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[求助]
50金求助翻译下面几段文章(求助完毕）
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哪位英文和医药都很好的翻译大侠帮我翻译一下这几段文章，谢谢！ 1、The present invention relates to pharmaceutical antibacterial compositions containing a penem antibiotic as an active ingredient, which are stable and show good gastrointestinal absorption. 2、Penem compounds are non-natural beta -lactam compounds the design of which is based on the concept of fusing the structures of penicillin and cephalosporin (for example, see Woodward, R. B., In Recent Advances in the Chemistry of beta -Lactam Antibiotics, Elks, J., Ed., The Chemical Society, London, 1977, Spec. No. 28, pp. 167-180; Japanese Patent Public Disclosure(Kokai) Nos. 207387/86, 162694/88, 222486/85 and 119486/79). They are a novel type of antibiotic having both the wide antibacterial spectrum and high safety of penicillin and cephem antibiotics belonging to beta -lactam antibiotics, as well as the potent antibacterial activity and high beta -lactamase stability of carbapenem antibiotics.Sodium (+)-(5R, 6S)-6-[(R)-1-hydroxyethyl]-7-oxo-3- [(R)-2-tetrahydrofuryl]-4-thia-1-azabicyclo [3.2.0] hept-2-ene-2-carboxylate 5/2 hydrate (faropenem sodium, hereinafter referred to as compound 1) is currently used as an oral drug for various infectious diseases and is reported to show potent antibacterial activity against not only methicillin-sensitive Staphylococcus aureus (MSSA), Streptococcus pyrogenes and Streptococcus pneumoniae but also gram-positive bacteria for which conventional beta -lactam drugs have proved ineffective such as penicillin-resistant pneumococci (PRSP), oral staphylococci and enterococci, also showing a wide antibacterial spectrum covering gram-negative bacteria such as Haemophilus influenzae and anaerobic bacteria such as the genus Bacteroides, which activity is due to its novel skeleton penem ring ((Kagaku Ryoho no Ryoiki The Field of Chemotherapy), Vol. 13, No. 10, pp. 74-80, 1997). This compound is also reported to have potent antibacterial activity against pathogenic bacteria of periodontis such as Porphyromonas gingivalis (CHEMOTHERAPY, Vol. 42, S-1, pp. 38-50, 1994) as well as potent antibacterial activity against bacterial strains from dental infectious diseases which have recently become more and more resistant (Journal of Japan Chemotherapy Society, Vol. 45, No. 11, pp. 965-971, 1997). 3、However, penem compounds are chemically unstable materials susceptible to hydrolysis, oxidation, photoisomerization and the like, in much the same way as other beta -lactam compounds. 4、Moreover, water-soluble beta -lactam compounds are known to show poor gastrointestinal absorption as compared with fat-soluble compounds (Akinobu Otsuka et al., Pharmaceutics, Revised 2nd Edition., Nankodo). Such drugs tend not to produce a reliable therapeutic effect, and , antibacterial compounds such as penem compounds also have a tendency to affect the flora of enteric bacteria thereby inducing loose stools or diarrhea. 