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Development of spray-dried amorphous solid dispersions of tadalafil using glycyrrhizin for enhanced dissolution and aphrodisiac activity in male rats.
Muqtader Ahmed, Mohammed; Fatima, Farhat; Abul Kalam, Mohd; Alshamsan, Aws; Soliman, Gamal A; Shaikh, Abdul Azim; Alshahrani, Saad M; Aldawsari, Mohammed F; Bhatia, Saurabh; Khalid Anwer, Md.
Afiliación
  • Muqtader Ahmed M; Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.
  • Fatima F; Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.
  • Abul Kalam M; Nanobiotechnology Unit, Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
  • Alshamsan A; Nanobiotechnology Unit, Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
  • Soliman GA; Department of Pharmacology, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.
  • Shaikh AA; Riyadh Pharma Medical and Cosmetics Company Limited, Riyadh, Saudi Arabia.
  • Alshahrani SM; Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.
  • Aldawsari MF; Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.
  • Bhatia S; Amity Institute of Pharmacy, Amity University Haryana, 122413, India.
  • Khalid Anwer M; Natural and Medical Sciences Research Center, University of Nizwa, Oman.
Saudi Pharm J ; 28(12): 1817-1826, 2020 Dec.
Article en En | MEDLINE | ID: mdl-33424269
Tadalafil (TDL) is a phosphodiesterase-5 inhibitor (PDE5I), indicated for erectile dysfunction (ED). However, TDL exhibits poor aqueous solubility and dissolution rate, which may limit its application. This study aims to prepare amorphous solid dispersion (ASD) by spray-drying, using glycyrrhizin-a natural drug carrier. Particle and physicochemical characterizations were performed by particle size, polydispersity index measurement, yield, drug content estimation, Fourier Transformed Infrared (FTIR) spectroscopy, Differential scanning calorimetry (DSC), X-Ray Diffraction (XRD), Scanning Electron Microscopy (SEM) and dissolution study. In order to evaluate the aphrodisiac activity of the prepared ASD, sexual behavior study was performed in male rats. It is further considered for the stability study. Our results revealed that TDL-GLZ spray-dried dispersion was a successful drug-carrier binary mixture. XRD and SEM showed that ASD of TDL with GLZ presented in the amorphous state and dented-spherical shape, unlike the drug indicating crystalline and spiked shaped. The optimized ASD3 formulation with particle size (1.92 µm), PDI (0.32), yield (97.78%) and drug content (85.00%) showed 4.07 folds' increase in dissolution rate compared to pure TDL. The results obtained from the in vivo study exhibit significantly improved aphrodisiac activity with ASD3. The stability study revealed that the prepared ASD3 did not show any remarkable changes in the dissolution and drug content for 1 month storage at room temperature.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Saudi Pharm J Año: 2020 Tipo del documento: Article País de afiliación: Arabia Saudita Pais de publicación: Arabia Saudita

Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Saudi Pharm J Año: 2020 Tipo del documento: Article País de afiliación: Arabia Saudita Pais de publicación: Arabia Saudita