Oral self emulsifying powder of lercanidipine hydrochloride: Formulation and evaluation

Kallakunta, Venkata Raman; Bandari, Suresh; Jukanti, Raju; Veerareddy, Prabhakar Reddy

doi:10.1016/j.powtec.2012.01.032

Cited by 123 publications

(68 citation statements)

References 25 publications

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“…Chemically it is 2[(3,3-diphenylpropyl) (methyl) amino]-1, 1-dimethylethyl methyl 2,6-dimethyl-4-(3-nitrophenyl)-1, 4-dihydropyridine-3, 5-dicarboxylate hydrochloride (16). As per BCS classification, lercanidipine HCl is a BCS class II drug that is freely soluble in methanol and practically insoluble in water, having a pKa value of 6.83 (17,18). Commercially, it is available in tablet dosage forms in strengths of 10 and 20 mg. Lercanidipine HCl is not official in any pharmacopeia and currently no quality control or discriminatory dissolution method is available for raw material and tablets (19).…”

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confidence: 99%

Dissolution Method Development and Validation for Lercanidipine Hydrochloride Tablets

Shaikh¹,

Patel²,

Patel³

et al. 2018

Dissolution Technol.

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Lercanidipine hydrochloride (HCl) is L-type calcium channel blocker widely used in the management of hypertension. According to the BCS classification system, it is classified under BCS class II drugs, showing low solubility and high permeability. The dissolution profile and thus the in vivo performance of this class of drugs widely depend on their solubility and hence their behaviour in dissolution medium. Lercanidipine HCl is not official in any pharmacopeia, so no official dissolution method is available. The present work is mainly focussed on development and validation of a dissolution test that can be used as a quality control test for lercanidipine HCl tablets and formulations. Saturation solubility and sink conditions that can be achieved in different media suggested that 0.1 N HCl, acetate buffer pH 4.5, and phosphate buffer pH 6.8 can be used as a dissolution medium. Dissolution tests of lercanidipine HCl tablets were carried out in these different media at different rotation speeds using a USP type II (paddle) apparatus. The most suitable dissolution conditions were 0.1 N HCl pH 1.2 (900 mL at 37 ± 0.5 °C) as a dissolution medium and a paddle apparatus at 100 rpm for 60 min. The analysis of released lercanidipine HCl was done by ultraviolet spectrophotometry. The developed method was validated according to ICH guidelines. This method showed linearity with an r 2 value of 0.999 within the concentration range of 2-20 µg/mL. The method was found to be accurate with recoveries ranging from 98.50% to 103.72%. The interday and intraday precision was below RSD 2%. The developed method can effectively be used for quality control evaluation of lercanidipine HCl tablets.

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mentioning

confidence: 99%

Dissolution Method Development and Validation for Lercanidipine Hydrochloride Tablets

Shaikh¹,

Patel²,

Patel³

et al. 2018

Dissolution Technol.

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“…Since both drug solubilization and formulation stability will decline with this phase separation, the cloud point of the formulation should be higher enough than 37°C (body temperature). 27,31 In this study, both nanocarrier formulations exhibited cloudiness at 85°C, with a drop in percentage transmittance from 95.5% ± 0.071% to 74.8% ± 2.899%. Results confirmed the stability of all SNEDDS formulations regarding separation at gastrointestinal tract temperature.…”

Section: Cloud-point Measurementmentioning

confidence: 54%

Nanoemulsion liquid preconcentrates for raloxifene hydrochloride: optimization and in vivo appraisal

Elsheikh¹,

Elnaggar²,

Gohar³

et al. 2012

IJN

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Raloxifene hydrochloride (RLX) is a selective estrogen-receptor modulator for treatment of osteoporosis and prevention of breast and endometrial cancer. By virtue of extensive presystemic clearance, RLX bioavailability is only 2%. The current study aimed to tailor and characterize RLX-loaded self-nanoemulsifying drug-delivery systems (SNEDDS) using bioactive excipients affecting drug metabolism. The potential of oral nanocarriers to enhance RLX delivery to endocrine target organs was assessed in fasted and fed female Wistar rats using high-performance liquid chromatography. RLX was loaded in the dissolved and dispersed status in the alkalinized (A-SNEDDS) and nonalkalinized (NA-SNEDDS) systems, respectively. Optimization and assessment relied on solubility studies, emulsification efficiency, phase diagrams, dilution robustness, cloud point, particle size, zeta potential (ZP), polydispersity index (PDI), and transmission electron microscopy. In vitro release was assessed using dialysis bag versus dissolution cup methods. NA-SNEDDS were developed with suitable globule size (38.49 ± 4.30 nm), ZP (31.70 ± 3.58 mV), PDI (0.31 ± 0.02), and cloud point (85°C). A-SNEDDS exhibited good globule size (35 ± 2.80 nm), adequate PDI (0.28 ± 0.06), and lower ZP magnitude (−21.20 ± 3.46 mV). Transmission electron microscopy revealed spherical globules and contended data of size analysis. Release studies demonstrated a nonsignificant enhancement of RLX release from NA-SNEDDS compared to drug suspension with the lowest release shown by A-SNEDDS. A conflicting result was elucidated from in vivo trial. A significant enhancement in RLX uptake by endocrine organs was observed after nanocarrier administration compared to RLX suspension. In vivo studies reflected a poor in vitro/in vivo correlation, recommended nanocarrier administration before meals, and did not reveal any advantage for drug loading in the solubilized form (A-SNEDDS). To conclude, NA-SNEDDS possessed superior in vitro characteristics to A-SNEDDS, with equal in vivo potential. NA-SNEDDS elaborated in this work could successfully double RLX delivery to endocrine target organs, with promising consequences of lower dose and side effects of the drug.

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“…The resultant weakened emulsions were checked physically for any physical changes, for example, (coalescence of droplet, precipitation or phase separation) after 24 h keeping [2] 7) Viscosity [21] Brookfield DV III ultra V6.0 RV cone and plate rheometer (Brookfield Engineering Laboratories, Inc, Middleboro, MA, axle # CPE40) was utilized to decide the thickness of various plans at 25±1.0°C.…”

Section: ) Effect Of Ph and Robustnessmentioning

confidence: 99%

Self-Emulsifying Drug Delivery System

Talegave¹

2017

WJPR

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Self-emulsifying drug delivery system are the unique mixture of oil, solvent surfactant, co-surfactant, co-solvents. These are the effective approach to solving the solubility of poorly soluble drug. From couple of years aqueous solubility is biggest issues to the formulator for formulation and development of novel drug delivery. SEDDSs are Good strategy for enhancement of oral absorption and bioavailability of BCS class 2 and class 4 drugs. For these system oral route is most convenient than other route. Requirement of this system is due to poor solubility and oral absorption of highly lipid soluble drug. Those drug which is formulated by SEDDS will have good pharmaceutical market. These system have ability to form emulsification with the solid as well as liquid dosage form .SEDDS are very quickly dispersed in the gastro-intestinal fluid and making micro or Nano-emulsion containing solubilized drug. These article covers formulation, Evaluation, future aspect and application part of self-emulsifying drug delivery system.

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Oral self emulsifying powder of lercanidipine hydrochloride: Formulation and evaluation

Cited by 123 publications

References 25 publications

Dissolution Method Development and Validation for Lercanidipine Hydrochloride Tablets

Dissolution Method Development and Validation for Lercanidipine Hydrochloride Tablets

Nanoemulsion liquid preconcentrates for raloxifene hydrochloride: optimization and in vivo appraisal

Self-Emulsifying Drug Delivery System

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