Prolonged-release minitablets with carbamazepine – preliminary observations <i>in vitro</i>

Dzajkowska, Magdalena; Kotlowska, Hanna; Anna, Madanecka; Szczepanska, Maja; Dagmara, Doniza; Anna, Sosnowicz; Sznitowska, Małgorzata

doi:10.1111/jphp.12670

“…The time for carbamazepine to achieve peak concentration was longer for the CPH pectin matrix modified-release formulations (formulation A: 12 ± 1.28 µ g/mL and formulation B: 12 ± 1.43 µ g/mL) as compared to Tegretol CR ® (8 ± 2.23 µ g/mL). The matrix formulations demonstrated a prolonged release of carbamazepine, which is known to enhance patient compliance and reduce frequency of dosing [ 47 , 48 ]. Even though the difference in time to achieve peak concentration between formulation A, formulation B, and Tegretol CR ® (the standard drug) was not significant ( p < 0.05), the findings suggest a modest improvement in the release profiles of the CPH pectin-based carbamazepine matrix formulations.…”

Section: Discussionmentioning

confidence: 99%

A Pharmacokinetic Evaluation of a Pectin-Based Oral Multiparticulate Matrix Carrier of Carbamazepine

Amponsah

¹

,

Yeboah

²

,

Kukuia

³

et al. 2021

Advances in Pharmacological and Pharmaceutical Sciences

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Background. Carbamazepine is a drug used in the treatment of neurological disorders such as epilepsy. However, due to its erratic absorption, oral bioavailability is often poor. There is, therefore, the need to develop alternative formulations for carbamazepine with better pharmacokinetic characteristics. Aim. The aim of this study was to formulate an oral modified-release multiparticulate matrix of carbamazepine from cocoa pod husk (CPH) pectin and evaluate the pharmacokinetic profile of this formulation using in vitro and in vivo models. Methods. CPH pectin was extracted from cocoa pod husks with hot aqueous and citric acid solutions. Oral multiparticulate carbamazepine matrices were formulated from CPH pectin cross-linked with calcium. The formulation was evaluated for carbamazepine content and release profile in vitro. For in vivo pharmacokinetic profile estimation, rats were put into 4 groups of 5 animals each to receive carbamazepine multiparticulate matrix formulations A and B, carbamazepine powder, and Tegretol CR®. Animals in each group received 200 mg/kg of each drug via the oral route. Maximum plasma concentration C max , area under the concentration-time curve (AUC), elimination rate constant K e , and terminal half-life t 1 / 2 of the formulations were estimated by noncompartmental analysis. Results. The pectin extraction from fresh cocoa pod husks using hot aqueous and citric acid solutions gave pectin yields of 9.63% and 11.54%, respectively. The drug content of carbamazepine in CPH pectin formulations A and B was 95% and 96%, respectively. There was controlled and sustained release of carbamazepine for both formulations A and B in vitro. AUC0⟶36 (176.20 ± 7.97 µg.h/mL), C max (8.45 ± 0.71 μg/mL), T max (12 ± 1.28 h), and t 1 / 2 (13.75 ± 3.28 h) of formulation A showed a moderately enhanced and comparable pharmacokinetic profile to Tegretol CR® (AUC0⟶36: 155 ± 7.15 µg.h/mL, C max : 8.24 ± 0.45 μg/mL, T max : 8.0 ± 2.23 h, and t 1 / 2 : 13.51 ± 2.87 h). Conclusion. Findings from the study suggest that formulations of CPH pectin had the potential to control and maintain therapeutic concentrations of carbamazepine in circulation over a period of time in the rat model.

