Drug-Polymers Composite Matrix Tablets

The purpose of this research was to see how the physicochemical properties and porosity of matrix tablets containing various types of hydroxypropyl methylcellulose (HPMC) K series affected the release of propranolol hydrochloride (PNL). PNL is a class I drug (high solubility and permeability) according to the Biopharmaceutics Classification System (BCS), making it an excellent model drug used for studying extended-release drug products. The direct compression method was used to prepare the HPMC-based matrix tablets. PNL and the excipients were found to be compatible using Fourier transform infrared spectroscopy (FTIR), powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC). The surfaces of all the compressed HPMC-based matrix tablets were rough, with accumulated particles and small holes. The compressed HPMC-based matrix tablet porosity was also determined by using mercury porosimetry. The compressed HPMC-based matrix tablets made of low viscosity HPMC had tiny pores (diameter < 0.01 μm). The shorter polymeric chains are more prone to deformation, resulting in a small pore proportion. The compressed HPMC-based matrix tablets sustained the release of PNL for over 12 h. The release exponent values (n), which reflect the release mechanism of the drug from the tablets, ranged from 0.476 to 0.497. These values indicated that the release was governed by anomalous transport. The compressed HPMC-based matrix tablets have the potential for a sustained release of PNL.

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1. Introduction

Hydrophilic matrices are monolithic systems of a matrix containing one or more hydrophilic excipients and an active pharmaceutical ingredient [1]. From a practical aspect, a direct compression hydrophilic matrix tablet is one of the simplest ways of developing an oral extended-release dosage form. The direct compression hydrophilic matrix tablet is typically favored for manufacturing because of its numerous advantages, such as current technology, ease of manufacture, and low production cost [2,3,4]. Hydrophilic polymers are the most used hydrophilic excipients in developing compressed hydrophilic matrices. Following exposure to water, the hydrophilic polymers swell and form a gel layer [5,6]. The gel layer regulates the drug release mechanism by controlling water entry and drug molecules&#; diffusion [7]. In some hydrophilic matrices, an anomalous transport could occur [8]. This phenomenon corresponds to the combined effect of diffusion with polymer relaxation and/or matrix erosion [9]. In combination with the expansion of the gel layer, other phenomena and characteristics such as matrix erosion, the internal structure of the matrix, and matrix porosity determine the release behavior of the drug from the hydrophilic matrix [1,4,10]. The interplay of hydration, gelling, swelling, erosion, and maybe even the final breakup of the dosage form ( ) can cause drug release from a hydrophilic matrix tablet [11]. The hydrophilic matrix absorbs water and forms the hydrated gel layer around the dry core after being immersed in the fluid. Furthermore, the hydrated tablet may swell. The drug&#;s release may be affected over time by the growth of the hydrated gel layer and the migration of fluid into the tablet, resulting in the loss of the dry core. Some hydrophilic matrices may also erode and disintegrate over time, potentially resulting in drug release. To develop an oral extended-release matrix, understanding the impact of the hydrophilic polymer in releasing drugs from the hydrophilic matrix is crucial.

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Hydroxypropyl methylcellulose (HPMC), also called hypromellose, has a cellulosic backbone that is partly substituted with methoxy and hydroxypropoxy groups. It is an enzyme-resistant, water-soluble hydrophilic polymer that is stable over a pH range of 3.0&#;11.0 [12]. HPMC is an inactive pharmaceutical ingredient for use in oral, ophthalmic, nasal, and topical formulations, and it is approved by the US Food and Drug Administration [12,13,14]. There are several commercially available HPMC grades; the substituent&#;s viscosity and extent differ among the various HPMC grades. In the development of drug delivery technology, the study of hydrophilic polymers has received considerable attention. The hydrophilic matrix&#;s performance depends on the polymer type and viscosity grade, the presence of certain excipients, and even on factors associated with the material manufacturing, such as porosity [1,2,15]. Numerous researchers have studied the effects of different viscosity grades and degrees of substitution of HPMC on the compaction properties and drug release behavior of matrices [15,16,17,18]. Moreover, the effect of the type of preparation procedure used to make a drug-loaded matrix incorporating HPMC and another excipient, lactose, on drug release was recently studied [19]. Compared to the physical mixture, it has been shown that co-processed excipients did not affect the drug release rate of tablets manufactured by direct compression [19]. The impact of HPMC viscosity grades on drug release has also been investigated for buccal delivery systems [20]. However, none of them have looked at the impact of HPMC viscosity grades on drug release and the porosity of monolithic matrices made under constant compression force for oral drug administration. The information about the effects of HPMC grades on the porosity and release characteristics of the hydrophilic matrix can be beneficial in interpreting the behavior of the HPMC-based system when utilized to manufacture oral drug delivery tablets.

This study used different HPMC viscosity grades to prepare the compressed HPMC-based matrix tablets at the constant compaction force, and the manufactured tablets were characterized. Propranolol HCl (PNL), a beta-blocker, was used as a model drug. PNL is a class I drug (high solubility and permeability) according to the Biopharmaceutics Classification System (BCS), making it an excellent model drug used for the study of extended-release drug products [21,22]. The compatibility among the drug, HPMC, and other excipients was verified using Fourier transform infrared spectroscopy (FT-IR), powder X-ray diffraction (PXRD), and differential scanning calorimetry (DSC). The morphology and porosity of the compressed HPMC-based matrix tablets were examined using scanning electron microscopy (SEM) and mercury porosimetry. Finally, the release of the PNL from the compressed HPMC-based matrix tablets was determined.

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