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Development of monolithic osmotic pump tablet system for isosorbide-5-mononitrate delivery and evaluation of it in vitro and in vivo.
Drug Dev Ind Pharm. 2009 Apr; 35(4):499-507.DD

Abstract

The objective of this study is to develop the monolithic osmotic pump tablet system (MOTS) containing isosorbide-5-mononitrate (5-ISMN), and to evaluate its in vitro and in vivo properties. The influences of tablet formulation variables, size and location of the delivery orifice, membrane variables, and pH value of the dissolution medium on 5-ISMN release from MOTS have been investigated. These results demonstrated that the tablet core played an important role in MOTS, and membrane variables could affect the 5-ISMN release rate. The optimal formulation of 5-ISMN MOTS was determined by uniform design. Furthermore, the dog pharmacokinetics and relative bioavailability of the test formulation (5-ISMN MOTS) have been compared with the reference formulation (Imdur: 60 mg/tablet, a sustained release, SR, tablet system) following an oral single dose of 60 mg given to each of six Beagle dogs. The mean drug fraction absorbed by the dog was calculated by the Wagner-Nelson technique. The results showed that drug concentration in plasma could be maintained more stable and longer after the administration of 5-ISMN MOTS compared with the matrix tablets of Imdur, and a level A "in vitro-in vivo correlation" was observed between the percentage released in vitro and percentage absorbed in vivo. It is concluded that 5-ISMN MOTS is more feasible for a long-acting preparation than 5-ISMN SR tablet system as once-a-day treatment, and it is very simple in preparation, and can release 5-ISMN at the rate of approximately zero order for the combination of hydroxypropylmethyl cellulose as retarder and NaCl as osmogent.

Links

Publisher Full Text (DOI)

Authors+Show Affiliations

Duan X
Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, Liaoning, People's Republic of China.
Liu Q
No affiliation info available
Zhang Y
No affiliation info available
Bi K
No affiliation info available
Chen X
No affiliation info available
Wang Y
No affiliation info available
Luo G
No affiliation info available

MeSH

AnimalsBiological AvailabilityChromatography, GasChromatography, High Pressure LiquidDelayed-Action PreparationsDogsDrug CompoundingDrug Delivery SystemsIn Vitro TechniquesIsosorbide DinitrateMaleOsmosisTabletsTechnology, PharmaceuticalTime FactorsVasodilator Agents

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

18979308

Citation

Duan, Xueyan, et al. "Development of Monolithic Osmotic Pump Tablet System for Isosorbide-5-mononitrate Delivery and Evaluation of It in Vitro and in Vivo." Drug Development and Industrial Pharmacy, vol. 35, no. 4, 2009, pp. 499-507.
Duan X, Liu Q, Zhang Y, et al. Development of monolithic osmotic pump tablet system for isosorbide-5-mononitrate delivery and evaluation of it in vitro and in vivo. Drug Dev Ind Pharm. 2009;35(4):499-507.
Duan, X., Liu, Q., Zhang, Y., Bi, K., Chen, X., Wang, Y., & Luo, G. (2009). Development of monolithic osmotic pump tablet system for isosorbide-5-mononitrate delivery and evaluation of it in vitro and in vivo. Drug Development and Industrial Pharmacy, 35(4), 499-507. https://doi.org/10.1080/03639040802459437
Duan X, et al. Development of Monolithic Osmotic Pump Tablet System for Isosorbide-5-mononitrate Delivery and Evaluation of It in Vitro and in Vivo. Drug Dev Ind Pharm. 2009;35(4):499-507. PubMed PMID: 18979308.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of monolithic osmotic pump tablet system for isosorbide-5-mononitrate delivery and evaluation of it in vitro and in vivo. AU - Duan,Xueyan, AU - Liu,Qingfei, AU - Zhang,Yu, AU - Bi,Kaishun, AU - Chen,Xi, AU - Wang,Yiming, AU - Luo,Guoan, PY - 2008/11/4/pubmed PY - 2009/5/26/medline PY - 2008/11/4/entrez SP - 499 EP - 507 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 35 IS - 4 N2 - The objective of this study is to develop the monolithic osmotic pump tablet system (MOTS) containing isosorbide-5-mononitrate (5-ISMN), and to evaluate its in vitro and in vivo properties. The influences of tablet formulation variables, size and location of the delivery orifice, membrane variables, and pH value of the dissolution medium on 5-ISMN release from MOTS have been investigated. These results demonstrated that the tablet core played an important role in MOTS, and membrane variables could affect the 5-ISMN release rate. The optimal formulation of 5-ISMN MOTS was determined by uniform design. Furthermore, the dog pharmacokinetics and relative bioavailability of the test formulation (5-ISMN MOTS) have been compared with the reference formulation (Imdur: 60 mg/tablet, a sustained release, SR, tablet system) following an oral single dose of 60 mg given to each of six Beagle dogs. The mean drug fraction absorbed by the dog was calculated by the Wagner-Nelson technique. The results showed that drug concentration in plasma could be maintained more stable and longer after the administration of 5-ISMN MOTS compared with the matrix tablets of Imdur, and a level A "in vitro-in vivo correlation" was observed between the percentage released in vitro and percentage absorbed in vivo. It is concluded that 5-ISMN MOTS is more feasible for a long-acting preparation than 5-ISMN SR tablet system as once-a-day treatment, and it is very simple in preparation, and can release 5-ISMN at the rate of approximately zero order for the combination of hydroxypropylmethyl cellulose as retarder and NaCl as osmogent. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/18979308/Development_of_monolithic_osmotic_pump_tablet_system_for_isosorbide_5_mononitrate_delivery_and_evaluation_of_it_in_vitro_and_in_vivo_ DB - PRIME DP - Unbound Medicine ER -