Rectal bioavailability of amoxicillin sodium in rabbits: Effects of suppository base and drug dose

Purohit, Trusha J.; Hanning, Sara M.; Amirapu, Satya; Wu, Zimei

doi:10.1016/j.jconrel.2021.09.015

Cited by 4 publications

(17 citation statements)

References 50 publications

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“…The formulations showed a disintegration time between 13 and 19 minutes (Table 1). These values are in agreement with the literature and compatible with the compendial data [14,29].…”

Section: Disintegration Timesupporting

confidence: 92%

“…Both medicated and unmedicated suppositories were found physically robust and the breakpoint of each type of formulation was found to be above 2 kg/cm 2 . In terms of durability and robustness, the literature data also support this finding [14]. Additionally, it was also determined that the mechanical strength of WH15 suppositories was significantly decreased by the addition of the oils (p < 0.05).…”

Section: Hardnessmentioning

confidence: 53%

“…On the other hand, the type of suppository base, aqueous solubility, and small molecular size of the drug are critical parameters for the formulation [13]. While alternative rectal formulations have been presented (hollow type suppositories or in situ gelling systems), conventional rectal suppositories stay the most common rectal dosage form [14].…”

Section: Introductionmentioning

confidence: 99%

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Preparation and characterization studies of etodolac suppositories: investigation on oleaginous blends of Witepsol® H15

ÖZDEMİR¹,

Uner²,

KARAKÜÇÜK³

2023

jrp

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Etodolac is a non-steroidal anti-inflammatory drug that is categorized as a BCS class-II drug due to its low aqueous solubility and high permeability. Frequent dosing, extensive liver metabolism, and low dissolution rates are major limitations of etodolac. The present study focuses on the designing of novel suppository base blends for providing an effective delivery of etodolac. The oils (Caprylic/capric triglyceride, isopropyl isostearate, and isopropyl palmitate) were added to Witepsol ® H15 to form suppository base blends. White, odorless, and torpedo-shaped suppositories were developed by using two parts of Witepsol ® H15 and one part of the oil. All of the suppositories prepared with different blends were found uniform in weight and content. The mechanical strength of all suppositories was in an acceptable range for suppositories (2.0 -3.8 kg/cm 2 ). The suppositories showed a disintegration time between 13 and 19 minutes. First-order release kinetics were observed after the in vitro release studies. The suppository base blends released 85%-90% of etodolac in the first hour while 60% of etodolac was released from Witepsol ® H15 base alone. Prolonged drug release was achieved after 2 hours all of the formulations reached the plateau levels. The oil blends exhibited higher release percentages (96% -99%) than plain Witepsol ® H15 base (89%). Therefore novel suppository base blends could be a promising formulation ingredient for the etodolac suppositories.

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“…The formulations showed a disintegration time between 13 and 19 minutes (Table 1). These values are in agreement with the literature and compatible with the compendial data [14,29].…”

Section: Disintegration Timesupporting

confidence: 92%

Section: Hardnessmentioning

confidence: 53%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Preparation and characterization studies of etodolac suppositories: investigation on oleaginous blends of Witepsol® H15

ÖZDEMİR¹,

Uner²,

KARAKÜÇÜK³

2023

jrp

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“…Plasma samples were proximately moved to Eppendorf tubes after being separated and stored at -20°C until analysis. HPLC analysis was utilized to determine the drug's plasma concentration, and the following steps were used for HPLC analysis (Purohit et al, 2021;Purohit et al, 2020).…”

Section: In Vivo Bioavailability Studymentioning

confidence: 99%

Mastic gum aided amoxicillin trihydrate gastro retentive mucoadhesive microspheres: In vivo evaluation

Sowjanya

Ahad²

2022

Bangladesh J. Sci. Ind. Res.

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The primary objective of the study is to test gastro retentive mucoadhesive Amoxicillin trihydrate (ATH) microspheres for various in vivo properties. Several metrics were used to assess the improved ATH Mastic gum mucoadhesive microspheres (AMMM) in vitro. In vivo testing was conducted using formula-8 (AMMM-8), as suggested by prior study results by Soujanya et al., 2022. Four healthy rabbits of both sexes were used to assess the availability of plasma medicines. Pharmacokinetic parameters were measured in plasma samples. The study revealed that in vivo animal studies in rabbits showed good drug levels of ATH. After a single dose of formulation AMMM-8 (44.28mg/kg), the symmetrical mean Cmax (25.69±0.11μg/ml) tmax (6h), AUC (0-10h) (185.1±1.28 μg.h/ml), AUC (0-∞) (269.1±4.68 μg.h/ml), and AUMC (840.42±2.23 μg.h/ml) were better than ATH. According to the findings, ATH reached systemic circulation faster than the pure medication and had acceptable kinetic values. Bangladesh J. Sci. Ind. Res. 57(3), 187-194, 2022

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“…The model component chosen in this work, amoxicillin sodium (C 16 H 18 N 3 NaO 5 S, CAS: 34642-77-8, Figure 1), is one of the most important β-lactam antibiotics and is used against Gram-positive and Gram-negative bacteria. 33 Rod-shaped crystals with a high aspect ratio are usually obtained through reactive−antisolvent coupled crystallization, which led to low bulk density, poor compressibility, and poor flowability and hence poor performance of filtration and drying. It is difficult for amoxicillin sodium to crystallize spontaneously due to the high free energy barrier of its primary nucleation caused by the high viscosity of the selected solution system.…”

Section: Introductionmentioning

confidence: 99%

Spherulitic Growth Strategy for Agitation-Induced Formation of Spherical Amoxicillin Sodium Products

Cui

Yang

Yin

et al. 2022

Ind. Eng. Chem. Res.

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In industrial crystallization, spherical crystals have gained increasing interest due to their excellent physicochemical properties, such as high bulk density, flowability, stability, etc. However, their formation mechanism is still not well understood and is often oversimplified. In this work, spherical amoxicillin sodium crystals were obtained via a spherulitic growth strategy. It was found that agitation immediately after the addition of crystal seeds was critical for inducing radial noncrystallographic branching and spherulite formation of amoxicillin sodium. Without agitation during the aging period after seed addition, only discrete rodshaped crystals were obtained. The formation mechanism of amoxicillin sodium spherulites was studied using process analytical technology (PAT) tools, including focused beam reflectance measurement (FBRM) and particle video microscope (PVM). The result was indicative of a three-step morphological evolution process: formation of polycrystalline agglomerates, noncrystallographic branching, and spherulite growth. During this process, agitation immediately after seed addition could help to solute diffusion and induce the agglomeration of small crystals that result from secondary nucleation. The polycrystalline agglomerates serve as the cores for further noncrystallographic branching and growth. On this basis, a new spherulitic growth strategy was proposed by the large addition of crystal seeds as the growth substrates of new branching and spherulite growth. High agitation rates during the aging period can increase the mass ratio of spherulites, and high initial supersaturation can promote branching. Compared with the discrete rod-shaped crystals, spherulites self-regulate the final size greatly up to three times and have a higher bulk density as well as much lower hygroscopicity.

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Rectal bioavailability of amoxicillin sodium in rabbits: Effects of suppository base and drug dose

Cited by 4 publications

References 50 publications

Preparation and characterization studies of etodolac suppositories: investigation on oleaginous blends of Witepsol® H15

Preparation and characterization studies of etodolac suppositories: investigation on oleaginous blends of Witepsol® H15

Mastic gum aided amoxicillin trihydrate gastro retentive mucoadhesive microspheres: In vivo evaluation

Spherulitic Growth Strategy for Agitation-Induced Formation of Spherical Amoxicillin Sodium Products

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