Bilastine (BLS) is non-sedating new-brand H1 antihistamine that has selective peripheral effects, the drug has a problem of an insufficient aqueous solubility and accordingly low dissolution rate, and low bioavailability. Solid dispersion (SD) is one of the most effective techniques for improving the solubility and the dissolution rate of poorly soluble drugs by the dispersion of drug within an inert hydrophilic carrier. The aim of this study is to increase the solubility and dissolution rate of the BLS using SD technique. Twenty-nine BLS SD formulas were prepared using different carrier polymers include Pluronic 407 (Poloxamer407), Poloxamer188, Urea, Polyethylene glycol 6000 (PEG6000) and Polyvinylpyrrolidone (PVP K30) and employing two different preparation methods (solvent evaporation and kneading method) at different drug: polymer ratios (1:1 ,1:3,1:5,1:10,1:15). The prepared SD formulas were evaluated for their percent yield, drug content, aqueous solubility, dissolution rate, PXRD, and FTIR. The SD technique successfully improved the solubility and dissolution rate of BLS. The improvement was largely dependent on the polymer type and drug: polymer ratio. The solubility improvement using different polymers was in the following order: PVP K30> PLX188> PEG6000> Urea> PLX407. The solid dispersion formula that showed the best outcomes in terms of dissolution improvement was prepared using the solvent evaporation technique employing PVP K30 at ratio of drug: polymer of 1:15. The optimized formula showed 10.2 folds increment in the solubility compared to pure BLS. It can be concluded that the SD technique can successfully improve the solubility and dissolution rate by solvent evaporation method with careful selection of the carrier polymer and drug: polymer ratio.
Etoricoxib (EXB) is a highly selective cox-2 inhibitor which belongs to the non-steroidal anti-inflammatory drug (NSAID). EXB is a class II drug according to the biopharmaceutical classification system (BCS), which possess a very low aqueous solubility in water. In the present study, many trials were made to improve the aqueous solubility and dissolution rate of EXB by solid dispersion technique.
Eighteenth EXB formulas were formulated as a solid dispersion using a variety of hydrophilic polymers (as carriers) including poloxamer 407 (PXM 407), poloxamer 188 (PXM 188) and polyethylene glycol 4000 (PEG 4000) at different drug: polymer ratios (1:1, 1:3 and 1:5). These formulas were prepared by two methods; solvent
... Show MoreEbastine (EBS) is a non-sedating antihistamine with a long duration of action. This drug has predominantly hydrophobic property causing a low solubility and low bioavailability. Surface solid dispersions (SSD) is an effective technique for improving the solubility and dissolution rate of poorly soluble drugs by using hydrophilic water insoluble carriers.
The present study aims to enhance the solubility and dissolution rate of EBS by using surface solid dispersion technique. Avicel® PH101, Avicel® PH 102, croscarmellose sodium(CCS) and sodium starch glycolate(SSG) were used as water insoluble hydrophilic carriers.
The SSD formulations of EBS were prepared by the solvent evaporation method in different drug: carrier
... Show MoreSolid dispersion is an attractive tool of pharmaceutical technology used to improve the physical properties of drugs. Among these properties is to enhance the solubility of the drugs.
Rebamipide is a poorly soluble drug of class IV of biopharmaceutical classification system (BCS).
Rebamipide is used as potent antiulcer, mucoprotective drug, by stimulating the generation of prostoglandine enhanced mucosal protection.
Rebamipide was formulated as a solid dispersion using different polymers such as pluronic F-127, PEG6000, PVP K30, and TPGS by using different preparation methods solvent evaporation, fusion, and kneading methods.
It was seen that rebamipide was successfully dispersed in a homogenous solid dispersion matrix by sol
Atorvastatin (ATR) is a poorly water-soluble anti-hyperlipidemic drug. The drug belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersion is an effective technique for enhancing the solubility and dissolution of drugs. Phospholipid solid dispersion (PSD) using phosphatidylcholine (PC) as a carrier with or without adsorbent (magnesium aluminum silicate, silicon dioxide 15nm, silicon dioxide 30nm, calcium silicate) was used to prepare ATR PSD using different drug: PC: adsorbent ratios by solvent evaporation method. The resulted PSD was evaluated for its percentage yield, drug content, solubility, dissolution rate, Fourier transforma
... Show MoreAtorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs.
The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxam
... Show MoreAtorvastatin have problem of very slightly aqueous solubility (0.1-1 mg/ml). Nano-suspension is used to enhance it’s of solubility and dissolution profile. The aim of this study is to formulate Atorvastatin as a nano-suspension to enhance its solubility due to increased surface area of exposed for dissolution medium, according to Noyes-Whitney equation.
Thirty one formulae were prepared to evaluate the effect of ; Type of polymer, polymer: drug ratio, speed of homogenization, temperature of preparation and inclusion of co-stabilizer in addition to the primary one; using solvent-anti-solvent precipitation method under high power of ultra-sonication.
... Show MoreBackground: 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 MoreNimodipine (NMD) is a dihydropyridine calcium channel blocker useful for the prevention and treatment of delayed ischemic effects. It belongs to class ? drugs, which is characterized by low solubility and high permeability. This research aimed to prepare Nimodipine nanoparticles (NMD NPs) for the enhancement of solubility and dissolution rate. The formulation of nanoparticles was done by the solvent anti-solvent technique using either magnetic stirrer or bath sonicator for maintaining the motion of the antisolvent phase. Five different stabilizers were used to prepare NMD NPs( TPGS, Soluplus®, HPMC E5, PVP K90, and poloxamer 407). The selected formula F2, in which Soluplus
has been utilized as a stabilizer, has a par
... 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 MoreSolid 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
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