Enteric and hydrophilic polymers enhance dissolution and absorption of poorly soluble acidic drugs based on micro-environmental pH-modifying solid dispersion

Zhang, Shudong; Xu, Xiaolin; Sun, Weiwei; Zhang, Zhe; Pan, Baoliang; Qin, Hu

doi:10.1016/j.ejps.2021.106074

Cited by 5 publications

(1 citation statement)

References 37 publications

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“…14 The dependent solubility of VH incorporated the pH modifier like fumaric acid in the formulation which helps to maintain the microenvironment around the drug substance in acid nature and by improve the dissolution profile of the drug product in pH 6.8 PBS. 16 It was supported by the in vitro dissolution profiles of VHMT formulation with (F1a) and without fumaric acid (F2) with 10%w/w coating of EC shown in (Figure 6).…”

Section: In Vitro Dissolution Studiesmentioning

confidence: 71%

Design and Development of Multiparticulate Mini Tablets of Verapamil Hydrochloride for Pulsatile Drug Delivery

Kumar¹,

Nadendla²

2023

Ind. J. Pharm. Edu. Res.

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Objectives: The objective of the research was to develop and evaluate the multiparticulate pulsatile release minitablets of verapamil hydrochloride for the treatment of hypertension at a desired time to mimic the circadian rhythms and improve the patient compliance. Materials and Methods: Formulation was prepared by CODAS technology. It was designed to initiate the release of verapamil after 4h lag time and reached the therapeutic levels at in the early morning hours, when the blood pressure is at its highest. The core minitablets were prepared by wet granulation process and coated with water insoluble polymer like ethylcellulose along with hydrophilic plasticizer. The formulation attributes were optimized and evaluated the in vitro performance. Results: The in vitro dissolution studies revealed that the coating build-up of ethylcellulose controls the initial lag time and release rate of drug product. Among the formulations (F1a) 10% w/w ethylcellulose coated minitablets showed lag time for 4 hr and controlled the release up to 24 hr. The formulation optimization studies illumined the critical attributes like fumaric acid (F2), which modified the microenvironment and improved the dissolution profile of drug product in phosphate buffer. The optimized formulation (F1a) was compared against the marketed product (CALAPTIN 120 mg SR tablets) and observed that the dissolution behaviour of the drug product followed first-order kinetics. Conclusion:The outcomes were presumed that the pulsatile release has been accomplished from coated minitablets with a lag time of 4hr, which is reliable with the demands of the chronotherapeutic drug delivery by efficiently control the blood pressure at early morning.

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Section: In Vitro Dissolution Studiesmentioning

confidence: 71%