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Preparation and in vitro-in vivo evaluation of none gastric resident dipyridamole (DIP) sustained-release pellets with enhanced bioavailability.
Int J Pharm. 2012 Jan 17; 422(1-2):9-16.IJ

Abstract

The objective of this study was to develop none gastric resident sustained-release pellets loaded with dipyridamole with a high bioavailability. Two different kinds of core pellets, one containing citric acid as a pH-modifier (CAP) and, the other without pH-modifier (NCAP) were prepared by extrusion-spheronization and then coated with mixtures of enteric soluble and insoluble polymers (referred to as CAP(1) and NCAP(1)) or insoluble polymer alone (referred to as CAP(2) and NCAP(2)). The relative bioavailability of the sustained-release pellets was studied in fasted beagle dogs after oral administration using a commercially available immediate release tablet (IRT) as a reference. The in vitro release, in vivo absorption and in vitro-in vivo correlation were also evaluated. Results revealed that the plasma drug concentrations after administration of CAP(2), NCAP(1) and NCAP(2) were undetectable, indicating that the drug release was almost zero from the preparations throughout the gastro-intestinal tract. The C(max), T(max) and AUC((0→24)) of CAP(1) were 0.78 ± 0.23 (μg/ml), 3.80 ± 0.30 (h), and 6.74 ± 0.47 (μg/mlh), respectively. While the corresponding values were 2.23 ± 0.32 (μg/ml), 3.00 ± 0.44 (h) and 9.42 ± 0.69 (μg/mlh) for IRT. The relative bioavailability of CAP(1) was 71.55% compared with IRT. By combined incorporation of a pH-modifier into the core of pellets to modify the inner micro-environment and employing mixtures of enteric soluble and insoluble polymers as a retarding layer, drugs with high solubility in stomach and limited solubility in small intestine, such as DIP, could be successfully formulated as sustained release preparations with no pH-dependence in drug release and enhanced bioavailability.

Authors+Show Affiliations

Department of Pharmaceutics, Shenyang Pharmaceutical University, Wen Hua Road No. 103 Shenyang 110016, China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

22001837

Citation

Xu, Lishuang, et al. "Preparation and in Vitro-in Vivo Evaluation of None Gastric Resident Dipyridamole (DIP) Sustained-release Pellets With Enhanced Bioavailability." International Journal of Pharmaceutics, vol. 422, no. 1-2, 2012, pp. 9-16.
Xu L, Luo Y, Feng J, et al. Preparation and in vitro-in vivo evaluation of none gastric resident dipyridamole (DIP) sustained-release pellets with enhanced bioavailability. Int J Pharm. 2012;422(1-2):9-16.
Xu, L., Luo, Y., Feng, J., Xu, M., Tao, X., He, H., & Tang, X. (2012). Preparation and in vitro-in vivo evaluation of none gastric resident dipyridamole (DIP) sustained-release pellets with enhanced bioavailability. International Journal of Pharmaceutics, 422(1-2), 9-16. https://doi.org/10.1016/j.ijpharm.2011.10.014
Xu L, et al. Preparation and in Vitro-in Vivo Evaluation of None Gastric Resident Dipyridamole (DIP) Sustained-release Pellets With Enhanced Bioavailability. Int J Pharm. 2012 Jan 17;422(1-2):9-16. PubMed PMID: 22001837.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation and in vitro-in vivo evaluation of none gastric resident dipyridamole (DIP) sustained-release pellets with enhanced bioavailability. AU - Xu,Lishuang, AU - Luo,Yanfei, AU - Feng,Jia, AU - Xu,Ming, AU - Tao,Xiaoguang, AU - He,Haibing, AU - Tang,Xing, Y1 - 2011/10/06/ PY - 2011/08/03/received PY - 2011/09/05/revised PY - 2011/10/01/accepted PY - 2011/10/18/entrez PY - 2011/10/18/pubmed PY - 2012/4/28/medline SP - 9 EP - 16 JF - International journal of pharmaceutics JO - Int J Pharm VL - 422 IS - 1-2 N2 - The objective of this study was to develop none gastric resident sustained-release pellets loaded with dipyridamole with a high bioavailability. Two different kinds of core pellets, one containing citric acid as a pH-modifier (CAP) and, the other without pH-modifier (NCAP) were prepared by extrusion-spheronization and then coated with mixtures of enteric soluble and insoluble polymers (referred to as CAP(1) and NCAP(1)) or insoluble polymer alone (referred to as CAP(2) and NCAP(2)). The relative bioavailability of the sustained-release pellets was studied in fasted beagle dogs after oral administration using a commercially available immediate release tablet (IRT) as a reference. The in vitro release, in vivo absorption and in vitro-in vivo correlation were also evaluated. Results revealed that the plasma drug concentrations after administration of CAP(2), NCAP(1) and NCAP(2) were undetectable, indicating that the drug release was almost zero from the preparations throughout the gastro-intestinal tract. The C(max), T(max) and AUC((0→24)) of CAP(1) were 0.78 ± 0.23 (μg/ml), 3.80 ± 0.30 (h), and 6.74 ± 0.47 (μg/mlh), respectively. While the corresponding values were 2.23 ± 0.32 (μg/ml), 3.00 ± 0.44 (h) and 9.42 ± 0.69 (μg/mlh) for IRT. The relative bioavailability of CAP(1) was 71.55% compared with IRT. By combined incorporation of a pH-modifier into the core of pellets to modify the inner micro-environment and employing mixtures of enteric soluble and insoluble polymers as a retarding layer, drugs with high solubility in stomach and limited solubility in small intestine, such as DIP, could be successfully formulated as sustained release preparations with no pH-dependence in drug release and enhanced bioavailability. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/22001837/Preparation_and_in_vitro_in_vivo_evaluation_of_none_gastric_resident_dipyridamole__DIP__sustained_release_pellets_with_enhanced_bioavailability_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(11)00909-4 DB - PRIME DP - Unbound Medicine ER -