HPLC法测定头孢氨苄甲氧苄啶胶囊含量的方法改进

目的以HPLC法同时测定复方头孢氨苄甲氧苄啶胶囊中头孢氨苄与甲氧苄啶的含量。方法以0．02mol·L^-1磷酸溶液（用20％氢氧化钠调节pH值至3．5±0．05）-乙腈（85：15）为流动相,检测波长为235nm。结果头孢氨苄在10．00～90．00）μg·mL^-1、甲氧苄啶在2．00～18．00μg·mL^-1。范围内,峰面积与其浓度呈良好线性关系;头孢氨苄平均回收率为100．0％、RSD为0．15％;甲氧苄啶平均回收率为100．1％、RSD为0．19％。结论以本文中采用的流动相,对头孢氨苄甲氧苄啶胶囊进行测定,结果头孢氨苄、甲氧苄啶两组分分离度较好,峰形对称,结果准确;本法为测定头孢氨苄甲氧苄啶胶囊的含量提供了一种新的选择。     

褶合光谱法同时测定复方头孢氨苄胶囊中二组分的含量

目的：用褶合光谱法不经分离同时测定复方头孢氨苄胶囊中头孢氨苄和甲氧苄啶二组分的含量。方法：结合计算机信息处理技术,利用褶合曲线分析法同时测定复方头孢氨苄胶囊中二组分的含量。结果：头孢氨苄和甲氧苄啶的平均回收率分别为99．85％（RSD=0．47％）和100．04％（RSD=1．65％）。结论：此方法不需分离,可同时测定吸收光谱互相重叠的复方剥剂中待洲组分的含量,方法可靠,操作简单,结果准确。     

用反相高效液相色谱法测定复方头孢氨苄胶囊中头孢氨苄和甲氧苄？…

建立一种用反相高效液相色谱法检测复方制剂中头孢氨苄和甲氧苄啶含量的方法。头孢氨苄浓度为０．０５～２．００ｍｇ／ｍＬ、甲氧苄啶浓度为０．０１～０．４０ｍｇ／ｍＬ时存在良好的线性关系,头孢氨苄回收率为１００．４％,ＲＳＤ＝０．５８％（ｎ＝７）;甲氧苄啶回收率为１００．２％,ＲＳＤ＝０．６２％（ｎ＝７）。     

高效液相色谱法测定复方头孢氨苄片中头孢氨苄和甲氧苄啶的含量

目的 建立高效夜相色谱法测定复方头孢氨苄片中头孢氨苄和甲氧苄啶的含量。方法采用C18柱，以水-甲醇-3.86醋酸钠-4％醋酸(790：192:15．3)为流动相，流速为1．0／min，检测波长为271nm。结果 头孢氨苄和甲氧苄啶分别在120-280ug／ml和30-70ug／ml的范围内呈良好的线性关系，平均回收率分别为100．3％(RSD=0．8％)和99．8％(RSD=0．9％)。结论 该方法灵敏、快速、准确。     

用反相高效液相色谱法测定复方头孢氨苄胶囊中头孢氨苄和甲氧苄啶的含量

建立一种用反相高效液相色谱法检测复方制剂中头孢氨苄和甲氧苄啶含量的方法 .头孢氨苄浓度为 0 .0 5～ 2 .0 0mg/mL、甲氧苄啶浓度为 0 .0 1～ 0 .40mg/mL时存在良好的线性关系 .头孢氨苄回收率为 10 0 .4% ,RSD =0 .5 8% (n =7) ;甲氧苄啶回收率为 10 0 .2 % ,RSD =0 .6 2 % (n =7) .     

