New Formulation Technique for Solubility and Dissolution Rate Enhancement of Poorly Soluble Drugs

Harmalkar, Divya; Godinho, Soraiya; Bhide, Prashant Jivaji; Kumar, Lalit; Shirodkar, Rupesh Kalidas

doi:10.1007/s11094-019-02069-x

Cited by 5 publications

(5 citation statements)

References 13 publications

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“…The FTIR spectrum of EBS exhibited characteristic bands at 3051 cm -1 for C-H stretching of the ring, 2943,2916, 2819 cm -1 for CH-stretch of ( CH3 and CH2), also strong and sharp band at 1678 cm -1 for ketonic carbonyl group (C=O stretch), 1454 cm -1 for aromatic C=C stretch of phenyl ring, and C-N stretching at 1269cm -1 . These results were in agreement with the previous studies (35)(36)(37) . The FTIR spectrum of CCS exhibited characteristic bands at 3360 and 3240 cm -1 for alcoholic O-H groups, 2904 cm -1 for aliphatic C-H stretching of (CH2), and weak band at 1732, 1720 cm -1 for C=O of carboxylic groups.…”

Section: Fourier Transforms Infrared Spectroscopy (Ftir)supporting

confidence: 94%

“…The diffraction pattern of the pure EBS showed a highly crystalline nature, indicated by numerous intensive peaks at a diffraction angle of 2θ (5.84°, 11.54°, 18.68°, 19.06°, 19.39°) throughout the scanning range. These values approached the previously reported data (36,39) . On the other hand, the CCS diffractogram did not show sharp peaks, but only some peaks with low intensity at 18.41°, 22.9°, 43.95°, 64.29°, 77.38° related to its amorphous nature (40) .…”

Section: Powder X-ray Diffraction (Pxrd)supporting

confidence: 92%

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Solubility and Dissolution Enhancement of Ebastine by Surface Solid Dispersion Technique

Hussein¹,

Al-Khedairy

2021

IJPS

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Ebastine (EBS) is a non-sedating antihistamine with a long duration of action. This drug has predominantly hydrophobic property causing a low solubility and low bioavailability. Surface solid dispersions (SSD) is an effective technique for improving the solubility and dissolution rate of poorly soluble drugs by using hydrophilic water insoluble carriers. The present study aims to enhance the solubility and dissolution rate of EBS by using surface solid dispersion technique. Avicel® PH101, Avicel® PH 102, croscarmellose sodium(CCS) and sodium starch glycolate(SSG) were used as water insoluble hydrophilic carriers. The SSD formulations of EBS were prepared by the solvent evaporation method in different drug: carrier weight ratios and evaluated for their percentage yield, drug content , water solubility, dissolution study in 0.1 N HCl, crystal lattice using powder X-ray diffraction (PXRD) and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier interaction. Most of the prepared SSD formulas showed improvement of drug solubility. The best result was obtained with formula SSD16 (EBS:CCS 1:15) that showed high percentage yield (98.5%), high drug content (98.39%) and 8.2 fold increase in solubility compared to solubility of pure drug with improved dissolution rate. The drug was converted to amorphous form without chemical interaction with the carrier.

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Section: Fourier Transforms Infrared Spectroscopy (Ftir)supporting

confidence: 94%

Section: Powder X-ray Diffraction (Pxrd)supporting

confidence: 92%

Solubility and Dissolution Enhancement of Ebastine by Surface Solid Dispersion Technique

Hussein¹,

Al-Khedairy

2021

IJPS

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“…To obtain maximum therapeutic benefits from EBT, its oral bioavailability should be enhanced [ 7 ]. For that purpose, several approaches have been employed by scientists to increase the bioavailability of EBT, such as complexation, nanoparticle formulation, fast disintegrating tablets and microemulsion, as well as spray drying technique [ 8 , 9 , 10 , 11 ]. Importantly, researchers are also exploring different ways to enhance absorptions of drug molecules to increase oral bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

