Preparation and in vitro/in vivo evaluation of revaprazan hydrochloride nanosuspension

Li, Wei; Yang, Yonggang; Tian, Yuan; Xu, Xinlan; Chen, Yang; Mu, Liwei; Zhang, Yaqiong; Fang, Liang

doi:10.1016/j.ijpharm.2011.01.059

Cited by 63 publications

(23 citation statements)

References 23 publications

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“…The enthalpy value for the drug nanosuspension was found to be very less as compared to plain CRV. This decrease in enthalpy value and low melting point indicate low lattice energy and it was very well reported that the particles with lower lattice energy are easier to dissolve (32).…”

Section: Discussionsupporting

confidence: 55%

Nanosuspension Based In Situ Gelling Nasal Spray of Carvedilol: Development, In Vitro and In Vivo Characterization

2012

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Abstract. The objective of the present investigation was to develop in situ gelling nasal spray formulation of carvedilol (CRV) nanosuspension to improve the bioavailability and therapeutic efficiency. Solvent precipitation-ultrasonication method was opted for the preparation of CRV nanosuspension which further incorporated into the in situ gelling polymer phase. Optimized formulation was extensively characterized for various physical parameters like in situ gelation, rheological properties and in vitro drug release. Formation of in situ gel upon contact with nasal fluid was conferred via the use of ion-activated gellan gum as carrier. In vivo studies in rabbits were performed comparing the nasal bioavailability of CRV after oral, nasal, and intravenous administration. Optimized CRV nanosuspension prepared by combination of poloxamer 407 and oleic acid showed good particle size [d (0.9); 0.19 μm], zeta potential (+10.2 mV) and polydispersity (span; 0.63). The formulation containing 0.5%w/v gellan gum demonstrated good gelation ability and desired sustained drug release over period of 12 h. In vivo pharmacokinetic study revealed that the absolute bioavailability of in situ nasal spray formulation (69.38%) was significantly increased as compared to orally administered CRV (25.96%) with mean residence time 8.65 h. Hence, such in situ gel system containing drug nanosuspension is a promising approach for the intranasal delivery in order to increase nasal mucosal permeability and in vivo residence time which altogether improves drug bioavailability.

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Section: Discussionsupporting

confidence: 55%

Nanosuspension Based In Situ Gelling Nasal Spray of Carvedilol: Development, In Vitro and In Vivo Characterization

2012

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“…9 Nanosuspension is more applicable for drugs that are characterized by high permeability and low solubility such as revaprazan. 10 Nanosuspension can be prepared either by the precipitation "bottom-up" or by the disintegration "top-down" technologies. The top-down technologies, which are sometimes also called comminution, include high-pressure homogenization, media milling, and a combination of precipitation and high-pressure/ultrasonic homogenization.…”

Section: Introductionmentioning

confidence: 99%

Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation

Ahmed¹

2016

IJN

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In this study, optimized freeze-dried finasteride nanoparticles (NPs) were prepared from drug nanosuspension formulation that was developed using the bottom–up technique. The effects of four formulation and processing variables that affect the particle size and solubility enhancement of the NPs were explored using the response surface optimization design. The optimized formulation was morphologically characterized using transmission electron microscopy (TEM). Physicochemical interaction among the studied components was investigated. Crystalline change was investigated using X-ray powder diffraction (XRPD). Crystal growth of the freeze-dried NPs was compared to the corresponding aqueous drug nanosuspension. Freeze-dried NPs formulation was subsequently loaded into hard gelatin capsules that were examined for in vitro dissolution and pharmacokinetic behavior. Results revealed that in most of the studied variables, some of the quadratic and interaction effects had a significant effect on the studied responses. TEM image illustrated homogeneity and shape of the prepared NPs. No interaction among components was noticed. XRPD confirmed crystalline state change in the optimized NPs. An enhancement in the dissolution rate of more than 2.5 times from capsules filled with optimum drug NPs, when compared to capsules filled with pure drug, was obtained. Crystal growth, due to Ostwald ripening phenomenon and positive Gibbs free energy, was reduced following lyophilization of the nanosuspension formulation. Pharmacokinetic parameters from drug NPs were superior to that of pure drug and drug microparticles. In conclusion, freeze-dried NPs based on drug nanosuspension formulation is a successful technique in enhancing stability, solubility, and in vitro dissolution of poorly water-soluble drugs with possible impact on the drug bioavailability.

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“…In-vitro Dissolution Studies: 21,36,37 In-vitro dissolution of Diacerein nanosuspension was studied for 60 min using USP apparatus type 2 (paddle type) at 75 rpm (Electrolab Dissolution Tester TDT-06P, USP) using 900 ml citrate buffer pH 6.0 as dissolution medium maintained at 37°±5°C. Diacerein nanosuspension (5ml) was accurately inserted in the medium and sample aliquots of 5ml sample was withdrawn from the vessel and filtered through 0.22µm syringe filter at predetermined time intervals (2, 4, 6, 8, 10,15, 20, 30, 45 and 60 min) and replaced with 5ml fresh dissolution media.…”

Section: Differential Scanning Calorimetry (Dsc)mentioning

confidence: 99%

“…So, the aim of the current research work is to improve the aqueous solubility and dissolution rate of Diacerein via nanosuspension preparation. 28,29 . Poloxamer 407 with the concentration of 1% of the drug amount was used as stabilizer.…”

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confidence: 99%

Untitled

2017

IJPSR

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ABSTRACT:Diacerein is an Osteoarthritic drug that exhibited suboptimal oral bioavailability upon oral administration of conventional dosage form. Nanosuspension gaining more attention for improving oral bioavailability of such drugs. This study was aimed to enhance the solubility and dissolution of diacerein by preparing Nanosuspension. Diacerein Nanosuspension was prepared using combination of High Speed Homogenization (HSH) and Media Milling (MM), Poloxamer 407 (stabilizer) and ZrO 2 beads (milling media). Various formulation and processing parameters were optimized in preliminary studies. Concentration of stabilizer and milling media were optimized for Cumulative percentage release (%CPR), saturation solubility (SS) and mean particle size (MPS) using 3 2 full factorial design. Optimized batch was derived statistically using desirability function of Minitab17. Model was validated by formulating checkpoint batch. Accelerated stability study was carried out for optimized batch. Identification and compatibility study of drug and stabilizers were carried out using FTIR and DSC studies. Preliminary parameters were optimized by varying one parameter at a time, while keeping other constant by trial and error method. Optimized batch has 100%w/v milling media and 1%w/v of Poloxamer407. %CPR, SS and MPS were found to be 97.74%, 1.245mg/ml and 221.5nm respectively. Four hundred times enhancement in SS that of bulk drug and 97.74%CPR at 2min was observed after nanonization. It was concluded that Combination of HSH and MM technique can be successfully used for preparation of Diacerein Nanosuspension. Prepared nanosuspension significantly enhances solubility and in-vitro dissolution of Diacerein.

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Preparation and in vitro/in vivo evaluation of revaprazan hydrochloride nanosuspension

Cited by 63 publications

References 23 publications

Nanosuspension Based In Situ Gelling Nasal Spray of Carvedilol: Development, In Vitro and In Vivo Characterization

Nanosuspension Based In Situ Gelling Nasal Spray of Carvedilol: Development, In Vitro and In Vivo Characterization

Preparation of finasteride capsules-loaded drug nanoparticles: formulation, optimization, in vitro, and pharmacokinetic evaluation

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