scholarly journals Crystal modifications and dissolution rate of piroxicam

2011 ◽  
Vol 61 (4) ◽  
pp. 391-402 ◽  
Author(s):  
Lim Lyn ◽  
Huan Sze ◽  
Adhiyaman Rajendran ◽  
Gorajana Adinarayana ◽  
Kamal Dua ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Crystal Modification ◽  
Solvent Mixtures ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Crystal Forms ◽  
Peg 4000 ◽  
Enhanced Solubility ◽  
Crystal Modifications ◽  
Pvp K30

Crystal modifications and dissolution rate of piroxicam Piroxicam is a nonsteroidal anti-inflammatory drug with low aqueous solubility which exhibits polymorphism. The present study was carried out to develop polymorphs of piroxicam with enhanced solubility and dissolution rate by the crystal modification technique using different solvent mixtures prepared with PEG 4000 and PVP K30. Physicochemical characteristics of the modified crystal forms of piroxicam were investigated by X-ray powder diffractometry, FT-IR spectrophotometry and differential scanning calorimetry. Dissolution and solubility profiles of each modified crystal form were studied and compared with pure piroxicam. Solvent evaporation method (method I) produced both needle and cubic shaped crystals. Slow crystallization from ethanol with addition of PEG 4000 or PVP K30 at room temperature (method II) produced cubic crystal forms. Needle forms produced by method I improved dissolution but not solubility. Cubic crystals produced by method I had a dissolution profile similar to that of untreated piroxicam but showed better solubility than untreated piroxicam. Cubic shaped crystals produced by method II showed improved dissolution, without a significant change in solubility. Based on the XRPD results, modified piroxicam crystals obtained by method I from acetone/benzene were cube shaped, which correlates well with the FTIR spectrum; modified needle forms obtained from ethanol/methanol and ethanol/acetone showed a slight shift of FTIR peak that may be attributed to differences in the internal structure or conformation.

scholarly journals Assessment of dissolution profile of Pantoprazole tablets available in Bangladesh

2012 ◽  
Vol 4 (2) ◽  
pp. 58-62
Author(s):  
Aparajita Malakar ◽  
Bishwajit Bokshi ◽  
Utpal Kumar Karmakar
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Water Soluble ◽  
Dissolution Profile ◽  
Coating Materials ◽  
Volatile Solvents ◽  
Kneading Method ◽  
Enhanced Solubility ◽  
Materials Used ◽  
Liquisolid Compacts

The aim of the present study was to increase the solubility of a poorly water soluble BCS class II drug, valsartan. Liquisolid technology and solid dispersion by kneading method were techniques used to improve the solubility of the drug by using non-volatile solvents and some hydrophilic carriers. Liquisolid compacts were prepared by dissolving the drug in suitable non volatile solvents. The various non volatile solvents used were PG, PEG, and glycerine. The carrier coating materials play an important role in improving the solubility of the drug. The dissolution rate of the drug was increased by using propylene glycol as non-volatile solvent at 20:1 ratio of carrier to coating material. Solid dispersion by kneading method were another attempt to improve solubility the various carrier materials used were PVP K 30, PEG 6000 and mannitol, these carriers are used in various ratios to improve its solubility. The dissolution rate of drug using solid dispersion kneading method with mannitol was increased at 1:3 ratio. The DSC and FTIR studies revealed no drug excipients interactions, whereas XRD revealed the reduced crystalinity of drug, which showed enhanced solubility. From the results it was concluded that the liquisolid compacts enhanced the solubility of valsartan in comparison to traditional solid dispersion method.DOI: http://dx.doi.org/10.3329/sjps.v4i2.10441  S. J. Pharm. Sci. 4(2) 2011: 58-62

scholarly journals PREPARATION AND CHARACTERIZATION OF NANOCRYSTALS FOR SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT OF PALIPERIDONE USING DIFFERENT HYDROPHILIC CARRIERS: IN VITRO-IN VIVO STUDY

