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Puerarin temperature-sensitive and bioadhesive in situ gel -type eye research

Author: QiHongYi
Tutor: WuChunJie
School: Chengdu University of Traditional Chinese Medicine
Course: Pharmacy
Keywords: Ocular drug delivery system Situ gel Bioadhesion Puerarin Poloxamer homologues Carbopol Hydroxypropyl -β- cyclodextrin
CLC: R283
Type: Master's thesis
Year: 2007
Downloads: 255
Quote: 4
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Abstract

Eye special physiological structure and effective protection mechanisms, the development of new formulations to the eye brings many challenges. Drops are still the most widely used ophthalmic formulations, ophthalmic preparations currently about 90% of the amount. Although accurate dose eye drops, convenient administration, patient compliance is high, but there are many problems: after administration, the drug is rapidly with loss of tear, corneal retention time is very short, low bioavailability, and, drain into system cycle, but also easy to cause systemic adverse reactions. Since the presence of corneal physiological barrier, most drugs across the cornea permeability is not ideal, it is difficult to maintain the inner eye lesion site higher concentrations, play a greater effect. To solve the above problems, the subject to anti-glaucoma drugs puerarin as a model drug use penetration enhancers to improve their penetration of the cornea, and then developed based on Poloxamer analogs and Carbopol in situ gelling and novel bioadhesive ocular drug delivery system This system can be administered in the form of eye drops, eye drops which retain the traditional advantages of the tear diluted by conjunctival instillation, at physiological temperature and still gelling, not with the tear loss, and has a biological adhesion to the cornea to maintain a longer residence time before, continue to maintain the effective drug concentration, thus overcoming the deficiencies of traditional drops. Topics were six aspects: (1) hydroxypropyl-β-cyclodextrin (HPCD) puerarin solubility and permeability of the cornea using a phase solubility experiments and in vitro corneal diffusion experiments. The results showed that the solubility of puerarin with HPCD concentration increases linearly; HPCD can significantly improve the corneal permeability of puerarin, but with the increasing concentration of HPCD puerarin apparent permeability coefficient decreases. (2) pharmaceutical formulations optimization study first composite design - response surface methodology for temperature-sensitive in situ gel part of the system optimization, the results 21.0% (w / v) of Poloxamer407 (P407) and 5.0% (w / v) of Poloxamer188 (P188) (P407/P188) to determine the best candidate for the prescription. Bioadhesive and then the type and concentration of excipients were screened, 0.1% (w / v) and 0.2% (w / v) of Carbopol1342 (CP1342) was investigated as a further object, in addition, also on the other recipe components were screening. (3) Evaluation of in vitro preparations to establish a preparation method for the determination; rheology on preparations, biological adhesion and in vitro release of three aspects of the evaluation. The results showed that a combination of the two combined polymer gel (P407/P188/0.1% CP1342 and P407/P188/0.2% CP1342) was significantly higher than the shear stress shear rate for each individual homologues and CP1342 Poloxamer the shear stress, and in physiological conditions, the performance of a hysteresis of pseudoplastic flow behavior; P407/P188 on the nature and temperature-sensitive gelling properties CP1342 bioadhesive combined effect of two polymer gel composition were demonstrated excellent bioadhesive capacity; puerarin mainly by diffusion via slow release polymer gel composition for 8 hours. (4) preparation of puerarin diffusion behavior of a free-diffusion model. The results showed that puerarin polymer gel in combination than alone in the diffusion coefficient and CP1342 Poloxamer homologues of diffusion coefficient; as the polymer concentration increases, the diffusion coefficient decreases; puerarin between concentration and diffusion coefficient There was no significant correlation; HPCD smaller effect on the diffusion coefficient: As the temperature increases, resulting in reduced diffusion coefficient of puerarin. (5) preparation of puerarin tear elimination kinetics and pharmacodynamics preliminary evaluation of tear elimination kinetics showed that the concentration of each prescription puerarin tear - time curve similar to the overall trend, but each time point, the combination of polymer gel tear puerarin concentrations are high relative to other prescriptions. Two combinations of the polymer gel AUC _{0 → 480min}, respectively, 4.43 and 5.26 times the analog containing puerarin tear (STF) of the AUC (0 → 480min) value; preliminary experimental results show pharmacodynamic , the combination of polymer gel to be able to maintain intraocular pressure lowering effect of 24h, significantly better than the STF (8h), relatively better than the P407/P188 and CP1342 (respectively,> 8 h and <24 h). STF than two polymer gel composition has a smaller T _max (P <0.05), AUC _{0 → 24h}, respectively 3.09 and 3.61 times the STF (P <0.05). (6) preparation of the Stability and eye irritation studies conducted a preliminary stability study on factors influencing the results indicate that the product should be dark, cool place. Accelerated stability tests show that the product has good stability, preliminary forecast valid up to two years; eye irritation after repeated administration study showed that treatment group and the control group showed no abnormality irritant, with high security sex.

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