Aerosol Research_526

By Betty Miller,2014-10-30 09:10
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Aerosol Research_526

Aerosol Research

     Abstract Aerosol Research in recent years, mainly from the formula research, preparation, quality control, efficacy study and clinical application areas are reviewed. And looked forward to their development prospects.

     Key words aerosol; Review

     Aerosol refers to extracts of medicinal drugs or drug powder with the appropriate propellant loaded in a special pressure valve system, strict sealing containers, when used with the pressure of propellant would be the contents were

    fine mist or other forms spray forms. Can be applied to the respiratory tract, skin, or other cavity of limited effect, or systemic therapeutic effect, which has become indispensable in pharmaceutical preparations as a dosage form. "The United

    States Pharmacopoeia" 22 edition of income contained in the aerosol has reached more than 30 kinds of medicines, China's 2005 edition of "Chinese Pharmacopoeia" there are two kinds of income contained in [1], in recent decades, aerosol with quick

    and efficient features , in the treatment of respiratory, cardiovascular system, surgical bleeding, burns, etc. were received remarkable results. Especially in the quantitative inhalation, systemic treatment such as in-depth research to

    fully demonstrate their superiority, it has been increasing in our country a wide range of clinical applications, now in recent years, the research and application of aerosols are summarized as follows:

     1 Formulations

     Aerosol in the formulation design can be based on

    clinical treatment needs, requirements and administration site nature of the drug to carry out set of square. Such as: Select β adrenergic receptor stimulant isoprenaline hydrochloride [2] as an active ingredient, its relaxing bronchial smooth

    muscle have a stronger role in lifting the bronchial spasm, bronchial asthma attending suitable for preparing the aerosol , select the oral spray delivery method.

     The function of Chinese medicine formulations attending primary consideration. Such as: Chuankening Ping aerosol [3], from ephedra, ginkgo, Sophora flavescens, Scutellaria baicalensis and other ingredients. Ephedra King and the temperature of its medicinal drug Xuanfei asthma; sex level of ginkgo Tameomi drug phlegm down and dirty, grabbing the lung

    Dingchuan; with a mixture of cold lung of Sophora In addition to hot-fall from the sky, so in order to bitter cold of the skullcap Xiehuo detoxification of the reactive increase monarch and officials, various drugs were played with the heat

    phlegm, asthma Zhixiao achievements.

     2 Preparation

     Aerosol process of drug preparation is the key point, according to the type of prescription composition and aerosol dubbed decentralized systems required. Aerosol preparation,

    may be appropriate to add according to the nature of the potential drug solvent such as ethanol, additional agents such as Span 80, Tween 80 and so since solubilization or

    emulsification, made solution, Suspension, emulsion

    differentType. Such as drug solubility in the propellant F12 in the poor design of ethanol in a prescription for latent solvent, vitamin C for antioxidant, made of clarity solution [2]. Wang Lishu, etc. [4] using orthogonal design the best clarity aerosol compound Danshen preparation process by adding

    propylene glycol 1.5 ml, Span -60 0.05%. Yang Giessen et al

    [5] on the vagina with herbal foam aerosols orthogonal results show that when the two fluoro-dichloro-7.0 g, aqueous phase is

    21.0 g, the use of Tween 80 0.51 g, Span -80 1.24 g, group

    percent of emulsifier, oil water, emulsifiers (1:3:0.25)

    is the optimal solution.

     Traditional Chinese medicine is a traditional Chinese medicine extracts of aerosol propellants in aerosol containers

    with the compatibility made. Relatively active ingredient a single aerosol medicine, Chinese medicine has a complexity. If he asks for he possesses the dosage is small, high bioavailability, efficacy and strong advantages of traditional Chinese medicine active ingredients extracted and refined the study is bound to become a key link. Chinese herbs commonly used formulations of water, alcohol or water and alcohol references, Shen law process, is also useful and effective part of the organic solvent extraction. Liu Gang et al [6] In

    the compound pairs spend research and development of aerosol extraction process selection of water extraction and alcohol precipitation method, each 12-fold increase of water, boiling

    3 times, 1.5 h / times, this extraction process is most

    reasonable; Concentrate the relative density of 1.09 ~ 1.12, use 60% ethanol, precipitate 16 h. Fang Ephedra percolation optimum process as follows: fine herbs 1 ~ 2 nm, alcohol consumption 8 times the concentration of 60 percent ethanol,

    filtration rate per minute, 4 ~ 5 ml. The best preparation process for the liquid ethanol concentration of 95%, liquid dosage 1 g, projectile dosage 2 g.