5、Thus, the application range, administration route and dosage form of penem compounds have been limited due to their instability and poor gastrointestinal absorption. 6、Syrup is a dosage form which is easy to swallow even for seniors and children. It is a dosage form with excellent characteristics which masks a bitter or unpleasant taste of drugs with the sweetening effect and consistency of sugars and various flavoring agents, and improves palatability with suitable colorants giving a pleasant color and the like. Dry syrups to be dissolved or suspended before use have been studied in the case of active ingredients unstable in water. Dry syrups are dissolved or suspended before use in an aqueous liquid such as water, juice or milk as a solvent. 7、Several dry syrup formulations have been developed for antibiotics which are generally unstable in water. Examples include macrolide antibiotic formulations such as josamycin propionate (Josamy Dry Syrup TM from Yamanouchi Pharmaceutical) or erythromycin ethylsuccinate (Erythrocin Dry Syrup TM from Dainippon Pharmaceutical) and cephem antibiotic formulations such as cefpodoxime proxetil (Banan Dry Syrup TM from Sankyo). all of which are used as suspensions in water added before use. 8、When dry syrups are used as suspensions in hospitals, for example, they are often combined with water and kept to stand before they are taken by inpatients. Also at home, dry syrups are mostly taken in divided portions after being dispersed or dissolved in water. In these cases, suspensions are allowed to stand and insoluble ingredients precipitate to affect homogeneity of active ingredients and therefore the dosage regimen is not faithfully followed. 9、From the viewpoint of palatability, patients' rejection of medication must be avoided, especially in the case of children having a disease. However, suspensions are not only disliked for their texture but are also responsible for oral or digestive discomfort due to the presence of insoluble ingredients, leading to children to reject second and subseqeuent doses. In seniors, insoluble ingredients may enter the gaps between false teeth to cause pain. This decreases patient compliance and therefore the dosage regimen is not faithfully followed. 10、 It is known that alpha , omega -diamineacetate compounds form complexes with a metal ion such as copper or iron, and thus inhibit decomposition reactions which are catalyzed by heavy metals, making them suitable for use as stabilizers against components susceptible to such reactions such as fats and the active ingredients of some drugs. 