Bioavailability Enhancement of Rizatriptan Benzoate by Oral Disintegrating Strip: In vitro and In vivo Evaluation

Bhagawati, S. T.; Chonkar, Ankita; Dengale, Swapnil J.; Reddy, Sreenivasa M; Bhat, Krishnamurthy

doi:10.2174/15672018113109990048

Cited by 6 publications

(6 citation statements)

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“…The MRT of the two formulations was 2.9 ± 0.7 h and 2.3 ± 0.9 h, respectively, indicating that the retention time of ZMT in vivo was nearly similar. The obtained results are consistent with the earlier work of Singh et al and Bhagawati et al [ 44 , 45 ]. The above results show improved absorption of ZMT-OFDFs compared to ZMT intragastric suspensions in the rats.…”

Section: Resultssupporting

confidence: 93%

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Development and Characterizations of Pullulan and Maltodextrin-Based Oral Fast-Dissolving Films Employing a Box–Behnken Experimental Design

et al. 2022

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Migraine is a neurological disorder characterized by severe headaches, visual aversions, auditory, and olfactory disorders, accompanied by nausea and vomiting. Zolmitriptan (ZMT®) is a potent 5HT1B/1D serotonin receptor agonist frequently used for the treatment of migraine. It has erratic absorption from the gastrointestinal tract (GIT), but its oral bioavailability is low (40–45%) due to the hepatic metabolism. This makes it an ideal candidate for oral fast dissolving formulations. Hence, the current study was undertaken to design and develop oral fast-dissolving films (OFDFs) containing ZMT for migraine treatment. The OFDFs were formulated by the solvent casting method (SCM) using Pullulan (PU) and maltodextrin (MDX) as film-forming agents and propylene glycol (PG) as a plasticizer. The strategy was designed using Box–Behnken experimental design considering the proportion of PU:MDX and percentage of PG as independent variables. The effectiveness of the OFDF’s was measured based on the following responses: drug release at five min, disintegration time (D-time), and tensile strength (TS). The influence of formulation factors, including percent elongation (%E), thickness, water content, moisture absorption, and folding endurance on ZMT-OFDFs, were also studied. The results showed a successful fabrication of stable ZMT-OFDFs, with surface uniformity and amorphous shape of ZMT in fabricated films. The optimized formulation showed a remarkable rapid dissolution, over 90% within the first 5 min, a fast D-time of 18 s, and excellent mechanical characteristics. Improved maximum plasma concentration (C max) and area under the curve (AUC 0–t) in animals (rats) treated with ZMT-OFDFs compared to those treated with an intra-gastric (i-g) suspension of ZMT were also observed. Copolymer OFDFs with ZMT is an exciting proposition with great potential for the treatment of migraine headache. This study offers a promising strategy for developing ZMT-OFDFs using SCM. ZMT-OFDFs showed remarkable rapid dissolution and fast D-time, which might endeavor ZMT-OFDFs as an auspicious alternative approach to improve patient compliance and shorten the onset time of ZMT in migraine treatment.

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Section: Resultssupporting

confidence: 93%

“…Whereas the SEM image of ZMT-OFDFs displayed a smooth surface without any scratches or traverse striations on the surface ( Figure 8 B). The results indicated the proper miscibility and uniform distribution of ZMT in the OFDFs [ 14 , 44 ].…”

Section: Resultsmentioning

confidence: 99%

Development and Characterizations of Pullulan and Maltodextrin-Based Oral Fast-Dissolving Films Employing a Box–Behnken Experimental Design

et al. 2022

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“…Furthermore, no significant (p < 0.05) variation in MRT between tested and reference formulations revealed that the RZT retention duration in vivo was approximately identical. The obtained results agree with previous studies [28,51]. However, the pharmacokinetic parameters of RZT-ODFs were only preliminary investigated in rats.…”

Section: Supplementary Materialssupporting

confidence: 90%

“…In contrast, the SEM image of RZT-ODFs reveals a homogeneous surface devoid of cracks or transverse ridges (Figure 1B). The findings suggested adequate miscibility and a consistent dispersion of RZT throughout the ODFs [28].…”

