Preparation and characterization of rilpivirine solid dispersions with the application of 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.v4i2.10440 S. J. Pharm. Sci. 4(2) 2011: 48-57

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DEVELOPMENT OF AMORPHOUS BINARY AND TERNARY SOLID DISPERSIONS OF NATEGLINIDE FOR IMPROVED SOLUBILITY AND DISSOLUTION

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2020v12i4.37600 ◽

2020 ◽

pp. 106-112

Author(s):

SHRADHA S. TIWARI ◽

SHAILESH J. WADHER ◽

SURENDRA G. GATTANI

Keyword(s):

Solid Dispersion ◽

Water Solubility ◽

Solid Dispersions ◽

Physicochemical Characterization ◽

Dissolution Behavior ◽

Enhanced Solubility ◽

Ft Ir ◽

Ternary Solid Dispersion ◽

Ternary Solid Dispersions

Objective: Nateglinide is a commonly used oral hypoglycemic, biopharmaceutical classification system Class II drug, which shows relatively poor water solubility and variable bioavailability. The objective of the present investigation was to develop the binary and ternary solid dispersions of nateglinide for improved solubility and dissolution. Methods: Nateglinide solid dispersions were prepared by a common solvent evaporation method. Polymers like soluplus, kolliphor P188, sylloid 244FP, gelucire 48/16, affinisol (HPMCAS), HPβCD, βCD were used in different combinations. The physicochemical characterization of the optimized ternary dispersion was studied by using FT-IR, DSC, and PXRD. Solubility and dissolution behavior of all dispersions were studied. Result: From all prepared ternary solid dispersions, nateglinide dissolution was significantly faster than pure nateglinide. With ternary solid dispersion of NTG, soluplus and kolliphor P188 there was a big improvement in solubility and dissolution. This combination enhanced the solubility of NTG by 23 folds. Another ternary dispersion of NTG with soluplus and gelucire 48/16 enhanced solubility by 25 fold. Conclusion: Ternary solid dispersion found superior over binary dispersions. For the ternary dispersions, showing the best solubility, tablets were prepared. Dissolution and drug release from the formulated tablet was as good as a marketed product.

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Synthesis and Characterization of a New Norfloxacin/Resorcinol Cocrystal with Enhanced Solubility and Dissolution Profile

Pharmaceutics ◽

10.3390/pharmaceutics14010049 ◽

2021 ◽

Vol 14 (1) ◽

pp. 49

Author(s):

Hanan Fael ◽

Rafael Barbas ◽

Rafel Prohens ◽

Clara Ràfols ◽

Elisabet Fuguet

Keyword(s):

Dissolution Rate ◽

Shake Flask ◽

Ph Value ◽

Dissolution Profile ◽

Ph Values ◽

Enhanced Solubility ◽

Poorly Soluble ◽

Transformation Experiment ◽

Solvent Mediated Transformation

A new cocrystal of Norfloxacin, a poorly soluble fluoroquinolone antibiotic, has been synthetized by a solvent-mediated transformation experiment in toluene, using resorcinol as a coformer. The new cocrystal exists in both anhydrous and monohydrate forms with the same (1:1) Norfloxacin/resorcinol stoichiometry. The solubility of Norfloxacin and the hydrated cocrystal were determined by the shake-flask method. While Norfloxacin has a solubility of 0.32 ± 0.02 mg/mL, the cocrystal has a solubility of 2.64 ± 0.39 mg/mL, approximately 10-fold higher. The dissolution rate was tested at four biorelevant pH levels of the gastrointestinal tract: 2.0, 4.0, 5.5, and 7.4. In a first set of comparative tests, the dissolution rate of Norfloxacin and the cocrystal was determined separately at each pH value. Both solid forms showed the highest dissolution rate at pH 2.0, where Norfloxacin is totally protonated. Then, the dissolution rate decreases as pH increases. In a second set of experiments, the dissolution of the cocrystal was evaluated by a unique dissolution test, in which the pH dynamically changed from 2.0 to 7.4, stepping 30 min at each of the four biorelevant pH values. Results were quite different in this case, since dissolution at pH 2 affects the behavior of Norfloxacin at the rest of the pH values.