11、Among alpha , omega -diamineacetate compounds, disodium ethylenediaminetetraacetate is thought to increase penetration into intercellular spaces by forming a complex with a calcium ion thereby retaining the structure of intracellular spaces of gastrointestinal mucosa (Ryuji Iga et al., Recent Advances in Biopharmacy, 1994, Yakujinippo) 12、 As described above, there are demands for widely applying penem compounds having high safety and potent antibacterial activity as pharmaceutical antibacterial compositions, but the actual demands have not been sufficiently satisfied because any techniques for formulating them into various dosage forms such as oral formulations or solutions have not been developed. For children and seniors, safe and effective antibacterial compositions which ensure proper patient compliance and require only an easy-to-follow dosage regimen would be especially desirable. [ Last edited by xinyi299 on 2008-8-30 at 15:47 ] |
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9楼2008-08-27 13:08:25
★ ★
xinyi299(金币+2,VIP+0):首先谢谢你的回应！但是你是不是用翻译软件弄的，文章很不通顺许多地方还是没有翻译。
xinyi299(金币+2,VIP+0):首先谢谢你的回应！但是你是不是用翻译软件弄的，文章很不通顺许多地方还是没有翻译。
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1 ，本发明涉及制药抗菌成分含有青霉烯抗生素作为一个积极的成分，这是稳定和具有良好的胃肠道吸收。 2 ，青霉烯化合物的非天然β -内酰胺类化合物的设计，这是概念的基础上，融合结构的青霉素和头孢菌素（例如，见伍德沃德，铷，在最近的进展，在化学β -内酰胺类抗生素， elks女士，教育署，化学，社会，伦敦， 1977年，规格第28号，第167-180 ;日本专利公开披露（ kokai ）号八十六分之二十○万七千三百八十七， 88分之162694 ， 85分之222486和119486 / 79 ） 。他们是一种新型的抗生素都具有广泛的抗菌谱和高度的安全青霉素和cephem抗生素，属于β -内酰胺类抗生素，以及作为强大的抗菌活性和高β -内酰胺酶稳定的碳青霉烯类antibiotics.sodium （ + ） - （ 5 R ， 6 S ） -6 -[ （ ） - 1 -羟乙基] - 7 -氧- 3 - [ （ ） - 2 - t etrahydrofuryl] - 4 -硫杂- 1 -氮杂双环[ 3 .2.0]庚- 2 -节能- 2 -羧酸5 / 2水合物（法罗培南钠，以下简称为化合物1 ）是目前用来作为口服药物，为各种传染病和报道，以显示强大的抗菌活性，不仅对甲氧敏感的金黄色葡萄球菌（军用半自动） ，链球菌pyrogenes和肺炎链球菌，但也克阳性菌为常规β -内酰胺类药物已证明无效，如青霉素耐药pneumococci （减贫战略文件） ，口腔葡萄球菌和肠球菌，也显示出广泛的抗菌谱，包括革兰阴性菌如流感嗜血杆菌和厌氧菌如属杆菌，这活动是由于其新颖的骨架青霉烯环（ （化学ryoho没有ryoiki领域的化疗） ，第13卷，第10号，第74-80 ， 1997年） 。这种化合物也据报，有强大的抗菌活性对病原菌periodontis ，如牙龈卟啉菌（化疗，第二卷42 ，第S - 1 ，第38-50 ， 1994年） ，以及强大的抗菌活性对菌株从牙科感染疾病已成为最近越来越多的抗性（杂志日本社会的化疗，第二卷45 ，第11号，第965-971 ， 1997年） 。3 ，不过，青霉烯化合物的化学性质不稳定的材料，容易水解，氧化，光致异构化和喜欢，在许多相同的方式与其他β -内酰胺类化合物。 4 ，此外，水溶性β -内酰胺类化合物是众所周知的，以显示穷人的胃肠道吸收相比，脂溶性化合物（ akinobu大冢等人，药物制剂，经修订的第二版，楠科多） 。这类药物通常不会产生一个可靠的治疗效果，并且抗菌化合物，如青霉烯化合物也有一个趋势，影响植物区系的肠道细菌，从而诱使松散，粪便或腹泻。 5 ，因此，应用范围，给药途径和剂型的青霉烯化合物已有限，由于其不稳定和穷人的胃肠道吸收。 六，糖浆是一种剂型，这是很容易吞咽，甚至为老人和儿童。这是一个剂型具有优良的特点，口罩，苦或不愉快的滋味药物与脱臭效果和一致性，糖和各种调味剂，提高适口性与合适的着色剂提供一个舒适的颜色和喜欢。干糖浆要解散或暂停使用前，已研究了在该案件的活性成分不稳定，在水中。干糖浆是解散或暂停使用前，在一水液，例如水，果汁或牛奶作为溶剂。 七，几个干糖浆配方，已开发了抗生素，且一般不稳定，在水中。例子包括大环内酯类抗生素的配方，例如交沙霉素丙酸（ josamy干糖浆技术备忘录，从山制药）或琥乙红霉素（ erythrocin干糖浆技术备忘录，由大日本制药制药）和cephem抗生素的提法，如头孢泊肟酯（巴南干糖浆技术备忘录，由三共） 。所有这些都是用来作为悬浮在水中补充，然后才开启使用。8 ，当干糖浆被用作悬浮在医院，举例来说，他们往往是结合水和维持的立场之前，他们所采取的住院病人。此外，在家里，干糖浆，大多采取的分部分后，被分散或溶解在水中。在这些情况下，悬浮物容许的立场和不溶性成分的沉淀，影响均匀性的活性成分，因此，给药方案是不是忠实地遵循。 9 ，从观点的适口性，病人的排斥反应的药物必须避免，尤其是在案件的儿童有一种疾病。不过，悬浮物，不仅不喜欢他们的纹理，而且还负责口头或消化道不适，由于存在不溶性的成分，导致儿童拒绝第二和subseqeuent剂量。在老人，不溶性成分可进入之间的差距镶假牙造成的痛苦。这个跌幅的病人依从，因此，给药方案是不是忠实地遵循。 10 ，这是众所周知， α ， ω - diamineacetate化合物的形式，配合与金属离子如铜或铁，从而抑制分解反应是催化重金属，使它们适合用作稳定剂对组件容易受到这种反应，这种作为油脂和活性成分的一些药物。11 ，其中α ， ω - diamineacetate化合物，钠盐的ethylenediaminetetraacetate被认为是增加渗透到间位，形成一个复杂的与钙离子，从而保留了结构内的空间胃肠粘膜（隆治伊贺等人，最近的进展biopharmacy ， 1994年， yakujinippo ） 12 ，如上文所述，有要求，广泛应用青霉烯化合物具有高度的安全和强大的抗菌活性，作为抗菌成分的药品，但实际需求没有得到充分满足，因为任何技术制订成各种剂型，如口服剂型或解决方案尚未开发。为儿童和老人，安全和有效的抗菌成分，确保适当的遵守和病人只需要一个易于遵循的给药方案，将特别是可取的。 |
2楼2008-08-25 13:28:42
★ ★ ★ ★ ★ ★ ★ ★ ★ ★
xinyi299(金币+10,VIP+0):谢谢!
