Aim: The present study aims to improve the poor water solubility of zaltoprofen which is a non-steroidal anti-inflammatory drug (NSAIDs) with a potent analgesic effect using solid dispersion then formulate it as a hollow type suppository to be more convenient for geriatric patients. Materials and Method: Zaltoprofen solid dispersions were prepared by solvent evaporation technique in different zaltoprofen: Soluplus® ratios. Results: Among the formulations tested, zaltoprofen solid dispersion preparation using 1:5 (zaltoprofen: Soluplus®) ratio showed the highest solubility and selected for further investigation. Solid dispersion characterization was evaluated by differential scanning calorimetry (DSC), X-ray diffraction study (XRD) and Fourier transformation infrared spectroscopy (FTIR). DSC and XRD analysis showed a complete transformation of zaltoprofen in the solid dispersion from a crystalline state to amorphous state. The selected zaltoprofen solid dispersion was further incorporated into hollow type suppositories using witepsol H 35 as a suppositories base. The hollow type suppositories were evaluated for hardness test (breaking strength), melting time, softening time and in vitro drug dissolution rate. Formula F8 containing zaltoprofen solid dispersion in the whole of hollow type suppository showed the shortest and significantly the highest dissolution rate profile (100% within 15 min) compared to other hollow type suppository formulas prepared that contain zaltoprofen powder in its whole. Conclusion: It is concluded that the development of zaltoprofen solid dispersions using Soluplus® as hollow-type suppositories could be used as a promising approach for improving the solubility of poorly water-soluble drugs
Solid dispersion (SD) is one of the most widely used methods to resolve issues accompanied by poorly soluble drugs. The present study was carried out to enhance the solubility and dissolution rate of Aceclofenac (ACE), a BCS class II drug with pH-dependent solubility, by the SD method. Effervescent assisted fusion technique (EFSD) using different hydrophilic carriers (mannitol, urea, Soluplus®, poloxamer 188, and poloxamer 407) in the presence of an effervescent base (sodium bicarbonate and citric acid) in different drug: carrier: effervescent base ratio and the conventional fusion technique (FSD) were used to prepare ACE SD. Solubility, dissolution rate, Fourier transformation infrared spectroscopy (FTIR), PowderX-ray diffraction
... Show MorePatch in transdermal drug delivery(TDDS) used to overcome the hypodermic drawback, but these patch also have absorption limitation for hydrophilic and macromolecule like peptide and DNA. So that micronized projection have the ability for skin penetration developed named as microneedle. Microneedle drug delivery system is a novel drug delivery to overcome the limitation of TDDS like skin barrier restriction for large molecule. Microneedle patch can penetrate through skin subcutaneous into epidermis, avoiding nerve fiber and blood vessel contact. There are many type of microneedle patch like solid, polymer, hallow, hydrogel forming microneedle and dissolving microneedle with different method of microfabrication
Selexipag is an orally selective long-acting prostacyclin receptor agonist, which indicated for the treatment of pulmonary arterial hypertension. It is practically insoluble in water ( class II, according to BCS). This work aims to prepare and optimized Selexipag nanosuspensions to achieve an enhancement in the in vitro dissolution rate. The solvent antisolvent precipitation method was used for the production of nanosuspension, and the effect of formulation parameters (stabilizer type, drug: stabilizer ratio, and use of co-stabilizer) and process parameter (stirring speed) on the particle size and polydispersity index were studied. SLPNS prepared with Soluplus® as amain stabilizer (F15) showed the smallest particle size 47nm wi
... Show More“Orodispersible Tablet†a tablet that is to be placed in oral cavity where it disperses rapidly by saliva with no need for water before swallowing. Zaltoprofen (ZLP) is one of NSAIDs which is used in the treatment of rheumatoid arthritis and osteoarthritis as well as to relieve inflammation and pain after surgery, injury and tooth extraction. The present study was aimed to prepare rapidly dissolved lyophilized Zaltoprofen tablet with different pharmaceutical excipients and studying the factors affecting pharmaceutical properties like (solubility, disintegration time DT, dissolution, etc.) of tablets. The lyophilized disintegrating tablets (LDTs) were prepared using Zydis technique by lyophilization an aqueous
... 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 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 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 (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 MoreEtoricoxib (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
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