Povećanje oslobađanja gliklazida iz smjesa dobivenih geometrijskim miješanjem

The poorly water soluble antidiabetic drug gliclazide was selected to study the effect of excipients on dissolution rate enhancement. Ordered mixtures of micronized gliclazide with lactose, mannitol, sorbitol, maltitol and sodium chloride were prepared by manual shaking of glass vials containing the drug and excipient(s). Different water soluble excipients, addition of surfactant and superdisintegrant, drug concentration and carrier particle size influenced the dissolution rate of the drug. Dissolution rate studies of the prepared ordered mixtures revealed an increase in drug dissolution with all water soluble excipients. The order of dissolution rate improvement for gliclazide was mannitol > lactose > maltitol > sorbitol > sodium chloride. Composite granules of the particle size range 355-710 µm were superior in increasing the drug dissolution rate from ordered mixtures. Reducing the carrier particle size decreased the dissolution rate of the drug, as well as the increase in drug concentration. Kinetic modeling of drug release data fitted best the Hixson-Crowell model, which indicates that all the ordered mixture formulations followed the cube root law fairly well.Teško topljivi antidijabetik gliklazid izabran je za proučavanje utjecaja pomoćnih tvari na povećanje oslobađanja. Homogene smjese mikroniziranog gliklazida s laktozom, manitolom, sorbitolom, maltitolom i natrijevim kloridom pripravljene su ručnim tresenjem staklenih bočica s lijekom i pomoćnom tvari/tvarima. Na oslobađanje lijeka utjecali su vrsta vodotopljivog ekscipijensa, dodatak surfaktanta i superdezintegratora, udio lijeka i veličina čestica punila. Sve vodotopljive pomoćne tvari povećavale su oslobađanje ljekovite tvari i to sljedećim redom: manitol > laktoza > maltitol > sorbitol > natrijev klorid. Najbolje oslobađanje lijeka bilo je iz kompozitnih granula veličine 355 do 710 µm. Iz smjesa s manjom veličinom čestica punila i većim udjelom lijeka oslobađanje lijeka bilo je manje. Kinetičko modeliranje oslobađanja najbolje je odgovaralo Hixson-Crowellovom modelu, što ukazuje na to da sve formulacije prilično dobro slijede zakon trećeg korijena

A REVIEW ON HYDROTROPY: A POTENTIAL APPROACH FOR THE SOLUBILITY ENHANCEMENT OF POORLY SOLUBLE DRUG: Jyoti Joshi, Nidhi Nainwal Sharma, Vikas Anand Saharan

Solubility is one of the significant parameters to accomplish wanted centralization of medication in foundational flow for pharmacological reaction to appear. Medication adequacy can be seriously constrained by poor watery dissolvability, and a few medications additionally show reactions because of their poor solvency. There are numerous strategies which are utilized to upgrade the fluid solvency. The capacity to increment watery solvency would thus be able to be a profitable guide to expanding proficiency as well as lessening reactions for specific medications. The ability to augment watery dissolvability would subsequently have the option to be a beneficial manual for extending capability just as diminishing responses for explicit medications. Therapeutic adequacy of a medication relies on the bioavailability and at last on the solvency of medication particles. Solvency is one of the significant parameters to accomplish wanted convergence of medication in fundamental course for pharmacological reaction to appear. Because of cutting edge inquire about and advancement, there are assortments of new medications and their subordinates are accessible. In any case, over 40% of lipophilic medication up-and-comers neglect to achieve showcase because of poor bioavailability, despite the fact that these medications may display potential pharmacodynamic exercises. The lipophilic medication that achieves market requires a high portion to accomplish appropriate pharmacological activity. Hydrotropy is one of the solvency improvement methods which upgrade dissolvability to numerous folds with utilization of hydrotropes such as sodium benzoate, sodium citrate, urea, niacinamide, and so forth and have numerous focal points as, it does not require substance alteration of hydrophobic medications, utilization of natural solvents, or readiness of emulsion framework and so forth

Phytosome: Drug Delivery System for Polyphenolic Phytoconstituents: Phytosome

Several plant extracts and phytoconstituents, despite having excellent bioactivity in vitro, demonstrate less or no in vivo actions due to their poor lipid solubility or improper molecular size or destruction in gut. Drug delivery system for polyphenolic phytoconstituents (phytosomes) was prepared by complexing polyphenolic phyto phytoconstituents (phytosomes) was prepared by complexing polyphenolic phyto to each other on a molecular level. Bioavailability is enhanced due to their capacity to each other on a molecular level. Bioavailability is enhanced due to their capacity to each other on a molecular level. Bioavailability is enhanced due to their capacity have the capacity to deliver the standardized plant extracts and phytoconstituents through several routes of drug administration. Only a few natural drugs have been through several routes of drug administration. Only a few natural drugs have been applications of phytosomes numerous studies are undergoing and lots more is expected in the forthcoming years. The techniques used for such formulations are expected in the forthcoming years. The techniques used for such formulations are patentable and highly profitable

