SUMMARY
This research article contains the results of the suppositories stability with MacluraPomifera extract studies during their storage. The observation was carried out at two temperature regimes: at 15-25 °C and 815 °C. The Control of drug had been performed every 3 months during 27 months.The preparations were evaluated by their physical-chemical properties, according to the State Pharmacopoeia of Kazakhstan on such parameters as: appearance, average weight, the total deformation time, melting point, and acid number. Qualitative and quantitative assessment of the drug was carried out by the amount of isoflavones, phytosterols and triterpenes. It was found that suppositories remain stable for 24 months at the temperature of 8-15 °C.
Key words: suppositories, MacluraPomifera, stability, prostatitis, isoflavones, phytosterols.
Currently, prostate diseases are a very common ailment. The most frequent pathologies in urological practice are prostatitis, benign prostatic hyperplasia and prostate cancer. Chronic prostatitis is up to 35% of all visits to the doctor, and most often inflammation of the prostate gland have men who are younger than 50 years [ , 2].
At the same time the need of prostatoprotectors for the Kazakhstan's market is covered almost exclusively by imported drugs, whereas, for example, in Russia and Ukraine a big part of preparations for the treatment of prostate diseases are domestic developments [3].
One of the perspective dosage forms for drugpossession that possess prostatoprotectors properties are suppositories [4, 5, 6, 7]. To treat prostate diseases in their various forms, we developed suppositories with Maclurapomifera extract. The main biologically active substances of the suppositories are triterpenes, phytosterols and isoflavones that are known for their anti-inflammatory, antioxidant, anti-proliferative and reparative actions [8,9,10].
One of the main indicators of the quality of the drug is the stability of its physical-chemical, pharmaceutical and consumer properties. Shelf-life of the drug depends on many factors; with the deterioration of any one of them during the storage indicates negative processes taking place in the composition of the drug [11, 12].
Goal of this work
The aim of this paper is to study the stability and the shelf life determination of developed suppositories with MacluraPomifera extract.
Materials and Methods
The objects of the study were the suppositories with MacluraPomifera oil extract that was obtained by pouring into PVC forms, tallow was used as a base.
To study the stability of suppositories during the storage and for the experimental determination of the expiry date we have made several series of the drug in PVC film and stored it. The tested suppositories were stored under two temperature modes: the 1st 15-25 °C;the 2nd 8-15 °C. Drug control was performed by every 3 months for 27 months.
Table 1 - Assessment of the suppositories WithMacluraPomifera extract
|
Quality parameter |
Quality standard |
|
Description |
Suppositories white or cream color, same size, torpedoshaped, homogeneous on the cut |
|
Identification |
A Chromatogram should have two purple spots at Rf 0.8 and 0.57, two yellow spots with Rf 0.45 and 0.21. |
|
Melting point |
Not above 37 ° C. |
|
A full deformation |
Not more than 15 minutes |
|
Average weight of the suppository |
2,1 ± 5% |
|
Acid number |
Not more than 2 |
|
Quantitative determination of:
|
At least 2 mg At least 1 mg |
Grading was carried out according to the State Pharmacopoeia of Kazakhstan on such parameters as: appearance, average weight, the total deformation time, melting point, and acid number [13].
Identification oftriterpenes and isoflavones which are contained in the suppositories were determined by thin-layer chromatography on the thin Sorbent layer at 'Sorbfil' plates in the solvent system: hexane-ethyl acetate (9:2). Blots showed a 1% solution of vanillin in 95% ethyl alcohol. After drying under the heating lupeol and в-sitosterol is detected as purple spots with values of 0.8 and 0.57 Rf; osayin and pomiferin are detected as yellow spots with values of 0.45 and 0.21 Rf.
For the quantitative determination of the isoflavones amount it was using the method of differential spectrophotometry based on the selective interaction of aluminum chloride solution with the compounds of the flavonoid structure. Absorbance was measured in the visible region of the spectrum at 419 nm.
For the development of the method of quantitative determination of the amount of the triterpenes and phytosterols in the suppositories we used their ability to move in the non-polar solvents from unsaponifiable fraction, and further to give colored complexes by interreaction with concentrated sulfuric acid. The absorbency of the derived colored solution was determined at spectrophotometer at a wavelength of 309 nm.
Quality indicators of the suppositories with MacluraPomifera extract is shown in Table 1.
Results and Discussion
According to the obtained data the suppositories with the MacluraPomifera extract laid down on storage at room temperature and under 8-15 ° C, meet the quality indexes .
According to the results shown in tables 2 and 3, during the entire duration of the study the appearance and the average weight of suppositories remained stable. Melting point the total deformation time of the suppositories with MacluraPomifera extract did not exceed 37 ° C and 15 minutes, respectively, as at the suppositories that were kept at 15-25 ° C, as well as at 8-15 ° C.
Identification of the suppositories showed the constancy of qualitative composition during their storage. In the chromatography assay on the plates there were no additional spots that indicates the absence of degradation products.
The acid number and the active substance content of the suppositories changed according to conditions and time of the storage. At the keeping of the drug at the temperature of 8-15 °C these indicators changed slightly, whereas at the room temperature, during observation, acid number increased and reduced the number and amount of the triterpenes and phytosterols mostly in amounts of isoflavones. The results are not out of range at that.
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Thus the suppositories with oil extract of MacluraPomifera are stable during 24 months at the temperature of 8-15°С, this fact allow us to recommend their shelf life for 2 years.
Conclusions
- It was studied the stability of the suppositories with oil MacluraPomifera extract under the influence of various storage conditions and time.
- It was found that suppositories remain stable for 24 months at the temperature of 8-15 ° C.
- Based on these results the recommended shelf life of suppositories with oil MacluraPomifera extract is 2 years.
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