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Fenugreek
Published in Dilip Ghosh, Prasad Thakurdesai, Fenugreek, 2022
Ujjwala Kandekar, Sunil Ramdasi, Prasad Thakurdesai
Solubility is an essential parameter for the dissolution and bioavailability of drugs (Patel and Jain 2014). The solubility of galactomannan depends on the pattern and degree of substitution of the galactosyl unit. The higher degree of galactose substitution in fenugreek offers a significantly higher number of hydroxyl groups resulting in enhanced binding with the water molecules. Similarly, mannose is a linear unit that shares properties like cellulose and insolubility in water (Mittal, Mattu, and Kaur 2016; Pollard and Fischer 2006; Prajapati, Jani, Moradiya, and Randeria 2013). Fenugreek gum exhibits an almost 1:1 ratio galactose to mannose with more galactose units. Therefore, fenugreek galactomannan’s solubility is higher than other galactomannans such as guar gum and locust bean gum (Izydorczyk, Cui, and Wang 2005). The solubility of the gums has a positive correlation with temperature. The higher molecular weight of galactomannan makes it solubilize at a higher temperature than the lower molecular weight galactomannans. Other factors affecting galactomannan solubility are particle size, pH, impurities, time spent, and dissolution media (Rodriguez-Canto et al. 2019).
Bioavailability and Granule Properties
Published in Dilip M. Parikh, Handbook of Pharmaceutical Granulation Technology, 2021
Drug dissolution is a prerequisite for drug absorption, which, in turn, influences the rate and extent at which the administered dose of a drug reaches the general circulation. For many drugs that cross intestinal mucosa easily, the onset of drug levels will be controlled by the time required for the dosage form to release its drug content and then for the drug to dissolve. Dissolution is a process by which a solid substance dissolves. As a fundamental property of a solid, it is controlled by the affinity between the solid and the liquid medium that surrounds it. The proliferation of interest in drug dissolution may be attributed, primarily, to drugs that tend to be very hydrophobic, because the rate-limiting step in the drug absorption process from the gastrointestinal tract is often drug dissolution from the solid dosage form. Approximately 40% of the compounds that enter the development phase fail to reach the market [8]. The main reason for failure is poor biopharmaceutical properties, which include low aqueous solubility, chemical instability, insufficient intestinal absorption, intestinal and/or hepatic metabolism, biliary excretion, and high systemic clearance. Even a highly potent compound can become not developable unless it manifests adequate pharmaceutical properties. For example, to be effective, an orally administered compound must be absorbable across the gastrointestinal mucosa. Consequently, a major challenge confronted by the medicinal chemists is the design of a potential therapeutic agent that exhibits desired physicochemical properties, including intestinal permeability.
Bayesian Methods for In Vitro Dissolution Drug Testing and Similarity Comparisons
Published in Emmanuel Lesaffre, Gianluca Baio, Bruno Boulanger, Bayesian Methods in Pharmaceutical Research, 2020
In harmony with the European and Japanese Pharmacopoeia, USP<711> describes the multi-stage testing that serves as a market standard for the expected quality of dissolution performance for many immediate or extended release drug products. USP<711> specifies the conditions for IV dissolution determination, such as dissolution medium and apparatus, gives the number of units to be tested, and places limits on the expected measurement results. IV dissolution measurements consist of the estimated amount of drug dissolved (usually expressed as a percent of the unit active ingredient label claim, %LC) as a function of time during agitation within a commercial dissolution apparatus. Rapidly dissolving or immediate release (IR) product units must generally exhibit a minimum % dissolution (referred to as Q) at some specified early time (e.g. 30 or 45 minutes) to assure adequate bioavailability. Extended release (ER) products generally have minimum and/or maximum % dissolution limits at an early, intermediate, and later time to assure the integrity of the release mechanism.
Methylprednisolone 100 mg tablet formulation with pea protein: experimental approaches over intestinal permeability and cytotoxicity
Published in Drug Development and Industrial Pharmacy, 2023
Erhan Koc, Fatih Ciftci, Hilal Calik, Seval Korkmaz, Rabia Cakir Koc
Dissolution testing is an important quality control measure used to ensure that tablets meet these requirements and that patients receive the expected therapeutic benefits from their medicines. The dissolution test assesses how quickly and to what extent a pharmaceutical dosage form, such as a tablet or capsule, forms a solution. For a drug to be bioavailable and therapeutically effective, it must dissolve. Dissolution rate is critical in determining the therapeutic efficacy, bioequivalence and bioavailability of active pharmaceutical ingredients in the early stages of drug development. The purpose of these tests is to assess the race and extent of dissolution of the API in gastrointestinal fluids, which is an important element in predicting its absorption and distribution in the body. As a result, dissolution testing is an important technique in the development of new drugs and generic versions of established drugs [30].
3D printing of immediate-release tablets containing olanzapine by filaments extrusion
Published in Drug Development and Industrial Pharmacy, 2021
Ukti Bhatt, Tushar Kanti Malakar, Upadhyayula Suryanarayana Murty, Subham Banerjee
In vitro drug release study from pristine olanzapine, olanzapine-Kollicoat IR physical mixtures (PMs), and olanzapine-loaded 3D printed IR tablet was performed using USP Type II paddle apparatus (DS8000, LabIndia Pvt. Ltd., Mumbai, India) at a wavelength of 250 nm using UV spectrophotometer (UV-2600, Shimadzu, Japan). 500 ml of Milli-Q water having pH 7.1 was taken as an experimental dissolution medium. The rotation speed of 50 rpm with a temperate set at 37 °C (±0.5) was maintained throughout the in vitro sink conditions. At a pre-determined interval of time, an aliquot of 2.0 ml samples was withdrawn, centrifuged to remove any undissolved particles (which may interfere in the analysis), and analyzed. Drug dissolution studies were conducted three times and the average percentage of cumulative drug release as a function of time was determined.
Development and characterization of lyophilized cefpodoxime proxetil-Pluronic® F127/polyvinylpyrrolidone K30 solid dispersions with improved dissolution and enhanced antibacterial activity
Published in Pharmaceutical Development and Technology, 2021
A considerable interest has recently been focused to the design of SD to enhance the solubility of poorly water-soluble active agents. SDs are described as the distribution of the active substance in a biologically inert carrier like a polymer, which prepared by different methods (Bikiaris 2011). The active agent may be molecularly distributed within the SD network, as in the case of solid solutions, or may be present in an amorphous or crystalline form. The improved dissolution rate of active agent from SDs is attributed to the combined effect of numerous pathways. Whether the active substance is molecularly distributed in the carrier or the drug is in an amorphous form, there is no energy is needed to break down the crystal structure and the dissolution of drug is much quicker. In the event of solid solutions, dissolution rate is calculated by dissolution rate of the carrier. Other mechanisms capable of improving the rate of drug dissolution involve reduction of particle size and decreased agglomeration, enhanced drug solubilization, and wettability with the carrier (Chiou and Riegelman 1971; Craig 2002).