Huang Yuan
(Key Laboratory of Drug Targeting and Novel Drug Delivery Systems, West China School of Pharmacy, Sichuan University)
,
Zheng ling Ii
(Key Laboratory of Drug Targeting and Novel Drug Delivery Systems, West China School of Pharmacy, Sichuan University)
,
Liu Jun
(Key Laboratory of Drug Targeting and Novel Drug Delivery Systems, West China School of Pharmacy, Sichuan University)
,
Zhang Zhi rong
(Key Laboratory of Drug Targeting and Novel Drug Delivery Systems, West China School of Pharmacy, Sichuan University)
HPMC (Hydroxypropyl methylcellulose) was chemically modified, using maleic anhydrides, to obtain pH-sensitive HPMCAM (Hydroxypropyl methylcellulose acetate maleate) polymers for use as novel duodenum-specific coating agents. The pharmaceutical properties of HPMCAM, such as film forming, acid values,...
HPMC (Hydroxypropyl methylcellulose) was chemically modified, using maleic anhydrides, to obtain pH-sensitive HPMCAM (Hydroxypropyl methylcellulose acetate maleate) polymers for use as novel duodenum-specific coating agents. The pharmaceutical properties of HPMCAM, such as film forming, acid values, pH-sensitive values, water vapor permeability, tensile strength and Tg, were investigated, and found to show good film forming properties. The pHsensitive values were 3.0 to 3.7. In vitro results demonstrate that HPMCAM could completely suppress drug release within 2h in a simulated gastric fluid (pH 1.2) and rapidly release the drug in a simulated pathological duodenal fluid (pH 3.4). These results indicate that HPMCAM might be a useful material for a duodenum-specific drug delivery system.
HPMC (Hydroxypropyl methylcellulose) was chemically modified, using maleic anhydrides, to obtain pH-sensitive HPMCAM (Hydroxypropyl methylcellulose acetate maleate) polymers for use as novel duodenum-specific coating agents. The pharmaceutical properties of HPMCAM, such as film forming, acid values, pH-sensitive values, water vapor permeability, tensile strength and Tg, were investigated, and found to show good film forming properties. The pHsensitive values were 3.0 to 3.7. In vitro results demonstrate that HPMCAM could completely suppress drug release within 2h in a simulated gastric fluid (pH 1.2) and rapidly release the drug in a simulated pathological duodenal fluid (pH 3.4). These results indicate that HPMCAM might be a useful material for a duodenum-specific drug delivery system.
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문제 정의
Both cause the quick release, reaching the maximum concentration in aro니nd 12 min. This kind of release behavior goes against the treatment of duodenal ulcers, whereas the press- coated tablets prepared in this study reach the anticipated objective of this experiment. That is: they were hardly soluble in the simulated gastric fluid, but had good solubility in the simulated pathological duodenal fluid, reaching their maximum concentration, ensuring the drug accumulated on the surface of d니。denal ulcer, thereby achieve the maximum effect.
대상 데이터
The obtained polymers were dissolved in methanol/ methylene chloride 1:1 (v/v), the solutions cast on glass plates and dried to form films 30 to 50 jim thick. The films were cut into 3 mm sq니are pieces. The diss이니tion pH of the film was measured at 37±0.
성능/효과
In conclusion, a series of polymers, with different pH- sensitive value, can be obtained by adjusting the ratios of HPMC/Maleic anhydrides/ acetic anhydrides. From the in vitro tests, the pH-sensitive value of HPMCAM-6 was found to be around 3.
참고문헌 (9)
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MU, Xiao-hong, ZHANG, Ru-hua, and ZHU, Hong-jie, The Water Vapor Permeability of Free Film of Hydroxypropylmethyl Cellulose Phthalate (HPMCP) and Effect of Additives. Zhong Guo Yao Xue Za Zhi, 29, 470-473 (1994)
Kokubo, Hiroyasu and Nishiyama, Yuichi, U.S.Patent 6258799 (2001)
Konorev, M. R., Eradication of Helicobacter pylori from the stomach and duodenum of patients with duodenal ulcers. Int. J. Antimicrobial Agents, 17, 425-426 (2001)
Eiji, Fukui, Nobuteru, Miyamura, and Masao Kobayashi, An in vitro investigation of the suitability of press-coated tablets with hydroxypropylmethylcellulose acetate succinate (HPMCAS) and hydrophobic additives in the outer shell for colon targeting. J. Control Release, 70, 97-107 (2001)
Mela, G. S., Savarino, V., and Vigneri, S., Optimizing the information obtained from continuous 24-hour gastric pH monitoring. Am. J. Gastroenterol, 87, 961-966 (1992)
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