from various trials. Flow rates in the mobile process were set to 1 mL/min. Conclusion: Atoltivimab, Maftivimab, and Odesivimab analysis was completed in 7 minutes over a good linear concentration range of 5ng/mL to 100ng/mL (r2 = 0.999), 5ng/mL to 100ng/mL (r2 = 0.999), and 5ng/mL to 100ng/mL (r2 = 0.9998). The findings of the precision and recovery studies are within the appropriate range.

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