Coated dextrin microcapsules of amlodipine incorporable into orally disintegrating tablets for geriatric patients

Jang, Dong‐Jin; Bae, Soo Kyung; Oh, Euichaul

doi:10.1016/j.biopha.2014.10.010

Cited by 14 publications

(5 citation statements)

References 29 publications

(62 reference statements)

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“…In this study, to manufacture RDS, dextrin was selected as an effective diluent to compose a matrix. It has been used as a polymeric carrier in various kinds of solid dosage forms, since it is stable and compatible with hydrophilic or hydrophobic material and also has good free-flowing and water-soluble properties suitable for improved dissolution or reconstitution of the solid dosage form [ 31 , 32 ]. Due to these merits of dextrin, it was confirmed that RDS could be perfectly recovered to nanosuspension before the spray-drying process as it was well reconstituted in water ( Figure 1 D).…”

Section: Resultsmentioning

confidence: 99%

“…Dextrin has various advantages as a pharmaceutical excipient. Dextrin is known to be eligible as an immediate-dissolving solid dosage formulation forming polymer due to its non-toxic, high water-soluble, and biocompatible properties [ 31 , 32 ]. Dextrin is an excellent wall-forming material for micro-encapsulation of core materials [ 33 , 34 ].…”

Section: Introductionmentioning

confidence: 99%

“…Dextrin is an excellent wall-forming material for micro-encapsulation of core materials [ 33 , 34 ]. Unlike many other polymers, solid dosage forms made of dextrin have non-sticky and free-flowing properties [ 31 , 32 ], which can be beneficial to further unit operations after the drying process. The redispersibility, morphology, crystallinity, physical stability, dissolution, and pharmacokinetic profile of celecoxib nanosuspension or RDS were characterized.…”

Section: Introductionmentioning

confidence: 99%

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Development and Evaluation of a Reconstitutable Dry Suspension to Improve the Dissolution and Oral Absorption of Poorly Water-Soluble Celecoxib

Kim

Park²,

Park

et al. 2018

Pharmaceutics

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This study aims at developing and evaluating reconstitutable dry suspension (RDS) improved for dissolution rate, oral absorption, and convenience of use of poorly water-soluble celecoxib (CXB). Micro-sized CXB particle was used to manufacture nanosuspension by using bead milling and then RDS was made by spray-drying the nanosuspension with effective resuspension agent, dextrin. The redispersibility, morphology, particle size, crystallinity, stability, dissolution, and pharmacokinetic profile of the RDS were evaluated. RDS was effectively reconstituted into nanoparticles in 775.8 ± 11.6 nm. It was confirmed that CXB particles are reduced into needle-shape ones in size after the bead-milling process, and the description of CXB was the same in the reconstituted suspension. Through the CXB crystallinity study using differential scanning calorimetry (DSC) and XRD analysis, it was identified that CXB has the CXB active pharmaceutical ingredient (API)’s original crystallinity after the bead milling and spray-drying process. In vitro dissolution of RDS was higher than that of CXB powder (93% versus 28% dissolution at 30 min). Furthermore, RDS formulation resulted in 5.7 and 6.3-fold higher area under the curve (AUC∞) and peak concentration (Cmax) of CXB compared to after oral administration of CXB powder in rats. Collectively, our results suggest that the RDS may be a potential oral dosage formulation for CXB to improve its bioavailability and patient compliance.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Development and Evaluation of a Reconstitutable Dry Suspension to Improve the Dissolution and Oral Absorption of Poorly Water-Soluble Celecoxib

Kim

Park²,

Park

et al. 2018

Pharmaceutics

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“…10 tablets were pulverized. A blend equivalent to 20 mg LCD was dissolved in methanol, diluted and the absorbance was measured at λ max of 239 nm 21 .…”

Section: Uniformity Of Drug Contentmentioning

confidence: 99%

Fabrication and Characterization of Lercanidipine Hydrochloride Solid Dispersions by Fusion Technique

