Ophthalmic compositions comprising bilastine, a beta-cyclodextrin and at least one gelling agent
A technology of composition and cyclodextrin, which is applied in the direction of medical preparations containing active ingredients, drug combinations, non-active ingredients of polymer compounds, etc.
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Embodiment 1
[0161] Example 1. More than 6.5mg / mL bilastine in water at 25°C in the presence of 9% different β-cyclodextrins Stability in solution at different pH values
[0162] This example shows that five cyclodextrins (β-CD, HP-β-CD, CM-β- Stability of CD, DM-β-CD and SBE-β-CD) in aqueous solution at different pH values. Each pH value was obtained by starting with an alkaline solution and adjusting as shown below.
[0163] Bilastine in non-buffered solution (pH adjusted)
[0164] a. 7 mg / mL bilastine solution in alkaline medium: Add 70 mg of bilastine to a 10 mL volumetric flask. Approximately 5 mL of deionized water was added followed by 1M NaOH dropwise while shaking the mixture until all the bilastine was dissolved. Next, 900 mg of the corresponding cyclodextrin was added and the mixture was shaken until the cyclodextrin was completely dissolved (except in specific cases which did not result in completely dissolved β-CD). The volume was then adjusted to 10 mL.
[0165] b....
Embodiment 20
[0180] Example 2. Ocular Bioadhesion of 0.4% w / v Bilastine and 9% HPB in Different Compositions
[0181] Bioadhesion of compositions containing 0.4% w / v bilastine and 9% HPB in the eyes of animals (rats) was measured by positron emission tomography (PET) scanning. The compositions contain varying amounts of viscosifiers and tonicity agents (methylcellulose and glycerin) and gelling agents (sodium hyaluronate and / or gellan gum). Positron Emission Tracer 18 The addition of FDG made it possible to measure the average residence time of each composition in rat eye tissue.
[0182] Table 4 Mean ocular residence time (ART) of compositions of the invention comprising 0.4% w / v bilastine and 9% HPB
[0183]
[0184] Table 4 shows when sodium hyaluronate (HA), gellan gum (GG), or a mixture of AH and GG were combined with bilastine and HPB cyclodextrin with and without methylcellulose (MC) and glycerin Use to achieve maximum residence time, or ocular bioadhesion. Thus, the result...
Embodiment 3
[0185] Example 3. Preclinical in vivo efficacy of ophthalmic formulations
[0186] animal model
[0187] Male Dunkin-Hartley guinea pigs, weighing 300-349 g at receipt (Harlan Laboratories Inc. / Envigo) were used and maintained in standard housing conditions (2 animals / cage). Animals (6-10 per group) were not used again until after a washout period of at least 4 days between consecutive uses to allow complete recovery of the eye conjunctiva.
[0188] Experimental procedure
[0189] Two aqueous ophthalmic formulations of bilastine were prepared at concentrations of 0.4% and 0.6% w / v bilastine. Both formulations also contained 90 mg / mL HPB, 0.1 mg / mL methylcellulose, 1 mg / mL sodium hyaluronate, and 16.1 mg / mL glycerin.
[0190]The ophthalmic formulation was applied by instillation in the right eye (25 μL), and the animal was kept immobilized for 2 to 3 minutes to ensure persistence of the product in the conjunctival sac. Next, with commercially available eye drops, the le...
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