Abstract:Recent advances in drug delivery systems have aimed to achieve better patient compliance. One of these advances is the formulation of orally disintegrating tablets (ODTs) that dissolve instantaneously, releasing drugs within a few seconds without the need of water. The main objective of this paper was to prepare and develop ODTs of clopidogrel. The ODTs were prepared by direct compression. The effect of three superdisintegrants, namely crospovidone, croscarmellose sodium, and sodium starch glycolate, using thr… Show more
“…This may be due to the conversion of the hydrochloride salt to its less soluble free base [15]. Similar pH dependent Meclizine HCl release was also observed by Mahrous et al [2]. …”
Section: Discussionsupporting
confidence: 57%
“…It is also indicated for pruritus, anaphylactic reactions and vertigo associated with diseases affecting the vestibular system (e.g., Meniere disease, labyrinthitis) [1, 2]. It is more frequently prescribed because of fewer adverse effects [1].…”
Section: Introductionmentioning
confidence: 99%
“…Literature survey results show that lipid based ER pellets of Meclizine HCl have not been reported yet. Meclizine HCl has a plasma elimination half-life of 5–6 h [1, 2]. For the treatment of vertigo, the standard dose is 25–100 mg/day, given in two or more divided doses [4].…”
BackgroundAntiemetic agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The approved therapeutic dose and shorter elimination half-life make Meclizine HCl a potential candidate to be formulated in extended release dosage form. This study was aimed to develop extended release Meclizine HCl pellets by extrusion spheronization using natural and synthetic lipids. Influence of lipid type, drug/lipid ratio and combinations of different lipids on drug release and sphericity of pellets were evaluated.MethodsThirty two formulations were prepared with four different lipids, Glyceryl monostearate (Geleol®), Glyceryl palmitostearate (Precirol®), Glyceryl behenate (Compritol®) and Carnauba wax, utilized either alone or in combinations of drug/lipid ratio of 1:0.5–1:3. Dissolution studies were performed at variable pH and release kinetics were analyzed. Fourier transform infrared spectroscopy was conducted and no drug lipid interaction was found.ResultsSphericity indicated by shape factor (eR) varied with type and concentration of lipids: Geleol® (eR = 0.891–0.997), Precirol® (eR = 0.611–0.743), Compritol® (eR = 0.665–0.729) and Carnauba wax (eR = 0.499-0.551). Highly spherical pellets were obtained with Geleol® (Aspect ratio = 1.005–1.052) whereas irregularly shaped pellets were formed using Carnauba wax (Aspect ratio = 1.153–1.309). Drug release was effectively controlled by three different combinations of lipids: (i) Geleol® and Compritol®, (ii) Geleol® and Carnauba wax and (iii) Geleol®, Compritol® and Carnauba wax. Scanning electron microscopy of Compritol® pellets showed smooth surface with pores, whereas, irregular rough surface with hollow depressions was observed in Carnauba wax pellets. Energy dispersive spectroscopy indicated elemental composition of lipid matrix pellets. Kinetics of (i) Geleol® and Compritol® pellets, explained by Korsmeyer-Peppas (R2 = 0.978–0.993) indicated non-Fickian diffusion (n = 0.519-0.597). Combinations of (ii) Geleol® and Carnauba wax and (iii) Geleol®, Compritol® and Carnauba wax pellets followed Zero-order (R2 = 0.991–0.995). Similarity test was performed using combination of Geleol® and Compritol® (i) as a reference.ConclusionsMatrices for the extended release of Meclizine HCl from extruded-spheronized pellets were successfully formed by using three lipids (Geleol®, Compritol® and Carnauba wax) in different combinations. The encapsulated pellets of Meclizine HCl can be effectively used for treatment of motion sickness, nausea and vertigo for extended period of time.