Reddy

Dugasani²,

Devanna

2022

Int J Life Sci Pharm Res

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The authors aimed to design solid dispersions with Lercanidipine Hydrochloride (LCD) with PVP K-30, Poloxamer-188, and HPMC K4M as carriers. Various mixtures of LCD and Polymers (PVP K-30, Poloxamer-188, and HPMC K4M) were made in 1:1, 1:3, 1:5 and 1:7 ratios, and the solid dispersion was prepared by melting tactic, later compressed into tablets. Drug excipient compatibility studies were examined by DSC and FTIR studies. LCD was found to compatible with carriers used. The LCD solid dispersion was measured for physicochemical quality both in solid dispersions SD, and tablet states. The LCD solid dispersions found to have excellent flow possessions and compression assets. The yield of prepared solid dispersion was observed to be more than 90%), and the formulation LPOX-3 has showed a good yield of 98.9±1.95%, The tablets which were compressed from solid dispersions were found to have a uniform in size, shape, color, and consistency. The tablets were observed to have a uniform in thickness, and weight and ranged from 300.2±1.64 to 301.7±1.64 mg. The loss on friability was less than 1%, and the hardness was more than 4 Kg/cm2 indicates significant mechanical strength and the LCD content was also found to be uniform (96.8±1.35 to 99.9±2.34). The solubility of LCD was found to be good in 0.1N HCl and diminished with an increase in pH of the buffer. LCD released from the tablets were firstly by eruption followed by zero order. The dissolution was found to be good in solid dispersions with LCD: Poloxamer-188 at the ratio of 1:5. The results obtained were satisfactory. The study concludes that LCD solid dispersions (LPOX-3) with 1:5 ratios of LCD and Poloxamer-188 was found to be a better carrier than PVP K-30, and HPMC K4M in increasing the solubility of LCD from the solid dispersions.

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“…The ODT form of Amlodipine besylate is comparatively bioequivalent to conventional tablets 54,55 . ODT Amlodipine was successfully tested in geriatric patients 56 . The main drawback of using ODT Amlodipine is its bitter taste 57 .…”

Section: Amlodipinementioning

confidence: 99%

Mucosal delivery systems of antihypertensive drugs: A practical approach in general practice

Biały¹,

Wojcik²,

Młynarczuk-Biały³

2018

BIOMED PAP

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Patients who are unable to receive oral medication (p.o.) are a major problem in outpatient settings, especially in home health care systems. Mucosal administration of drugs offers an alternative to the oral route, especially when the parenteral mode cannot be used. There are three main pathways of mucosal administration: sublingual/buccal, intranasal and rectal. We discuss the possibility of mucosal delivery of antihypertensive drugs. Perindopril arginine and Amlodipine besylate are registered in the EU as orodispersible tablets for oromucosal delivery, however, they are not available in all countries. For this reason, we describe other drugs suitable for mucosal delivery: Captopril and Nitrendipine in the sublingual system and Metoprolol tartrate, Propranolol and Furosemide by the transrectal route. Based on the published data and common clinical practice we discuss the use of mucosal delivery systems of all these antihypertensive drugs with special attention to their pharmacokinetics. We illustrate this mini-review with a case report of the prolonged-term use of mucosal delivery of sublingual Captopril and Nitrendipine combined with rectal Metoprolol tartrate and Furosemide in a patient with severe hypertension unable to receive medication p.o. This is also a report on the first human use of Furosemide-containing suppositories as well as prolonged-term transmucosal administration of these four drugs, describing a practical approach leading to successful control of severe hypertension with four antihypertensive drugs delivered via the mucosal route. The treatment was effective and without side effects; however, the long-term safety and efficacy of such therapy must be confirmed by randomized clinical trials.

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Coated dextrin microcapsules of amlodipine incorporable into orally disintegrating tablets for geriatric patients

Cited by 14 publications

References 29 publications

Development and Evaluation of a Reconstitutable Dry Suspension to Improve the Dissolution and Oral Absorption of Poorly Water-Soluble Celecoxib

Development and Evaluation of a Reconstitutable Dry Suspension to Improve the Dissolution and Oral Absorption of Poorly Water-Soluble Celecoxib

Fabrication and Characterization of Lercanidipine Hydrochloride Solid Dispersions by Fusion Technique

Mucosal delivery systems of antihypertensive drugs: A practical approach in general practice

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