2018 ◽  
Vol 11 (4) ◽  
pp. 393
Author(s):  
Moon Rajkumar ◽  
Gattani Surendra
Keyword(s):  
Dissolution Rate ◽  
Antipsychotic Agent ◽  
Aqueous Solubility ◽  
In Vivo Study ◽  
Scanning Calorimetry ◽  
Antisolvent Precipitation ◽  
Enhanced Solubility ◽  
Pure Drug

 Objective: The objective of this study was to increase the solubility and dissolution rate of paliperidone (PAL) by preparing its nanocrystals using different hydrophilic carriers by antisolvent precipitation technique.Methods: The nanoparticles (NP) were characterized for aqueous solubility, drug content, Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction, scanning electron microscopy, particle size, and in vitro-in vivo analysis.Results: The results showed improved solubility and dissolution rate of NPs when compared to pure drug and physical mixture (PM). Solubility data showed a linear graph giving an indication that there is a gradual increase in the solubility profile of the drug with an increase in concentration of the carriers. At highest concentration, the solubility of NPs with Plasdone S630, Povidone K-25, and PVP K-30 found to be increased by 12 folds, 9 folds and 6 folds, respectively, as compared to pure drug. The release profile of NPs with Plasdone S630 in terms of dissolution efficiency at 60 min (DE60), initial dissolution rate (IDR), amount release in 15 min (Q15 min), and time for 75% release (t75%) shows better results when compared to pure drug, PM, and also NPs with povidone 25 and povidone 30. In vivo study reveals that optimized NPs elicited significant induction of cataleptic behavior which is the indication of antipsychotic agent(s) effect.Conclusion: The process antisolvent precipitation under constant stirring may be a promising method to produce stable PAL NPs with markedly enhanced solubility and dissolution rate due to nanonization with the increased surface area, improved wettability, and reduced diffusion pathway.

scholarly journals Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

2021 ◽  
Vol 9 (2) ◽  
pp. 127-135
Author(s):  
Anil Raosaheb Pawar ◽  
Pralhad Vitthalrao Mundhe ◽  
Vinayak Kashinath Deshmukh ◽  
Ramdas Bhanudas Pandhare ◽  
Tanaji Dilip Nandgude
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Peg 4000

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

scholarly journals Mechanochemical Formation of Racemic Praziquantel Hemihydrate with Improved Biopharmaceutical Properties

Pharmaceutics ◽  
2020 ◽  
Vol 12 (3) ◽  
pp. 289
Author(s):  
Debora Zanolla ◽  
Dritan Hasa ◽  
Mihails Arhangelskis ◽  
Gabriela Schneider-Rauber ◽  
Michele R. Chierotti ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Polymorphic Form ◽  
In Vitro Tests ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Experimental Conditions ◽  
Intrinsic Dissolution ◽  
Intrinsic Dissolution Rate ◽  
X Ray ◽  
Enhanced Solubility

Praziquantel (PZQ) is the first-line drug used against schistosomiasis, one of the most common parasitic diseases in the world. A series of crystalline structures including two new polymorphs of the pure drug and a series of cocrystals of PZQ have been discovered and deposited in the Cambridge Structural Database (CSD). This work adds to the list of multicomponent forms of PZQ a relevant example of a racemic hemihydrate (PZQ-HH), obtainable from commercial PZQ (polymorphic Form A) through mechanochemistry. Noteworthy, the formation of the new hemihydrate strongly depends on the initial polymorphic form of PZQ and on the experimental conditions used. The new PZQ-HH has been fully characterized by means of HPLC, Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA), Hot-Stage Microscopy (SEM), Powder X-Ray Diffraction (PXRD), Scanning Electron Microscopy (SEM), FT-IR, polarimetry, solid-state NMR (SS-NMR), solubility and intrinsic dissolution rate (IDR), and in vitro tests on Schistosoma mansoni adults. The crystal structure was solved from the powder X-ray diffraction pattern and validated by periodic-DFT calculations. The new bioactive hemihydrate was physically stable for three months and showed peculiar biopharmaceutical features including enhanced solubility and a double intrinsic dissolution rate in water in comparison to the commercially available PZQ Form A.

