药物制剂新技术国家重点实验室
平台技术 Technique
缓/控释制剂技术平台 Modified Release Formulation Technology Platform
在现有的缓/控释制剂技术基础上，借鉴国内外先进技术，加强在定速释放、定位释放及定时释放等方面的应用基础研究，并在重点制备技术上取得创新成果，使缓/控释给药系统的技术及质量控制研究达到国内领先的水平，并具有一定的国际影响力，从而推动国内企业相关技术的整体发展和更新。Based on the present modified
release formulation technology, we will adapt the advanced technologies from
abroad to improve our basic research in time-, speed- and position-programmed
drug release systems, and achieve innovation outcome in key preparation
technologies. We are aiming to reach an advanced level in modified release
formulation technology and quality control, enhance our international
influence, and thus promote the development and updates
of overall domestic enterprise-related technology.
1.1 骨架型缓/控释制剂 Matrix-Type Formulation
骨架型缓/控释制剂在释药机理上属于扩散控释系统，临床应用中最常用的为口服制剂。按制剂骨架材料的不同可分为：不溶性骨架缓/控释片、亲水凝胶骨架缓/控释片、蜡质骨架缓/控释片。进行工艺设计时，结合具体品种的特点，对制备工艺中可能影响产品质量的环节和工艺参数进行详细的考察，同时进行对不同骨架材料的性质及安全性，相容性方面的研究，并提出和改进评价骨架缓/控释片体外释放行为的方法和模型，以便于定量和定性地研究和比较各制剂的体外溶出释放曲线。
The matrix-type extended and controlled
release formulations are diffusion-controlled systems by their drug release
mechanism. In clinical applications, they are mostly used as oral solid
tablets. According to the matrix materials, they can be classified into water-insoluble
matrix tablets, hydrophilic gellable matrices and waxy matrices. During the process design, the process parameters which may affect product
quality will be examined in detail, combined with the characteristics of
specific materials. The properties, safety and compatibility of different
matrix materials wll be studied, and the methods and models for evaluating the
drug release behavior of the matrix extended and controlled release tablets
will be put forward and improved, so as to study the in vitro dissolution
release profile quantitatively and qualitatively and compare different
formulations.
1.2 膜控型缓/控释制剂 Membrane-Controlled Release
常见的膜控型微丸通常由丸芯和外层聚合物衣膜组成，将分别对丸芯和外层衣膜进行改变，一方面，可以改变微丸结构，比如采用将药物制成固体分散体包在空白丸芯表面；另一方面，通过调节衣膜材料的种类、用量及在包衣材料中加入水溶性小分子物质来调节衣膜的组成，以此来调节膜控型微丸的释药速率。还可利用衣膜材料不同的功能特性或不同类型材料的组合调节药物的释放速率。
Membrane-controlled pelllets are commonly
composed of core pellets and outer polymer coating, and the core and the outer
coating can be adjusted separately. On the one hand, the core sturcture can be
modified, for example, by coating the
drugs made from solid dispersions on the blank pill core surface. On the
other hand, the drug release rate of the membrane-controlled pellets can be
regulated by regulating the type and amount of coating material or by adding
small water-soluble molecules to adjust the coating composition. Membrane materials
with special functional features or combination of different types of materials
can also be used to regulate the drug release rate of the pellets.
1.3 定位释药系统 Positioning Drug Delivery Systems
根据药物在胃肠道的释药部位不同可分为胃定位释药系统和结肠定位释药系统。国内已经起步多年的定位给药制剂研究大多仍未走出实验室研究阶段。国外已经上市的一些结肠定位给药系统也多为pH依赖型，其包衣材料大都采用pH依赖型丙烯酸树脂，单纯利用时滞效应或pH值差异设计的结肠定位给药制剂都难以达到理想的定位释药效果。我们会进一步研发和生产这类剂型，从多种途径入手，结合生物粘附、pH敏感、离子敏感、肠内微生物敏感等多种解决方案，形成定位释药技术平台，推动新型缓控释制剂的发展。
According to the
different parts where the drug releases in the gastrointestinal tract, the
positioning drug delivery system can be divided into the stomach- and
colon-targeted drug delivery systems. China has already started research in
positioning drug formulations for many years, most of which, however, limited
in the laboratory research stage. Some colon-targeted drug delivery systems
launched in foreign countries are mostly pH-dependent type, and they mainly use
acrylic resins as coating materials. Simply using the lag-time effect or the pH
difference to design colon-specific drug delivery agents, it is difficult to
achieve the desired positioning release effect. We will further develop and
manufacture such dosage forms, from a variety of approaches, combining
biological adhesion, pH-sensitive, ion-sensitive, sensitive to intestinal
microbial, to form a targeting drug delivery technology platform and to promote
the development of new extended and controlled release formulations.
1.4 渗透泵型 Osmotic Pump Controlled Release Systems
渗透泵型控释制剂作为缓控释制剂的典型代表，是以渗透压作为释药动力，以零级释放动力学为特征的一种制剂技术。我们对渗透泵型控释制剂的研究，从包衣膜和片芯处方两个方面着手。一方面，改变膜的通透系数和包衣膜厚度，从而保证释药的安全性和释药速率的恒定。另一方面，通过改变难溶性主药的溶解度来增加药物的溶出，主要方法有：环糊精包合技术，成盐及加入助溶剂。
Osmotic pump preparations are
typical representative of controlled release formulations, and this formulation
technique uses the osmotic pressure as a driving force, characterized by
zero-order release kinetics. Our research in osmotic pump formulations will
start from two aspects, the core prescription and the coating film. On the one
hand, we can change the membrane permeability and the thickness of coating
layer, in order to ensure the safety and constancy of the drug release rate. On
the other hand, we can improve the solubility of insoluble drugs to increase
the drug dissolution through several methods: cyclodextrin complexation
technology, salting and using of cosolvent, for example.