高效液相色谱法测定甲氧苄啶片的含量

目的建立甲氧苄啶片含量的高效液相色谱（HPLC）测定法。方法采用十八烷基硅烷键合硅胶柱;流动相为乙腈-水．三乙胺：200：799：1（冰醋酸调pH至5．9）;检测波长271nm;流速1．0ml·min^-1。甲氧苄啶易溶于醋酸,用少量冰醋酸溶解甲氧苄啶,用水稀释后测定含量。结果甲氧苄啶质量浓度在5—70mg·L^-1范围内与峰面积呈良好线性关系,r=0．9999,平均回收率为98．9％,RSD为0．36％（n=6）。结论本法操作简单,结果准确,重现性好,可用于甲氧苄啶片的含量测定。     

HPLC法测定头孢氨苄甲氧苄啶颗粒含量的方法改进

目的头孢氨苄甲氧苄啶颗粒是由头孢氨苄和甲氧苄啶组成的复方制剂,本实验用HPLC法同时测定其两种成分的含量。方法用十八烷基硅烷键合硅胶为填充剂,以0.025mol/L磷酸溶液-乙腈（80：20）为流动相,检测波长为235nm,流速为每分钟0.8ml,理论塔板数按头孢氨苄峰计数应不低于3000。结果头孢氨苄在10.00～50.00μg/ml,甲氧苄啶在2.00～10.00μg/ml范围内,峰面积与其浓度呈良好线性关系,头孢氨苄的加样平均回收率为99.43%,RSD为0.28%,甲氧苄啶的加样平均回收率为99.21%,RSD为0.61%。结论与原标准相比,所得的头孢氨苄,甲氧苄啶两种成分峰面积与其浓度呈良好线性关系,峰形对称,拖尾因子小,结果比较准确。     

高效液相色谱法测定联磺甲氧苄啶片中3组分含量

目的建立测定联磺甲氧苄啶片含量的高效液相色谱（HPLC）法。方法采用Zorbax C18柱（150mm×4．6mm，5μm）为色谱柱，以水-乙腈-三乙胺（799：200：1，用氢氧化钠试液或冰醋酸调节pH值至5．9）为流动相，检测波长为240nm，流速为1．0mL／min，进样量为20μL，枉温为30℃。结果磺胺嘧啶和磺胺甲嗯唑质量浓度在5～100μg／mL范围内，甲氧苄啶质量浓度在2～40μg／mL范围内与峰面积线性关系良好；平均回收率磺胺嘧啶为99.91％（RSD为0.2％），磺胺甲嗯唑为99．76％（RSD为0．2％），甲氧苄啶为99．80％（RSD为0．4％）。结论HPLC法分离度好，快速、简便，可同时测定3种组分，可作为该产品的质量控制方法。     

系数倍率分光光度法测定复方头孢氨苄胶囊中头孢氨苄及甲氧苄氨嘧啶含量

系数倍率分光光度法测定复方头孢氨苄胶囊中头孢氨苄及甲氧苄氨嘧啶含量于治国，宋洪杰，尚飞沈阳药学院药学系沈阳１００１５陈宁宁辽凯药业有限公司沈阳ｌ１００１５复方头孢氨苄胶囊为ＣＬＸ（头孢氨苄）和ＴＭＰ（甲氧苄氨嘧啶）的复方制剂．现行药品标准［１］分别采...     

高效液相色谱法测定头孢氨苄甲氧苄啶胶囊的含量均匀度

目的建立头孢氨苄甲氧苄啶胶囊含量均匀度的测定方法。方法以0.025 mol/L磷酸溶液（用20%氢氧化钠调节pH至3.0）-乙腈（85∶15）为流动相,流速1 mL/min,检测波长235 nm,用高效液相色谱法测定含量。结果头孢氨苄质量浓度在12.5～125μg/mL、甲氧苄啶质量浓度在2.5～25μg/mL范围内与峰面积线性关系良好,平均回收率分别为99.9%和99.8%,RSD分别为0.38%和0.95%（n=9）。结论所用方法简便快捷,能准确地测定产品的含量均匀度,可用于头孢氨苄甲氧苄啶胶囊的质量控制。     

Madaline 网络用于药物复方制剂的含量测定

目的　用 Madaline 网络进行复方头孢氨苄胶囊中头孢氨苄(CEX)和甲氧苄氨嘧啶(TMP)的含量测定。方法　通过 Madaline 网络变换,多组分体系中各组分的重叠光谱转换成互不干扰的谱峰;利用模拟样品得到变换后光谱与相应组分浓度的关系,在此基础上对待测样品进行含量测定。结果　复方制剂中 CEX 和 TMP 的平均回收率和相对标准偏差分别为100.1% ,0.4%和100.4% ,1.3%。结论　将 Madaline 网络用于药物制剂分析,可得到满意结果,值得进一步推广应用     

