Study On G-0618's Mucosal Delivery Of New Dosage Forms

Vascular dementia (VD) the recent years presented potentia l of the rapid rise,aggra vated along with the urbaniza tion and the aging tendency. In China, the oldpopulation already surpassed 120,000,000 people, the old age disease's diseaseincidence rate also year by year enhances. But receives along with the resident theenhancement, causes the senior citizen to the quality of life request also along with itenhancement.Under this tendency, to such as disease's and so on vascular thedementia treatment med icine's dema nds also largely enhances. VD sick ness is onekind of function drops, needs to take med icine for a long time treatment disease,enhances along with the social development and the people regarding this kind ofdisease's value degree, treats the med icine to this kind of disease the dema nd to growunceasingly. In demonstrated to doctor's survey result in that 8.16% doctors thoughtthis kind of market med icine supplies serious insufficient, 63.2% doctors thought thatthe market supplies are insufficient.Therefore this article by through the expansion blood vessel of brain, improvesthe brain metabolism, thus has good therapeutic action G-0618 to VD is the modelmed icine. Using mucous membrane absorption and the biologica l exploitability highcharacteristic, unified G-0618 the physics and chemistry nature to develop the G-0618two kind of mucous membranes quick ly to give the medicine new dosage-form—nasal powders and sublingua l tablets were the developed and their in vitro qualitiesand in vivo the pharmacod ynamics were intensively studied. Is for the purpose ofpreparing the effect to be fast, the biologica l exploitability is high, the stability is good,easy to operate G-0618 dosage-form.Firstly, G-0618 is poor aqueous solubility and chemica l stability, the researchfocused on the solubility, stability and the relationships of the two influencing factors.The results show that the lower the pH value of med ia and the use of mixed solvents can significa ntly increase the solubility of G-0618; the different added CD can alsoincrease the solubility, but the effect was not obvious. The find ings indica ted that G-0618 solution is relatively stable in the pH value of between 3 to 5; different pHregulator of G-0618 can affect the stability; the different added CD can notsignifica ntly improve the stability of solution.Looking from the G-0618 solubility and the chemica lly stable findings, make itthe chemica l stability good solution preparation difficulty to be very big, therefore, wemake it the solid preparation—nasal powders and sublingua l tablets .The excipients of G-0618 nasal powders were first screened before prescriptionScreening and preparation technology study. According to the inha lation qualityrequirements of Chinese Pharmacopoeia 2005 edition , the hygroscopicity, fluid ity andjet drops of severa l excipients are inspected. The results showed that 100 mesh lactosenasal powder is the idea l excipients. On this basis, the different prescription of nasalpowder G-0618 are prepared and their stability are compared. The results confirmedthe prescription is better stable by addingβ-CD tha n ohters. Then inspected the quantitywhichβ-CD joins, has determined the G-0618 nasal powders prescription composition. Finally,three batches of G-0618 nasal powder are prepared and their quality are evaluated.The results showed that the content and content uniformity of G-0618 nasal powderare in complia nce with the releva nt requirements and have a good stability , study onmucosa l toxicity of toad palate proved that the nasal powder has not almostciliotoxicity. Therefore, the G-0618 nasal powder reach experiment anticipated goal.In G-0618 sublingua l tablets prescription screening and in the preparation craft'sresearch, first has carried on the inspection to the sublingua l tablets supplementarymateria l's water absorbability and which possibly existed with various supplementarymateria ls between has conducted the research to G-0618. Based on this, the referencerelated literature, draws up the sublingua l tablets the basic prescription. Uses thesingle factor experimental techniq ue, in the stop plate is heavy, in the sheetingstrength's situation, take sublingua l tablets degree of hardness and the disintegrationtime as the target, optimized auxilia ries proportion, disintegration med icina lpreparation type and amount used, the bond type, chooses the disintegration time to belong, the degree of hardness big prescription, takes the sublingua l tablets the bestprescription. Then, the preparation different prescription G-0618 sublingua l tablets ,conducts the investigation into stability. Has determined the G-0618 hypoglossis pieceprescription composition. In addition, also to the wet lega l system materia l sheeting law,the pellet dry temperature and the time has carried on as well as a wet lega l system grain of sheeting and the powder direct sheeting makes the hypoglossis piece thestable difference to carry on the inspection. The find ings indica ted that a wet lega lsystem grain of sheeting and the powder direct sheeting make the sublingua l tabletsthe stability not to have the obvious difference, and confirmed in a wet lega l systemgrain of sheeting chooses the pellet dry condition is very reasonable. Therefore, in thisresearch designated finally uses the wet lega l system grain of sheeting law. Accordingto the sublingua l tablets best prescription and the preparation craft, have preparedthree raid of G-0618 sublingua l tablets and carry on vitro quality rating. The resultindica ted that makes G-0618 sublingua l tablets its content, the content uniformity, thedisintegration time, the sublingua l tablets qualitative indices and so on time to meetthe hypoglossis piece related quality requirement completely, and the feeling in themouth and the stability are good, achieves the experiment anticipated goal.Lastly, used the medicine effect law to study G-0618 after the nasal cavity andthe sublingua l mucous membrane absorption possibility. Take the big mouse as theobject of study, after studying G-0618 passes through the nasal cavity and thesublingua l separately for the medicine, to the big mouse thrombus forms the influence,comes by this to expla in the G-0618 nasal powders and sublingua l tablets in humanbody absorption situation indirectly. The find ings indica ted that the big mouse gave G-0618 after the nasal cavity and the sublingua l produces the remarkable anti-thrombusto form the function, the nasal cavity gives the medicine quick ly for the medicineabsorption rate in the sublingua l. The above result prompt, G-0618 gives the medicineafter the nasal cavity or the sublingua l, has had the good in vivo absorption. Therefore,may forecast that the G-0618 nasal powders and sublingua l tablets will have the goodabsorption in the human body.The G-0618 nasal powders and sublingua l tablets two kind of new dosage-forms,in domestic and foreign have not seen the report, thus has the innova tion and theimportant clinica l practice value.