Strychnos nux-vomica seeds: Pharmacognostical standardization, extraction, and antidiabetic activity

Background: Strychnos nux-vomica, commonly known as kuchla, contains strychnine and brucine as main constituents. Minor alkaloids present in the seeds are protostrychnine, vomicine, n-oxystrychnine, pseudostrychnine, isostrychnine, chlorogenic acid, and a glycoside. Seeds are used traditionally to treat diabetes, asthma, aphrodisiac and to improve appetite. Objective: The present study was aimed to evaluate the various pharmacognostical characters and antidiabetic activity of S. nux-vomica seed. Materials and Methods: Pharmacognostical characters were performed as per the WHO guideline. Extraction was carried out in petroleum ether, chloroform, alcohol, hydroalcoholic, aqueous, and phytochemical constituents present in extracts were detected by different chemical tests. Among these extracts hydroalcoholic, aqueous extracts were evaluated for antidiabetic activity on the basis of extractive yield and phytoconstituents, in alloxan-induced diabetic rats using gliclazide as standard. Results: Various analytical values of S. nux-vomica extract were established. Phytoconstituents present in S. nux-vomica extracts were detected. Conclusion: S. nux-vomica extracts show antihyperglycemic activity in experimental animals

A review on the clean-up technologies for heavy metal ions contaminated soil samples

The soil contamination with heavy metal ions is one of the grave intricacies faced worldwide over the last few decades by the virtue of rapid industrialization, human negligence and greed. Heavy metal ions are quite toxic even at low concentration a swell as non-biodegradable in nature. Their bioaccumulation in the human body leads to several chronic and persistent diseases such as lung cancer, nervous system break down, respiratory problems and renal damage etc. In addition to this, the increased concentration of these metal ions in soil, beyond the permissible limits, makes the soil unfit for further agricultural use. Hence it is our necessity, to monitor the concentration of these metal ions in the soil and water bodies and adopt some better technologies to eradicate them fully. From the literature survey, it was observed that three main types of techniques viz. physical, chemical, and biological were employed to harness the heavy metal ions from metal-polluted soil samples. The main goal of these techniques was the complete removal of the metal ions or the transformation of them into less hazardous and toxic forms. Further the selection of the remediation technology depends upon different factors such as process feasibility/mechanism of the process applied, nature and type of contaminants, type and content of the soil, etc. In this review article, we have studied in detail all the three technologies viz. physical, chemical and biological with their sub-parts, mechanism, pictures, advantages and disadvantages

A Clinical Insight on New Discovered Molecules and Repurposed Drugs for the Treatment of COVID-19

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) began churning out incredulous terror in December 2019. Within several months from its first detection in Wuhan, SARS-CoV-2 spread to the rest of the world through droplet infection, making it a pandemic situation and a healthcare emergency across the globe. The available treatment of COVID-19 was only symptomatic as the disease was new and no approved drug or vaccine was available. Another challenge with COVID-19 was the continuous mutation of the SARS-CoV-2 virus. Some repurposed drugs, such as hydroxychloroquine, chloroquine, and remdesivir, received emergency use authorization in various countries, but their clinical use is compromised with either severe and fatal adverse effects or nonavailability of sufficient clinical data. Molnupiravir was the first molecule approved for the treatment of COVID-19, followed by Paxlovid™, monoclonal antibodies (MAbs), and others. New molecules have variable therapeutic efficacy against different variants or strains of SARS-CoV-2, which require further investigations. The aim of this review is to provide in-depth information on new molecules and repurposed drugs with emphasis on their general description, mechanism of action (MOA), correlates of protection, dose and dosage form, route of administration, clinical trials, regulatory approval, and marketing authorizations

A Clinical Insight on New Discovered Molecules and Repurposed Drugs for the Treatment of COVID-19

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) began churning out incredulous terror in December 2019. Within several months from its first detection in Wuhan, SARS-CoV-2 spread to the rest of the world through droplet infection, making it a pandemic situation and a healthcare emergency across the globe. The available treatment of COVID-19 was only symptomatic as the disease was new and no approved drug or vaccine was available. Another challenge with COVID-19 was the continuous mutation of the SARS-CoV-2 virus. Some repurposed drugs, such as hydroxychloroquine, chloroquine, and remdesivir, received emergency use authorization in various countries, but their clinical use is compromised with either severe and fatal adverse effects or nonavailability of sufficient clinical data. Molnupiravir was the first molecule approved for the treatment of COVID-19, followed by Paxlovid™, monoclonal antibodies (MAbs), and others. New molecules have variable therapeutic efficacy against different variants or strains of SARS-CoV-2, which require further investigations. The aim of this review is to provide in-depth information on new molecules and repurposed drugs with emphasis on their general description, mechanism of action (MOA), correlates of protection, dose and dosage form, route of administration, clinical trials, regulatory approval, and marketing authorizations