DEVELOPMENT OF DOMESTIC INFUSION DRUGS BASED ON PARACETAMOL

The intravenous form of paracetamol compared with
oral more reliably supports effective drug concentration
in blood plasma that promotes a higher therapeutic effect.
Recent studies have confirmed that the use of the
intravenous form of paracetamol to deal with postoperative
pain multimodal analgesia modes results in reducing
the frequency and quantity of opioids administered ,
and, as a consequence, its associated side effects. The
drug Paracetamol , infusion solution 10 mg / ml to 100
ml glass bottles is a drug - generic . His qualitative and
quantitative composition is developed from the study of
literature data about the drug - similar to " Perfalhan , 10
mg / ml solution for infusion in 100 mL " company
Bristol - Myers Squibb, France and experimental work.
The aim of our study is development and support of the
national composition of the infusion of the drug on the
basis of paracetamol, selection of excipients that provide
stability of the active substances. Materials and
methods. The object of the study was the substance of
paracetamol manufactured by Zhejiang Kangle Pharmaceutical
Co. , Ltd, China. During the work conducted
qualitative and quantitative monitoring sample preparation
for indicators of stability: pH content of the active
ingredient , transparency, color, impurities , contamination
by the methods described in the SFU [and nor- ral
documentation to the drug . One potential factor of instability
is the effect of paracetamol oxygen, due to the
presence in the molecule of paracetamol and -NH possibility
of oxidation. Results and Discussion. Paracetamol
is derived atsetamina . Substance acetylation are p -
aminophenol with acetic anhydride . Saturated aqueous
solution has a pH of paracetamol - ment about 6 . Paracetamol
is a crystalline white powder , sparingly soluble
in water, soluble in 96% alcohol, very slightly soluble in
metilenhloride . . Active substance enters in comparison
drug in the concentration of 10 mg/ml. Stable aqueous
solution decreases in acidic and alkaline environments
where paratse - tamol gradually destroyed to acetic
acid or p - aminophenol To prevent oxidation of the
drug administered antioxidant - sodium metabisulfite in
concentrations generally 1.0 g / l. In order to prevent the
negative - tive impact of oxygen on paracetamol solution
10 mg / mL drug preparation was conducted under
nitrogen gas protection . It is established that the use of
nitrogen gas protection affects the quality of the drug.
Prepared sample preparation without nitrogen gas protection
did not meet project MKYA in terms of " 4 -
aminophenol " and " color ", besides a slight tendency
pH change and reducing quantitative content of active
ingredient. Therefore, the production of the drug " Paracetamol
, infusion solution 10 mg / ml. in bottles of 100
ml " necessary solution prepared bubbling nitrogen for
20 minutes. It is established that the use of nitrogen gas
protection affects the quality of the drug. the manufacture
of the drug " Paracetamol , infusion solution 10 mg
/ ml. in bottles of 100 ml " necessary solution prepared
bubbling nitrogen for 20 minutes. Calculated theoretical
osmolarity of the drug- 299,47 мОsм / l. Solution osmolarity
close to osmolarity of blood, which is an important
criterion when used in injection therapy. Conclusions.
Theoretically grounded and experimentally
confirmed rational composition drug infusion composition
based on paracetamol. Selected auxiliaries and processing
methods in the preparation of the solution , prevents
oxidation of the main active ingredient , and also
provide the optimum level of osmolarity solution. Results
of this development are used during compile of
registration dossier of preparation, analytical and technological
normative documents on his production and
control of quality of intermediate products and prepared
products.