xinyi299(金币+10,VIP+0):谢谢!
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1.近来出现的药用抗菌药物含有表霉烯作为活性成分，这种成分稳定并且胃肠吸收很好。 2.表霉烯不是天然的beta-内酰胺化合物，它的设计糅合了青霉素和头孢菌素的概念（例如，参见Woodward, R. B., In Recent Advances in the Chemistry of beta -Lactam Antibiotics, Elks, J., Ed., The Chemical Society, London, 1977, Spec. No. 28, pp. 167-180; Japanese Patent Public Disclosure(Kokai) Nos. 207387/86, 162694/88, 222486/85 and 119486/79）。它们是一类广谱和高安全性的beta-内酰胺类抗菌素，具有有效的抗菌活性和对beta-内酰胺酶高度稳定的碳杂青酶烯抗菌素。 hept-2-ene-2-carboxylate 5/2 hydrate（法罗培南钠，以下称化合物1）近来常用于口服治疗各类传染病，据报道，它不仅对甲氧苯青霉素敏感的金黄色葡萄球菌（MSSA），热原性链球菌和肺炎链球菌有效，而且对传统beta-内酰胺类无法治愈的革兰氏阳性菌，如青霉素耐药的肺炎球菌（PRSP），口腔葡萄球菌和肠道球菌也有效，显示了很广的抗菌谱，包括革兰氏阴性菌如嗜血杆菌和厌氧菌如拟杆菌，它的活性取决于其新颖的表霉烯环骨架。 据报道该化合物对致病菌如Porphyromonas gingivalis（CHEMOTHERAPY, Vol. 42, S-1, pp. 38-50, 1994）有效，并且对近来抗药性越来越强的牙科感染疾病也有效（Journal of Japan Chemotherapy Society, Vol. 45, No. 11, pp. 965-971, 1997）。 3.然而，与其他beta-内酰胺类化合物一样，表霉烯类化合物在化学上对水解，氧化，光致异构化等不稳定。 4.另外，水溶性的beta-内酰胺化合物夹较脂溶性的化合物胃肠吸收差（Akinobu Otsuka et al., Pharmaceutics, Revised 2nd Edition., Nankodo）。这类化合物可能得不到可靠的疗效，并且抗菌化合物如表霉烯化合物可能会影响肠道细菌而导致腹泻。 5.因此，由于不稳定和胃肠吸收较差，表霉烯类化合物的应用范围，给药途径和剂量受到限制。 6. 糖浆对于老人和小孩来说都是容易吞服的剂型。这种剂型的优越性在于利用了糖和各种调味剂的甜味和粘度来掩盖了药物的苦味和难吃的味道，并且用适当的着色剂使药物看起来颜色和外观更好。 7.已研制出的几种抗生素糖浆剂型在水中都不稳定。包括大环内酯类抗生素剂型如交沙霉素丙酯（Yamanouchi制药公司的娇沙干糖浆）或者乙琥红霉素乙基琥珀酸酯（Dainippon制药公司的红霉素干糖浆）和头孢烯类抗生素剂型如普赛头孢泊肟（Sankyo制药公司的搏拿干糖浆）。这些在用药之前都先制成水混悬液。 8. 当医院里用干糖浆制成混悬剂时，例如，常常先用水混匀后静置，然后在给药。家庭用药时，干糖浆也常常先分散溶解在水里后再分成几份服用。在这些情况下，混悬剂可以静止并且其中的不溶性沉淀成分会影响活性成分的均匀性，因此就无法严格的遵守剂量规定了。 9.在口味方面，应该避免病人拒绝治疗，尤其是小孩患病的情况下。然而，混悬剂因为其中的不溶成分不仅因为其质地不佳，还因为口感不佳和消化上带来的不适，导致小孩拒绝后续用药。对于老人，不溶性的成分可能进入假牙的缝隙而导致疼痛。这就降低了病人的顺应性，因此给药方案就难以遵守了。 10. 众所周知，alpha,omega-醋酸二胺化合物与金属离子如铜或铁形成复合物，可以防止重金属催化的降解反应，使这类化合物适用于作对这类反应敏感的化合物如脂肪和一些药物活性成分的稳定剂。 11.在alpha,omega-醋酸二胺化合物中，依地酸钠与钙离子形成复合物而提高了细胞间隙的穿透性，因此保护了胃肠道粘膜的细胞间隙的结构(Ryuji Iga et al., Recent Advances in Biopharmacy, 1994, Yakujinippo)。 12.综上所述，急需高安全性和高抗菌活性的表霉烯类化合物作为药用抗菌化合物，但是因为还没有任何一种技术把它们成功的制成不同的剂型如口服剂型或者溶液剂，所以并不能满足现在的皮且需求。对于小孩和老人，尤为需要能保证适当的顺应性和便于吞服的剂型的安全有效的抗真菌成分。 自己翻译的，花了不少时间！  |
3楼2008-08-26 10:41:39
感谢楼上虫友！
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感谢这位虫友，虽然不是很流畅但是大概意思出来了，看得出你是自己翻译的，各位大侠能不能再帮我翻译以下几段，不甚感激！将有重金酬谢！ [0013] As a result of careful studies of formulation techniques focusing on stability in aqueous solution and gastrointestinal absorption of penem compounds with a view to developing a technique for administering penem compounds as pharmaceutical antibacterial compositions, the present invention has been accomplished. Specifically, the inventors have found that penem compounds are stable in solvents comprising water and, more surprisingly, improved gastrointestinal absorption can be imparted to these compounds by incorporating an alpha , omega -diamineacetate compound into the composition. [0014] Accordingly, the present invention provides pharmaceutical antibacterial compositions containing a penem compound as an active ingredient, which can be formulated into various dosage forms such as oral formulations and solutions, particularly syrups, especially dry syrups which allow highly water-soluble penem compounds to be administered to seniors and children as clear aqueous solutions with good compliance. [0015] Compositions of the present invention are pharmaceutical antibacterial compositions containing a penem compound as an active ingredient, an alpha , omega -diamineacetate compound and optionally other additives. DETAILED DESCRIPTION OF THE INVENTION [0016] Penem compounds used in