Formulation and stability of rofecoxib suppositories

Aboutaleb, A.; Abdel-Rhman, A. A.; Samy, E.; Tawfeek, Hesham M.

doi:10.1016/s1773-2247(06)50070-x

“…Furthermore, the fact that, LOR being water insoluble drug 15,16 has high affinity towards the fatty bases than PEGs base 14 . This result also agrees with Abou-Taleb et al, 2006 who found that the release of rofecoxib, selective cox-II inhibitor, from PEGs bases was higher than those of fatty bases e.g., witepsol E-75 and suppocire AM and CM 4 . Also, it was found that the release of verapamil hydrochloride from PEG suppositories was greater than the release from witepsols and suppocire AM based bases 17 .…”

Section: Physical Characteristics Of Lor Suppositoriessupporting

confidence: 91%

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2013

IJPSR

0

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ABSTRACT:The aim of the present study was to formulate lornoxicam into rectal suppositories as a new dosage form, to avoid its reported gastric irritation and to provide a rapid onset of action for children. Suppositories were prepared using fatty bases namely; witepsol H-15, suppocire AML, CM, witepsol E-75 and water soluble bases; mixtures of poly(ethylene glycol), PEGs, with different molecular weights. The prepared suppositories were investigated for their weight variation, drug content, melting point, fracture point, disintegration time and in-vitro release pattern. Moreover, aging study was performed both at room temperature and in refrigerator for 6 month. In-vivo study was also carried out in rabbits and the pharmacokinetic parameters were estimated. The prepared suppositories complied with the USP 34 pharmacopoeial requirements and PEGs-based suppositories released significantly higher amounts of lornoxicam compared with fatty bases (p<0.05, ANOVA/Dunnett). Furthermore, lornixocam in selected formulations was found to be stable in both fatty and PEGs bases after the aging study. Formulation No. 5 showed a higher C max of 1.832±0.35 µg/ml, short t max of 1 hr and absolute bioavailability of 80.1%. These findings suggest that lornoxicam was successfully formulated into rectal suppositories with a higher bioavailability.

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“…In Vitro Drug Release Studies. Curcumin is a hydrophobic drug, and therefore, hydrophilic bases were chosen to prepare suppositories as the hydrophobic drug exhibits a greater tendency to diffuse out of hydrophilic bases [32,33]. Polyethylene glycol exhibits greater water-absorbing properties that, in turn, enable dissolution medium penetration into the base following moistening and drug desorption.…”

Section: Measurement Of Deformation Time (Liquefaction Time)mentioning

confidence: 99%

An Efficient Herbal Approach for Treating Fungal Infection in Cervical Cancer Patients by Developing and Optimizing a Vaginal Suppository

Ghazwani

¹

,

Hani

²

,

Osmani

³

et al. 2021

International Journal of Polymer Science

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Aim. The study is aimed at developing curcumin suppositories as a promising approach for natural antifungal management of vaginal candidiasis in cervical cancer patients to eradicate side effects produced by current antifungal drugs. The objective of the study was to optimize the suppositories using optimal (custom) design employing Design-Expert 13 software to recognize the concentration of polyethylene glycols (PEG) and Poloxamer 407 and obtain a stable suppository. Methodology. Combinations of PEG 1500 (10%–40%), PEG 6000 (40%–60%), and Poloxamer 407 (5%–30%) were entered as factors, and the responses evaluated were hardness, deformation time, and % drug release. In addition, the formulation was also evaluated for visual examination, weight variation, pH determination, drug content, hardness test, disintegration time, melting zone, deformation time, in vitro drug release, antifungal activity, and stability tests. Results. Suppositories were devoid of holes and cracks, with a characteristic odor and a dark yellowish-orange color. All formulations passed the weight variation test. Formulations exhibited pH ranging from 5.5 to 6.5. Drug content was observed to be 98.65 ± 0.041 % – 99.85 ± 0.041 % . The hardness of the formulation was between 2.9 and 4.2 kg/cm2. The disintegration time ranged from 11 ± 0.052 min to 20 ± 0.011 min . The melting point was between 41 ± 0 . 31 ° C and 58 ± 0 . 62 ° C . Deformation time ranged from 10 ± 0.45 to 35 ± 0.52 min . Most of the formulations resulted in 90% of drug release at 40 min, and the zone of inhibition noted was 19.6 ± 0.4 mm . All the selected factors have a significant effect on the response chosen for the study. Conclusion. The optimized curcumin vaginal suppository formulation can be an efficient herbal treatment devoid of side effects to treat vaginal candidiasis in cervical cancer patients.

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“…Different approaches have been developed to solve the problem of low oral bioavailability including the use of surfactants [6], cosolvents [6], inclusion complexes [7], solid dispersions [8], self-emulsifying systems [9], prodrugs [10], solid lipid nanoparticles [11] and micro-environmental buffering systems [12]. Formulation of drug adsorbates and co-adsorbates are among the most promising techniques adopted for dissolution enhancement [13][14][15]. Adsorbents with large surface areas have the potential to carry different drugs onto their surfaces hence, increasing their dissolution and bioavailability [13,16].…”

Section: Introductionmentioning

confidence: 99%

Glibenclamide Mini-tablets with an Enhanced Pharmacokinetic and Pharmacodynamic Performance

Tawfeek

¹

,

Roberts

²

,

Hamd

³

et al. 2018

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In an attempt to decrease the dose, anticipated side effects, and the cost of production of glibenclamide, GLC, a potent oral hypoglycemic drug, the enhancement of the dissolution and hence the oral bioavailability were investigated. Adsorption and co-adsorption techniques using carriers having a very large surface area and surface active agents were utilized to enhance the drug dissolution. Moreover, the Langmuir adsorption isotherms were constructed to identify the type and mechanism of adsorption. The optimized formulation showing the highest in vitro release was compressed into mini-tablet to facilitate drug administration to elderly patients and those having swallowing difficulties. The produced mini-tablets were tested for their mechanical strength and in vitro release pattern. In addition, the pharmacodynamic and pharmacokinetic studies in New Zealand rabbits were performed using the optimized mini-tablet formulation. Mini-tablets containing GLC co-adsorbate with Pluronic F-68 and Laponite RD showed 100 ± 1.88% of GLC released after 20 min. Pharmacodynamic studies in rabbits revealed significantly higher (p ≤ 0.05) hypoglycemic effect with the optimized mini-tablets at a lower GLC dose compared to mini-tablets containing the commercial GLC dose. Moreover, pharmacokinetic analysis showed significantly higher (p ≤ 0.05) AUC, C, and shorter T. The optimized mini-tablet formulation showed 1.5-fold enhancement of the oral bioavailability compared to mini-tablets containing untreated GLC. It could be concluded that the co-adsorption technique successfully enhanced the oral bioavailability of GLC. Furthermore, the produced mini-tablets have a higher oral bioavailability with a lower GLC dose, which could offer economic benefit for industry as well as acceptability for patients.

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Formulation and stability of rofecoxib suppositories

Cited by 7 publications

References 22 publications

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An Efficient Herbal Approach for Treating Fungal Infection in Cervical Cancer Patients by Developing and Optimizing a Vaginal Suppository

Glibenclamide Mini-tablets with an Enhanced Pharmacokinetic and Pharmacodynamic Performance

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