     3 Quality+Control">Quality Control

     "Chinese Pharmacopoeia" 2005 edition of the appendix

    "General Preparation" provides all types of aerosols must be leak rate checks. Should be non-quantitative aerosol spray

    valve rate, the total emission inspection, quantitative aerosol valve should be pressed a bottle of the total times, the amount of spray per actuation, or pushed the main content of each examination, inhalation aerosol with Suspension Check for size. In addition to the provisions of aerosol medicine pharmacopoeia routine screening, but also to make qualitative and quantitative examination.

     Aerosol Qualitative inspection methods are mainly TLC, such as Liu Gang et al [7] on the compound pairs of flowers aerosol prescriptions were seven Chinese herbal medicines all the TLC, the results of stability, spots were clear with good

    reproducibility .

     Aerosol quantitative inspection methods are mainly UV spectrophotometry, TLC, gas chromatography, high performance liquid chromatography method. Gan Ke-su, etc. [8] using UV

    spectrophotometry the content of salbutamol sulfate aerosol to

    determine the maximum ultraviolet absorption wavelength, in the (240 ? 1) was measured wavelength absorption. The linear range of 2.0 ~ 16.0 g / ml with absorbance A linear relationship was good. The method is accurate, simple, rapid

    and applicable to the determination of goods. Zhao-Hua Wang et

    al [9] also used dual-wavelength TLC-scanning throat Ling

    aerosol content of borneol, the average recovery was 97.18%, RSD = 2.14%, method is simple, stable and reliable. Zhao Lijun, etc. [10] carried out by gas chromatography

    determination of gold content of borneol Blue Aerosol Research. With polyethylene glycol (PEG)-20M as the stationary

    phase, using hydrogen flame detector (200 ?), the results of

    borneol 1.3 ~ 38.7 mg / ml range of good linearity (r = 0.999

    3), the average recovery was 99.1% The average RSD less than 2.0%, its quality control to provide an effective method. Hong-Ming Liu et al [11] using HPLC determination of matrine in Qingyan aerosol content, Ai-Hua Song, etc. [12] have also

    established HPLC Determination of Salmeterol Xi-naphthoic

    acid, naphthoic acid aerosols in the Xi-salmeterol HPLC

    method, the results are accurate and reliable, are suitable for preparation of quality control.

     In addition, the literature also reported quantitative

    examination of several specific ways: such as Kent et al [13] used convolution spectrometry good fast Aerosol lidocaine and chlorhexidine acetate content, using this method without Simultaneous determination of two points separating the content, methods, accurate, simple and fast. Li Li-Qing et al

    [14] using flow-injection technology, has established

    chemiluminescence salbutamol tablets and aerosol content of the method, method CV of 1.4%, the method is simple, sensitive and consistent results with pharmacopoeia method. Ding Jijun

    et al [15] studied the high performance capillary electrophoresis Determination of insulin aerosol content of the method, the results of the method can be simple, fast and economical measure of insulin aerosol content, can be used

    similar to the quality control of pharmaceutical preparations and content determination.

     4 Pharmacodynamic study

     Pharmacodynamic evaluation of the main from the evaluation of drug efficacy in the main role of the beginning, from the drug for clinical anti-anticipated, diagnosis, cure

    for purposes other than the beginning of a wide range of pharmacological effects. Only a comprehensive pharmacological effects of drugs in order to have a basic understanding of the role of the principal to make the right evaluation of


     Ou Jie Wen et al [16] study has confirmed the two ether-

    type alkali aerosols have a topical anesthesia with lidocaine effect. Yao Zhen equal [17] through the cold pain Aerosol studies to prove efficacy and toxicology tests AFS has a

    bleeding, swelling, and analgesic effect. At the same time proved that the product to animals no significant systemic or local adverse reactions. SGPT test shows AFS no toxic effect on animal liver. Zan-Cong Shen et al [18] The study found that

    insulin aerosol at the same dose, oral inhalation and intratracheal administration of two kinds of channels in normal and diabetic rats showed a significant hypoglycemic effect, after intratracheal administration of the bioavailability than oral inhalation. Insulin aerosol can effectively reduce blood glucose in normal and diabetic rats, in order to further develop the clinical treatment of diabetes lay the foundation for a new dosage form.