the present invention are not specifically limited so far as they have antibacterial activity and safety including the absence of immunogenicity and oral toxicity and are pharmaceutically acceptable. These may be free carboxylic acids or pharmaceutically acceptable salts thereof with alkali metals or alkali earth metals such as sodium, potassium, calcium or magnesium, or amino acids such as lysine, or ammonium, and may also be used as solvates such as hydrates. When pharmaceutical compositions of the present invention are required to be water-soluble, penem compounds as active ingredients can be appropriately selected, taking into account their water solubility. [0017] Penem compounds used in the present invention include faropenem sodium mentioned above (compound 1), which may optionally be substituted at 3-position by 1,4-dioxane-2-yl, ethylsulfanyl, 3-tetrahydrofurylmethyl, methoxymethyl, ((aminocarbonyl)oxy)methyl, (4R)-pyrrolidine-2-thione-4-ylthio and other groups. [0018] The amount of active ingredients to be contained in the composition of the invention can be determined appropriately depending on the nature of the active ingredient, the disease to be treated or other factors. When compound 1 is used, it is incorporated at about 10-90% by weight for tablets, about 50-99.9% by weight as solids for injections and about 2-20% by weight for dry syrups in terms of the free anhydride relative to the total composition. [0019] alpha , omega -Diamineacetate compounds are linear hydrocarbons having an aminoacetate group at each end. Linear hydrocarbons of alpha , omega -diamineacetate compounds used in the present invention may contain an aminoacetate group(s) in the chain. The size the hydrocarbon chain is not limited, but preferably ethylene is desirable. [0020] Examples of alpha , omega -diamineacetate compounds include polyaminocarboxylic acid chelating agents such as ethylenediaminetetraacetic acid, hydroxyethylethylenediaminetriacetic acid, dihydroxyethylethylenediaminediacetic acid, 1,3-propanediaminetetraacetic acid, diethylenetriaminepentaacetic acid, triethylenetetraminehexaacetic acid and salts thereof. They may be used as solvates such as hydrates. Especially, ethylenediaminetetraacetic acid and salts thereof are preferably used in respect of safety, specifically calcium ethylenediaminetetraacetate, disodium calcium ethylenediaminetetraacetate, sodium ethylenediaminetetraacetate, disodium ethylenediaminetetraacetate, tetrasodium ethylenediaminetetraacetate, tetrasodium ethylenediaminetetraacetate tetrahydrate. The present invention is not limited to these examples, but one or more alpha , omega -diamineacetate compounds can be appropriately selected and used. [0021] The amount of alpha , omega -diamineacetate compounds to be added in compositions of the present invention depends on the nature of the compound or the dosage form of the composition, but can be determined by evaluating the stability in solvents comprising water and the gastrointestinal absorption of the penem compound. Normally, they are contained at about 0.1-100%, preferably about 0.1-20% relative to active ingredients as free anhydrides. [0022] In the present invention, stability of penem compounds is improved. Therefore, pharmaceutical antibacterial compositions of the present invention can be used as formulations to be administered in the state where they are dissolved or suspended in a solvent comprising water, i.e. (1) solutions