• Archives of Pharmacal Research
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• 제12권2호
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• pp.88-93
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• 1989

In order to obtain some informations about the effect of molecular weight on the release rate of drug from drug carrier, two types of poly-L-glutamic acid (PLGA)-cytarabine (ara-C) conjugates, PLGA-ara-C:I and PLGA-ara-C:II, were synthesized using two types of PLGA having different average molecular weight, 43,000 and 77,800, respectively. The PLGA-ara-C conjugates were synthesized by mixed anhydride method and found to be covalently linked. Both types of conjugates charged negatively at biological pH. The pH-dependent release rate of ara-C was observed in both cases, and the release rate was accelerated in basic, acidic conditions (the k values were 0.015 $day^{-1}$ at pH 7.0, 0.024 $day^{-1}$ at pH 5.0, and 0.059 $day^{-1}$ at pH 9.0 in the case of PLGA-ara-C:I) and in the presence of pretense. The time required for the release of 16.5% of ara-C from PLGA-ara-C:I were 8 hr and 144 hr in the presence and absence of protease, respectively. Although both types of conjugates showed similar drug substitution ratio, they showed different release rates. Between the two types of conjugates, PLGA-ara-C:II showed the faster release rate (0.030 vs 0.042 $day^{-1}$ in pH 7.4 phosphate buffer solution at $37^{\circ}C$) and the smaller activation energy for the release of drug (12.5 vs 7.7 Kcal/mol) than PLGA-ara-C:I. The characteristic effect of molecular weight on the release rates of PLGA-ara-C conjugates suggests that the drug release rate might be effectively controlled over a prolonged period of time by the combined use of the different types of PLGA-ara-C conjugates having different molecular weights.

• 약학회지
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• 제49권4호
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• pp.255-259
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• 2005

Financial standing of National Health Insurance has been experiencing a grave deterioration during the last 4-5 years, and the yearly amount paid by the insurance for drug expense rose up to 4 trillion won recently. Furthermore, the ratio of drug expenses in the total expenditure of the insurance reached about $25\%$, showing the tendency to be levelled off. As a measure to improve the financial deterioration of the insurance and to encourage generic substitution among the health professionals, we compared pharmacokinetic parameters of brand name drug (Lamisil) and generic drug (Muzonal) containing terbinafine HCl in healthy volunteers. The area under the curve (AUC) of the two drugs showed $2220.4\pm784.7\;and\;2143.1\pm861.6hr{\cdot}ng/ml$ in the corresponding order and no statistically significant difference was identified. The peak concentration $(C_{max})$ of the generic drug demonstrated $566.6\pm246.2 ng/ml$ compared to $550.8\pm204.0$ of brand name drug, which was not significantly different either. Time to reach peak concentration showed about 6 minutes difference between the drugs, which has no clinical significance to the treatment of dermatomycosis and dermatophytosis.

• Macromolecular Research
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• 제12권1호
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• pp.63-70
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• 2004

We have synthesized various types of poly(ethylene glycol) (PEG)-ibuprofen conjugates by the nucleophilic substitution of bromo-terminated PEG with ibuprofen-Cs salt; PN (Pluronic) was also used in place of PEG. All the bromo-terminated PEGs and PN were obtained in high yield. Conversions of the terminal hydroxyl groups to bromo-termini were quantitative, as were the drug conjugation processes. The Ι$_1$/Ι$_3$values obtained from solutions of the ibuprofen-conjugated prodrugs are summarized in relation to those of ibuprofen in water and in aqueous solutions of the original PEG, PN, and several ordinary surfactants. We believe that the fully hydrophilic PEG is completely hydrated and forms no hydrophobic pocket by segment aggregation. These results indicate that the probe environment is significantly hydrophobic, particularly in the solution of prodrug PN, for which the ratio is similar to that obtained from typical micelles of surfactants. The results suggest, therefore, that the present synthetic method is very useful for preparing PEG-based prodrugs from pharmaceuticals having carboxyl functionalities.

