Pharmaceutical co-crystals are novel class of pharmaceutical substances, which possess an apparent probability of advancement of polished physical properties offering stable and patentable solid forms. These multi-component crystalline forms influence pertinent physicochemical parameters like solubility, dissolution rate, chemical stability, physical stability, etc. which in turn result in the materials with superior properties to those of the free drug. Co-crystallization is a process by which the molecular interactions can be altered to optimize the drug properties. Co-crystals comprise a multicomponent system of active pharmaceutical ingredient (API) with a stoichiometric amount of a pharmaceutically acceptable coformer incorporated in the crystal lattice. By manufacturing pharmaceutical co-crystals, the physicochemical properties of a drug can be improved thus multicomponent crystalline materials have received renewed interest in the current scenario due to the easy administration in the pharmaceutical industry. There is an immense amount of literature available on co-crystals. However, there is a lack of an exhaustive review on a selection of coformers and regulations on co-crystals. The review has made an attempt to bridge this gap. The review also describes the methods used to prepare co-crystals with their characterization. Brief description on the pharmaceutical applications of co-crystals has also been incorporated here. Efforts are made to include reported works on co-crystals, which further help to understand the concept of co-crystals in depth.
Background and Objective:Transmucosal analgesic delivery is a promising approach to periodontal postoperative pain management. The purpose of this clinical trial is to appraise the effectiveness of transmucosal drug delivery system with meloxicam films and to identify its minimum effective dosage via this route after periodontal flap surgery.Materials and Methods:The analgesic mucoadhesive films were formulated using meloxicam and hydroxypropyl methyl cellulose polymer by solvent casting method. The sample size consisted of 60 chronic periodontitis patients who require periodontal flap surgery. The subjects were randomized using lottery method into four groups (Group A - 45 mg; B - 30 mg; C - 20 mg; D - 10 mg meloxicam per film). After periodontal flap surgery, the respective meloxicam mucoadhesive films were placed over the surgical site and were removed on 4th day of postsurgery. The primary outcome measure was postsurgical pain level and recorded at 1st, 2nd, 3rd, 4th, 5th, 24th, and 48th h using a 0–10 mm visual analog scale with markings from 0 = no pain to 10 = extreme pain.Results:The postoperative pain control observed in Groups A and B was found to be effective, and the patient comfort level was very satisfactory. Whereas in Group C, it was found to be high in the first 3 h postsurgically, after which adequate pain relief was seen. Group D exhibited inadequate pain relief. No adverse reactions were noted after applying the film in any of the groups.Conclusion:Transmucosal delivery of meloxicam was found to be effective and safe in postsurgical pain control of periodontal flap surgery. The minimum effective dosage via this route for meloxicam was found to be with 30 mg mucoadhesive films.
Objectives: The objective of the study was to compare solubilization approaches, namely cosolvency, micelle solubilization, complexation, pH adjustment and hydrotrophy, on BCS class II drug modafinil solubility. Methods: Altered solubility study of modafinil was carried out in numerous water-cosolvent mixtures. Similar type of study was performed using different ionic and non-ionic surfactants using phase solubility analysis. Furthermore, solubility behavior with two cyclodextrins namely beta cyclodextrin and maltodextrin were examined. Solubility studies were conducted in buffers of different pH ranging from 1.2 to 8 at different temperatures (25°C and 37°C). The effect of hydrotrophy on the solubility of modafinil was also studied. Results: Outcomes showed that ethanol is depicted to enhance solubility by greater height. It is found that ionic surfactants were better solubilizers than non-ionic surfactants. The capacity of solubilization is depicted to enhance with rise in hydrocarbon chain length of surfactant, denoting that hydrocarbon core of micelles as the center of solubilization. Highest solubility and binding constants were achieved with use of beta cyclodextrins followed by maltodextrins. The buffers of pH 2 and pH 3 have shown highest solubility when compared to others. Sodium thiocyanate salt had shown highest solubility of the drug. Conclusion: As a consequence, the study provides dataset so as to contrast effects of numerous solubilizers on modafinil solubility and also gives an insight of the mode of solubilization by aforementioned techniques.
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