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According to the theory of the formation mechanism and prevention of myopia and visual fatigue, drug and supplement proper eye function nutrients, can alleviate and eliminate the eye of the tension adjustment to eliminate eye fatigue, reduce intraocular pressure, to prevention and treatment of myopia such as the compound eye drops neostigmine (Ming neostigmine containing methyl sulfate, taurine, vitamin B 6 and chlorpheniramine maleate sensitive). However, due to the the eye special partial physiological environment as well as high sensitivity, typically less drug absorption, low bioavailability, poor adherence of some of the common formulations of patients, leading to poor efficacy. Pharmacy means there are limitations in the application of the eye, the ophthalmic dosage form design more difficult. In situ gel (in situ gel, also known as the environmentally-sensitive gel) is administered in a solution state immediately after the phase transition occurs at the administration site, to form a semi-solid formulation of the non-chemical crosslinking. The delivery system of both the advantages of the solution with a gel formulation, particularly suitable for use as a carrier for ophthalmic administration. Can effectively achieve the purpose of the sustained release their use in the eye, and the bioadhesive, sustained release and absorption, thereby effectively enhancing the bioavailability, reducing the frequency of administration, and to improve patient compliance, and effectively improve the efficacy. This paper ophthalmic in situ gel matrix screening, the compound methyl sulfate Neostigmine temperature sensitive eye gel Preparation and prescription screening quality research, in vitro release investigation, stability and stimulating visits. Situ gel formation mechanisms are mainly three categories, namely temperature-sensitive, pH-sensitive, ion-sensitive. According to the requirements of the special physiological and environmental conditions of the eye (pH value of 7.2 to 7.4, the surface temperature of 34 to 35 ° C, the tears Na , K of Ca < / sup>, and tear will be placed in the eye of the drug) was diluted situ gel matrix suitable for ocular use, the pH-sensitive in situ gel matrix material selected carbomer P934, P940, and investigated its bioadhesive material HPMC combination, the final selection of suitable eye prescription: 0.02% P934, 0.02% P940 and 0.5% HPMC (K 4 M) in combination. The matrix material of the ion sensitive mainly investigated deacetylation gellan gum, 0.45% deacetylation gellan gum matrix formulation suitable for use eye. The temperature-sensitive materials investigated poloxamer P407, and to consider the 10% P188 to adjust its gelling temperature, and the final selection of the matrix formulation suitable for use eye: 24% P407 10% P188 combined. Experiment found that Compound A sulfuric acid neostigmine components of interaction with the matrix, the vitamin B 6 cause the ion-sensitive gelling matrix solution, maleate, chlorpheniramine and vitamin B 6 cause the pH-sensitive matrix solution to form a precipitate. Therefore, the final selection of the temperature-sensitive matrix material as the the compound methyl sulfate Neostigmine eye situ gel matrix. Final prescription sulfate neostigmine A 0.001%, 0.1% taurine the 0.1% Vitamins B for 6 , 0.01% maleate chlorpheniramine, 24% poloxamer P407, 10 % poloxamer P188, plus 0.05% benzalkonium chloride as a preservative. The of the compound methyl sulfate Neostigmine eye situ gel quality standard, including traits, checking items (pH value, gelling temperature, the material, identification, etc.), and established Determination. Appearance, pH value, gelling temperature and adhere to the provisions of ophthalmic preparations. The four components of the formulations were determined by HPLC to establish their respective chromatographic conditions. Fumble and established maleate chlorpheniramine about the solid phase extraction sample handling material inspection law. According the eye medication vivo characteristics to modified United States Pharmacopoeia dissolution assay method based on self-made glass mold (as a semi-permeable membrane dialysis bag, paddles fixed at a diameter of 3.5cm, effective drug delivery area for 9.62cm 2 ) investigated the preparation of vitamin B 6 , release of taurine drug. Release of 80% of the time-consuming 3 ~ 4h, have a good slow-release effect, to achieve effective in reducing the frequency of administration, and to improve patient compliance, and improve the therapeutic purposes. The effects of the the compound methyl sulfate Neostigmine eye situ gel stability and irritating. Results show that the present formulation is stable at low temperature conditions, in the heat and light under irradiation, traits and there is a certain change in the pH value, the amount of the preparation of certain components will change, and generation of impurities, i.e., the present formulations to dark refrigerated . The preparation has no significant irritation on rabbit eye, and comply with the requirements of the ophthalmic preparations. The significance of this study lies in for Compound A sulfuric new Sri Lanka clearly established a well equipped sustained-release effect, effectively improve patient compliance, suitable for eye use new formulation and its preparation process, not only to overcome the administration of eye drops frequently beneficial in the treatment of myopia such a need long-term repeated dosing ocular disease, low bioavailability, wasting large defects, but also to overcome the the eye ointment foreign body strong, can cause blurred vision and other defects.
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