Study On Oral Preparations Of Phloroglucinol

The pain caused by smooth muscle spasm is one of the most commonclinical emergencies, such as digestive system and biliarydysfunction caused by acute spasmodic pain, acute spastic pain inurethra, bladder and renal colic, spastic pain in gynecology andso on.Phloroglucinol is a unique structure of new smooth muscleantispasmodic drugs, which is characterized by the pro-muscular,directly into the gastrointestinal and urogenital spasm of smoothmuscle occurs, and it is less impact on normal smooth muscle.Currently, the drug of Phloroglucinol listed varieties inforeign countries is dominated by the French Laboratoire L.Lafonproduction for intravenous injection and lyophilized tablets fororal administration. In our country, the drug applies mainlyinjection and powder for injection needles, these dosage forms aremore single. Due to the phloroglucinol structural characteristics,it contains three phenolic hydroxyl groups and easily oxidized. Sothis drug has a certain degree of difficulty to prepare oralpreparations, and there is no its oral preparations available inour country. In this research, the reference is the listed of phloroglucinol freeze-dried tablet. Against the difficulties forpreparing oral preparation, we identified the study of phloroglucinolfilm-coated tablet. We prepared the oral film-coated tablet withstable properties by adding antioxidant and coating. In addition,preliminary studies of influence factors on the phloroglucinolfreeze-dried tablet have been carried out. This researchaccumulates data to the development of our domestic phloroglucinolfreeze-dried preparation.Method:1. We studied the related information about phloroglucinol andresearched relevant physical and chemical properties of this drug.In this experiment, we get the drug performulation research fromdrug stability to get more comprehensive understanding ofphloroglucinol characteristics.2. Combined with three phenolic hydroxyl groups and easily oxidizedcharacteristics of phloroglucinol, this thesis conducted a studyon the preparation phloroglucinol of film-coated tablets for oraladministration. We focus on three aspects of the film-coated tabletstudy mainly from the formulation, preparation technique offiltering and the establishment of quality standards andinvestigation of stability. We use antioxidant and wet granulationmethod to prepare plain tablets, and those tablets use coatingtechnology. We use high performance liquid chromatography tomeasure the dissolution, content, related substances and the methodis validated on methodology. We experimentize influence factorexperiment and accelerated testing to the preparation of thefinished products by using the method under the quality standards.In this experiment, we use the product properties, dissolution, related substances and content as the evaluation indicator toinspect the stability of the drug.3. To research the information on foreign phloroglucinol freeze-driedtablets formulation and preparation, we get a preliminary study onphloroglucinol freeze-dried oral preparations. By using liquidwater content and complex soluble as the evaluation indicator tocontrol this preparation formulation and freeze-dried process.From both pre-freezing and drying explore freeze-drying process.Furthermore, the relationship on freeze-dried contact area, thethickness of the freeze-dried and freeze-dried time is investigated.This experiment will accumulate experimental data in-depth studyof the freeze-dried preparation.Results:1. In phloroglucinol preformulation study, we have a certainunderstanding of the phloroglucinol physicochemical properties andthe stability of raw materials. This drug is prone to oxidationdamage, but high temperature, high humidity, and strong lightenvironment still have smaller impact. In addition, acid andalkali have a certain effect. The study of the drug raw materialslaid a certain foundation for the preparation.2. The study completed phloroglucinol film-coated tabletsformulation and preparation process test. Hardness and appearanceof the samples are in line with the relevant requirements of thepreparation. The results of methodology validation show that usinghigh performance liquid chromatography to determine thephloroglucinol sample dissolution, content and related substanceshave high accuracy and good reproducibility. In the formulationfiltering, we have chosen the solubilization adjuvants to accelerate the dissolution of the drug. The dissolution testresults show that the dissolution rate of the samples are fast, thesamples can play the role of quick release. The hardness of the plaintablet by using wet granulation method is high, those tablets areconducive to coating, but also to avoid splitting during storageprocedure. We experimentize influence factor experiment andaccelerated testing to tablets which is added antioxidant and usedcoating technology. The results show that the coated tablets reducethe phloroglucinol contact with air, and improve the stability ofthe drug.3. Due to the current development of domestic oral lyophilizedpreparations are not mature, this experiment get a preliminarystudy on phloroglucinol oral lyophilized preparation. In theformulation filtering, we have mainly a certain discussion on thechoice of lyoprotectant to ensure the sample appearance andformability. Another factor is the choice of lyophilized mold. Itplays an important role in controlling the lyophilized formulationtraits and lyophilization process. We conducted a preliminary studyfrom the lyophilized contact area and lyophilized thickness.Increasing the contact area and reducing the thickness are in favorof shortening the freeze-drying time within certain limits. Becausedifferent lyophilized preparation have different freeze-dried mold,the choice of freeze-dried mold contact area and thickness are alsodifferent, the freeze-drying process will change. In our futureresearch, according to different lyophilized preparationrequirements, we should make a selection on the formulations,freeze-dried molds and freeze-dried process parameters setting, inorder to ensure the properties of lyophilized preparations, shorten the freeze-drying time, optimization the freeze-drying process,improving the efficiency of freeze-drying.Conclusion:1. In the study, by adding antioxidant and film-coated preparationmethod, we effectively solve the difficulty problems faced with thepreparation of phloroglucinol oral preparations. Finally, weprepared a phloroglucinol dosage preparation. The samples ofphloroglucinol film-coated tablet are nature stable and easy touse.2. The results of the preliminary research on phloroglucinollyophilized oral preparations influence factors of freeze-driedshow that the choice of formulation, the parameter settings offreeze-drying process and the choice of the lyophilized contactarea and lyophilized thickness of the lyophilized mold play animportant role in the properties and preparation technology oflyophilized preparation. This experiment accumulates some data forthe lyophilized oral preparation.