Solid dispersion (SD) formulation has attracted much attention due to its potential in enhancing dissolution performances of poorly soluble active pharmaceutical ingredients (API). Recently, a review on dissolution performances of SDs classifies the improvement into 3 categories, where 82 % of the studies showed improved bioavailability, 8 % showed reduced bioavailability and 10 % revealed similar bioavailability as compared to pure APIs. This indicates the inconsistent degrees of dissolution improvement of poorly soluble APIs in SD. Although a few factors related to the choice of carriers have been suggested to contribute to the dissolution improvement, however, the underlying factor determining the discrepancy in the degree of dissolution improvement remains in vague. It is hypothesized that the API contributes to the degree of dissolution improvement of SD. Hence, the factor of amorphous solubility advantage of API which leads to the different degrees of dissolution enhancement of SD is investigated in this research. Polyvinylpyrrolidone vinyl acetate (PVPVA)-based SD is prepared with three poorly soluble APIs. Physicochemical properties of SD were characterized using infrared spectroscopy, differential scanning calorimetry (DSC) and X-ray powder diffraction. The dissolution efficiency of each SD was calculated and compared to physical mixture and pure API. Theoretical amorphous solubility advantage for each API was calculated using the thermal properties obtained from DSC. The calculated values were found to be correlating well with the dissolution enhancement of the respective SDs. Hence, this theoretical approach can be utilized as an initial screening tool of API candidates in SD formulation during early pharmaceutical development.
Background: Bilastine (BLA) is a second-generation H1 antihistamine used to treat allergic rhinoconjunctivitis. Because of its limited solubility, it falls under class II of the Biopharmaceutics Classification System (BSC). The solid dispersion (SD) approach significantly improves the solubility and dissolution rate of insoluble medicines. Objective: To improve BLA solubility and dissolution rate by formulating a solid dispersion in the form of effervescent granules. Methods: To create BLA SDs, polyvinylpyrrolidone (PVP K30) and poloxamer 188 (PLX188) were mixed in various ratios (1:5, 1:10, and 1:15) using the kneading technique. All formulations were evaluated based on percent yield, drug content, and saturation solubility. The fo
... Show MoreThe objective of the study to develop an amorphous solid dispersion for poorly soluble raltegravir by hot melt extrusion (HME) technique. A novel solubility improving agent plasdone s630 was utilized. The HME raltegravir was formulated into tablet by direct compression method. The prepared tablets were assessed for all pre and post-compression parameters. The drug- excipients interaction was examined by FTIR and DSC. All formulas displayed complying with pharmacopoeial measures. The study reveals that formula prepared by utilizing drug and plasdone S630 at 1:1.5 proportion and span 20 at concentration about 30mg (trail-6) has given highest dissolution rate than contrasted with various formulas of raltegravir.
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... Show MoreExperiments were conducted to study axial liquid dispersion coefficient in slurry bubble column of 0.15 m inside diameter and 1.6 m height using perforated plate gas distributor of 54 holes of a size equal to 1 mm diameter and with a 0.24 free area of holes to the cross sectional area of the column. The three phase system consists of air, water and PVC used as the solid phase. The effect of solid loading (0, 30 and 60 kg/m3) and solid diameter (0.7, 1.5 and 3 mm) on the axial liquid dispersion coefficient at different axial location (25, 50 and 75 cm) and superficial gas velocity covered homogeneous-heterogeneous flow regime (1-10 cm/s) were studied in the present work. The results show that the axial liquid dispersion coeffic
... Show MoreChilled ceilings systems offer potential for overall capital savings. The main aim of the present research is to investigate the thermal performance of the indirect contact closed circuit cooling tower, ICCCCT used with chilled ceiling, to gain a deeper knowledge in this important field of engineering which has been traditionally used in various industrial & HVAC systems. To achieve this study, experimental work were implemented for the ICCCCT use with chilled ceiling. In this study the thermal performances of closed wet cooling tower use with chilled ceiling is experimentally and theoretically investigated. Different experimental tests were conducted by varying the controlling parameters to investigate their effects
... Show MoreThe importance of research stems from the prominent role of leaders in the political, administrative, economic and societal spheres in general, which requires highlighting this angle. Research Hypothesis Modern policies work with mechanisms that limit the clear role of governors and transform the ruler into an executive man. It can be assumed that the type of public policy of the state is the only criterion that transfers the ruler from a ruler to an executive.
The heat and mass transfer coefficients of the indirect contact closed circuit cooling tower, ICCCCT, were investigated experimentally. Different experiments were conducted involving the controlling parameters such as air velocity, spray water to air mass flow rate ratio, spray water flow rate, ambient air wet bulb temperature and the provided heat load to investigate their effects on the performance of the ICCCCT. Also the effect of using packing on the performance of the ICCCCT was investigated. It was noticed that these parameters affect the tower performance and the use of packing materials is a good approach to enhance the performance for different operational conditions. Correlations for mass and heat transfer coefficients are pres
... Show MoreOral tablets containing solubilized drug in the presence of appropriate excipients may give us an immediate release of the drug. Phospholipid solid dispersion (PSD) is a branch of solid dispersion in which phospholipid acts as a hydrophilic polymer in the presence of a suitable adsorbent to enhance the solubility of poorly soluble drugs. The anti-hyperlipidemic drug Atorvastatin (ATR) is an example of such drug, as it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Phosphatidylcholine in combination with magnesium aluminum silicate as an adsorbent in a ratio of ATR: PC: MAS 1:3:4 was used to prepare ATR PSD by the solvent evaporation method, the
... Show MoreMeloxicam (MLX) is non-steroidal anti -inflammatory, poorly water soluble, highly permeable drug and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal tract. Solid dispersion (SD) is an effective technique for enhancing the solubility and dissolution rate of such drug.
The present study aims to enhance the solubility and the dissolution rate of MLX by SD technique by solvent evaporation method using sodium alginate (SA), hyaluronic acid (HA), collagen and xyloglucan (XG) as gastro-protective hydrophilic natural polymers.
Twelve formulas were prepared in different drug: polymer ratios and evaluated for their, percentage yield, drug content, water so
... Show MoreAt present, numerous novel chemical compounds face challenges related to their limited solubility in aqueous environments. These compounds are classified under the Biopharmaceutical Classification System (BCS) as either class II or class IV substances. Different carriers were used to increase their solubility. Candesartan cilexetil (CC) is one of the most widely used antihypertensive drugs, which belongs to class II drugs. The aim of this research was to enhance the solubility and dissolution rate of CC through a complexation approach involving β-cyclodextrin and its derivatives, specifically hydroxypropyl beta cyclodextrin (HP-β-CD), methyl beta cyclodextrin (M-β-CD), and sulfonyl ether beta-cyclodextrin (SBE-β-CD), serving as
... Show MoreSilybum marianum, from which silymarin (SM) is extracted, is a medicinal herb. In the Biopharmaceutics Classification System, it is of the class II type, meaning it is almost completely insoluble in water. It has a number of therapeutic properties, including anti-inflammatory as well as properties that promote wound healing.
This research target is to promote the dissolution and solubility of SM by employing a technique called solid dispersion and then incorporating the formula of solid dispersion into a topical gel that can be used for wound healing.
Solid dispersion is a technique used to enhance solubility and dissolve pharmaceuticals that are not water-soluble. This method is widely used because of its low cos
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