Preparation and evaluation of fenoterol hydrobromide suppositories

Ghorab, Dalia; Refai, Hanan; Tag, Randa

doi:10.5582/ddt.2011.v5.6.311

Cited by 15 publications

(14 citation statements)

References 21 publications

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“…These results are in agreement with that reported by Ghorab et al (2011) who found that the release rate of fenoterol hydrobromide from different PEG bases was dependent on their hydrophilic and lipophilic character.…”

Section: In Vitro Release From Peg Basessupporting

confidence: 95%

“…The Erweka method was used to measure the weight in kilograms a suppository can bear without breaking (Ghorab et al, 2011).…”

Section: Hardnessmentioning

confidence: 99%

“…Drug displacement values of the bases used were first determined and the amount of drug required was calculated (Ghorab et al, 2011). The fusion method was adopted to prepare the different suppositories.…”

Section: Preparation Of Mt Suppositoriesmentioning

confidence: 99%

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Pharmacokinetics and anti-hypertensive effect of metoprolol tartrate rectal delivery system

2014

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The main aim of this work was to develop rectal suppositories for better delivery of metoprolol tartrate (MT). The various bases used were fatty, water soluble and emulsion bases. The physical properties of the prepared suppositories were characterized such as weight variation, hardness, disintegration time, melting range and the drug content uniformity. The in vitro release of MT from the prepared suppositories was carried out. The evaluation of the pharmacological effects of MT on the blood pressure and heart rate of the healthy rabbits after the rectal administration compared to the oral tablets was studied. Moreover, the formulation with the highest in vitro release and the highest pharmacological effects would be selected for a further pharmacokinetics study compared to the oral tablets. The results revealed that the emulsion bases gave the highest rate of the drug release than the other bases used. The reduction effect of the emulsion MT suppository base on the blood pressure and heart rate was found to be faster and greater than that administered orally. The selected emulsion suppository base (F11) showed a significant increase in the AUC (1.88-fold) in rabbits as compared to the oral tablets. From the above results we can conclude that rectal route can serve as an efficient alternative route to the oral one for systemic delivery of MT which may be due to the avoidance of first-pass effect in the liver.

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Section: In Vitro Release From Peg Basessupporting

confidence: 95%

“…The Erweka method was used to measure the weight in kilograms a suppository can bear without breaking (Ghorab et al, 2011).…”

Section: Hardnessmentioning

confidence: 99%

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Pharmacokinetics and anti-hypertensive effect of metoprolol tartrate rectal delivery system

2014

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“…Suppositories containing 25 mg of sildenafil were prepared by a cream melting technique using Witepsol H-15 as a suppository base 21 . Primarily, an appropriate amount of Witepsol H-15 was melted in a water bath maintained at a temperature of 65 AE 2 C and was mixed with 25 mg of sildenafil powder.…”

Section: Preparation Of Svsmentioning

confidence: 99%

Sildenafil vaginal suppositories: preparation, characterization,in vitroandin vivoevaluation

Shanmugam

Kim

Park

et al. 2013

Drug Development and Industrial Pharmacy

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“…On the other hand, when administered intravenously, some anticancer drugs, such as epirubicin, may cause damage to the vein into which it is injected [2]. The rectal route for drug administration possesses the advantage of the decreased side effects by avoiding both oral unpleasant taste and reducing GI irritation [3]. However, the conventional solid suppository has the drawbacks of patient discomfort, leading to decreased patient compliance.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Epirubicin in Thermogelling and Bioadhesive Liquid and Solid Suppository Formulations for Rectal Administration

Yi-Jun

Lin

2013

IJMS

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Temperature sensitive Pluronic (Plu) and pH-sensitive polyacrylic acid (PAA) were successfully mixed in different ratios to form in situ gelling formulations for colon cancer therapy. The major formulations were prepared as the liquid and solid suppository dosage forms. Epirubicin (Epi) was chosen as a model anticancer drug. In vitro characterization and in vivo pharmacokinetics and therapeutic efficacy of Epi in six Plu/PAA formulations were evaluated. Our in vitro data indicate that Epi in Plu 14%/PAA 0.75% of both solid and liquid suppositories possess significant cytotoxicity, strong bioadhesive force, long-term appropriate suppository base, sustained release, and high accumulation of Epi in rat rectums. These solid and liquid suppositories were retained in the upper rectum of Sprague-Dawley (SD) rats for at least 12 h. An in vivo pharmacokinetic study using SD rats showed that after rectal administration of solid and liquid suppositories, Epi had greater area under the curve and higher relative bioavailability than in a rectal solution. These solid and liquid suppositories exhibited remarkable inhibition on the tumor growth of CT26 bearing Balb/c mice in vivo. Our findings suggest that in situ thermogelling and mucoadhesive suppositories demonstrate a great potential as colon anticancer delivery systems for protracted release of chemotherapeutic agents.

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Preparation and evaluation of fenoterol hydrobromide suppositories

Abstract: Fenoterol HBr is a bronchodilator known to be subject to first pass effect after oral administration. The aim of this study was to prepare and evaluate fenoterol HBr suppositories. Suppositories were prepared by a fusion method using different fatty bases, viz.

Cited by 15 publications

References 21 publications

Pharmacokinetics and anti-hypertensive effect of metoprolol tartrate rectal delivery system

Pharmacokinetics and anti-hypertensive effect of metoprolol tartrate rectal delivery system

Sildenafil vaginal suppositories: preparation, characterization,in vitroandin vivoevaluation

Evaluation of Epirubicin in Thermogelling and Bioadhesive Liquid and Solid Suppository Formulations for Rectal Administration

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