复方头孢氨苄胶囊的三波长分光光度测定法

用三波长分光光度法,不经分离可同时测定复方头孢氨苄胶囊中头孢氧苄和甲氧苄啶的含量。本法取样少,操作简迅,结果准确。两者的回收率分别为.100.28%和99.94%,变异系数为0.65%和0.49%。     

Comparative double-blind study of cefroxadine and cephalexin in the treatment of complicated urinary tract infection

To evaluate the efficacy, safety, and utility of cefroxadine (CXD) for the treatment of complicated urinary tract infections, a double blind study comparing CXD with cephalexin (CEX) was carried out. Patient received either 1,500 mg/day of CXD 3 times a day, or 2,000 mg/day of CEX 4 times a day for 5 days by oral route, and the following results were obtained. Of the 305 patients, clinical efficacies were evaluated in 220 cases (CXD 105 cases, CEX 115 cases) except that excluded or dropped out. Side effect was evaluated in 301 cases (CXD 150 cases, CEX 151 cases). There was no statistically significant difference in the back ground characteristics between the 2 groups. Overall clinical assessment by the committee according to the "Criteria for Evaluation of Clinical Efficacy of Antimicrobial Agents on Urinary Tract Infection" patients evaluated as better than "good" were 64 of 105 (61.0%) for CXD and 75 of 115 (65.2%) for CEX. The difference between the 2 groups was not statistically significant. In effect on pyuria, patients evaluated as better than "decreased" were 58 of 105 (55.2%) for CXD and 69 of 115 (60.0%) for CEX. The difference between the 2 groups was not statistically significant. In effect of bacteriuria, patients evaluated as better than "decreased" were 57 of 105 (54.3%) for CXD and 69 of 115 (60.0%) for CEX. The difference between the 2 groups was not statistically significant. Analyses were stratified according to classification by the type of infection, diagnosis, degree of pyuria before treatment, and bacterial count before treatment. There were no statistically significant differences between the 2 treatment groups as to any item. In evaluation by attending physician, patients evaluated as better than "good" were 81 of 140 (57.9%) for CXD, and 85 of 141 (60.3%) for CEX. Statistically significant difference was not observed between the 2 groups. In drug usefulness by attending physician, patients evaluated as better than "usefulness" were 106 of 140 (75.7%) for CXD, and 109 of 141 (77.3%) for CEX. The difference between the 2 groups was not statistically significant. In evaluation of the infections with sensitive species to both CXD and CEX by the committee according to "Criteria for Evaluation of Clinical Efficacy of Antimicrobial Agents on Urinary Tract Infections, overall clinical efficacies were evaluated in 102 (CXD 48 cases, CEX 54 cases) which were infected with sensitive species. There was no statistically significant difference in the back ground characteristics between the 2 treatment groups.(ABSTRACT TRUNCATED AT 400 WORDS)     

Study on the transfer of cefroxadine to human tears

A comparative study to determine the transfer of cefroxadine (CXD), an oral cephem antibiotic, to the human tears was undertaken using cephalexin (CEX) as the control drug. The mean tear levels of 250 mg each of CXD and CEX after oral administration in 6 volunteers were equally peaked at 0.26 micrograms/ml with CXD after 1 to 2 hours and with CEX after 2 hours. The changes of tear levels were also equal for both drugs. The ratios between the tear and the blood levels at 2 hours after oral administration were almost equal with 4.1% for CXD and 3.7% for CEX. From the above evidence it has been confirmed that the both drugs were equivalent with regard to the concentration profiles in human tears after oral medication.     

