Cocrystal Construction Between Rosuvastatin Calcium and L-asparagine with Enhanced Solubility and Dissolution Rate

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

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Difference in the Dissolution Behaviors of Tablets Containing Polyvinylpolypyrrolidone (PVPP) Depending on Pharmaceutical Formulation After Storage Under High Temperature and Humid Conditions

Journal of Pharmacy & Pharmaceutical Sciences ◽

10.18433/j3hw3q ◽

2016 ◽

Vol 19 (4) ◽

pp. 511 ◽

Cited By ~ 2

Author(s):

Yoh Takekuma ◽

Haruka Ishizaka ◽

Masato Sumi ◽

Yuki Sato ◽

Mitsuru Sugawara

Keyword(s):

High Temperature ◽

Benzoic Acid ◽

Dissolution Rate ◽

Simple Structure ◽

Pharmaceutical Formulations ◽

Magnesium Stearate ◽

Principal Agent ◽

Amino Groups ◽

Dissolution Tests ◽

Rosuvastatin Calcium

PURPOSE. Storage under high temperature and humid conditions has been reported to decrease the dissolution rate for some kinds of tablets containing polyvinylpolypyrrolidone (PVPP) as a disintegrant. The aim of this study was to elucidate the properties of pharmaceutical formulations with PVPP that cause a decrease in the dissolution rate after storage under high temperature and humid conditions by using model tablets with a simple composition. METHODS. Model tablets, which consisted of rosuvastatin calcium or 5 simple structure compounds, salicylic acid, 2-aminodiphenylmethane, 2-aminobiphenyl, 2-(p-tolyl)benzoic acid or 4.4’-biphenol as principal agents, cellulose, lactose hydrate, PVPP and magnesium stearate as additives, were made by direct compression. The model tables were wrapped in paraffin papers and stored for 2 weeks at 40°C/75% relative humidity (RH). Dissolution tests were carried out by the paddle method in the Japanese Pharmacopoeia 16th edition. RESULTS. Model tablets with a simple composition were able to reproduce a decreased dissolution rate after storage at 40°C/75% RH. These tablets showed significantly decreased water absorption activities after storage. In the case of tablets without lactose hydrate by replacing with cellulose, a decreased dissolution rate was not observed. Carboxyl and amino groups in the structure of the principal agent were not directly involved in the decreased dissolution. 2-Benzylaniline tablets showed a remarkably decreased dissolution rate and 2-aminobiphenyl and 2-(p-tolyl)benzoic acid tablets showed slightly decreased dissolution rates, though 4,4’-biphenol tablets did not show a decrease dissolution rate. CONCLUSIONS. We demonstrated that additives and structure of the principal agent were involved in the decreased in dissolution rate for tablets with PVPP. The results suggested that one of the reasons for a decreased dissolution rate was the inclusion of lactose hydrate in tablets. The results also indicated that compounds as principal agents with low affinity for PVPP may be easily affected by airborne water under high temperature and humid conditions. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2018.v11i4.24964 ◽

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.

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Enhanced Solubility and Dissolution Rate of Aceclofenac by Using Spray Drying Techniques

Intellectual Property Rights Open Access ◽

10.4172/2375-4516.1000140 ◽

2015 ◽

Vol 03 (02) ◽

Cited By ~ 1

Author(s):

Sahilhusen I Jethara ◽

Mukesh R Patel

Keyword(s):

Dissolution Rate ◽

Spray Drying ◽

Enhanced Solubility ◽

Drying Techniques

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Leveraging Framework Instability: A Journey from Energy Storage to Drug Delivery

Synlett ◽

10.1055/s-0040-1707139 ◽

2020 ◽

Vol 31 (16) ◽

pp. 1573-1580 ◽

Cited By ~ 1

Author(s):

Adam J. Matzger ◽

Kuthuru Suresh ◽

Vilmalí López-Mejías ◽

Saikat Roy ◽

Daniel F. Camacho

Keyword(s):

Drug Delivery ◽

Energy Storage ◽

Dissolution Rate ◽

Metal Organic Framework ◽

Porous Solids ◽

Energy Storage Materials ◽

Amorphous Form ◽

Amorphous Pharmaceuticals ◽

Enhanced Solubility ◽

Fast Dissolution

Amorphous pharmaceuticals often suffer from poor physical stability, which can negate their high solubility, fast dissolution rate, and better oral bioavailability vs. crystalline forms. This represents a major hurdle to processing, storage, and delivery of amorphous pharmaceuticals. Several approaches to addressing these problems have been pursued, but there is still a need for a general method for stabilizing the amorphous form. We describe a novel approach using a water-unstable metal-organic framework as a drug delivery vehicle that demonstrates improved amorphous form stability accompanied by remarkably enhanced solubility and a fast dissolution rate. This research project spanned eleven years from conception to realization and dissemination. With origins in understanding the stability or porous solids for energy storage materials, the work also highlights potential of basic science understanding to illuminate new areas of application.