“…This may be due to the conversion of the hydrochloride salt to its less soluble free base [15]. Similar pH dependent Meclizine HCl release was also observed by Mahrous et al [2]. …”
Section: Discussionsupporting
confidence: 57%
“…It is also indicated for pruritus, anaphylactic reactions and vertigo associated with diseases affecting the vestibular system (e.g., Meniere disease, labyrinthitis) [1, 2]. It is more frequently prescribed because of fewer adverse effects [1].…”
Section: Introductionmentioning
confidence: 99%
“…Literature survey results show that lipid based ER pellets of Meclizine HCl have not been reported yet. Meclizine HCl has a plasma elimination half-life of 5–6 h [1, 2]. For the treatment of vertigo, the standard dose is 25–100 mg/day, given in two or more divided doses [4].…”
BackgroundAntiemetic agent Meclizine HCl, widely prescribed in vertigo, is available only in immediate release dosage forms. The approved therapeutic dose and shorter elimination half-life make Meclizine HCl a potential candidate to be formulated in extended release dosage form. This study was aimed to develop extended release Meclizine HCl pellets by extrusion spheronization using natural and synthetic lipids. Influence of lipid type, drug/lipid ratio and combinations of different lipids on drug release and sphericity of pellets were evaluated.MethodsThirty two formulations were prepared with four different lipids, Glyceryl monostearate (Geleol®), Glyceryl palmitostearate (Precirol®), Glyceryl behenate (Compritol®) and Carnauba wax, utilized either alone or in combinations of drug/lipid ratio of 1:0.5–1:3. Dissolution studies were performed at variable pH and release kinetics were analyzed. Fourier transform infrared spectroscopy was conducted and no drug lipid interaction was found.ResultsSphericity indicated by shape factor (eR) varied with type and concentration of lipids: Geleol® (eR = 0.891–0.997), Precirol® (eR = 0.611–0.743), Compritol® (eR = 0.665–0.729) and Carnauba wax (eR = 0.499-0.551). Highly spherical pellets were obtained with Geleol® (Aspect ratio = 1.005–1.052) whereas irregularly shaped pellets were formed using Carnauba wax (Aspect ratio = 1.153–1.309). Drug release was effectively controlled by three different combinations of lipids: (i) Geleol® and Compritol®, (ii) Geleol® and Carnauba wax and (iii) Geleol®, Compritol® and Carnauba wax. Scanning electron microscopy of Compritol® pellets showed smooth surface with pores, whereas, irregular rough surface with hollow depressions was observed in Carnauba wax pellets. Energy dispersive spectroscopy indicated elemental composition of lipid matrix pellets. Kinetics of (i) Geleol® and Compritol® pellets, explained by Korsmeyer-Peppas (R2 = 0.978–0.993) indicated non-Fickian diffusion (n = 0.519-0.597). Combinations of (ii) Geleol® and Carnauba wax and (iii) Geleol®, Compritol® and Carnauba wax pellets followed Zero-order (R2 = 0.991–0.995). Similarity test was performed using combination of Geleol® and Compritol® (i) as a reference.ConclusionsMatrices for the extended release of Meclizine HCl from extruded-spheronized pellets were successfully formed by using three lipids (Geleol®, Compritol® and Carnauba wax) in different combinations. The encapsulated pellets of Meclizine HCl can be effectively used for treatment of motion sickness, nausea and vertigo for extended period of time.
“…The disintegration time was determined in phosphate buffer pH 6.8 using tablet disintegration test apparatus (Electrolab, ED-21, Mumbai, India) on six tablets according to the USP30-NF25 requirements for immediate release tablets. The tablet was put in 500 ml phosphate buffer pH 6.8 and the time taken for the tablet to disintegrate into fine particles was calculated (Mahrous et al, 2016).…”
Propafenone HCl (PPH), an antiarrhythmic drug, has a bitter taste, short half-life, delayed drug dissolution and side effects. Thus, the purpose of this work is to develop orally fast dissolving tablets (OFDTs) containing PPH to provide a rapid drug dissolution and subsequently give rapid onset of action of PPH as an antiarrhythmic drug. Moreover, OFDTs of PPH reduce its side effects and improve its bioavailability. Propafenone HCl (PPH), an antiarrhythmic drug, has a bitter taste, short half-life, delayed drug dissolution and side effects. Direct compression method was used for the preparation of 15 formulations OFDTs containing PPH using directly compressible excipients, subliming agent and superdisintegrants. The prepared tablets were undergone physical characterization, dissolution and stability studies. All pre- and post-compression tests met the pharmacopoeia specifications. dissolution of the prepared PPH OFDTs exhibited high dissolution rate than compared to the marketed tablets. It was found that the tablets prepared by using the higher concentration of crospovidone were found to dissolute the drug at a faster rate when compared to other concentrations. A formula containing croscarmellose sodium showed the higher present of PPH dissolved as compared to the other formulations. It was concluded that PPH OFDTs were formulated successfully with acceptable physical and chemical properties with rapid disintegration in the oral cavity, rapid onset of action, and enhanced patient compliance. It was found that F10 showed good stability upon storage at 25 and 40 °C for 3 months. Formulation of PPH OFDTs can result in a significant improvement in the PPH bioavailability since the first pass metabolism will be avoided.
“…Mahrous et al, studied the effect of three superdisintegrants; crospovidone, croscarmellose sodium, and sodium starch glycolate using ODTs of Clopidrogel, they reported that in-vitro disintegration tests and in vitro drug release, tablets showed a fast disintegration within seconds at pH 6.8 and more than 90% of the drug was released within 5 min in acidic medium 18 . Results obtained for the similarity factor at 6 h of release revealed differences in the release profile of the assayed formulations compared to the reference product Table 4.…”
Section: Fig 4: Release Profile Of Nifedipine At 12 H Of Release Of mentioning
Push-pull osmotic pumps are controlled drug delivery systems for drugs with a broad range of solubilities; especially drugs that are poorly water-soluble. The aim of the present study was to evaluate the performance of the superdisintegrants (SD), crospovidone (CPVP), croscarmellose sodium (CS), and sodium starch glycolate (SSG), in pushpull tablets containing Nifedipine (NP) as a model drug. We performed an in-vitro dissolution test with phosphate buffer (0.05M) at pH 7.5 for 12 h. The amount of released NP was determined using a UV/Visible spectro-photometric method at a wavelength of 238 nm. At 12 h of release, the profile of CPVP-and CS-containing osmotic tablets was like that of the reference product Adalat OROS ® , whereas the SSG-containing tablet showed differences. It is very important mention that in the first 6 h of the assay, all release profiles were different compared to the commercially available reference product. The tablets containing superdisintegrants showed faster drug delivery rates and a reduction in lag time.
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