1.5 离子交换控释型 Ion-Exchange Resins
将对影响含药树脂药物吸附和释放的因素进行研究，考察树脂粒径、反应温度、药物浓度对交换过程的影响，并对交换动力学进行拟合，考察不同条件下药物树脂交换反应速率常数和活化能，以得出药物和树脂的交换过程的影响因素。
We will investigate the factors that may affect the
drug adsorption and release in the drug-loaded resins, and examine the effects
of resin particle size, reaction temperature and drug concentration on the
ion-exchange process. By fitting the exchange kinetics,
the reaction rate constant and activation energy of drug and resin exchange
will be studied under different conditions, in order to figure out the key
factors that affect the drug and resin exchange process.
1.6 多单元组合释药系统 Multi-Unit Drug Release Systems
口服择时释药系统即根据疾病发病时间规律及治疗药物的时辰药理学特征设计不同的给药时间和剂量方案，使得制剂在疾病发作的重要时刻在预定时间内自动释放出有效治疗剂量的药物，从而达到最佳疗效。针对择时释药系统的设计要求，可通过将同一药物几种不同释放规律的小单元按照合适比例混合组成具有上述释药特征的“多单元组合释药系统”，多单元型给药系统中研究较多的分散单元包括微丸、微片、微球、包衣颗粒和包衣粉末等，采用骨架技术、薄膜包衣技术和离子交换树脂技术等缓控释制剂技术将多单元系统中的小单元制备成具有一定释放规律的微型隔室系统，再将多个小单元组合起来达到理想的释放行为。
of oral drug delivery systems are designed for different administration time
and dose regimen according to the circadian rhythm of the diseases and chronopharmacological characteristics
of the therapeutical drugs. These systems can automatically release an
effective dose of the drug after predetermined time delay at an
important moment in the onset of the disease, so as to achieve the optimal
results. To meet the requirements for the design of time-programmed drug
delivery systems, several small units of different release patterns of the same
drug can be mixed in a reasonable proportion to form the &multi-unit
combined drug delivery system&. The mostly studied dispersive units
in multi-unit drug delivery systems include pellets, mini-tablets,
microspheres, coated particles and coating powder, etc.. The small dispersive units
are formulated into micro-compartment systems with a certain release profile
via controlled release formulation technology such as matrix, film coating and
ion exchange resins, then multiple small units are combined to achieve the
desired release behavior.
微粒载药给药制剂技术平台 Micro/Nano Particulate Drug
Delivery Systems
加强微粒载药给药系统的应用基础研究，以提高制剂的稳定性、包封率、载药量以及复溶等关键技术为目标，开展产业化研究，解决载药微粒制剂的产业化工艺及技术和设备的配套，成为国内相关技术的推广平台。
Basic research in
particulate drug delivery system will be conducted to improve the key
techniques of formulations, including stability, encapsulation efficiency, drug
loading and redispersability. Industrialization study will focus on the
industrialization process and technology of particulate drug formulations and
the assorted machine.
2.1 脂质体给药系统 Liposomal Drug Delivery
脂质体由于具有高度安全性、生物相容性、广泛的载药性等特点，是极具研发前景的靶向、缓释药物载体。国内虽然上市了注射用紫杉醇脂质体，但与先进国家相比，无论品种的开发及产业化的发展数十年来一直是比较缓慢的，因此构建脂质体微粒给药系统技术平台已是当务之急，并将小试工艺放大到工业化大生产，最终产品能用于临床。 Liposomes are
promising drug targeting and controlled release systems, because of their good
safety, biocompatibility and drug loading capability. Although injectable
liposomal paclitaxel was launched in China, overall product development and
industrialization have been slow and fell behind developed countries in recent
years. It is urgent to construct technology platform for liposomal drug
delivery systems, scale up the pilot test to industrialized production, and put
the final products into clinical application.
2.2 载药乳剂给药系统 Emulsion Drug Delivery Systems
乳剂根据粒子大小不同，可分为普通乳、亚微乳和纳米乳。随着日益成熟的乳剂生产工艺和乳剂辅料的研究不断深入，为含药乳剂的开发生产创造有利的条件。但是目前乳剂载药系统还存在着许多技术问题，如载药乳剂载体含营养量过高，药物增溶量小及载药乳剂稳定性差等因素也成为制约载药乳剂产业化的瓶颈。如何解决上述问题，促进载药乳剂的产业化，形成载药乳剂给药系统工程技术平台，将成为研究工作的重点。
Emulsion systems, according
to their particle size, can be classified into emulsion,
submicro-emulsion and nano-emulsion. The growing maturity of emulsion
production process and further studies on the emulsion
excipient, are creating favorable conditions for development and
production of the drug-containing emulsion. But there are still many technical
issues in the current drug-loaded emulsion systems, such as the drug carrier
emulsions containing high nutrient levels, the limit of drug solubilization and
the poor stability of the drug- these issues have become a
bottleneck constraining industrialization of drug-loaded emulsion. How to solve
the above problems, promote the industrialization of drug-loaded emulsion, and establish
an engineering technology platform for drug-loaded emulsion delivery systems,
will be the focus of research.
扬子江药业集团
药物制剂新技术国家重点实验室
State Key Laboratory for Advanced and Novel Pharmaceutical Formulation Technology制备及其释药特性
preparation and release properties
制备及其释药特性
基于1个网页-
以盐酸维拉帕米为模型药物，制备了口服渗透泵片。通过考察渗透泵片体外释药各过程的速率，研究口服渗透泵制剂释药的基本过程及其特性。
The main processes of the drug delivery of oral osmotic pump system were studied to investigate its delivery characteristics, with verapamil hydrochloride as the model drug.
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