363618

Improvement of Class II Drug Properties by Crystal Agglomeration Design

Article

Last updated: 04 Jan 2025

Subjects

-

Tags

Pharmaceutics

Abstract

Repaglinide (RPG) is an antihyperglycemic drug; according to the Biopharmaceutical Classification System (BCS), it is considered a class II drug. It exhibits low oral bioavailability (about 56%) due to its poor water solubility and dissolution rate; also, it has very poor flowability. This study was introduced to design an RPG drug in the form of spherical crystal agglomerates using the spherical agglomeration technique to improve and solve these problems with the drug. Three solvents are used in this technique: a good solvent (acetone), a bad solvent (water), and a bridging liquid (chloroform). Different polymers were added in this process, like HPMC E5, Poloxamer 407, or PEG 6000, in various concentrations as a stabilizer. All developed agglomerates under an optical microscope have a nearly spherical shape with a particle size range of 342.52 to 529.2 μm. The percentage yield was 85.06% to 89.16%, and the drug content was 95.57% to 99.18%. Their flowability considerably improved where angle of repose (23.05 to 29.16), CI (12.73% to 18.92%), and HR (1.15 to 1.23) compared to pure RPG (49.36, 36.84%, and 1.58, respectively). The solubility improved by 1.8 to 3 folds compared to the drug, and the dissolution rate was significantly enhanced in all prepared agglomerates, where the complete release (99.89%) was observed in SA8 after 60 minutes. Scanning Electron Microscopy (SEM) confirmed that the crystals became more regular and spherical in shape. These results concluded that spherical crystallization could be an effective alternative method to improve RPG properties and enhance its bioavailability.

DOI

10.21608/aijpms.2024.234758.1236

Keywords

repaglinide, Spherical agglomerates, polymers, Spherical crystallization, Micrometric properties, Solubility, Dissolution

Authors

First Name

Maha

Last Name

Marzouk

MiddleName

A

Affiliation

Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt.

Email

mahamarzouk.pharmg@azhar.edu.eg

City

-

Orcid

-

First Name

Dina

Last Name

Osman

MiddleName

A

Affiliation

Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt.

Email

dosman1971@gmail.com

City

-

Orcid

-

First Name

Amany

Last Name

Abd El-Fattah

MiddleName

I

Affiliation

Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy (Girls), Al-Azhar University, Cairo, Egypt.

Email

dr.amanyhallol@gmail.com

City

-

Orcid

-

Volume

4

Article Issue

2

Related Issue

48196

Issue Date

2024-06-01

Receive Date

2023-09-06

Publish Date

2024-06-01

Page Start

125

Page End

140

Print ISSN

2735-4598

Online ISSN

2735-4601

Link

https://aijpms.journals.ekb.eg/article_363618.html

Detail API

https://aijpms.journals.ekb.eg/service?article_code=363618

Order

363,618

Type

Original research articles

Type Code

1,562

Publication Type

Journal

Publication Title

Azhar International Journal of Pharmaceutical and Medical Sciences

Publication Link

https://aijpms.journals.ekb.eg/

MainTitle

Improvement of Class II Drug Properties by Crystal Agglomeration Design

Details

Type

Article

Created At

27 Dec 2024