scholarly journals Preparation and evaluation of azithromycin binary solid dispersions using various polyethylene glycols for the improvement of the drug solubility and dissolution rate

2016 ◽  
Vol 52 (1) ◽  
pp. 1-13 ◽  
Author(s):  
Ehsan Adeli
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Water Soluble ◽  
Polyethylene Glycols ◽  
X Ray Diffraction ◽  
Drug Release Profile ◽  
Scanning Calorimetry ◽  
Peg 4000 ◽  
Poorly Soluble

ABSTRACT Azithromycin is a water-insoluble drug, with a very low bioavailability. In order to increase the solubility and dissolution rate, and consequently increase the bioavailability of poorly-soluble drugs (such as azithromycin), various techniques can be applied. One of such techniques is "solid dispersion". This technique is frequently used to improve the dissolution rate of poorly water-soluble compounds. Owing to its low solubility and dissolution rate, azithromycin does not have a suitable bioavailability. Therefore, the main purpose of this investigation was to increase the solubility and dissolution rate of azithromycin by preparing its solid dispersion, using different Polyethylene glycols (PEG). Preparations of solid dispersions and physical mixtures of azithromycin were made using PEG 4000, 6000, 8000, 12000 and 20000 in various ratios, based on the solvent evaporation method. From the studied drug release profile, it was discovered that the dissolution rate of the physical mixture, as the well as the solid dispersions, were higher than those of the drug alone. There was no chemical incompatibility between the drug and polymer from the observed Infrared (IR) spectra. Drug-polymer interactions were also investigated using Differential Scanning Calorimetry (DSC), Powder X-Ray Diffraction (PXRD) and Scanning Election Microscopy (SEM). In conclusion, the dissolution rate and solubility of azithromycin were found to improve significantly, using hydrophilic carriers, especially PEG 6000.

scholarly journals FORMULATION OF SOLID DISPERSIONS FOR ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF SIMVASTATIN

2021 ◽  
pp. 94-100
Author(s):  
PAYAL D. BORAWAKE ◽  
KAUSLYA ARUMUGAM ◽  
JITENDRA V. SHINDE
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Fourier Transforms ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Solvent Evaporation ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Drug Content ◽  
Pvp K30

Objective: The objective of the present work was to formulate the solid dispersions of simvastatin for enhancement of its aqueous solubility and dissolution rate. Methods: In the present study, solid dispersions of simvastatin were prepared by Kneading and Solvent evaporation methods. The polymeric carriers like Polyethylene glycol (PEG) 6000 and Polyvinyl Pyrrolidone (PVP) K30 were used in different ratios (ratio of drug: carrier was 1:1, 1:2) to formulate solid dispersions. The prepared solid dispersions were characterized by differential scanning calorimetry (DSC), Fourier transforms infrared spectroscopy (FTIR), and evaluated for drug content, percentage yield, saturation solubility, in vitro dissolution studies. The best formula of the solid dispersion was selected according to the solubility and dissolution data. Results: The F7 formulation was found to be an optimized formulation containing PVP K30 in the ratio 1:1 prepared by solvent evaporation technique. The Drug content was found to be higher i.e. 94.89 in the F7 batch. The FT-IR spectra revealed that there was no interaction between drugs and carriers. DSC thermogram indicated entrapment of simvastatin in PVP K30 and the conversion of crystalline simvastatin into an amorphous form. The F7 formulation showed maximum drug release i.e. 98.60% in 60 min which is 2 times greater than pure drug making it an optimized formulation. Conclusion: The solubility of simvastatin was successfully enhanced through the solid dispersion technique. Solid dispersions prepared with solvent evaporation method were more soluble than solid dispersions prepared with kneading method with carrier PVP K30.

