Gastroretentive delivery of rifampicin: In vitro mucoadhesion and in vivo gamma scintigraphy

Pund, Swati; Joshi, Amita; Vasu, Kamala K.; Nivsarkar, Manish; Shishoo, C. J.

doi:10.1016/j.ijpharm.2011.03.048

Cited by 39 publications

(17 citation statements)

References 33 publications

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“…Literature also supports the fact that MCC is the most (25). It is established that MCC pellets do not disintegrate, and drug release occurs via diffusion through an insoluble inert matrix (26).…”

Section: Selection Of Factors and Optimization Of Pellet Formulation mentioning

confidence: 82%

Melt-in-Mouth Multi-particulate System for the Treatment of ADHD: A Convenient Platform for Pediatric Use

2015

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Abstract. Generally, pellets obtained from extrusion/spheronization, containing microcrystalline cellulose (MCC), do not disintegrate. An attempt has been made to develop melt-in-mouth pellets of taste-masked atomoxetine hydrochloride, using extrusion-spheronization, for pediatric patients. Melt-in-mouth pellets were prepared using extrusion-spheronization method and optimized using 3 3 FFD. MCC (X 1 , %), mannitol (X 2 , %) and Indion 414: Pharmaburst 500 ratio (X 3 , ratio) were the factors (independent variables) studied, whereas responses studied (dependent variables) were friability (Y1, %), yield (Y2, %) shape (Y3, roundness) in vitro disintegration time (Y4, seconds). The optimized formulation obtained from FFD was characterized for friability, shape and morphology, in vitro disintegration time, porosity, moisture uptake, in vitro release study and in vivo taste and disintegration time in healthy human volunteers. Randomized, two-treatment, two-sequence, two-period, single dose, crossover sensory evaluation study of taste-masked melt-in-mouth pellet was carried out in 10 healthy human subjects. A statistically significant polynomial mathematical relationship was generated between the factors and responses to obtain an optimized formulation. The optimized formulation was characterized (in vitro and in vivo) and exhibited a rapid drug release in vitro attributed to fast disintegration of pellets and high solubility of drug in 0.1 N HCl and buffer (pH 6.8). In vivo, 40% of volunteers ranked taste-masked optimized formulation as slightly bitter while 60% ranked it as no taste. The optimized pellets were conveniently administered in volunteers and exhibited rapid in-vivo disintegration in the oral cavity. Melt-in-mouth pellets can be a used as a platform technology for administering drugs to paediatric patients accurately and conveniently resulting in patient compliance.

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Section: Selection Of Factors and Optimization Of Pellet Formulation mentioning

confidence: 82%

Melt-in-Mouth Multi-particulate System for the Treatment of ADHD: A Convenient Platform for Pediatric Use

2015

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“…Therefore, 99mTc acts as the marker for locating the transit of the floating atenolol tablet. 11 It was observed in the gamma images that optimized formulation (batch F2) was retained in the stomach more than 6 hours.A measurable number of counts of 99mTc-tagged atenolol formulation (F2) for the 6-hour Study period shown good gastro-retention (Shown in Figure 4). A representative rabbit gamma scintigraphic image has been shown at 0, 2 and 5 h in fig.…”

Section: Gamascintigraphy Studymentioning

confidence: 95%

“…Radiolabel efficiency was evaluated using thin layer chromatography. 11 Instant thin layer chromatographic silica gel plates were used as a stationary phase and 100 % acetone was used as mobile phase. Percent radio labeling was calculated as follows.…”

Section: Preparation and Administration Of The Radio Labeled Tabletmentioning

confidence: 99%

“…The technique of Gamascintigraphy has become the most popular method to investigate the gastrointestinal performance of the product. 11 Tc 99m is inexpensive and readily available through the use of portable generators. 19 Tc -99 m possesses most of the characteristics of an ideal radionuclide and hence found widespread applications in nuclear and in pharmaceutical formulation development.…”

Section: Gamascintigraphy Studymentioning

confidence: 99%

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Gamascintigraphic in Vivo-in Vitro Evaluation of Floating Matrix Tablet

Shinde¹,

Joshi²,

Dhas³

2014

IJPER

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Background of the work: Gastroretentive drug delivery system can retain the dosage form in the gastric region for several hours. Prolong gastric retention helps in improving bioavailability and improves solubility of drugs that are less soluble in a high pH environment. For designing of GRDDS Atenolol was selected as a model drug. It has been used for the treatment of hypertension. Atenolol has short elimination half-life, stable at pH 1.2 and as the pH increase, the drugs becomes unstable and thus low oral bioavailability.In order to improve its therapeutic effectiveness Atenolol is designed in the form of floating tablet formulation. Purpose: The aim of the present

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“…The procedure was then similar to that used for the preparation of MPs (batch B1) [14] . Radiolabel efficiency was checked using thin layer chromatography (TLC) [15] . Instant TLC silica gel plates were used as a stationary phase and 100 % acetone was used as mobile phase.…”

Section: Residual Solventmentioning

confidence: 99%

Formulation and Development of Gastroretentive Dipyridamole Microspheres: Proof of Concept by In vitro-In vivo Assessment

Vanshiv¹,

Joshi²,

Aware³

2018

pharmaceutical-sciences

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Vanshiv, et al.: Gastroretentive Dipyridamole MicrospheresThe present research was aimed at development and optimization of dipyridamole gastroretentive microspheres. Gastro retention was achieved using swellable polymeric material such as hydroxypropyl methylcellulose K4M, ethyl cellulose as release retardant using solvent diffusion evaporation method. 3 2 factorial design was applied for the development of best optimized formulation. The design was developed by considering two independent variables, ethyl cellulose, and stirring speed. Their effect on drug release, entrapment efficiency, particle size was analysed using response surface methodology. Formulation B1 among all formulations tested was found to be the best as it demonstrated prolonged floating time, maximum entrapment efficiency and drug release in a controlled manner. Formulation B1 was characterized further for presence of residual solvent by gas chromatography/mass spectrometry and the result showed absence of residual solvent. Gastro retention was assessed using the in vivo gamma scintigraphy technique in albino rabbits and the results indicated prolonged gastric retention. Pharmacokinetic study comparing pure dipyridamole and dipyridamole microspheres was conducted and C max , T max and K el were estimated. In vitro-in vivo correlation was determined using Wagner-Nelson function. Pharmacokinetic study revealed improved bioavailability (30 %) as compared to pure dipyridamole. Good correlation was obtained with a regression coefficient of 0.9704. The in vivo gamma scintigraphy and pharmacokinetic studies confirmed gastric retention of the prepared dipyridamole floating microspheres. Accelerated stability studies indicated integrity of the developed formulations.

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Gastroretentive delivery of rifampicin: In vitro mucoadhesion and in vivo gamma scintigraphy

Cited by 39 publications

References 33 publications

Melt-in-Mouth Multi-particulate System for the Treatment of ADHD: A Convenient Platform for Pediatric Use

Melt-in-Mouth Multi-particulate System for the Treatment of ADHD: A Convenient Platform for Pediatric Use

Gamascintigraphic in Vivo-in Vitro Evaluation of Floating Matrix Tablet

Formulation and Development of Gastroretentive Dipyridamole Microspheres: Proof of Concept by In vitro-In vivo Assessment

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