ABSTRACT
Aim Enteric microspheres were prepared to prevent the interaction of drug with gastric acid and to improve its bioavailability. Methods The enteric microspheres with a matrix structure were successfully produced using a spherical crystallization technique. Hydroxypropyl methylcellulose phthalate ( HP-55 ), an enteric material, was coprecipitated with the drug by salting-out effect during the preparation process. A mixture of water and ethanol was chosen as a good solvent and dichloromethane was used as a the first time to prepare microspheres by making the water-soluble drug and water-insoluble excipient coprecipitated. In vivo test demonstrated that the drug absorption from the enteric oleanolic acid dihemiphthalate sodium (OADHPS) microspheres was significantly prolonged compared to that with OADHPS powder after a lag-time. Furthermore, the drug bioavailability was 181.6% greater than that with the OADHPS powder. Conclusion The microspheres of water soluble drug could be prepared by using water phase replacing organic phase as poor solvent which decrease the quantity of organic solvent and benefit the environment prevention.
ABSTRACT
Objective To study the relative bioavailability after ig rats with Ophiopogon japonicus saponin enteric microsphere in single-dose so as to give directly preparation quality evaluation. Methods(Establishing the) analysis method of HPLC-MS and dealing with the blood sample by solid phase extraction. Determining the diosgenin concentration in plasma after ig Ophiopogon japonicas saponin enteric microsphere and the suspension as comparison in single-dose, and calculating pharmacokinetic parameters and relative bioavailability. Results C_(max), t_(max), and AUC_(0-72) were (637.81?17.23) ng/mL, (4.0?0.0) h, and 7 840.01?412.03, respectively. Conclusion The characteristics of absorption, distribution, and elimination are resembled in rats between two preparations by ig in single-dose. The pharmacokinetic parameters are also identical. The relative bioavailability is (91.10?3.44)%.
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Objective To explore the prescription factor on Ophiopogon japonicus saponin enteric microsphere by spray drying technique. Methods Observing the type and content of enteric coating material, the type of plasticizer, the type and dosage of antistickiness material by single factor. Optimizing the prescription by orthogonal test design. Results Both Eudragit Ⅱ and micronization silica gel made in China could meet the need of the preparation. The best prescription included the proportion between drug and enteric coating material (1∶4), the dosage of castor oil (1%), and the dosage of micronization silica gel (1.5%). Conclusion O. japonicus saponin enteric microsphere accorded with the expecting demand. The kind of medical subsidiary material made in China will be the main raw material in producing the enteric microsphere. The study of prescription design will provide the basis for realizing microencap-sulation in Chinese materia medica.
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AIM: To explore the effect of drug content and encapsulated efficency of microsphere ophiopogon saponin preparation, providing more precise computational method. METHODS: Ophiopogon saponin enteric microsphere was prepared by spray drying technique, and the sum of saponin was determined by colorimetric analysis to evaluate the drug content and encapsulated efficency. RESULTS: The encapsulated efficency (%) was 94.75? 2.68. The drug content (mg/g) was 54.81? 2.12. CONCLUSION: The drug content the encapsulated efficency can affect the clinical dosage and the encapsulated efficency stands for the preparation process and the quality. So we should detect both drug content and the encapsulated efficency to evaluate preparation quality evaluation.
ABSTRACT
AIM:To prepare ophiopogonin enteric microsphere and to carry out the comprehensive evaluation.METHODS:The microsphere was prepared by spray-drying technology,it was evaluated by common index、 enteric index and physical index.RESULTS:Yield was(81.7? 2.1)%,embedding ratio was(86.55? 0.86)%,drug loading was(23.1? 0.2)%.The drug released degree in artificial gastric juice within 2 hours was(9.18? 0.08)%.The drug released rate in artificial intestinal juice within 45 minutes was(73.79? 0.29)%.The equilibrium moisture content decreased from 12.9% to 5.8%.CONCLUSION:An comprehensive evaluation was established.