International Journal of Pharmaceutical Sciences and Drug Research最新文献

{"title":"Preparation and Evaluation of Extended Release Trilayered Matrix Tablets of Ramipril Using Design of Experiment","authors":"K. Ashwin, T. R. Reddy, P. Nirmala","doi":"10.25004/ijpsdr.2021.130605","DOIUrl":"https://doi.org/10.25004/ijpsdr.2021.130605","url":null,"abstract":"The current work is aimed to design, prepare, and evaluate the trilayer matrix tablets incorporated with ramipril for extended drug release. Twenty-seven formulations (RF1-RF27) for active layer (middle layer) were prepared by direct compression method using 33 Response surface method of polymers of different HPMC K4M, HPMC K15M and xanthan gum (low, middle, and high concentrations) by using Design of experiment software. Based on physico-chemical properties and drug release one formulation was chosen and formulated into extended release trilayered matrix tablets were by varying proportions of polymers by direct compression method and they were evaluated. The best optimized formulation was characterized for FTIR studies. Out of 27 active layer formulations, RF23 was chosen as best based with maximum drug release of 98.11% and was formulated into extended release trilayered matrix tablets (ARF23-HRF23) by varying proportions of polymers. The range of swelling index for all batches (ARF23-HRF23) was 82.34 to 97.46%, similarly the range of drug content was 95.49 to 99.11% and drug released in 24 hours sustainably over an extended period was 84.98 to 98.26% with all highest values exhibited by GRF23. The release order kinetics data indicate the zero-order release with highest (R2) = 0.983 for GRF23 better when compared to marketed product which followed first order showed R2 value 0.962. Further the formulation (GRF23) showed best fit to Korsmeyer-Peppas plots i.e., 0.957 indicating non Fickian (anomalous) transport coupled diffusion and erosion. The FT-IR data assure the compatibilityof drug and excipients. GRF23 was found to be stable for 180 days at accelerated conditions.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":"45 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90491330","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"ANTIUROLITHIATIC ACTIVITY OF NATURAL CONSTITUENTS ISOLATED FROM AERVA LANATA FLOWERS","authors":"Subhashini Naikal James Prameela, Shilpika Nagula","doi":"10.25004/ijpsdr.2020.120610","DOIUrl":"https://doi.org/10.25004/ijpsdr.2020.120610","url":null,"abstract":"A well-known traditional herb Aerva lanata, broadly used in India for treatment of different ailments such as urolithiasis. Pashanabheda is used as antiurolithiatic in Ayurveda. In the present study, flowers of A. lanata were selected for isolation of active constituents and screening for in vitro antiurolithiatic potentials, as literature supports that flowers have the highest quantity of natural components when compared with the other parts. Hydroalcoholic (80%-water, 20%-alcohol) extract of A. lanata flowers was prepared and fractionation with different organic solvents.. The two fractions (ethyl acetate and n-butanol) were subjected to isolation of active constituents using column chromatography technique, followed by purification of the isolated constituents by preparative high performance thin layer chromatography (HPTLC)and then the individual components were characterized by IR spectrophotometery. Finally, in vitro antiurolithiatic activity was screened by nucleation and aggregation assay. In the aggregation assay, gradual decrease in the calcium oxalate (CaOx) crystal nucleation as well as growth was observed by light microscopy. The findings of the nucleation assay indicate that phytoconstituents inhibited the crystallization of CaOx in solution. The size and the number of calcium oxalate crystals decreased with increasing concentration of the phytoconstituents. The increasing concentrations of Quercetin and betulin (100, 200, 300, 400 and 500 μg/mL) inhibited the CaOx crystal growth. The isolated quercetin and betulin from A. lanata have shown antiurolithiatic effect by significantly reducing the CaOx crystal growth.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":"192 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78532369","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Formulation and Evaluation of Gliclazide Solid Dispersions Incorporated Tablets for Controlled Drug Release","authors":"R. Sunitha, K. Venugopal, S. Satyanarayana","doi":"10.25004/ijpsdr.2020.120606","DOIUrl":"https://doi.org/10.25004/ijpsdr.2020.120606","url":null,"abstract":"The current study deals with formulation and evaluation of gliclazide solid dispersion with HP β Cyclodextrin to enhance solubility and incorporate into tablet formulation for controlled release of gliclazide. Gliclazide solid dispersion (SD) prepared using varying ratios of HP β Cyclodextrin and evaluated. The optimized SD formulation incorporated into tablet by using hydroxypropyl cellulose, HPMC K 100M. The drug dissolution from tablet formulation analyzed and characterize. The formulation SD3 