A double-blind comparison between cefaclor and cephalexin in the treatment of dental infections

A comparative clinical study of cefaclor (CCL) with cephalexin (CEX) was carried out by randomized double-blind techniques in order to contemplate the clinical efficacy, side effects and usefulness in treatment of 243 patients with dental infections. In the CEX group, CEX was orally administered 4 times a day at a daily dosage of 1,000 mg for 3 to 5 days. In the CCL group, CCL was orally administered 3 times a day at a daily dosage of 750 mg for 3 to 5 days and 1 capsule of placebo was also given every evening in order to keep the blindness of the administration. Evaluable cases for efficacy of athe drugs were 213 consisting of 108 for CCL and 105 for CEX. There were no significant differences in background of the patients and severity of the disease between 2 treatment groups. Clinical effectiveness on the 3rd day was 89.7% in CCL group and 78.6% in CEX group, showing significant difference between 2 treatment groups. Clinical effectiveness on the final day of administration was 94.4% in CCL group and 92.4% in CEX group, showing no significant difference between 2 treatment groups. Side effects were found in 10.5% of 114 patients receiving CCL and in 4.5% of 112 patients with CEX, and there was no significant difference between 2 treatment groups. The side effects were mostly gastrointestinal origin. According to the judgement by physicians in charge, no significant difference was seen in clinical usefulness between the 2 drugs.     

Evaluation of in vitro antibacterial potencies of oral antibiotics against sputum isolates

Susceptibility of 162 sputum isolates to oral antibiotics was measured by an agar dilution method. The sputum isolates included S. pneumoniae 25 strains, S. aureus 30 strains, H. influenzae 37 strains, K. pneumoniae 51 strains and E. coli 19 strains. Minimal inhibitory concentration (MIC) values of cefaclor (CCL), cephalexin (CEX), ampicillin (ABPC) and minocycline (MINO) were measured for each strains. Eighty percent of S. pneumoniae strains were inhibited at 0.024 to 0.05 micrograms/ml of ABPC, 0.39 to 0.78 micrograms/ml of CCL, and 1.56 to 3.13 micrograms/ml of CEX and MINO. ABPC, CCL and CEX were considered to be effective clinically when they were used with the usual dosage. However, about 30% of strains were resistant to the usual dosage of orally administrated MINO. Eighty percent of S. aureus strains were inhibited at 0.20 to 0.39 microgram/ml of MINO and 3.13 to 6.25 micrograms/ml of the other 3 drugs. MINO is the most effective with the usual dosage. Twenty to 40% of strains showed resistance to CCL, CEX and ABPC. Eighty percent of H. influenzae strains were inhibited at 0.39 micrograms/ml of ABPC, 0.78 to 1.56 micrograms/ml of MINO, 3.13 micrograms/ml of CCL and 12.5 to 25 micrograms/ml of CEX. ABPC should be selected as the first choice antibiotic. However, there were 2 ABPC-resistant strains that were highly susceptible to CCL. Eighty percent of K. pneumoniae strains were inhibited at 0.39 to 0.78 micrograms/ml of CCL, 3.13 to 6.25 micrograms/ml of MINO and CEX, and 12.5 to 25 micrograms/ml of ABPC. CCL seemed to be only effective oral antibiotic for K. pneumoniae infection.(ABSTRACT TRUNCATED AT 250 WORDS)     

Comparative studies of the efficacy, safety and usefulness of S6472, cefaclor and cephalexin on complicated urinary tract infection by the double-blind method

To objectively evaluated the usefulness of the standard formulation of cefaclor (CCL) and the long-acting formulation of cefaclor (S6472) in noncatheterized complicated urinary tract infection (UTI), a double-blind comparison study was carried out using cephalexin (CEX) as a control. Patients were orally treated with either 500 mg of CCL 3 times/day, 750 mg of S6472 2 times/day, or 500 mg of CEX 4 times/day for 14 days. Overall clinical effect was evaluated on days 5 and 14 in accordance with the UTI therapeutic evaluation standard, with check for recurrence on day 21. There was no demographic difference between the groups. There was no difference in the effective rate on day 5 among the 3 treatment groups: 58.1% in S6472 group, 66.0% in CCL group and 61.9% in CEX group. Nor on day 14, was there any significant difference in the effective rate among the 3 groups: 70.8% in S6472 group, 63.4% in CCL group and 61.8% in CEX group. Stratification analyses (by UTI group, infection site, in- or out-patient, time of starting treatment, pretreatment severity of pyuria, total number of bacteria before treatment) revealed no significant difference among the 3 groups. Therapeutic effect evaluated by physicians in charge was not significantly different among the 3 groups on day 5 or day 14. In terms of overall therapeutic effect, all 3 products were very effective in patients infected with sensitive bacteria: On day 5, 85.4% in S6472 group, 84.4% in CCL group, and 83.7% in CEX group. There was no significant difference among the 3 groups on either day. The incidence of side effects was not significantly different among the 3 groups: 4 out of 129 patients treated with S6472 (3.1%), 2 of 131 treated with CCL (1.5%) and 2 of 128 with CEX (1.6%). Clinical laboratory tests revealed 4 abnormal findings in 4 patients treated with S6472, 6 findings in 4 treated with CCL, and 4 findings in 2 treated with CEX, showing no significant difference in incidence among the 3 groups. Both side effects and abnormal clinical laboratory findings were mild and reversible. Physicians in charge judged the usefulness of the 3 drugs on days 5 and 14, taking efficacy and safety into consideration. Significant difference was not observed. The presence of recurrence was examined 7 days after drug withdrawal in patients regarded as remarkable responders to 14-day treatment by overall therapeutic effect evaluation.(ABSTRACT TRUNCATED AT 400 WORDS)     

