Solubility Enhancement Of Fenofibrate By Solid Dispersion Technique

Pharmaceutical scientists have to account for multiple properties when developing new drugs, and they need to understand what could affect different patients when developing these drugs. Solubility is one of these properties, and it is the ability of a solid, liquid, or gaseous substance to dissolve in a solid, liquid or gaseous solvent, and it is critical to absorption into the body. In drug discovery over the years, the number of insoluble drug candidates has increased recently, with almost 70% of new drug candidates showing poor water solubility.

Which brand of painkilling medicine dissolves the fastest and does flavor, coating, and color of the pill affect the dissolution time? If several different pain neutralizing pills are placed in stomach acid and timed in order to find out which pill dissolves first, then the most effective pill will be the first to dissolve. In order to test this, eight different types of pain neutralizing medicine were put into simulated stomach acid and timed. Normal strength, liquid gel capsules, and children's flavored pills were all tested. In order to accurately simulate stomach acid, vinegar, which has the same pH levels of stomach acid, was heated to thirty seven degrees Celsius and stirred constantly and evenly. The pills tested were Advil, Children's

Continually, the solution was allow to cool down, before it was reheated to dissolve the solid. The solution stood undisturbed until crystals were formed. Solubility tests were performed on all possible solvent-solute pairings. The most efficient pair was

For example, in some alkaline solvents acidic products will become deprotonated, keeping them soluble in water. The target compound can then be extracted as a free base. The extract results then are isolated by the addition of two immiscible solvents. Two solvents that cannot be mixed are used so that there is a clear separation between the aqueous and organic layer. The component needed for extraction is contained in the organic layer. This is because the compound is more soluble to the composition of the organic layer.

Proposed mode of action for RIS (benzisoxazole derivative) is blocking of 5-HT2A and dopamine D2 receptors. Despite of its potential, RIS is reported to have higher log P value along with poor water solubility and is classified as biopharmaceutical classification system (BCS) class II drug [6]. This poor water solubility leads to limited oral bioavailability through gastrointestinal tract as well as by parenteral route and limits the use of aforementioned drug candidate [4]. Various solubility enhancement techniques can be used to enhance apparent solubility of BCS class II drugs such as salt formation, solid state modification, use of co-solvents, hydro-trophy, complexation with cyclodextrins size reduction etc. Researchers have reported solid dispersion [7], self-nano-emulsifying powder [8] and co-solvent [9] approach for enhancement of RIS water solubility. Use of sodium lauryl sulphate (SLS) in marketed formulation (Risperdal®) of drug presents the probability of solubility enhancement with the use of surfactant [10]. All these approaches have their own advantages and limitations like toxicity issues associated with use of co-solvents [11] (generally water miscible organic solvents) and surfactants beyond a particular level

The purpose of this investigation is to find out if the coating on pills makes it harder to dissolve.

There are many different types of pills that humans use for various reasons, and each one is designed to cure or contain a certain problem or pain. This form of medication is usually compacted in a small tablet, sometimes with a coating on top, and meant for the user to swallow as a whole without allowing it to dissolve before entering the stomach. However, considering that people seem to want the fastest relief possible that they can get from their bodily ailments, the research question of this experiment was: Which class of pills dissolve the fastest?

"Absorption depends on the drug’s ability to cross cell membranes and resist extensive breakdown by the stomach, liver, and intestines.

This experiment investigates the effect of stomach acid at different pH levels on the solubility of metformin hydrochloride tablets. According to my results, the metformin hydrochloride tablets dissolved at a faster rate in the simulated stomach acid with less alcohol, and therefore, more acidic. This conclusion, proves the hypothesis stated above. As predicted, the simulated acid with less traces of alcohol was a more suitable environment for the medicine to dissolve at a faster rate. Consequently, the tablets took a longer time to dissolve in the acid with a greater concentration of alcohol. In consideration of the uncertainties, the two graphs above show that as the pH level increases and becomes more basic, the amount of time for the tablets

