Bacampicillin hydrochloride
(Synonyms: 盐酸巴氨西林) 目录号 : GC33926
Bacampicillin盐酸盐是青霉素类抗生素，是Ampicillin的前药，具有口服生物有效性。
Cas No.:37661-08-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Bacampicillin hydrochloride is a penicillin antibiotic, is a prodrug of ampicillin with improved oral bioavailability.
| Cas No. | 37661-08-8 | SDF | |
| 别名 | 盐酸巴氨西林 | ||
| Canonical SMILES | O=C([C@@H](C(C)(C)S[C@]1([H])[C@@H]2NC([C@H](N)C3=CC=CC=C3)=O)N1C2=O)OC(OC(OCC)=O)C.[H]Cl | ||
| 分子式 | C21H28ClN3O7S | 分子量 | 501.98 |
| 溶解度 | DMSO : ≥ 5.1 mg/mL (10.16 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9921 mL | 9.9606 mL | 19.9211 mL |
| 5 mM | 0.3984 mL | 1.9921 mL | 3.9842 mL |
| 10 mM | 0.1992 mL | 0.9961 mL | 1.9921 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Bacampicillin hydrochloride: chemistry, pharmacology, and clinical use
Pharmacotherapy 1982 Nov-Dec;2(6):313-21.PMID:6762528DOI:10.1002/j.1875-9114.1982.tb03206.x.
Bacampicillin hydrochloride is an orally administered ester of ampicillin that is rapidly and completely hydrolyzed in vivo to ampicillin. The most notable advantage of bacampicillin over ampicillin is its superior bioavailability--bacampicillin achieves significantly higher blood and tissue levels and attains peak blood levels more rapidly than equimolar doses of oral ampicillin. In addition, the percentage of an oral dose of ampicillin that is absorbed decreases sharply as the size of the dose is increased from 500 mg to 2 g; this phenomenon is not observed with equipotent doses of bacampicillin. The enhanced absorption of bacampicillin in the upper gastrointestinal tract results in a frequency of diarrhea that appears to be markedly lower than that of ampicillin and similar to that observed with amoxicillin. Apart from the sizable differences between bacampicillin and ampicillin with regard to oral absorption, the pharmacokinetic and pharmacologic profiles of these two agents are essentially identical. Twice daily dosing (pulse dosing) with bacampicillin has been shown in numerous clinical trials to be of equivalent efficacy to ampicillin given four times daily or amoxicillin given three times daily in the treatment of infections of the upper respiratory tract, lower respiratory tract, skin and soft tissues, and urinary tract. The unanswered question is whether twice daily ampicillin or amoxicillin would yield similar results.
Correlation between the bioavailability of microencapsulated Bacampicillin hydrochloride in suspension and in vitro microcapsule dissolution
J Pharm Sci 1984 Feb;73(2):141-5.PMID:6707871DOI:10.1002/jps.2600730202.
The relative bioavailability of microencapsulated Bacampicillin hydrochloride in suspension was correlated with the in vitro dissolution half-lives of the microcapsules. Simultaneously, a sensory evaluation was performed to evaluate the taste acceptability of the suspension. The in vitro dissolution half-life is directly related to the coating thickness of the microcapsules. The four suspensions of Bacampicillin hydrochloride, containing microcapsules with different coating thickness, were given as single 400-mg oral doses to 12 healthy volunteers after overnight fasting using a crossover design with balanced sequences. Bacampicillin is a prodrug of ampicillin, the concentration of which was determined in plasma and urine by bioassay. There were significant inverse linear relationships between the dissolution half-life and plasma peak concentration, area under the curve, and urinary recovery. The terminal exponential disposition phases of the curves were similar for all four suspensions. There was a significant direct linear relationship between the dissolution half-life and overall taste and bitterness. The results show that the mean bioavailability of Bacampicillin hydrochloride from a microcapsule suspension can be predicted from an in vitro dissolution half-life. The results also suggest that Bacampicillin hydrochloride can be given in a suspension with sufficient microcapsule film thickness to reduce the bitter taste of the drug and still retain adequate bioavailability.
Comparative study of bacampicillin and ampicillin in the treatment of uncomplicated gonorrhoea
Br J Vener Dis 1980 Jun;56(3):151-5.PMID:7000303DOI:10.1136/sti.56.3.151.
