Preparation and Evaluation of Sparf

Preparation and Evaluation of Sparfloxacin Parenteral
Dosage Form
Sparfloxacin is a synthetic fluoroquinolone broad spectrum anti microbial agent used in the treatment of
bacterial infections and it is presently available in the market only as tablet dosage form. It is preferred in the
treatment of adults with community acquired pneumonia, acute bacterial exacerbations of chronic bronchitis
caused by susceptible organism. The present study was undertaken with an intention to develop a stable and
effective parenteral formulation, containing the drug sparfloxacin. Sparfloxacin is a water insoluble drug. The
effects of various co solvents in the solubility of sparfloxacin have been evaluated. Sparfloxacin was tried with
co solvents such as PEG-400, Propylene glycol, Glycerin, Ethanol, Tween 80. The drug was made into injection
formulation for administration with infusions. PEG-400 was selected as co solvent and formulation have been
formulated in different combinations along with ethyl alcohol. Various batches of sparfloxacin injection
formulation were prepared in order to assess the influence of heat, light, atmospheric oxygen and antioxidant
on the stability of the drug and the formulations were also subjected to accelerated stability testing in order
to predict approximate shelf-life of the product.
List of ingredients used is given in Table 1.
Preformulation Studies2,3,4,5,6
Solubility studies of Sparfloxacin in different
solvents (saturation solubility method)
Excess of drug was added to different solvents in
10 ml stoppered volumetric flasks. Then Drug was
made to dissolve in the solvent by placing the
volumetric flask in the shaker bath at 25° C for 6
hours. The volumetric flasks were then placed at
room temperature for 24 hours. The solutions were
filtered and appropriate dilutions were made to
measure absorbances at 286nm using UV visible
spectrophotometer, and water as blank. The data
are given in Table 3.
Effect of Temperature on Stability of Drug
1% Sparfloxacin solution in 0.0.1N NaOH is filled
into vials. The vials were sealed and placed at
refrigeration, room-temperature, 50°C, 75°C and
95°C for 1 week and observed for colour change
and crystal growth. The samples placed at
refrigeration and room temperature served as
controls. The data are given in Table 4.
Light Stability of Drug
1% of Sparfloxacin solution in 0.0.1N NaOH is
filled in to 20ml glass vials (amber and clear).
Also samples of drug substance are placed in an
open perti dish to expose a large surface. Drug and
dilutions placed in a light-resistant amber coloured
glass vials, foil wrapped and in a cardboard box as
controls. This is carried out for 4 weeks with
weekly examinations for visible colour change or
precipitation in solution in clear vials, the
compound can be considered as potentially light
sensitive and should be handled accordingly. The
data are given in Table 5.
Effect of Oxygen on Drug
1% of Sparfloxacin in 0.0.1N NaOH is filled into
vials and placed at 30°C and 40°C. One group is
purged and another group is sealed with air.
Solutions are observed for colour change and drug
content. The data are given in Table 6 to 11.
FORMULATION DEVELOPMENT
Attempts were made to develop a stable parenteral
formulation using cosolvent/s along with other
excipients. The dose selected for formulation was
400 mg of Sparfloxacin in 2ml solvent. The
prepared formulations contain the following
ingredients along with their concentrations are
given in Table 2.
Thus prepared formulations were assayed for drug
content respectively and 10ml of these were placed
at 5°C, room temperature (RT), 37°C, 40°C and
45°C for six weeks and observed for crystal
growth, clarity, pH change, and drug content.

Hasil (Bahasa Indonesia) 1:

Persiapan dan evaluasi Sparfloxacin ParenteralBentuk sediaanSparfloxacin adalah fluoroquinolone sintetis spektrum yang luas anti mikroba agen yang digunakan dalam pengobataninfeksi bakteri dan tersedia saat ini di pasar hanya sebagai bentuk dosis tablet. Itu lebih disukai diperawatan orang dewasa dengan masyarakat memperoleh pneumonia, akut bakteri yang mengalami eksaserbasi bronkitis kronisdisebabkan oleh organisme rentan. Penelitian ini dilakukan dengan maksud untuk mengembangkan yang stabil danefektif formulasi parenteral, yang mengandung obat sparfloxacin. Sparfloxacin adalah obat tidak larut air. TheEfek berbagai co pelarut di kelarutan sparfloxacin telah dievaluasi. Sparfloxacin diadili denganCo pelarut PEG-400, Propylene glycol, gliserin, etanol, Tween 80. Obat dijadikan injeksiformulasi untuk administrasi dengan infus. PEG-400 Terpilih sebagai pelarut co dan formulasi telahdirumuskan dalam kombinasi yang berbeda dengan etil alkohol. Berbagai kumpulan sparfloxacin injeksiformulasi telah dipersiapkan untuk menilai pengaruh panas, cahaya, atmosfer oksigen dan antioksidanpada stabilitas obat dan formulasi juga mengalami pengujian dalam rangka stabilitas dipercepatuntuk memprediksi perkiraan rak-hidup produk.Daftar bahan-bahan yang digunakan diberikan dalam tabel 1.Studies2 preformulation, 3, 4, 5, 6Kelarutan studi Sparfloxacin dalam berbagaisolvents (saturation solubility method)Excess of drug was added to different solvents in10 ml stoppered volumetric flasks. Then Drug wasmade to dissolve in the solvent by placing thevolumetric flask in the shaker bath at 25° C for 6hours. The volumetric flasks were then placed atroom temperature for 24 hours. The solutions werefiltered and appropriate dilutions were made tomeasure absorbances at 286nm using UV visiblespectrophotometer, and water as blank. The dataare given in Table 3.Effect of Temperature on Stability of Drug1% Sparfloxacin solution in 0.0.1N NaOH is filledinto vials. The vials were sealed and placed atrefrigeration, room-temperature, 50°C, 75°C and95°C for 1 week and observed for colour changeand crystal growth. The samples placed atrefrigeration and room temperature served ascontrols. The data are given in Table 4.Light Stability of Drug1% of Sparfloxacin solution in 0.0.1N NaOH isfilled in to 20ml glass vials (amber and clear).Also samples of drug substance are placed in anopen perti dish to expose a large surface. Drug anddilutions placed in a light-resistant amber colouredglass vials, foil wrapped and in a cardboard box ascontrols. This is carried out for 4 weeks withweekly examinations for visible colour change orprecipitation in solution in clear vials, thecompound can be considered as potentially lightsensitive and should be handled accordingly. Thedata are given in Table 5.Effect of Oxygen on Drug1% of Sparfloxacin in 0.0.1N NaOH is filled intovials and placed at 30°C and 40°C. One group ispurged and another group is sealed with air.Solutions are observed for colour change and drugcontent. The data are given in Table 6 to 11.FORMULATION DEVELOPMENTAttempts were made to develop a stable parenteralformulation using cosolvent/s along with otherexcipients. The dose selected for formulation was400 mg of Sparfloxacin in 2ml solvent. Theprepared formulations contain the followingingredients along with their concentrations aregiven in Table 2.Thus prepared formulations were assayed for drugcontent respectively and 10ml of these were placedat 5°C, room temperature (RT), 37°C, 40°C and45°C for six weeks and observed for crystalgrowth, clarity, pH change, and drug content.