et al. 2021

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The main objective of this research work was the development and evaluation of transfersomes integrated oral films for the bioavailability enhancement of Ebastine (EBT) to treat allergic rhinitis. The flexible transfersomes, consisting of drug (EBT), lipid (Phosphatidylcholine) and edge activator (EA) Polyoxyethylene sorbitan monooleate or Sorbitan monolaurate, were prepared with the conventional thin film hydration method. The developed transfersomes were further integrated into oral films using the solvent casting method. Transfersomes were evaluated for their size distribution, surface charge, entrapment efficiency (EE%) and relative deformability, whereas the formulated oral films were characterized for weight, thickness, pH, folding endurance, tensile strength, % of elongation, degree of crystallinity, water content, content uniformity, in vitro drug release and ex vivo permeation, as well as in vivo pharmacokinetic and pharmacodynamics profile. The mean hydrodynamic diameter of transfersomes was detected to be 75.87 ± 0.55 nm with an average PDI and zeta potential of 0.089 ± 0.01 and 33.5 ± 0.39 mV, respectively. The highest deformability of transfersomes of 18.52 mg/s was observed in the VS-3 formulation. The average entrapment efficiency of the transfersomes was about 95.15 ± 1.4%. Transfersomal oral films were found smooth with an average weight, thickness and tensile strength of 174.72 ± 2.3 mg, 0.313 ± 0.03 mm and 36.4 ± 1.1 MPa, respectively. The folding endurance, pH and elongation were found 132 ± 1, 6.8 ± 0.2 and 10.03 ± 0.4%, respectively. The ex vivo permeability of EBT from formulation ETF-5 was found to be approximately 2.86 folds higher than the pure drug and 1.81 folds higher than plain film (i.e., without loaded transfersomes). The relative oral bioavailability of ETF-5 was 2.95- and 1.7-fold higher than that of EBT-suspension and plain film, respectively. In addition, ETF-5 suppressed the wheal and flare completely within 24 h. Based on the physicochemical considerations, as well as in vitro and in vivo characterizations, it is concluded that the highly flexible transfersomal oral films (TOFs) effectively improved the bioavailability and antihistamine activity of EBT.

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“…Histamine is one of the prominent mediators of most forms of urticaria; therefore, antihistamines (especially H 1 antihistamines) are usually used for the treatment of patients with chronic urticaria (Harmalkar et al., 2019 ; Mehetre et al., 2019 ). Clinically, urticaria is found in all age groups.…”

Section: Introductionmentioning

confidence: 99%

Carbopol emulgel loaded with ebastine for urticaria: development, characterization,in vitroandin vivoevaluation

et al. 2021

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Urticaria affects all age groups of a population. It is triggered by allergens in foods, insect bites, medications, and environmental conditions. Urticaria is characterized by itching, a burning sensation, wheals and flares, erythema, and localized edema. The aim of this study was to develop a polymeric dosage form of ebastine using Carbopol 940 and mixture of span and tween. The emulsion was prepared, the gelling agent was added and the desired emulgel loaded with active drug was formulated. The formulations were subjected to physical stability, pH, viscosity, spreadability, drug content analysis, thermal analysis, in vitro drug release, and in vivo anti-allergic activity in animal model. The formulated emulgel exhibited good physical stability. The pH of the formulation was in the range of 5.2 ± 0.17 to 5.5 ± 0.20 which is suitable for topical application. Insignificant changes ( p > .05) were observed in viscosity and spreadability of stored emulgels. The drug content was in the official limit of Pharmacopeia (i.e. 100 ± 10%). DSC measurements predicted that there is no interaction between the active moiety and excipients in emulgel formulation. The optimized formulation (ES3) released 74.25 ± 1.8% of ebastine after 12 h. The ebastine emulgel showed significant ( p < .05; ANOVA) in vivo anti-allergic activity as compared to commercial product Benadryl ® in histamine-induced allergy in rabbits. This study concluded that a topical drug delivery of ebastine-loaded emulgel could be well tolerated and safe for the treatment of urticaria/hives.

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New Formulation Technique for Solubility and Dissolution Rate Enhancement of Poorly Soluble Drugs

Cited by 5 publications

References 13 publications

Solubility and Dissolution Enhancement of Ebastine by Surface Solid Dispersion Technique

Solubility and Dissolution Enhancement of Ebastine by Surface Solid Dispersion Technique

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

Carbopol emulgel loaded with ebastine for urticaria: development, characterization,in vitroandin vivoevaluation

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