Novel Aceclofenac cocrystals with l-Cystine: Virtual coformer screening, mechanochemical synthesis, and physicochemical investigations

2020 ◽  
Vol 17 ◽  
Author(s):  
Saroj Kumar ◽  
Amresh Gupta ◽  
Rammani Prasad ◽  
Satyawan Singh
Keyword(s):  
Dissolution Rate ◽  
Mechanochemical Synthesis ◽  
Screening Method ◽  
Research Work ◽  
Crystalline Solid ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Grinding Method ◽  
Enhanced Solubility ◽  
And Performance

Aim: Current work focuses on the improvement of solubility and dissolution of ACF by the cocrystal approach. Background: Aceclofenac (ACF) is one of the commonly used nonsteroidal anti-inflammatory drug (NSAID) representing the variety of therapeutic applications including management of pain, inflammation, rheumatoid arthritis, and osteoarthritis, etc. But very low solubility and dissolution rate of ACF compromise its therapeutic utility. Now a day's cocrystallization technique has emerged as a novel technique for modulation of said problems. Objective: The Specific objectives of this research work were mechanochemical synthesis, characterization, and performance evaluation of aceclofenac cocrystal. Method: ACF was screened with various pharmaceutically acceptable coformers (Selected from GRAS and EAFUS list) using MOPAC software and physical screening method to find out novel cocrystals of ACF with enhanced solubility and dissolution rate. Novel cocrystals (multi-component crystalline solid) of ACF with l-cystine were prepared by neat grinding method and by liquid assisted grinding method. The synthesized cocrystals (ACF-l-CYS NG and ACF-l-CYS LAG) were characterized carefully by differential scanning calorimetry (DSC), infrared spectroscopy (IR), and powder X-ray diffraction (PXRD) to verify the formation of the cocrystals. Pharmaceutically significant properties such as powder dissolution rate, solubility, and stability of the prepared cocrystals were evaluated. Results: Compared to pure ACF, the prepared cocrystals showed superior solubility and dissolution rate. The prepared cocrystals were found to be stable and non-hygroscopic under study conditions. Conclusion: The cocrystallization technique was successfully utilized to increase the solubility and dissolution rate of aceclofenac.

Formulation and Evaluation of Benidipine Nano-suspension by Precipitation Method using Central Composite Design

2021 ◽  
Vol 14 (3) ◽  
pp. 5492-5500
Author(s):  
Sejal Patel ◽  
Anita P Patel
Keyword(s):  
Particle Size ◽  
Polymer Concentration ◽  
In Vitro Dissolution ◽  
Precipitation Method ◽  
Tween 20 ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Rate Of Dissolution ◽  
Central Composite ◽  
Pvp K30

In the interest of administration of dosage form oral route is most desirable and preferred method. Poor solubility and slow dissolution rate major challenges in upcoming and existing therapeutically active compound. Water insoluble drug indicate insufficient bioavailability as well dissolution resulting in fluctuating plasma level. Benidipine (BND) is Biopharmaceutical Classification System Class-II drug having low solubility and high permeability, antihypertensive drug has lower bioavailability. The purpose of the present study was to improve solubility as well dissolution profile of Benidipine HCL. BND nanosuspension was formulated using precipitation technique. Various polymers were evaluated  viz. HPMC E15, Tween 20, PVP K30 in preliminary trial to stabilized nanosuspension but PVP K30 was selected among them. The solubility of BND was carried out using different solvents like Ethanol, Acetonitrile; Acetone. Ethanol was used as a preferred solvent as BND shows high solubility in it.  The effect of different important process parameters e.g. selection of polymer concentration X1(10 mg), solvent concentration X2 (0.2 ml) were investigated by Central Composite factorial design to accomplish desired particle size and rate of dissolution. Stirring speed and time of stirring was kept constant as 1000 rpm and 2h respectively. To achieve optimized batch, 9 formulations (F1-F9) were prepared.  The optimized batch had 237 nm particle size Y1, and showed in-vitro dissolution Y2 98±0.72 % in 30 mins related to pure BND (58±0.25%) and zeta potential was -15.3. None of interaction between drug and polymer was confirmed by Differential scanning calorimetry (DSC) and FT-IR analysis. The obtained results showed that issues related particle size (nm) and rate of dissolution of BND has been solved when nanosuspension can be prepared by precipitation method by considering optimized parameter due to formation of nanosized particles