or suspensions in solvents comprising water or (2) formulations to be dissolved or suspended before use. These formulations include injections, solutions, syrups, ophthalmic solutions, suspensions, emulsions, aerosols, elixirs, capsules containing a solution or suspension, liniments, lemonades or lotions. For example, injections may be either solutions or formulations to be dissolved or suspended before use. As used herein, formulations to be dissolved or suspended before use mean formulations which are shipped in a solid form but dissolved or suspended between opening and application. Normally, they are dissolved or suspended immediately before application. [0023] Various dosage forms of formulations to be administered in the state where they are dissolved or suspended in a solvent comprising water can be prepared by incorporating an active ingredient, an alpha , omega -diamineacetate compound and other additives via the routine process for each dosage form. For example, injections may contain as other additives (1) isotonizing agents such as sodium chloride, D-mannitol, D-sorbitol, (2) pH modifiers such as hydrochloric acid, citric acid, sodium hydroxide, (3) buffers such as sodium citrate, phosphoric acid, sodium phosphate, potassium phosphate, sodium acetate, boric acid, (4) soothing agents such as procaine hydrochloride and surfactants. The amounts of these additives can be appropriately determined depending on the pharmaceutical characteristics desired or other factors. [0024] Pharmaceutical antibacterial compositions of the present invention are useful not only as the formulations described above but also as any other formulations prepared by processes including the step of bringing active ingredients into contact with water, e.g. the step of adding active ingredients dissolved in water because stability of penem compounds is improved in the present invention. Examples of such other formulations include tablets, capsules, pills, granules, fine granules and powders prepared via such an operation as fluidized bed granulation, agitating granulation, kneading granulation,or coating. [0025] In the present invention, pharmaceutical antibacterial compositions having good gastrointestinal absorption can be obtained by incorporating an alpha , omega -diamineacetate compound. Thus, pharmaceutical antibacterial compositions of the present invention are useful as oral formulations such as tablets, capsules, solutions, syrups, pills, granules, fine granules, powders, troches, aerosols, elixirs, lemonades, etc. [0026] These formulations can be prepared by incorporating an active ingredient, an alpha , omega -diamineacetate compound and other additives via the routine process for each dosage form. For example, tablets may contain (1) excipients such as lactose, starches or microcrystalline celluloses, (2) binders such as hydroxypropylcellulose or polyvinylpyrrolidone, (3) disintegrating agents such as starches or sodium carboxymethylcellulose, (4) lubricants such as magnesium stearate or talc, (5) coating bases such as hydroxypropylmethylcellulose or Eudragit, as well as plasticizers and colorants. The amounts of these additives can be appropriately determined depending on the pharmaceutical characteristics desired or other factors. [0027] Pharmaceutical antibacterial compositions of the present invention are useful as (1) oral formulations dissolved or suspended in water and (2) oral formulations to be dissolved