comprising of drug and polymer in 1:3 ratio displayed 43-fold increase in solubility when compared to pure drug. The formulation SD13 displayed maximum yield of 98.96% and maximum drug content of 99% chosen optimal for tablet formulation. FTIR studies revealed that there is no incompatibility between drug and polymers found. XRD studies revealed that the optimized solid dispersion formulation was found to be in amorphous state. Around 15 formulations of controlled release tablet blends evaluated for micrometric properties show that all the formulations posses’ good flow properties. Formulation F15 with maximum drug content of 99.99% and drug release of 99.96 % over 16h was chosen optimal and characterized. The release kinetics suggest that drug release followed zero order and release from tablets was anomalous non- fickian diffusion super case II transport. The results show that combination of solid dispersion and application of hydrophilic and hydrophobic polymers in matrix formation can facilitate better dissolution and absorption profile with greater patient compliance.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":"296 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"74414223","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Molecular-Docking Study of quinazolin-4(3H)-one derivatives against GABAa Receptor Signifies the Novel Approach to Epilepsy Treatment","authors":"Suraj G. Malpani, P. Mohanty, Ashish Jain","doi":"10.25004/ijpsdr.2020.120521","DOIUrl":"https://doi.org/10.25004/ijpsdr.2020.120521","url":null,"abstract":"Nowadays, a lot of new active substances as antiepileptic agents have been developed. One of the protein targets of antiepileptic is selective GABA. Selective GABA is the regulator of CNS activity. In this research, quinazolinone derivatives were used to design the antiepileptic agent through a selective GABA activation. The potential activity of quinazolinone derivatives could be increased by substitution in position 3 of quinazolinone. Molecular docking of selective GABA activation was required to predict their antiepileptic activity. The molecular docking of quinazolinone derivatives was carried out using Autodock viva Ver.1.1.2. Twenty quinazolinone derivatives were docked into GABAa with PDB code 4cof. The interaction was evaluated based on the docking score. Diazepam was used as the reference standard for this research. Twenty quinazolinone derivatives showed the approximate docking score -7.1 to -9.3 kcal/mol. All twenty quinazolinone derivatives which value that have greater docking score compared to diazepam used as a standard compound. Derivative Q-18 had higher binding energy than other quinazolinone derivatives because it has the smallest docking score. All new quinazolinone derivatives are feasible to be synthesize and performed their in vitro evaluation.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":"31 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85602898","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Stability-Indicating Method Development and Validation for Simultaneous Estimation of Ombitasvir, Paritaprevir, and Ritonavir in Formulation by Ultra Performance Liquid Chromatography","authors":"S. L. Maneka, R. T. Saravanakumar, A. Male","doi":"10.25004/ijpsdr.2020.120505","DOIUrl":"https://doi.org/10.25004/ijpsdr.2020.120505","url":null,"abstract":"Aim of the present research work was to develop a sensitive, precise and robust stability-indicating UPLC method for the simultaneous estimation of ombitasvir, paritaprevir and ritonavir in formulations. The chromatographic separation of mixture of ombitasvir, paritaprevir and ritonavir was attained in isocratic method utilizing a mobile phase of 0.01N Potassium dihydrogen orthophosphate (pH 5.3) and methanol in the proportion of 60:40%v/v utilizing a BEH C18 column which has dimensions of 100 x 3 mm, 1.7m particle size and the flow rate of 0.3 ml/min. The detection system was monitored at 252nm wavelength maximum with 0.2 ml injection volume. The retaining time for ombitasvir, paritaprevir and ritonavir was achieved at 1.765 min, 2.192 min, and 1.326 min respectively. Ombitasvir, paritaprevir and ritonavir and their combined drug formulation were exposed to thermal, acidic, oxidative, photolytic, and alkaline conditions. The present method was validated as per the guidelines given by the ICH for specificity, accuracy, sensitivity, linearity and precision. The developed method was highly sensitive, rapid, precise and accurate than the earlier reported methods. The total run time was decreased to 3.0 min; hence, the technique was more precise and economical. Stability studies directed for the suitability of the technique for degradation studies of ombitasvir, paritaprevir and ritonavir. The projected method can be utilized for routine analysis in quality control department in pharmaceutical trades.