Formulation Evaluation and Characterization of Fast Dissolving Tablets of Rofecoxib

2021 ◽  
pp. 60-64
Author(s):  
Preeti Mehra ◽  
Vishal Kapoor ◽  
Naveen Gupta ◽  
Dharmendra Singh Rajpoot ◽  
Neeraj Sharma
Keyword(s):  
Solid Dispersion ◽  
Water Solubility ◽  
Solid Dispersions ◽  
Amorphous State ◽  
Dissolution Profile ◽  
Major Drawback ◽  
Peg 4000 ◽  
Dissolution Efficiency ◽  
Pvp K30

Rofecoxib, a new non-steroidal anti-inflammatory agent mainly used for the treatment of osteoarthritis and rheumatoid arthritis. The major drawback of Rofecoxib is its very low water solubility, which results in poor bioavailability after oral administration. Hence, an attempt was made to formulate fast dissolving tablets of Rofecoxib. The solid dispersions of Rofecoxib were prepared with PEG-4000 and PVP K30 by solvent evaporation method. The characterization of prepared solid dispersions by FTIR, XRPD and DSC, which reveals lack of interaction with carriers and dictates amorphous state of solid dispersions. Solid dispersion of Rofecoxib with PVP K30 (1:6) showed maximum dissolution, therefore compressed into tablets by using microcrystalline cellulose, lactose and crosspovidone. The dissolution profile of developed fast dissolving tablets containing solid dispersion of Rofecoxib (1:6) was studied. The formulated formulations showed optimum dissolution efficiency.

scholarly journals DEVELOPMENT AND EVALUATION OF LAMOTRIGINE SOYA LECITHIN SOLID DISPERSION: IN VITRO AND PHARMACODYNAMIC INVESTIGATION

2019 ◽  
pp. 115-122
Author(s):  
SURESH GAUTAM ◽  
YOGESH NIKALAJE ◽  
DARSHANA BHADRE ◽  
RASHMI TRIVEDI ◽  
MILIND UMEKAR ◽  
...  
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Neurodegenerative Disorder ◽  
Water Soluble ◽  
Dissolution Profile ◽  
Onset Of Action ◽  
Uniform Size ◽  
Soya Lecithin ◽  
Enhanced Solubility

Objective: Epilepsy is a common neurodegenerative disorder characterized by spontaneous and repeated attacks of convulsions. It requires immediate pharmacotherapy to prevent its progression to status epilepticus. However, most of the anticonvulsant drugs are poorly water-soluble and demonstrate the delayed onset of action. Thus there is a need to improve its solubility for the better pharmaceutical profile. The objective of the present investigation was to enhance the solubility of lamotrigine incorporating soya lecithin as a phospholipid carrier by solid dispersion technique Methods: Solid dispersions of lamotrigine were prepared with soya lecithin by the solvent method. The effect of concentration of phospholipid and solvents on aqueous solubility and dissolution profile of lamotrigine was analyzed. Results: Ethanol increased lamotrigine solubility with soya lecithin in ratio 5:1. X-ray diffraction and scanning electron micrograph indicated a smaller crystallite size of lamotrigine with fairly uniform size distribution in the lamotrigine-soya lecithin solid dispersion. The resultant solid dispersion also significantly delayed the onset of clonic convulsion (875.8 s) as compared to control (85.5 s) and offered complete protection (100%) against the pentylenetetrazole induced seizures in the rat as compared to control (33.33%). Also, solid dispersion with maximum drug content (77.68%) and dissolution rate (91.40%) was formulated as an orodispersible tablet and characterized for its pharmaceutical properties. Conclusion: It can be concluded that the solid dispersion of lamotrigine incorporated with soya lecithin demonstrated enhanced solubility and dissolution rate may have potential clinical application.

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