The most commonly used water miscible cosolvents are polyethylene glycol 300 and 400, propylene glycol, ethanol, glycerin, dimethylacetamide (DMA), N-Methyl-2-pyrrolidone (NMP), dimethylsulfoxide. Yalkowsky, S.H. et al studied effect of cosolvents on solubility of cyclosporin A in presence of propylene glycol, poly ethylene glycol, tetra hydro furfuryl alcohol, glycerine, ethanol [31]. Poly ethylene glycol 400, Propylene glycol, Ethanol has been used as co solvent for increasing solubility of Ibuprofen [35]. Poly ethylene glycol 400, water can be used as co solvent to enhance the solubility of Valdecoxib [36]. Solubility of carbendazim can be increased by using cosolvents poly ethylene glycol 400, propylene glycol, glycerine, and ethanol

Review the four factors of dissolving you have just investigated. Given the correct solvent for a solute, what could you do to hasten the solution process?

Maheshwarihave proposed the concept of mixed solvency. His opinion is that all substances whether liquids, gases or solids is solubilizing powder and hence concentrated aqueous solution containing various dissolved substances can also improve the solubility of poorly water soluble drugs. Melted (temperature less than 100 ºC), PEG 400, PEG 6000 and PEG 8000 dissolves diclofenac sodium (melting point: 283 ºC). This also shows that melted PEGs act as solvent for diclofenac sodium. Melted urea (M.P.: 132-135 ºC) dissolves diclofenac sodium (M.P.: 283ºC). This shows that melted urea act as solvent for diclofenac sodium. Melted ibuprofen (M.P.:78ºC) dissolves diclofenac sodium (M.P.:283ºC), salicylic acid (M.P.:159ºC) and niacinamide(M.P.:132ºC), which another time shows that melted ibuprofen act as solvent for diclofenac sodium, salicylic acid and niacinamide respectively.In supercritical fluid technology

Oral drug delivery is the simplest and easiest way of administering drugs, Because of the greater stability, smaller bulk, accurate dosage and easy production, solid oral dosages forms have many advantages over other types of oral dosage forms. Therefore, most of the new chemical entities (NCE) under development these days are intended to be used as a solid dosage form that originate an

A native conformation of protein is only marginally stable than unfolded states, and most of proteins are prone to aggregate in liquid state to form non-native supra structures. The loss of unique globular structures and aggregation of proteins are problematic in biopharmaceutical formulations due to the reduction of therapeutic potency and the possibility of inducing undesired immune responses[1]. For several decades, it has been pursued to develop formulation methods of preserving the protein stability. One of effective way to improve protein stability is mixing cosolvents in protein-water system[2, 3]. The present of excipient molecules such as salts, carbohydrates, amino acids, and surfactants change the equilibrium of protein denaturation and aggregation[4-10]. A great interest has been raised in understanding of the effects of excipients on proteins in an effort to find ideal formulation recipes[11].

The purpose of writing this review was to investigate, compile, recent, current and past literatures. In recent years several advancements has been made in research and development of oral drug delivery system. Various drugs, which are unstable in alkaline pH, soluble in acidic pH, having narrow absorption window, site of action specific to stomach can be developed by using this technique. Gastro-retentive drug delivery systems (GRDDS) can improve the controlled delivery of drugs that have an absorption window by continuously releasing the drug for a prolonged period of time before it reaches to absorption site. These include floating system, swelling system, expanding system, low density systems, high density system, bioadhesive and mucoadhesive systems etc. In fact the buoyant dosage unit enhances gastric residence time (GRT) without affecting the intrinsic rate of emptying. GRDDS is an approach to prolong gastric residence time, thereby targeting site-specific drug release in upper gastro intestinal tract improving the oral sustained delivery of drug. For minimizing the limitations and achieving better gastric retention various combinational approaches floating and swelling, floating and bio-adhesion, etc., multi-particulate systems, super porous hydrogel etc., have been discussed. The present review addresses briefly about suitable drug candidates, formulation considerations, physiological difficulties and classification, factors effecting gastric retention, merits,