Bacampicillin hydrochloride, a pro-drug ester of ampicillin trihydrate which is hydrolysed to ampicillin after absorption, was used in a randomised comparative study of ampicillin 3.5 g and bacampicillin 1.6g (each with probenecid 1 g) in the treatment of uncomplicated gonorrhoea. This dose of bacampicillin was selected because in serum it gives approximately the same peak concentration of ampicillin as 3.5 g of the present drug. Genital, pharyngeal, and anal cultures were performed at the initial visit and at follow up 5-9 days after treatment. There was no statistically significant difference in the microbiological or clinical response of patients with genital gonorrhoea who were treated with ampicilin and those treated with bacampicillin. At 5-9 days after treatment, 93% of the ampicillin-treated patients and 89% of the bacampicillin-treated patients had negative genital, pharyngeal, and anal culture results; furthermore, 87% and 89% respectively had no symptoms of infection. Fewer gastrointestinal side effects were noted in the patients treated with bacampicillin.
Pharmacokinetics of bacampicillin in equids
Am J Vet Res 1995 Nov;56(11):1486-92.PMID:8585661doi
Bacampicillin hydrochloride is an ester prodrug that is hydrolyzed to ampicillin after its absorption from the gastrointestinal tract. It was administered intragastrically at a dose rate of 13.5 mg/kg of body weight to ponies and horses, and was highly bioavailable (F = 41.0%), compared with other penicillins in adult horses. The high peak ampicillin plasma concentration of 6.1 +/- 0.5 micrograms/ml achieved and persistence of the antibiotic at concentration of 0.3 +/- 0.1 microgram/ml 6 hours after its intragastric administration, suggest that Bacampicillin hydrochloride may reach suitable bactericidal concentrations for treatment of infections caused by susceptible microorganisms. In a separate experiment, dichlorvos, an organophosphate compound that inhibits some of the esterase activity in plasma, was administered orally to the same animals at a dose rate of 40 mg/kg, followed by intragastric administration of Bacampicillin hydrochloride at a dose of 13.5 mg/kg. Plasma pseudocholinesterase and erythrocyte acetylcholinesterase activities were reduced to < 5% of reference (predichlorvos) values after dichlorvos administration. However, rate of hydrolysis of bacampicillin into ampicillin was not affected. Consequently, the disposition and fate of bacampicillin when administered intragastrically 1 day after dichlorvos administration were similar to the values obtained after administration of bacampicillin alone. Intragastric coadministration of probenecid at a dose rate of 75 mg/kg and bacampicillin at 13.5 mg/kg limited absorption of the antibiotic from the gastrointestinal tract. This suggests existence of a common transport mechanism for bacampicillin and probenecid in the gastrointestinal wall, and precludes use of this combination for treatment. The bioavailable fraction of ampicillin after combination treatment indicated prolonged residence time in the plasma, presumably as a consequence of reduced renal tubular secretion.
In vitro-in vivo evaluation of Bacampicillin hydrochloride from microcapsules of water-insoluble and an acid-soluble polymer
J Microencapsul 1985 Apr-Jun;2(2):123-36.PMID:3880480DOI:10.3109/02652048509031556.
Bacampicillin hydrochloride has been microencapsulated to mask its very bitter taste. The objective of the study was to compare the in vitro release and bioavailability of Bacampicillin hydrochloride from microcapsules coated with two principally different polymers: a water-insoluble polymer, ethylcellulose, and an acid-soluble polymer, Eudragit E 100. The last mentioned was supposed to have advantages from a bioavailability point of view since this polymer should dissolve rapidly upon reaching the stomach. In vitro release studies were performed in different types of media by using a flow-through cell technique and USP paddle apparatus. The in vivo study was performed on 20 healthy volunteers taking single 400 mg doses of the drug in the two microcapsule suspensions and a reference tablet according to a randomized cross-over design. When standard dissolution fluids were used, the Eudragit E 100-coated microcapsules revealed very rapid dissolution but were greatly dependent on buffer concentration and ionic strength. The ethylcellulose-coated microcapsules released the drug much more slowly than Eudragit E 100 when using standard dissolution fluids. They were also affected by buffer concentration and ionic strength. The reference tablet had a significantly higher bioavailability than the two microcapsule suspensions. In vitro-in vivo correlation was not obtained when using standard dissolution fluids according to USP. However when stimulated intestinal fluid was adjusted to have an ionic strength similar to intestinal fluid, a better in vitro-in vivo correlation was obtained. The Eudragit E 100 polymer did not give better bioavailability than ethylcellulose as a coating polymer on bacampicillin microcapsules.