• Bulletin of the Korean Chemical Society
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• 제33권12호
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• pp.4035-4040
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• 2012

Presented study describes the synthesis of photo cross-linkable and water soluble hydroxyethyl starch hydroxyethyl methacrylate (HESHEMA) samples with different degree of substitution (DS) by functionalization of hydroxyethyl starch (HES) with hydroxyethyl methacrylate (HEMA) or hydroxyethyl methacrylate carbonylimidazole (HEMACI) in DMSO using two different routes. It was revealed that the reaction time for HESHEMA synthesis can be reduced from 5 days to 24 h by conducting the reaction at $80^{\circ}C$ instead of at room temperature. Solubility of HESHEMA was found to be dependent on DS which in turn was dependent on ratio between HES and HEMA or HEMACI. HESHEMA samples with DS > 0.24 depicted insoluble in water, whereas the samples with DS < 0.05 did not form appreciable gel. HESHEMA samples with appropriate DS were converted into hydrogels by cross-linking polymer chains under UV radiations and resulting HESHEMA hydrogels showed swelling up to 1200%. Application of HESHEMA in controlled drug delivery was investigated by diffusion based encapsulation of Ondansetron, a serotonin 5-$HT_3$ receptor antagonist drug, mainly used for nausea and vomiting treatment.

• 대한의용생체공학회:의공학회지
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• 제10권3호
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• pp.237-242
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• 1989

The physical properties and drug release behaviours of polyethylene glycol grafted poly ${\gamma}$- benzyl L-glutamate (PEG- g- PBLG), polyethylene glycol crosslinked poly ${\gamma}$-benzyl L- glutamate(PEG-c-PBLG), and PBLG homopolymer are compared. PBLG containing PEG segements showed higher wettability and larger enlongation than PBLG homoplymer, but lower elastic modulus. The release rate of rhodamine is strongly influenced by the wettability of the polymer. Rhodamine is more rapidly released from PEG-c-PBLG membrane having a larger water contact angle than from other polymer having a lower water contact angle. The surfaces of PBLG derivative membranes are modified by substitution reaction using hydroxyalkylamine. The resulting polymer membranes showed hider wettability and swelling ratio than virgin membranes.

• 농약과학회지
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• 제15권4호
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• pp.507-528
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• 2011

포장에서 농약 살포액의 조제, 살포 등의 작업을 수행하는 농작업자는 피부노출, 호흡노출경로를 통해 농약에 노출되며, 이러한 상황에서의 농약 노출에 대한 합리적인 위해성 평가를 위해서는 해당 영농상황에서 노출량을 정량적으로 측정해야 한다. 농약 노출 측정방법으로 patch, 장갑, 양말, 마스크를 이용하는 방법과 호흡 노출은 주로 고체흡착제와 공기흡입펌프가 연결된 personal air monitor를 사용하는 것이 좋을 것으로 판단된다. 이 농작업자의 정량적 피부 노출 측정법으로 유효할 것으로 판단된다. 노출 재료에 침착/부착된 농약량이나 고체흡착제에 포집된 농약량을 신체 전체에 대한 농약 노출량으로 외삽하기 위한 EPA 자료를 대체할 수 있도록 한국 사람의 표준 신체표면적 및 호흡률을 제안하였다. 중요한 노출 인자인 피부노출의 의복 침투율과 피부 침투율, 그리고 호흡노출의 침투율을 UK-POEM과 관련된 연구결과를 참고하여 다양하게 제안하였다. 노출 평가를 위한 살포 시간은 노출 측정 재료에 침착된 농약이 분석이 될 만큼 충분한 농약이 포집될 수 있도록 살포시간이 충분해야 하는데, 국내의 SS기나 동력분무기의 경우는 1반복 당 모두 약 20~40분에 살포(약 0.1~0.2 ha)로 해서 3반복 측정 결과를 4시간으로 환산할 것을 제안하였다.