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Bioactive protein fraction DLBS1033 containing lumbrokinase isolated from Lumbricus rubellus: ex vivo, in vivo, and pharmaceutic studies.
Tjandrawinata, Raymond R; Trisina, Jessica; Rahayu, Puji; Prasetya, Lorentius Agung; Hanafiah, Aang; Rachmawati, Heni.
Afiliação
  • Tjandrawinata RR; Dexa Laboratories of Biomolecular Sciences, Dexa Medica, Cikarang, Indonesia.
  • Trisina J; Dexa Laboratories of Biomolecular Sciences, Dexa Medica, Cikarang, Indonesia.
  • Rahayu P; Dexa Laboratories of Biomolecular Sciences, Dexa Medica, Cikarang, Indonesia.
  • Prasetya LA; Dexa Laboratories of Biomolecular Sciences, Dexa Medica, Cikarang, Indonesia.
  • Hanafiah A; National Nuclear Energy Agency, Bandung, Indonesia.
  • Rachmawati H; School of Pharmacy, Bandung Institute of Technology, Bandung, Indonesia.
Drug Des Devel Ther ; 8: 1585-93, 2014.
Article em En | MEDLINE | ID: mdl-25284988
ABSTRACT
DLBS1033 is a bioactive protein fraction isolated from Lumbricus rubellus that tends to be unstable when exposed to the gastrointestinal environment. Accordingly, appropriate pharmaceutical development is needed to maximize absorption of the protein fraction in the gastrointestinal tract. In vitro, ex vivo, and in vivo stability assays were performed to study the stability of the bioactive protein fraction in gastric conditions. The bioactive protein fraction DLBS1033 was found to be unstable at low pH and in gastric fluid. The "enteric coating" formulation showed no leakage in gastric fluid-like medium and possessed a good release profile in simulated intestinal medium. DLBS1033 was absorbed through the small intestine in an intact protein form, confirmed by sodium dodecyl sulfate polyacrylamide gel electrophoresis (SDS PAGE) analysis. This result confirmed that an enteric coating formula using methacrylic acid copolymer could protect DLBS1033 from the acidic condition of the stomach by preventing the release of DLBS1033 in the stomach, while promoting its release when reaching the intestine. From the blood concentration-versus-time curve, (99m)Tc-DLBS1033 showed a circulation half-life of 70 minutes. This relatively long biological half-life supports its function as a thrombolytic protein. Thus, an enteric delivery system is considered the best approach for DLBS1033 as an oral thrombolytic agent.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Oligoquetos / Endopeptidases / Extratos de Tecidos / Fibrinolíticos Limite: Animals Idioma: En Revista: Drug Des Devel Ther Assunto da revista: FARMACOLOGIA / TERAPIA POR MEDICAMENTOS Ano de publicação: 2014 Tipo de documento: Article País de afiliação: Indonésia

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Oligoquetos / Endopeptidases / Extratos de Tecidos / Fibrinolíticos Limite: Animals Idioma: En Revista: Drug Des Devel Ther Assunto da revista: FARMACOLOGIA / TERAPIA POR MEDICAMENTOS Ano de publicação: 2014 Tipo de documento: Article País de afiliação: Indonésia
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