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Hot-Melt 3D Extrusion for the Fabrication of Customizable Modified-Release Solid Dosage Forms

Pharmaceutics ◽

10.3390/pharmaceutics12080738 ◽

2020 ◽

Vol 12 (8) ◽

pp. 738 ◽

Cited By ~ 1

Author(s):

Jaemin Lee ◽

Chanwoo Song ◽

Inhwan Noh ◽

Sangbyeong Song ◽

Yun-Seok Rhee

Keyword(s):

Dissolution Rate ◽

Dosage Form ◽

Amorphous State ◽

Dosage Forms ◽

Modified Release ◽

Solid Dosage Forms ◽

Solid Dosage Form ◽

Solid Dosage ◽

Enhanced Solubility ◽

Hot Melt

In this work, modified-release solid dosage forms were fabricated by adjusting geometrical properties of solid dosage forms through hot-melt 3D extrusion (3D HME). Using a 3D printer with air pressure driving HME system, solid dosage forms containing ibuprofen (IBF), polyvinyl pyrrolidone (PVP), and polyethylene glycol (PEG) were printed by simultaneous HME and 3D deposition. Printed solid dosage forms were evaluated for their physicochemical properties, dissolution rates, and floatable behavior. Results revealed that IBF content in the solid dosage form could be individualized by adjusting the volume of solid dosage form. IBF was dispersed as amorphous state with enhanced solubility and dissolution rate in a polymer solid dosage form matrix. Due to absence of a disintegrant, sustained release of IBF from printed solid dosage forms was observed in phosphate buffer at pH 6.8. The dissolution rate of IBF was dependent on geometric properties of the solid dosage form. The dissolution rate of IBF could be modified by merging two different geometries into one solid dosage form. In this study, the 3D HME process showed high reproducibility and accuracy for preparing dosage forms. API dosage and release profile were found to be customizable by modifying or combining 3D modeling.

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Preparation and characterization of rilpivirine solid dispersions with the application of enhanced solubility and dissolution rate

Beni-Suef University Journal of Basic and Applied Sciences ◽

10.1016/j.bjbas.2015.02.010 ◽

2015 ◽

Vol 4 (1) ◽

pp. 71-79 ◽

Cited By ~ 4

Author(s):

Pavan kommavarapu ◽

Arthanareeswari Maruthapillai ◽

Kamaraj Palanisamy ◽

Manasvi Sunkara

Keyword(s):

Dissolution Rate ◽

Solid Dispersions ◽

Enhanced Solubility

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Discovery, Characterization, and Pharmaceutical Applications of Two Loratadine–Oxalic Acid Cocrystals

Crystals ◽

10.3390/cryst10110996 ◽

2020 ◽

Vol 10 (11) ◽

pp. 996

Author(s):

Zhengxuan Liang ◽

Hongbo Chen ◽

Chenguang Wang ◽

Changquan Calvin Sun

Keyword(s):

Oxalic Acid ◽

Dissolution Rate ◽

Physical Stability ◽

Formulation Development ◽

Intrinsic Dissolution ◽

Intrinsic Dissolution Rate ◽

Conjugate Acid ◽

Enhanced Solubility ◽

Antihistamine Drug ◽

Low Solubility

Loratadine (Lor) is an antihistamine drug commonly used to relieve the symptoms of allergy. It has high permeability but low solubility under physiological conditions. To overcome the problem of low solubility, we synthesized and characterized two Loratadine multi-component crystalline phases with oxalic acid (Oxa), i.e., a 1:1 Lor-Oxa conjugate acid-base (CAB) cocrystal (Lor-Oxa CAB) and a 2:1 Lor-Oxa cocrystal monohydrate (Lor-Oxa hydrate). Both cocrystals exhibited an enhanced solubility and intrinsic dissolution rate (IDR) compared to Lor and adequate physical stability. The intrinsic dissolution rate of Lor-Oxa CAB is 95 times that of Lor, which makes it a promising candidate for tablet formulation development.

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Mechanochemical Formation of Racemic Praziquantel Hemihydrate with Improved Biopharmaceutical Properties

Pharmaceutics ◽

10.3390/pharmaceutics12030289 ◽

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.

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