In-situ freeze-drying - forming amorphous solids directly within capsules: An investigation of dissolution enhancement for a poorly soluble drug

In this study, a solubility enhancing technique, Self-emulsifying drug delivery system (SEDDS), was considered to be developed for Ibuprofen, a poorly soluble drug. Capmul PG 8 was used as a co-solvent. As surfactant, hydrophilic surfactant Cremophor EL was considered. A fixed amount of Ibuprofen was added with fixed amount of excipients. Capmul PG8 showed a good solubilizing capacity which dissolved 300 mg/ml of Ibuprofen. Cremophor EL also showed a good solubilizing capacity which dissolved 300 mg/ml of Ibuprofen. Ibuprofen is a poorly soluble drug which was used as experimental drug and pH 7.2 phosphate buffer was used as dissolution medium. The amount of drug was measured form the absorbance of UV spectrophotometer at 221 nm. A 3-level factorial design was carried out to optimize the formulation using design expert software trial version 8.0.3.1. Capmul PG8 and Cremophor EL were used as independent variables where percent drug release at 5, 15 and 45 minutes. The optimized formula contains 24.10 mg Capmul PG8 and 71.02 mg Cremophor EL which releases 27.78%, 44.6% and 74.24% ibuprofen at the mentioned time interval. The present study shows that the Capmul PG8 and Cremophor EL have effect the release profile of capsule Ibuprofen. It is found that it is possible to increase the release of Ibuprofen by using Capmul PG8 and Cremophor EL. DOI: http://dx.doi.org/10.3329/icpj.v1i6.10535 International Current Pharmaceutical Journal 2012, 1(6): 138-150

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APPLICATION OF LIQUISOLID TECHNIQUE FOR ENHANCEMENT OF DISSOLUTION OF WATER INSOLUBLE DRUG CHOLECALCIFEROL

INDIAN DRUGS ◽

10.53879/id.58.01.12717 ◽

2021 ◽

Vol 58 (01) ◽

pp. 64-72

Author(s):

Preha Handa ◽

◽

Nagoji Shinde ◽

Bhagvati Sivabalan ◽

Akhilesh Varma ◽

...

Keyword(s):

Oral Delivery ◽

Dissolution Enhancement ◽

Maximum Solubility ◽

Drug Candidates ◽

Poorly Soluble ◽

Burman Design ◽

Poorly Soluble Drug ◽

Plackett Burman Design ◽

Low Solubility ◽

Better Than

The issue of low solubility and bioavailability poses a significant challenge for most of the drug candidates for oral delivery. Liquisolid, a recently evolved technique for dissolution enhancement, can dodge these barriers. The purpose of this research was to increase the solubility of poorly soluble drug cholecalciferol by liquisolid technique. The cholecalciferol’s solubility studies were performed in a mixture of Polysorbate 80 and PEG 400 in different ratios (1:1, 1:2, 2:1, 1:3, and 3:1). Maximum solubility was observed in a 1:2 ratio. There were changes in the X-ray diffractogram and shifting of the endothermic peak in DSC from 85oC to 146oC, which indicated the drug’s conversion into an amorphous form. The liquisolid form was adsorbed on the carrier material and compressed. The optimization was done by using Plackett Burman Design with Design-Expert software. It was observed that the drugs release profile of the optimized formulation was better than the generic product and was comparable to Divisun tablets 2000 I.U (Innovator).

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Using pH Gradient Dissolution with In-Situ Flux Measurement to Evaluate Bioavailability and DDI for Formulated Poorly Soluble Drug Products

AAPS PharmSciTech ◽

10.1208/s12249-018-1164-3 ◽

2018 ◽

Vol 19 (7) ◽

pp. 2898-2907 ◽

Cited By ~ 4

Author(s):

Jane Li ◽

Konstantin Tsinman ◽

Oksana Tsinman ◽

Larry Wigman

Keyword(s):

Flux Measurement ◽

Ph Gradient ◽

Drug Products ◽

Poorly Soluble ◽

Poorly Soluble Drug

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Dissolution Enhancement of Atorvastatin Calcium by Cocrystallization

Advanced Pharmaceutical Bulletin ◽

10.15171/apb.2019.064 ◽

2019 ◽

Vol 9 (4) ◽

pp. 559-570 ◽

Cited By ~ 1

Author(s):

Reham Al-Kazemi ◽

Yacoub Al-Basarah ◽

Aly Nada

Keyword(s):

Dissolution Rate ◽

Dissolution Enhancement ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

Atorvastatin Calcium ◽

Molar Ratios ◽

Poorly Soluble ◽

Poorly Soluble Drug ◽

Physical Mixtures ◽

Biopharmaceutical Classification System

Purpose: To enhance the dissolution rate of the poorly soluble drug atorvastatin calcium (ATC) bycocrystallization with selected coformers. Enhancement of the dissolution rate and solubility of thedrug, which is classified as Class II of the Biopharmaceutical Classification System (BCS), is expectedto enhance the bioavailability.Methods: Two methods were used for preparing the cocrystals, solvent drop grinding (SDG) andsolvent evaporation (SE) method using 1:1, 1:3, and 1:10 drug-coformer molar ratios. Glucosaminehydrochloride (GluN) and nicotinamide (NIC) were investigated as coformers. The cocrystals,their physical mixtures, and the raw ATC were characterized by fourier transform infrared (FTIRspectroscopy), differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), massspectroscopy (MS), scanning electron microscopy (SEM), solubility, and dissolution rate studies.Results: SDG and SE were effective in improving the dissolution rate of ATC with both coformers.Drug: coformer ratio 1:3 was optimum. The solubility values for ATC, GluN-, and NIC-cocrystals were26, to 35 and 50 μg/mL, respectively. The dissolution rate of ATC from cocrystals was > 90% after 5minutes, compared to 41% untreated ATC.Conclusion: Cocrystallization significantly improved the solubility and dissolution, in comparison tothe untreated ATC.<br />

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In Situ Determination of the Increase in Saturation Solubility of Nanocrystals of Poorly Soluble Drugs

10.26226/morressier.57d6b2bdd462b8028d88d9ab ◽

2016 ◽

Author(s):

Roland Bodmeier

Keyword(s):

Poorly Soluble Drugs ◽

Saturation Solubility ◽

Poorly Soluble

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Studies on the Preparation, Characterization and Solubility of -Cyclodextrin-Roxythromycin Inclusion Complexes

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2009.2.2.5 ◽

2009 ◽

Vol 2 (2) ◽

pp. 523-530

Author(s):

D. Nagasamy Venkatesh ◽

S. Karthick ◽

M. Umesh ◽

G. Vivek ◽

R.M. Valliappan ◽

...

Keyword(s):

Dissolution Rate ◽

Inclusion Complexes ◽

Phase Solubility ◽

X Ray Diffraction ◽

Scanning Calorimetry ◽

X Ray ◽

Ir Studies ◽

Poorly Soluble ◽

Poorly Soluble Drug

Roxythromycin/ β-cyclodextrin (Roxy/ β-CD) dispersions were prepared with a view to study the influence of β-CD on the solubility and dissolution rate of this poorly soluble drug. Phase-solubility profile indicated that the solubility of roxythromycin was significantly increased in the presence of β-cyclodextrin and was classified as AL-type, indicating the 1:1 stoichiometric inclusion complexes. Physical characterization of the prepared systems was carried out by differential scanning calorimetry (DSC), X-ray diffraction studies (XRD) and IR studies. Solid state characterization of the drug β-CD binary system using XRD, FTIR and DSC revealed distinct loss of drug crystallinity in the formulation, ostensibly accounting for enhancement of dissolution rate.

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