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":"99 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85904244","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fluidized Hot Melt Granulation Technique: An Approach to Improve Micromeritics Properties and Dissolution Rate of Efavirenz","authors":"D. J. Modi, P. Shelat, D. Shastri","doi":"10.25004/ijpsdr.2020.120518","DOIUrl":"https://doi.org/10.25004/ijpsdr.2020.120518","url":null,"abstract":"The Fluidized hot melt granulation technique is a process by which pharmaceutical powders are efficiently agglomerated using a low melting binder. The effect of the binder properties and concentrations on agglomerate growth mechanisms were studied in this research paper using this technique with the primary objective of improvement in the solubility and dissolution rate of efavirenz by melt-dispersion granulation employing meltable hydrophilic carrier and then to convert the melt dispersion into flowable and compressible dispersion granules to yield a rapidly dissolving tablet formulation. The Optimized concentrations of co-polymers like PEG 6000, PEG 4000, Gelucire 50/13, Gelucire 44/14, Poloxamer 188 and Poloxamer 407 in different ratios (i.e., 1:1, 1:2, 1:3 and 1:4) as meltable binder along with the drug were sprayed dropwise over lactose as diluent loaded into fluid bed chamber for the preparation of the granules of efavirenz and characterized for its micromeritical properties, DSC, XRD etc. The tablets prepared from the granules were evaluated for drug dissolution rate. The prepared granules were found to have excellent flow properties indicated by mean diameter D50:138µm, Carr’s index 13.92% and the drug content uniformity of 98.10%. XRD data exhibited partial loss of crystallinity as indicated by significantly less intensity of efavirenz peak in sample than pure efavirenz. Drug release from tablet was fast found 99.12% w/v within 30 minutes. Absence of Efavirenz endothermic peak at higher proportions of meltable binder reported by DSC data exhibited amorphous form of efavirenz led to complete solubilization and thus faster dissolution rate of efavirenz.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":"39 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88662386","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Fourier Transform Infrared and Chromatographic Fingerprint of Essential Oil from Pogostemon benghalensis (Burm. F.) Kuntze","authors":"P. Premakumari, Manoj Gopal Sarayu, M. Kumaraswamy","doi":"10.25004/ijpsdr.2020.120508","DOIUrl":"https://doi.org/10.25004/ijpsdr.2020.120508","url":null,"abstract":"The purpose of the present research work is to investigate the functional group and category of secondary metabolites present in the essential oil (Eo) from Pogostemon benghalensis using Fourier transform infrared (FTIR) spectrometry, HPTLC and GC-MS technique. FTIR measures the vibrations of bonds within the functional groups and yields a spectrum that can be considered as biochemical or metabolic fingerprint of the plant product. Using FTIR spectra, it is possible to find out the minor changes of primary and secondary metabolic characteristic functional groups which are responsible for their biological feature of the species. FTIR is a nondestructive, cost effective, user and eco-friendly tool. Pogostemon benghalensis, a wild relative of P. cablin, the highly utilized and adulterated medicinal herb by the native people for the extraction of essential oil Patchouli. The fresh leaves were subjected to hydro distillation for the extraction of the essential oils and were analyzed using the above techniques. The FTIR spectral lines have shown diverse unique peaks of functional groups. FTIR confirmed the volatile compounds and indicated by their functional groups of the essential oils such as C-H (Alkene), C-H (aromatic) and C=C. Similarly, the analysis proved the presence of alcohols, p-substituted alcohols or phenols, alkanes, alkynes, alkenes, aldehyde, ester, ether, aliphatic amines, carboxylic acids, aromatics, ketones, disulphide, alkyl halides, halogen, and nitro derivatives. The intensity and estimation of predominant volatiles were analysed by   HPTLC, which showed 8 peaks with max Rf values ranged from 0.07 to 0.96. Further, the Eo was fractionated by with GC-MS technique and identified 41 volatile fractions in the oil.  Thus, the obtained data provides the biochemical profiles with overlapping signals of a wide array of molecules that are present in the cells. So, the usage of essential oils in pharmacy, cosmetology and aromatherapy industries may be substantiated. Further advanced spectroscopic analysis is required to identify the structure and nature of active principles present in the Eo.