or suspended before use, specifically solutions, syrups and dry syrups because the stability in the state where they are dissolved or suspended in a solvent comprising water and the gastrointestinal absorption of penem compounds are improved in the present invention. [0028] Dry syrups means syrups to be dissolved or suspended before use, but the present invention also preferably encompasses similar powdery oral formulations such as granules, fine granules or powders containing a high ratio of sucrose and substantially suitable to be dissolved or suspended before use as embodiments of the present invention. [0029] Dry syrups containing active ingredients to be homogeneously dissolved in water are one of the preferred embodiments of the present invention. [0030] As used herein, dry syrups to be dissolved in water mean those which become clear and leave no trace of precipitated ingredients when mixed with an appropriate amount of water. Generally, the amount of water in which dry syrups are dissolved or suspended is determined taking into account (1) the influence of the concentration on the stability of the active ingredient, (2) ease of handling in the medical field, and (3) palatability for patients. For example, Josamy Dry Syrup (Yamanouchi Pharmaceutical) and Erythrocin Dry Syrup W (Dainippon Pharmaceutical) among commercially available dry syrups are shown to prepare suspensions at concentrations of 30, 40 and 100 mg (potency) /mL in the package inserts. Pharmaceutical compositions of the present invention can be used as dry syrups to be homogeneously dissolved in water within a wide concentration range of active ingredients, specifically at a concentration of 5-200 mg (potency) /mL, for example, 40 mg (potency) /mL, because the stability in solution or suspension in aqueous solvents and the gastrointestinal absorption of penem compounds are improved in the present invention. This is an especially preferred embodiment for faithfully following the dosage regimen and improving compliance in seniors and children. [0031] Dry syrups can be prepared by incorporating an active ingredient, an alpha , omega -diamineacetate compound and other additives via the routine process for each dosage form. Such other additives include (1) excipients such as sucrose, lactose, fructose, mannitol, dextrose, (2) binders such as hydroxypropylcellulose or polyvinylpyrrolidone, (3) disintegrating agents such as starches, (4) plasticizers such as Macrogols, polyethylene glycol and triethyl citrate, (5) corrigents such as aspartame and citrate, (6) coating bases such as hydroxypropylmethylcellulose or Eudragit, as well as flavoring agents and colorants. The amounts of these additives can be determined as required depending on the desired pharmaceutical characteristics or other factors. [0032] Formulations prepared are packaged in the form suitable for each dosage form, such as bottling, divided powder, press through packaging, ampoules, vials. The dose of thus obtained formulations is typically 50-1500 mg (potency), preferably about 100-1000 mg (potency) daily per adult (60 kg) depending on the route of administration, the disease to be treated, the condition of the disease, the age and other factors. For children, the dose can be calculated on the basis of body weight. EXAMPLES [0033] The following examples further illustrate the present invention without, however, limiting the scope of the invention thereto. |
4楼2008-08-26 11:09:46