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“…E. Palazi et al [28]enhanced solubility of waterinsoluble drug felodipine by melt-extrusion process and sustained release action of drug was achieved using kollidon SR. C. Wiranidchapong et al [29] investigated the effect of storage temperature on drug release from matrices containing ibuprofen in Kollidon SR, the matrix tablets were produced by direct compression and then kept at 30 and 45°C for 3 months. Magdalena Czajkowska et al [30] formulated Prolonged-release mini tablets with carbamazepine Prolonged release of carbamazepine was obtained from both matrix-type by using kollidon SR. S. Engineer et al [31] studied the effects of temperature and humidity on tablets containing diphenhydramine hydrochloride which was prepared using direct compression technique with Kollidon SR; sustained-release tablets composed of Kollidon SR have been shown to be heat and moisture sensitive. J. Grund et al [32]studied the kollidon SR and other polymer properties on direct compression and drug release from water-insoluble controlled release matrix tablets and compared with regard to their properties in dry and wet state.…”

Section: Kollidon® Cl-f Cl-sfmentioning

confidence: 99%

A brief review on Kollidon

Jagtap¹,

Tagad²,

Shendge

³

2019

J. Drug Delivery Ther.

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Polyvinylpyrrolidone includes soluble and insoluble grades; soluble grades are synthesised by the mechanism of polymerization, the free radical polymerization into water by using hydrogen peroxide as an initiator, the mechanism which terminates the polymerisation reaction makes it probable to produce soluble polyvinylpyrrolidone of about any molecular weight. Cross-linked polymer shows yield through popcorn polymerisation of an N-vinylpyrrolidone which gets insoluble polyvinylpyrrolidone. Kollidon is in the market as a brand name for polyvinylpyrrolidone, kollidon family now is a set of common excipients based on polyvinylpyrrolidone for use in pharmaceutical industry. They have a great variety of applications in an oral formulation; the functions of oral formulation encompass fast disintegration, sustain drug release, solubility, bioavailability enhancement, and stabilize the active ingredient. Kollidon containing a mixture of polyvinyl acetate plus povidone are generally used in the formation of sustained release formulation. Owing to their high molecular weight, are recognized as a suitable vehicle for producing sustained release drug delivery system. In this review paper, applications of different grades of kollidon are organized in the form of tables and reviewed critically. Current literature of patents on kollidon based formulations is also presented.

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“…Assessment of film thickness and its uniformity can be performed Mini-tablets, thanks to their small size (up to 3-4 mm), offer a wide range of applications, especially in pediatric and geriatric populations [13][14][15][16]. They may be coated either in drum coaters, as with traditional tablets [17], or in a fluid bed system [18,19].…”

Section: Introductionmentioning

confidence: 99%

Assessment of Mini-Tablets Coating Uniformity as a Function of Fluid Bed Coater Inlet Conditions

Turk

¹

,

Šibanc

²

,

Dreu

³

et al. 2021

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This study concerned the quality of mini-tablets’ coating uniformity obtained by either the bottom spray chamber with a classical Wurster distributor (CW) or a swirl distributor (SW). Mini-tablets with a diameter of 2.0, 2.5, and 3.0 mm were coated with hypromellose using two different inlet air distributors as well as inlet airflow rates (130 and 156 m3/h). Tartrazine was used as a colorant in the coating layer and the coating uniformity was assessed by spectrophotometric analysis of solutions obtained after disintegration of the mini-tablets (n = 100). Higher uniformity of coating material distribution among the mini-tablets was observed in the case of SW distributor, even for the biggest mini-tablets (d = 3.0 mm), with an RSD no larger than 5.0%. Additionally, coating thickness was evaluated by colorimetric analysis (n = 1000), using a scanner method, and expressed as a hue value. A high correlation (R = 0.993) between inter-tablet variability of hue and UV-Vis results was obtained. Mini-tablets were successfully coated in a fluid bed system using both a classical Wurster distributor as well as a swirl generator. However, regardless of the mini-tablets’ diameter, better film uniformity was achieved in the case of a distributor with a swirl generator.

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Prolonged-release minitablets with carbamazepine – preliminary observations in vitro

Abstract: Prolonged release of CBZ was obtained from both matrix-type and coated MT. Further development of MT as a single unit or multicompartment prolonged-release new dosage form especially suitable for children has been justified.

Cited by 7 publications

References 20 publications

A Pharmacokinetic Evaluation of a Pectin-Based Oral Multiparticulate Matrix Carrier of Carbamazepine

A Pharmacokinetic Evaluation of a Pectin-Based Oral Multiparticulate Matrix Carrier of Carbamazepine

A brief review on Kollidon

Assessment of Mini-Tablets Coating Uniformity as a Function of Fluid Bed Coater Inlet Conditions

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