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":"14 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90871467","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Computational studies of Vitexin isolated from Vitex negundo against Rheumatoid Arthritis targets","authors":"R. Devi, S. Bhagavathy","doi":"10.25004/ijpsdr.2020.120510","DOIUrl":"https://doi.org/10.25004/ijpsdr.2020.120510","url":null,"abstract":"One of the chronic inflammatory autoimmune diseases that need attention to be treated is Rheumatoid arthritis. Especially RA encounters more female cases manifests progressive destruction of bone and cartilage. Expression of more inflammatory cytokines and Matrix Metallo-Proteins at the synovial tissue destruct collagen structure and worsen the condition. Generally anti-inflammatory drugs and immune-modulatory agents are used to deduce the progression of disease. Such chemical entities have proven many side effects and expensive. This study provides a glimpse of structural based drug designing using bioactive pharmakon from a folk chloric herb. Vitex negundo is a traditionally available plant that has been reported to possess pharmaco-beneficiary bioactive flavonoids especially, vitexin. Virtual screening involves docking of vitexin with three different targets that is responsible for triggering collagenase enzyme was achieved using Autodock. Binding energy of vitexin and TNF α receptor1(TNFR1) was found to be slightly higher when compared to docking results of TNF α converting enzyme (TACE) and Human Inhibitory Kinase β (hIKβ) proteins. The molecular interactions were visualized using BIOVIA discovery studio visualizer. This study may evident that vitexin has enhanced pharmacological benefits that need to be ensured through in vitro and in vivo assays.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":"17 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91275644","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Validation of In-vitro Deposition of Emitted Dose Method for Simultaneous Estimation of Formoterol Fumarate and Glycopyrrolate in combined Dry Powder Inhaler Aerosol Pharmaceutical Dosage Form","authors":"R. Kotak, C. Pandya, A. C. Pandya","doi":"10.25004/ijpsdr.2020.120511","DOIUrl":"https://doi.org/10.25004/ijpsdr.2020.120511","url":null,"abstract":"Formoterol Fumarate and Glycopyrrolate Dry powder inhaler is combined aerosol dosage form. The label claim of this combined dosage form is 25 mcg of Glycopyrrolate and 6 mcg of Formoterol Fumarate per respicap. It is prescribed for treatment of Asthma and COPD. Formoterol Fumarate is anti asthmatic drug (Bronchodilator) and Glycopyrrolate is quaternary ammonium compounds which is Anticholinergic Drug. A bronchodilator is a substance that dilates the bronchi and bronchioles, decreasing resistance in the respiratory airway and increasing airflow to the lungs while Glycopyrrolate blocks muscarinic receptors thus inhibiting cholinergic transmission. Glycopyrrolate is also known as Glycopyrronium Bromide, an Anticholinergic agent. It is used to inhibit salivation and excessive secretions of the respiratory tract preoperatively; reversal of neuromuscular blockade; control of upper airway secretions; and part of treatment for peptic ulcer.  The present study aimed to Validate HPLC method for determination of Deposition of emitted dose of Formoterol Fumarate and Glycopyrrolate Analytes. This study covers Precision, Linearity, Accuracy, Robustness, Ruggedness, stability of analytical solution and Specificity.  The chromatographic method uses a reversed phase column Purosphere star RP 18e (125 mm × 4.6 mm x 5 μm). The mobile phase was prepared by mixing Buffer : Acetonitrile : Methanol (68 : 24 : 8 %v/v/v) at flow rate 1.0 ml per min with UV and PDA detector 215 nm, column oven adjusted to 25° C with injection volume 100 μL. The method showed a successful application for determination of Formoterol Fumarate and Glycopyrrolate in Dry powder inhaler pharmaceutical formulation.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":"11 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84891115","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

{"title":"Synthesis and Antidiabetic Evaluation of Some Novel Nitrogen containing Small Heterocyclic Derivatives","authors":"G. Kaur, Isha Rani","doi":"10.25004/ijpsdr.2020.120507","DOIUrl":"https://doi.org/10.25004/ijpsdr.2020.120507","url":null,"abstract":"This article describes the synthesis, characterization and antidiabetic evaluation of some derivatives containing thiazolidinedione. The titled derivatives 4a-4y have been prepared by the condensation of chlorosulphonyl-benzylidine 2,4-thiazolidinedione with thiadiazole derivatives formed by the reaction of aromatic acid and thiosemicarbazide. The finalization of the reaction was affirmed by TLC and the structures of the derivatives were characterized and analyzed through FT-IR, 1H-NMR and 13C-NMR, Mass spectroscopy. Alloxan induced diabetes and oral glucose tolerance tests were done to evaluate for the anti-diabetic profile of the synthesized derivatives. Furthermore, docking of the compounds was done using V Life MDS software. The Dock score of the test compounds was in good correlation with the pharmacological activity results. The electron withdrawing substituents added on the core structure were more potent inhibitors than others.","PeriodicalId":14278,"journal":{"name":"International Journal of Pharmaceutical Sciences and Drug Research","volume":"33 10","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"91482102","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}