Quality by Design approach to understand the physicochemical phenomena involved in controlled release of captopril SR matrix tablets

Saurí, Josep; Millán, Diana; Suñé-Negre, Josep M.; Colom, Helena; Grau, Josep R. Ticó; Carmona, Montserrat Miñarro; Pérez-Lozano, Pilar; García-Montoya, Encarna

doi:10.1016/j.ijpharm.2014.10.050

Cited by 65 publications

(26 citation statements)

References 28 publications

(29 reference statements)

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“…In sample A10, a value of n lower than 0.45 was observed. Deviations from 0.45 values have been previously reported by other authors and interpreted in terms of polydispersion [ 33 ] and heterogeneity of the polymer layer [ 34 ].…”

Section: Resultsmentioning

confidence: 53%

Chitosan Spray-Dried Microparticles for Controlled Delivery of Venlafaxine Hydrochloride

et al. 2017

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Venlafaxine controlled drug delivery systems using different matrixes have been tested to reduce undesirable side effects in the treatment of depression. The legal status of chitosan (Cs) in Pharmacy has dramatically improved after its acceptance as excipient in several Pharmacopeias and, therefore, there is great interest in pharmaceutical formulations based on this polymer. In this paper, chitosan microcapsules cross-linked with sodium tripolyphosphate (TPP) for oral delivery of venlafaxine were formulated using the spray drying technique. The effect of chitosan physico-chemical properties, TPP concentration and TPP/Cs ratio on drug release was evaluated. The microcapsules were characterized in terms of size, zeta potential and morphology. The physical state of the drug was determined by X-ray diffraction (XRD) and the drug release from the microcapsules was studied in simulated gastric and intestinal fluids. The release pattern fitted well to the Peppas-Koersmeyer model with n exponents indicating anomalous transport.

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Section: Resultsmentioning

confidence: 53%

Chitosan Spray-Dried Microparticles for Controlled Delivery of Venlafaxine Hydrochloride

et al. 2017

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“…Microcapsules formed with EC and PEG 6,000 exhibited SR of MS in vivo and in vitro. The 18-h release behavior followed the Higuchi equation in water (19), and release rates in artificial gastric and intestinal fluid were similar and reproducible, with a release of ~80% of the encapsulated MS within 12 h. Furthermore, the novel microcapsule formula developed in the present study exhibited slower in vitro release of MS than the conventional tablet formula. These novel microcapsules are advantageous, as they achieve a more even SR in various environments, including water, artificial gastric fluid and artificial intestinal fluid.…”

Section: Discussionmentioning

confidence: 57%

“…The release equations of MS microcapsules in water, artificial gastric fluid, and in artificial intestinal fluid were determined to be Q=22.346t 1/2 +1.6068 (r= 0.992); Q=26.438t 1/2 +2.5376 (r=0.990); and Q=22.553t 1/2 -1.3337 (r=0.997), respectively. The cumulative release was found to fit the Higuchi equation (19), indicating that MS was released from microcapsules via diffusion. The MS microcapsules demonstrated a good SR profile in all three media, with a mean release of 96.1% within 18 h. When submerged in water, conventional SR-tablets exhibited a burst of release with >50% released in 2 h. Conversely, the MS microcapsule SR-tablets exhibited an almost linear SR in a 12-h test period (Fig.…”

Section: Level ------------------------------------------------------mentioning

confidence: 93%

Development of a sustained-release microcapsule for delivery of metoprolol succinate

Song

He²,

Ping

2017

Experimental and Therapeutic Medicine

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Sustained-release (SR) formulations of metoprolol succinate (MS) may minimize fluctuations in plasma concentration and decrease the resulting adverse events. The aim of the present study was to optimize the loading capacity of microcapsules and the SR of MS. A uniform design method was applied to optimize the formulation of SR microcapsules, composed of ethyl cellulose and polyethylene glycol 6,000, in one step via emulsion-solvent diffusion. release was studied, and the bioavailability of MS following dosing with novel microcapsules was compared with a commercially available MS formulation in beagle dogs. The present methodology achieved an entrapment efficiency of 83.2%, with 96.1% of drug released in 18 h, and the release was close to linear over a 12-h period. Pharmacokinetic studies of MS microcapsules in beagle dogs demonstrated a superior SR profile compared with conventional SR tablets. MS microcapsules were developed with high encapsulation efficiency, which had desirable SR properties and .

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“…Many researchers have reported the swelling properties of matrix tablets because they play a crucial role in drug release from the tablets [7,17,19]. The polymer-polymer and polymer-solvent interactions are major controlling factors of swelling and erosion [20]. When the media comes into contact with the tablets and water penetrates the tablets, consequently causing hydration, swelling, gel formation, and erosion may occur in parallel at the interface of the tablets.…”

Section: Swelling Behavior Of Hpmc Matrix Tablets )mentioning

confidence: 99%

Impact of Hydroxypropyl Methylcellulose (Hpmc) Type and Concentration on the Swelling and Release Properties of Propranolol Hydrochloride Matrix Tablets Usning a Simplex Centroid Design

Kraisit

2019

Int J App Pharm

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Objective: To prepare hydroxypropyl methylcellulose (HPMC) matrix tablets of propranolol hydrochloride (PNL) using a simplex centroid design.Methods: HPMC matrix tablets with different amounts and types of HPMC were prepared by direct compression. A simplex centroid design was used to evaluate tablet weight (1), thickness (Y2), hardness (Y3), axial swelling time at 0.5-12 h (Y4-Y9), radial swelling time at 0.5-12 h (Y10-Y15), and % released at 1-12 h (Y16-Y19). Results:The tablet weight, thickness, and hardness were 397.6-400.4 mg, 3.967-4.029 mm, and 106.9-139.0 N, respectively. The % swelling (axial) and % swelling (radial) Keywords: Hydroxypropyl methylcellulose (HPMC), Matrix tablets, Simplex centroid design, Design of experiment, Propranolol hydrochloride, Swelling, Release mechanism at 0.5-12 h were-8.715 to 59.889 and-1.887 to 49.287, respectively. The negative % swelling could be attributed to erosion of the tablets. The in vitro release of PNL from the tablets in buffer solution pH 1.2 (1 h) and pH 7.5 (3-12 h) was 21.12-76.22%. Tables with a high proportion of K100M HPMC had high PNL release, and the mechanism of PNL release was diffusion-and erosion-controlled. Conclusion:The simplex centroid design is potentially advantageous for formulating PNL-HPMC matrix tablets. I In nt te er rn na at ti io on na al l J Jo ou ur rn na al l o of f A Ap pp pl li ie ed d P Ph ha ar rm ma ac ce eu ut ti ic cs s

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Quality by Design approach to understand the physicochemical phenomena involved in controlled release of captopril SR matrix tablets

Cited by 65 publications

References 28 publications

Chitosan Spray-Dried Microparticles for Controlled Delivery of Venlafaxine Hydrochloride

Chitosan Spray-Dried Microparticles for Controlled Delivery of Venlafaxine Hydrochloride

Development of a sustained-release microcapsule for delivery of metoprolol succinate

Impact of Hydroxypropyl Methylcellulose (Hpmc) Type and Concentration on the Swelling and Release Properties of Propranolol Hydrochloride Matrix Tablets Usning a Simplex Centroid Design

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