Section: Appearance and Morphologymentioning

confidence: 89%

Rizatriptan-Loaded Oral Fast Dissolving Films: Design and Characterizations

Shah

Lina

et al. 2022

Pharmaceutics

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Rizatriptan (RZT) is an efficient anti-migraine drug which belongs to the class of selective 5 HT (1B/1D) serotonin receptor agonists. Nevertheless, RZT elicits several adverse effects and RZT nasal sprays have a limited half-life, requiring repeated doses that could cause patient noncompliance or harm to the nasopharynx and cilia. The current research aimed to develop orally disintegrating films (ODFs) of RZT employing maltodextrin (MTX) and pullulan (PUL) as film-forming polymers, as well as propylene glycol (PG) as a plasticizer. The ODFs were prepared by solvent casting method (SCM). The technique was optimized using Box–Behnken design (BBD), contemplating the ratios of PUL: MTX and different levels of PG (%) as factor variables. The influence of these factors was systematically analyzed on the selected dependent variables, including film thickness, disintegration time (D-time), folding endurance (FE), tensile strength (TS), percent elongation (%E), moisture content (%), and water uptake (%). In addition, the surface morphology, solid state analysis, drug content uniformity (%), drug release (%), and pH of the RZT-ODFs were also studied. The results demonstrated a satisfactory stable RZT-ODFs formulation that exhibited surface homogeneity and amorphous RZT in films with no discernible interactions between the model drug and polymeric materials. The optimized film showed a rapid D-time of 16 s and remarkable mechanical features. The in vitro dissolution kinetics showed that 100% RZT was released from optimized film compared to 61% RZT released from conventional RZT formulation in the initial 5 min. An animal pharmacokinetic (PK) investigation revealed that RZT-ODFs had a shorter time to achieve peak plasma concentration (Tmax), a higher maximum plasma concentration (Cmax), and area under the curve (AUC0−t) than traditional oral mini capsules. These findings proposed a progressive approach for developing anti-migraine drugs that could be useful in reducing the complications of dysphagia in geriatric and pediatric sufferers.

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“…The literature survey reveals that several analytical methods are reported for the determination of RIZ. Among these methods, liquid chromatography 22,23,24 , LC-MS/MS 25,26 , HPLC 27,28 are a few mention worth.…”

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confidence: 99%

Untitled

2020

IJPSR

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Simple, sensitive, and accurate spectrophotometry method one each for estimation of five drugs viz., chloroquine phosphate (CHP), granisetron hydrochloride (GRA), rizatriptan benzoate (RIZ), zoledronic acid (ZOL) and zolmitriptan (ZOT), have been developed. The method depends upon oxidation of each drug by excess N-Bromo succinimide (NS), and subsequent determination of UN reacted NBS by Rhodamine-B dye at λ max 557 nm. Beers law is obeyed between 2-14 µg mL-1 (for CHP); 52-14 µg mL-1 (for GRA); 1-7 µg mL-1 (for RIZ); 1-7 µg mL-1 (for ZOL) & 2-14 µg mL-1 (for ZOT). This method has been applied for the determination of drugs in their pure form as well as in tablet formulations. All the methods have been validated as per ICH guidelines. INTRODUCTION: Chloroquine Phosphate: Chloroquine phosphate (CHP) is an antimalarial drug whose structure is shown in Fig. 1A and chemically knows as 7chloro-4-4-diethylamino-1-methylbutyl amino-quinoline diphosphate. CHP is also used for the treatment of amebiasis, polymyositis, sarcoidosis rheumatoid arthritis, discoid lupus erythematosus, and photosensitive diseases 1. The literature survey reveals that several analytical methods are reported for the quantification of CHP. Among these methods, British Pharmacopoeia (BP) 2 , United States Pharmacopeia (USP) 3 , UVspectro-photometry 4 , HPLC 5 , HPTLC 6 , gas chromatography 7 , polarimetry 8 and electrophoresis 9 are a few mention worth.

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Bioavailability Enhancement of Rizatriptan Benzoate by Oral Disintegrating Strip: In vitro and In vivo Evaluation

Cited by 6 publications

References 0 publications

Development and Characterizations of Pullulan and Maltodextrin-Based Oral Fast-Dissolving Films Employing a Box–Behnken Experimental Design

Development and Characterizations of Pullulan and Maltodextrin-Based Oral Fast-Dissolving Films Employing a Box–Behnken Experimental Design

Rizatriptan-Loaded Oral Fast Dissolving Films: Design and Characterizations

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