赖诺普利微粒载药量与包封率影响因素研究

J4 ›› 2010, Vol. 9 ›› Issue (2): 6-10.

赖诺普利微粒载药量与包封率影响因素研究

1.大理学院药学院，云南大理 671000；2.上海交通大学药学院，上海 200240

收稿日期:2009-09-25 出版日期:2010-02-15 发布日期:2010-02-15
作者简介:吴俊珠，讲师，主要从事药剂学研究.
基金资助:
大理学院科研基金资助项目（2007X39）

Investigation on the Formulation Factors Influencing Drug Loading Capacity and Encapsulation Efficiency of Lisinopril Loaded Polyvinyl Alcohol Micro-particles

1. College of Pharmacy, Dali University, Dali, Yunnan 671000, China; 2. College of Pharmacy, Shanghai Jiaotong University, Shanghai 200240, China

Received:2009-09-25 Online:2010-02-15 Published:2010-02-15

摘要/Abstract

摘要：

目的：考察处方因素对赖诺普利聚乙烯醇微粒（LIS-PVA-MP）载药量与包封率的影响。方法：喷雾干燥法制备LIS-PVAMP，单因素考察聚乙烯醇（PVA）的醇解度、分子量、浓度和料液中投料比对载药量与包封率的影响，对结果进行单因素方差分析。结果：PVA醇解度、浓度、料液中投料比三个因素的不同水平组的指标均值存在显著性差异（α=0.05），PVA分子量的不同水平组的指标均值无显著性差异（α=0.05）。结论：PVA醇解度、浓度、料液中投料比对微粒载药量与包封率影响显著。

关键词: 赖诺普利, 微粒, 载药量, 包封率

Abstract:

Objective: To investigate the formulation factors influencing drug loading capacity and encapsulation efficiency （EE）of lisinopril-loaded polyvinyl alcohol（PVA）micro-particles（LIS-PVA-MP）. Methods: LIS-PVA-MP was prepared by spray-drying and the formulation factors influencing drug loading capacity and EE such as hydrolysis degree （HD）of PVA, molecular weight （Mw）of PVA, concentration of PVA and weight ratio of lisinopril to PVA in the feed solution were investigated by single factor experiments. Results: Differences were analyzed by one-way analysis of variance （ANOVA）. At the 0.05 level, the means are significantly different in the factors such as HD of PVA, concentration of PVA and weight ratio of lisinopril to PVA in the feed solution. However, at the 0.05 level, the means are not significantly different in the factor of Mw of PVA. Conclusion: All of the three factors, HD of PVA, concentration of PVA and weight ratio of lisinopril to PVA in the feed solution, have a significant influence on drug loading capacity and EE of LIS-PVA-MP.

Key words: lisinopril, micro-particles, drug loading capacity, encapsulation efficiency

中图分类号:

R972

吴俊珠, 王成军, 金拓. 赖诺普利微粒载药量与包封率影响因素研究[J]. J4, 2010, 9(2): 6-10.

WU Jun-Zhu, WANG Cheng-Jun, JIN Tuo. Investigation on the Formulation Factors Influencing Drug Loading Capacity and Encapsulation Efficiency of Lisinopril Loaded Polyvinyl Alcohol Micro-particles[J]. J4, 2010, 9(2): 6-10.

参考文献

〔1〕WALD N J，LAWM R. A strategy to reduce cardiovascular
disease by more than 80%〔J〕. BMJ，2003，326（7404）：
1419-1424.
〔2〕Fahey T，Brindle P，Ebrahim S. The polypill and
cardiovascular disease-May be appropriate for secondary，
but perhaps not for primary prevention〔J〕.BMJ，2005，330
（7499）：1035-1036.
〔3〕Robinson JG， Maheshwari N. A“poly -portfolio”for

secondary prevention：A strategy to reduce subsequent
events by up to 97% over five years〔J〕. AM J CARDIOL，
2005，95（3）：373-378.
〔4〕Don Poldermans，Robert Glazes，Stefanos Kargiannis，et
al. Tolerability and blood pressure-lowering efficacy of the
combination of amlodipine plus calsartan compared with
lisinopril plus hydrochlorothiazide in adult patients with
stage 2 hypertension〔J〕. Clinical Therapeutics，2007，29
（2）：279-289.
〔5〕David S Wald，Malcolm Law，Sarah Mills，et al. A
16-week，randomized，double-blind，placebo-controlled，
crossover trial to quantify the combined effect of an
angiotensin-converting enzyme inhibitor and a 茁-blocker
on blood pressure reduction〔J〕.Clinical Therapeutics，
2008，30（11）：2030-2039.
〔6〕Vijay Kumar， Bhagwat Prasad， Saranjit Singh .
Pharmaceutical issues in the development of a polypill for
the treatment of cardiovascular diseases〔J〕. Drug Discovery
Today：Therapeutic Strategies，2008，5（1）：63-71.
〔7〕Arthur H Kibbe. Handbook of pharmaceutical excipients
（3rd Edition）〔M〕.London：Pharmaceutical Press，2000：
424-425.
〔8〕Yong-Hong Liao，Marc B. Brown，Stuart A Jones，et al.
The effects of polyvinyl alcohol on the in vitro stability and
delivery of spray-dried protein particles fromsurfactant-free
HFA 134a-based pressurised metered dose inhalers〔J〕.
International Journal of Pharmaceutics，2005，304（1-2）：
29-39.
〔9〕OZMEN L，LANGRISH T A G，GIPPS E M. Spray drying
pharmaceutical products for nasal delivery：The effects of
feed solution properties and operating conditions on particle
size and density〔C〕/Leonardi E，Madhusudana C V. Heat
and Mass Transfer Australasia Proceedings of the Sixth
Australasian： Heat and Mass Transfer Conference，
December 9 -12，1996，Sydney，Australia. New York：
Begell House，1998：427-434.
〔10〕The United States Pharmacopeial Convention. The United
States Pharmacopeia〔S〕. Rockville，USA：2005（USP28-
NF23）：1139-1140.