Gato MA, Romero DA, Bellma MA, Morales LI, Botet GM

Language: Spanish
References: 8
Page: 5-12
PDF size: 115.00 Kb.

ABSTRACT

Objective: to develop a 2 % dorzolamide plus 0.5 % timolol eye drop solution with all the quality requirements to provide adequate therapeutic effect without adverse reactions for the patients.
Methods: three preliminary trials were prepared with dorzolamide chlorhydrate and timolol maleate, a buffer solution based on monohydrated citric acid/dehydrated trisodic citrate with pH range 5-6, benzalkonium chloride and 10 % HPMC F4M (hydroxypropilmetylcellulose). These components replaced those recommended in the literature review. The chemical and physical stability of this formulation was studied for three months in terms of organoleptic characteristics, active ingredient concentration, pH, fluidmetric properties, eye irritability and effectiveness of preserver. The study formulation allowed developing and validating the analytical technique of the Center for the Drug Research and Development. Linearity, precision, specificity and accuracy of the method were determined. Three 5 L pilot batches were prepared. Master Batch 5 mL low-density polyethylene plastic bottles were used for packing.
Results: active ingredients, dorzolamide chlorhydrate and timolol maleate, the pharmaceutical quality excipients and the packing material met the quality specifications according to USP 33. The physical and chemical analysis of the three batches at pilot and industrial scales met the quality specifications of the analytical technique devised by the Department of Stability of the Center for Drug Research and Development and the microbiological analysis reported in USP 33.
Conclusions: the achieved results allowed introducing the formulation at industrial scale and replacing the imported drug.

REFERENCES

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