In vitro susceptibilities of causative organisms isolated from patients with primary respiratory tract infections to BRL 25000 (clavulanic acid/amoxicillin)

The in vitro susceptibilities of various causative organisms recently isolated from patients with primary respiratory tract infections to BRL 25000 (a formulation of amoxicillin, 2 parts, and potassium clavulanate, 1 part), amoxicillin (AMPC), cefaclor (CCL), cephalexin (CEX), cefadroxil (CDX) and cefroxadine (CXD) were determined. beta-Lactamase producing strains were detected by nitrocefin chromogenic method and PCG acidometric method. The frequency of isolation of beta-lactamase production in strains of S. aureus, H. influenzae, B. catarrhalis and K. pneumoniae was 92%, 18%, 36% and 98%, respectively. Against S. aureus strains with MIC values to AMPC of less than or equal to 100 micrograms/ml and CEX of less than or equal to 25 micrograms/ml BRL 25000 showed MIC values in the range 0.39-6.25 micrograms/ml with inocula of 10(6) CFU/ml, while BRL 25000 required 12.5-100 micrograms/ml of concentrations for inhibition of the strains with MIC values to AMPC of greater than 100 micrograms/ml and CEX of greater than or equal to 25 micrograms/ml. Against S. pyogenes and S. pneumoniae BRL 25000 showed MIC values in the range less than 0.024-0.10 micrograms/ml with inocula of 10(6) CFU/ml, which is much more active than CCL, CEX, CDX and CXD and slight less active than AMPC. Against H. influenzae and B. catarrhalis BRL 25000 showed MIC values in the range 0.20-6.25 micrograms/ml with inocula of 10(6) CFU/ml, which showed most potent activity among the agents tested. The activity of BRL 25000 against K. pneumoniae was approximately equal to that of CCL and superior to that of AMPC, CEX, CDX and CXD.     

Formulation of carbenoxolone for delivery to the skin

Carbenoxolone (CEX), a semi-synthetic derivative of glycyrrhetinic acid, has previously been used as a disodium salt for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties. Although glycyrrhetinic acid is available in pharmaceutical and personal care products for skin care, the topical use of the free acid form of CEX, has not previously been reported. In this work we investigated the percutaneous penetration of CEX. Solubility and permeability studies were conducted using a range of solvents or skin permeation enhancers (SPEs) commonly used for skin delivery. Binary combinations of dimethyl isosorbide (DMI) and Transcutol™ (TC) with isopropyl myristate (IPM) were effective in promoting skin permeation of CEX although individual solvents were not. Alternative fatty acid esters to IPM were subsequently investigated with the most promising formulation consisting of TC and propylene glycol laurate (PGL). Interestingly, propylene glycol monolaurate (PGML) did not demonstrate comparable efficacy when combined with TC. A ternary formulation consisting of TC, PGL and IPM demonstrated the best permeation enhancement of CEX compared with all other vehicles. The findings confirm (i) the feasibility of promoting CEX penetration across the skin (ii) the synergistic effect of combinations of solvents and SPEs on dermal and transdermal delivery (iii) the necessity for more fundamental studies to explain the differential effects of fatty acid esters on the skin barrier.