     Experimental study of the efficacy of Chinese medicine

    aerosol studies are mainly in vitro and animal experiment method. In vitro experiment: Liu Gang, etc. [19] study of the antibacterial compound pairs spend the role of aerosol research shows that: The product of Staphylococcus aureus,

    Staphylococcus epidermidis, beta-hemolytic streptococcus, and

    other upper respiratory tract infection common pathogens have different degrees of inhibition. Huke Jie et al [20] found that Shuanghuanglian aerosol right syncytial virus, adenovirus type 7, influenza, parainfluenza virus inhibition is superior to injection; SHL injection of the Coxsackie B group 3 type 5 virus is stronger than that aerosol; two inhibitory drugs was superior to the control virus, the virus spirit medicine. Animal experiment: Song of Richland, etc. [21] in anesthetized dog heart function and hemodynamic studies have shown that: a quick onset of the living heart aerosol fast, ease of use characteristics such as drug delivery 5 ~ 15 min can

significantly lower blood pressure, slow heart rate to

    increase coronary blood flow, reducing total peripheral resistance and so on. Confirmed the pharmacological effects of this product, for clinical application to prevent coronary heart disease, angina pectoris provide a theoretical basis.

    Xiao Geng et al [22] To observe the Lectra asthma aerosol anti-asthmatic effect in experimental animals, results showed that asthma aerosol Lectra has a spasm, such as anti-

    inflammatory and anti-allergic effect, an effect similar to Western cholinergic blocker , hormones, etc., is expected to become a treatment for acute asthma attack high-performance,

    secure, traditional Chinese medicine compound aerosol.

     Clinical 5

     Aerosol through the respiratory tract, skin or mucous membrane channels such as administration, in the treatment of respiratory diseases has its unique advantages. As in the budesonide aerosol treatment of 49 patients with chronic asthmatic bronchitis, observing that airway inhalation of budesonide can significantly improve the clinical symptoms

    [23]. Wang Peilan, etc. [24] for compound albuterol sulfate aerosol treatment of chronic obstructive pulmonary disease (COPD) clinical study results showed that: compared with those before treatment, experimental and control groups and clinical

    manifestations of lung function were significantly improved. Clinical often glucocorticoid aerosol with β2-agonist

    combination therapy of asthma. Such as fluticasone propionate and asthma Kang-speed aerosol treatment of bronchiolitis clinical observation showed that the treatment group and the asthma Flixotide Kang-speed combination has obvious effects of asthma [25]. ZHANG Gui-ping, etc. [26] Application of

    Pulmicort inhalation treatment with Aux cough variant asthma (CVA), has made significant efficacy. Tips Oaks Treatment of

    asthma with Pulmicort is reasonable, curative effect, is worth popularizing. Traditional Chinese Medicine Traditional Chinese Medicine can only be changed aerosol treatment of chronic diseases, the traditional view, mainly used in clinical

    asthma, angina and other heavy, acute treatment effect is

remarkable. Yin-Wong carried out 315 cases of anti-asthmatic

    aerosol clinical trial results show that: the treatment group than the control group, can effectively improve the main

    symptoms such as cough and asthma yellow phlegm and reduce the wheezing sound, and can improve lung function, fast onset of action and role of a long time, without increasing blood pressure, accelerated heart rate and side effects such as liver and kidney dysfunction [27]. Sun Liangmei, etc. [28] observed Qingyan Lihou aerosol treatment of 300 cases of acute pharyngitis, the results of the treatment group than the control group, with a total effective rate was 93%. Aerosol compound Danshen significant effect on the angina pectoris

    quick, with an average onset time (3.24 ? 1.37) min [29];

    save the soul aerosol 201 cases by clinical observation, treatment of angina pectoris total effective rate was 92%, The majority of cases within 3 min onset, 5 min in pain, its

    analgesic efficacy similar to the role and nitroglycerin to obtain satisfactory results [30]. Reposted elsewhere in the paper for free download http://

