Formulation, in-vitro release and ex-vivo spasmolytic effects of mebeverine hydrochloride suppositories containing polycarbophil or polysorbate 80

Hosny, E. A.; Abd-Elhady, S. S.; Eltahir, K

doi:10.1016/0378-5173(96)04664-9

Cited by 19 publications

(15 citation statements)

References 14 publications

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“…These results are in agreement with De Stoppelaar et al who stated that the metoprolol concentration in plasma and urine gave an indication for a partial avoidance of the first pass effect after rectal administration (De Stoppelaar et al, 1999). The reducing effect of MT suppository formulations on the blood pressure was ranked as follows: emulsion base (F11)4fatty base (F1)4PEG base (F10).These results revealed that the pharmacological effect of the drug was greatly influenced by the type and nature of the suppository base used (Asikoglu et al, 1995;Hosny et al, 1996). Moreover, MT formulated in the emulsion suppository base (F11) gave the highest significant antihypertensive effect in the rabbits at the end of the experimental time (6 h) compared to the other two tested formulations (F1, F10).…”

Section: The Effect On Blood Pressurementioning

confidence: 74%

“…On the other hand, water soluble base liquefies by the absorption of water resulting in swelling and dissolution of the suppository. This leads to a dispersion process that is slower than the melting of the fatty base (Asikoglu et al, 1995;Hosny et al, 1996).…”

Section: The Effect On Blood Pressurementioning

confidence: 97%

“…A high hydroxyl value is an indication of the potential for a base to absorb the water. The presence of high hydroxyl values in the fatty bases could thus favor the formation of a water-in-oil emulsion, which will generally result in a slow transfer of drug molecules from the inner aqueous phase and retarded the release of the drug (Hosny et al, 1996;Tukker, 2009 (Calis et al, 1994).…”

Section: In Vitro Release From Fatty Suppository Basesmentioning

confidence: 98%

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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: The Effect On Blood Pressurementioning

confidence: 74%

Section: The Effect On Blood Pressurementioning

confidence: 97%

Section: In Vitro Release From Fatty Suppository Basesmentioning

confidence: 98%

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

2014

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“…The fastest release formula was F3, which contained an effervescent pair, in which diazepam reached its maximum release in about 5 minutes. The high release rate of diazepam from PEG suppositories may be due to both low affinity of the drug to the base and water solubility of the base, which allows the drug to be released by both diffusion and erosion mechanisms [12]. The dissolution of very slightly soluble substances, like diazepam, is usually the rate-limiting step in the absorptive process, therefore as much as we can enhance the dissolution rate, the absorption will be improved [13].…”

Section: In Vitro Release Rate Of Diazepam From Water-soluble and Watmentioning

confidence: 99%

Preparation and in Vitro Evaluation of Fast Release Diazepam Suppositories for Febrile Seizures

Alsamman

Othman

2017

Asian J Pharm Clin Res

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Objective: The objective of this study was to optimize the best formula for fast release suppositories of diazepam.Methods: Suppositories were prepared by fusion method using Witepsol H15 as oleaginous base, polyethylene glycol as a water-soluble polymer, and Poloxamer 188 as water miscible base. All suppositories were evaluated for physical characteristics, in vitro drug release and kinetic models. The effects of incorporating Tween 80 as a non-ionic surfactant, propylene glycol as a cosolvent, and effervescent pair on the release rate of diazepam from suppositories were investigated. Differential scanning calorimetry and Fourier transform infrared spectrometry were used to characterize physical mixtures of diazepam and the different used bases.Results: Many formulations of diazepam have been prepared and in vitro evaluated. PEG suppositories released diazepam more efficiently than poloxamer and witepsol suppositories. The including of an effervescent pair in the formulation of suppositories greatly enhanced the release of diazepam. The addition of tween 80 to witepsol suppositories, PG to poloxamer suppositories, increased the rate and extent of diazepam release. Conclusion:Fast release of diazepam has been obtained from suppositories containing the effervescent pair (formula F3), which also have good physical properties.

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“…The fastest release formula was F3, which contained an effervescent pair, in which diazepam reached its maximum release in about 5 minutes. The high release rate of diazepam from PEG suppositories may be due to both low affinity of the drug to the base and water solubility of the base, which allows the drug to be released by both diffusion and erosion mechanisms [11]. The dissolution of very slightly soluble substances, like diazepam, is usually the rate limiting step in the absorptive process, therefore as much as we can enhance the dissolution rate, the absorption will be improved [12].…”

Section: Alsamman and Othmanmentioning

confidence: 99%

Preparation and in Vitro Evaluation of Fast Release Diazepam Suppositories for Febrile Seizures

Alsamman

Othman

2017

Asian J Pharm Clin Res

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Objective: The objective of this study was to optimize the best formula for fast release suppositories of diazepam.Methods: Suppositories were prepared by fusion method using Witepsol H15 as oleaginous base, polyethylene glycol as water-soluble polymer and poloxamer 188 as water miscible base. All suppositories were evaluated for physical characteristics, in vitro drug release and kinetic models. The effects of incorporating Tween 80 as a nonionic surfactant, propylene glycol as a cosolvent, and effervescent pair on the release rate of diazepam from suppositories were investigated. Differential scanning calorimetry and Fourier transform infrared spectrometry were used to characterize physical mixtures of diazepam and the different used bases.Results: Fast release of diazepam has been obtained from suppositories containing the effervescent pair. Many formulations of diazepam have been prepared and in vitro evaluated. PEG suppositories released diazepam more efficiently than poloxamer and Witepsol suppositories. The including of an effervescent pair in the formulation of suppositories greatly enhanced the release of diazepam. The addition of Tween 80 to Witepsol suppositories, PG to poloxamer suppositories, increased the rate and extent of diazepam release. Conclusion:Fast release of diazepam has been obtained from suppositories containing the effervescent pair (formula F3), which also have good physical properties.

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Formulation, in-vitro release and ex-vivo spasmolytic effects of mebeverine hydrochloride suppositories containing polycarbophil or polysorbate 80

Cited by 19 publications

References 14 publications

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

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

Preparation and in Vitro Evaluation of Fast Release Diazepam Suppositories for Febrile Seizures

Preparation and in Vitro Evaluation of Fast Release Diazepam Suppositories for Febrile Seizures

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