Objective: Carbamazepine is typically used for the treatment of seizure disorders and neuropathic pain. One of the major problems with this drug is its low solubility in water; therefore the objective of this study was to enhance the solubility of carbamazepine by complexation with cyclodextrin to be formulated as effervescent and dispersible granules.Methods: Solvent evaporation method was used to prepare, binary (Carbamazepine/β-cyclodextrin) complex and ternary (Carbamazepine/β-cyclodextrin/hydroxypropyl methyl cellulose (HPMC E5). The more soluble complex will be further formulated as unit dose effervescent and dispersible granules. The complexes were evaluated for their solubility, drug content, percentage practical yield and differential scanning calorimetery (DSC) to confirm the formation of the complex.Results: The ratio of effervescent components, amount of effervescent base, amount of croscarmellose sodium (superdisintegrant) within the formula were found to play a role in the percentage of drug dissolved. Among the all prepared formulas, the effervescent granules containing ternary complex equivalent to 200 or 100 carbamazepine with effervescent base of 1:2:3.4 citric acid: tartaric acid: sodium bicarbonate not less than 48% w/w and 3% w/w croscarmellose sodium within the formula may be considered as a promising formulas regarding the amount of drug dissolved within 5 min.Conclusion: The solubility of carbamazepine was enhanced by complexation with β-cyclodextrin and HPMC E5 as a ternary complex. Hence effervescent and dispersible granules of carbamazepine with good flow properties can be successfully prepared by using this complex.
Atorvastatin (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 Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents. All solid dispersion adsorbate (SDA) formulas were prepared in ratios of 1:1:1 (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content, , dissolution, crystal structure using X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC) studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction. The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38 fold increase in solubility compared to solubility of pure ATR and solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility and dissolution .
Ondansetron hydrochloride (ONH) is a very bitter, potent antiemetic drug used for the treatment and/or prophylaxis of chemotherapy or radiotherapy or postoperative induced emesis. The objective of this study is to formulate and evaluate of taste masked fast dissolving tablet (FDTs) of ONH to increase patient compliance. ONH taste masked granules were prepared by solid dispersion technique using Eudragit E100 polymer as an inert carrier. Solvent evaporation and fusion melting methods were used for such preparation. Completely taste masking with zero release of drug in phosphate buffer pH 6.8was obtained from granules prepared by solvent evaporation method using drug: polymer ratio of 1:2, from which four formulas pass pre-compression evaluation and compressed to FDTs and evaluated for their drug content, in-vitro disintegration time, in-vivo disintegration time, wetting time and in vitro drug release profile. F7 which is prepared from solid dispersion product equivalent to the required dose of ONH , Crosspovidone as superdisintegrant, Aspartame as sweetener ,Ross berry as flavor ,Polyvinylpyrolidone K30.3.as binder ,Avicil PH102 and , mannitol as diluents give best in- vitro, in-vivo disintegration time and best drug release profile. Key words: Ondansetron hydrochloride, taste masking, solid dispersion, Eudragit E100.
In-situ gelation is a process of gel formation at the site of application, in which a drug product formulation that exists as a liquid has been transformed into a gel upon contact with body fluids. As a drug delivery agent, the in-situ gel has an advantage of providing sustained release of the drug agent. In-situ gelling liquid suppositories using poloxamer 188 (26-30% W/W) as a suppository base with 10% W/W naproxen were prepared, the gelation temperature of these preparations were measured and they were all above the physiological temperature. Additives such as polyvinylpyrrolidin "PVP" ,hydroxylpropylmethylcellulose "HPMC", sodium alginate and sodium chloride were used in concentration ranging from (0.25-1%W/W) to modulate the gelation temperature and gel strength .The best preparation was obtained through using a combination of poloxamer 188, sodium alginate, naproxen and distilled water (29,0.5,10and 60.5 % W/W respectively)with gelation temperature of 33.6ºC±0.2 and gel strength of 28±2 seconds. The release of drug from this preparation was sustained for about 12 hours and it was faster than conventional solid suppository (Proxen® 500) and oral tablets (Naproxen®500) using dialysis tubing method. Key words: - naproxen, in-situ gelation, liquid suppository, poloxamer188
Silymarin (SM) is a plant extract obtained from Silybum marianum( milk thistle). It is hepatoprotective drug class II type according to Biopharmaceutics Classification System. It is practically insoluble with low bioavailability. Micro/nanonization during crystallization, surface modification and crystal structure modification may improve the solubility and dissolution rate of poorly water-soluble drugs.The aim of this study was to enhance the water solubility and dissolution rate of SM by in-situ micronization using solvent change either by stirring or ultrasonic method. Polymers like gelatin, PVP-K30, HPMC15, pulullan were used to stabilize the prepared ultra-fine crystals. Effect of type and concentration of hydrophilic polymer, solvent: anti-solvent volume ratio and the effect of ultrasonic irradiation were studied. The prepared microcrystals were evaluated for their percent yield, water solubility, crystals structure by XRD, DSC, and SEM. Particle size and dissolution rate were also determined. Silymarin microcrystals prepared by ultrasonic method and stabilized by 0.1% w/v gelatin using 1:2 solvent: anti-solvent volume ratio showed the best results with percent yield 93.4±2.7% and particle size reduction from mean diameter of 1.5µm (untreated SM) to 0.43µm with uniform morphology and enhanced solubility for about four folds with improvement in dissolution.
Meloxicam (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 solubility, dissolution, crystal lattice using powder X-ray diffraction (PXRD) and studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-polymer interaction. All the prepared showed improvement of drug solubility except that prepared with HA. The best result was obtained with formula SD1 (MLX: SA 1:1) that showed a high percentage yield (97), high drug content (97.4±0.05) and increase in solubility compared to solubility of pure MLX with improved dissolution rate. the PXRD study revealed the conversion of the drug to amorphous form without chemical interaction according to FTIR results
Atorvastatin calcium (ATR) is an antihyperlipidemic agent used for lowering blood cholesterol levels. However, it is very slightly soluble in water with poor oral bioavailability, which interferes with its therapeutic action. It is classified as a class II drug according to Biopharmaceutical Classification System (low solubility and high permeability).
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