     Uniform distribution of aerosol can of drugs, local treatment can prevent irritation to the wound and has quick

    and positioning the role. Cold pain aerosol (AFS) treatment of 376 cases of acute pain cases, clinical observation results show that: overall response rate was 97.6%. AFS in the treatment of these patients found no allergies or skin

    irritation and other adverse reactions, 376 patients, only two patients because of mild skin damage, medication pain when the lesions Department has irritating, but tolerable. AFS is efficient, quick, safe, convenient new drug [31].

     6 Summary and discussion

     In summary, drug aerosol with a dose of small, evenly distributed, worked quickly, the role of a good, easy to use, etc., when inhaled can be reduced gastrointestinal side effects, topical and avoid irritation to the wound, and can be

    quantitatively valve control the dose, with a quick and positioning the role. Applicable to the treatment of respiratory diseases, all kinds of cavity diseases and systemic diseases, there are better clinical efficacy, achieved good economic and social benefits.

     I believe that in many types of aerosol, the quantitative aerosol (MDI) is the most convenient to use one of the suction device, and limited to the level of domestic economic development, health care spending is comparatively low,

    estimated at a very long period of time, MDI is still will be used for the main inhalation device. The use of inhaled aerosol propellant remaining in the some of the issues: first, propellant Freon (CFC) for some highly sensitive patients have cooling effect, but also destroy the ozone layer atmosphere is not conducive to environmental protection. May try to use new propellant hydrogen fluoride on behalf of the alkane (HFA), not to destroy atmospheric ozone layer, in the human body remains low toxicity to many compounds have good compatibility is a new type of projectile soluble agent, is currently recognized as The most promising alternatives. Followed by the pressure vessel and valve system is not perfect, could be further improved and increased breathing valve actuator

    devices to increase the storage mist unit. Again, incorrect use of inhaled aerosols affect the therapeutic effect. How patients, if not coordinated, will affect the drug in the lung deposition and therapeutic effect. And thus the patient must

    learn to master the press aerosol valve and inspiratory movements coordinated, that is, first slow breath, and then immediately jet lips, push the valve in the suction at the same time, remove the inhaler 5 ~ 10 s after breath-hold , and

    then quick breath. For its problems remains to be further examine ways to improve.

     In addition, foreign-listed drug aerosol, more than 200

    kinds of drugs produced in our country aerosol (excluding medicine) also has more than 20 kinds. Although the clinical

    use of Chinese medicine aerosol is not much, but the aerosol than western medicine has a more reliable basis and the clinical advantages such as low toxicity. The advantages of aerosol medicine in clinical practice to be able to give full play should be to focus on traditional Chinese medicine formulation and process optimization, the traditional Chinese medicine formula should not only consider the functional indications, should also be considered Medicine Smell, efficacy, dose, which contain components activity, select the

    small but efficient drug, preparation method takes into account the traditional fine to coarse-deposit process, should

    be considered an effective part of, or extract the active ingredients of the special process, select the advanced and

    reasonable process flow, it may be prepared by a small dose, drug-Qiang color light, tasty Chinese medicine aerosol in order to ensure the clinical efficacy of aerosol medicine. Chinese medicine has a long history thousands of years has accumulated a great deal of valuable experience to develop an efficient, quick, long-lasting, low toxicity, high-quality new

    formulation provides the most favorable conditions. We believe that the development of innovation based on inheritance, the use of advanced science and technology, new varieties of traditional Chinese medicine aerosols will continue to emerge, we continue to meet clinical needs. Study of traditional Chinese medicine aerosol preparations for the modernization of traditional Chinese medicine and Chinese medicine are of great

    significance to the world and are bound to bring about the development of drug aerosol broader space.


     [1] State Pharmacopoeia Commission. Chinese

    Pharmacopoeia, ? Department of [S]. Beijing: Chemical

    Industry Press, 2005:708.

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