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ENHANCEMENT OF GLIBENCLAMIDE DISSOLUTION RATE BY SOLID DISPERSION METHOD USING HPMC AND PVP

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i5.34137 ◽

2019 ◽

pp. 19-24 ◽

Cited By ~ 1

Author(s):

ARIF BUDIMAN ◽

IYAN SOPYAN ◽

DENIA SEPTY RIYANDI

Keyword(s):

Dissolution Rate ◽

Solid Dispersion ◽

Solid Dispersions ◽

Hydroxypropyl Methylcellulose ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

X Ray ◽

Rate Test ◽

Ft Ir

Objective: The aim of this study was to investigate the effects of changing in the proportions of the solid dispersion formula on the dissolution rate of glibenclamide. Methods: Solid dispersions were prepared by solvent evaporation method by using methanol as solvent, hydroxypropyl methylcellulose (HPMC) and polyvinyl pyrrolidone (PVP) as polymers. The prepared product was evaluated by the saturated solubility test and the dissolution rate test. The prepared product was characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD) and Scanning Electron Microscopy (SEM). Results: The result showed solid dispersion with a ratio of glibenclamide: PVP: HPMC (1: 3: 6) has the highest increase in solubility (20 fold) compared to pure glibenclamide. This formula also showed an improvement in dissolution rate from 19.9±1.19% (pure glibenclamide) to 99±1.60% in 60 min. Characterization of FT-IR showed that no chemical reaction occurred in solid dispersion of glibenclamide. The results of X-ray diffraction analysis showed an amorphous form in all solid dispersion formulas. The results of DSC analysis showed that endothermic peak melting point of solid dispersion occurred, and the morphology of solid dispersion was more irregular than pure glibenclamide based on SEM characterization Conclusion: The solid dispersion of glibenclamide using PVP: HPMC as carriers can increase the solubility and dissolution rate compared to pure glibenclamide.

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RETRACTED ARTICLE: Preparation/characterization of solid dispersions and enhancement of dissolution rate on celecoxib as BCS II class

Journal of Pharmaceutical Investigation ◽

10.1007/s40005-013-0090-3 ◽

2013 ◽

Vol 44 (5) ◽

pp. 399-399 ◽

Cited By ~ 2

Author(s):

Jung Hwan Lee ◽

Young Lae Kim ◽

So Jin Lee ◽

Jaewon Yang ◽

Jin Young Park ◽

...

Keyword(s):

Dissolution Rate ◽

Solid Dispersions ◽

Retracted Article

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Characterization of solid dispersions of Patchouli alcohol with different polymers: effects on the inhibition of reprecipitation and the improvement of dissolution rate

Drug Development and Industrial Pharmacy ◽

10.3109/03639045.2013.877482 ◽

2014 ◽

Vol 41 (3) ◽

pp. 436-444 ◽

Cited By ~ 4

Author(s):

Yun Long Chen ◽

Jin Bin Liao ◽

Yong Zhuo Liang ◽

Jian Hui Xie ◽

Qiong Wu ◽

...

Keyword(s):

Dissolution Rate ◽

Solid Dispersions ◽

Patchouli Alcohol

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Improvement of Solubility and Dissolution of Rilpivirine Solid Dispersions by Solvent Evaporation Technique and Novel Carriers

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2018.11.4.5 ◽

2018 ◽

Vol 11 (4) ◽

pp. 4177-4184

Author(s):

Bhikshapathi D. V. R. N. ◽

Vishwa M

Keyword(s):

Drug Release ◽

Dissolution Rate ◽

Solid Dispersion ◽

Drug Carrier ◽

Solid Dispersions ◽

Immediate Release ◽

Solvent Evaporation ◽

Onset Of Action ◽

Enhanced Solubility ◽

Evaporation Technique

Rilpivirine benzonitrile is a pharmaceutical drug used for the treatment of HIV infection it is characterized with poor solubility that limits its absorption and dissolution rate, which delays onset of action. In the present study, immediate release solid dispersion of antiretroviral Rilpivirine was formulated by solvent evaporation technique. Eighteen solid dispersions were prepared with 1:1:1, 1:2:1 and 1:3:1 ratios of drug: carrier: surfactant. There was significant improvement in the rate of drug release from all 18 solid dispersions and the formulation (SE12) comprising Rilpivirine: Kolliwax GMS II: SLS in 1:3:1 by solvent evaporation process has shown enhanced solubility about 30 folds and significant improvement in the rate of drug release. From powder X-ray diffraction (p-XRD) and by scanning electron microscopy (SEM) studies it was evident that polymorphic form of Rilpivirine has been converted into an amorphous form from crystalline within the solid dispersion formulation. The obtained results suggested that developed solid dispersion by solvent evaporation method might be an efficacious approach for enhancing the solubility and dissolution rate of Rilpivirine.

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