Co-crystals are one of the most popular ways to modify the physicochemical properties of active pharmaceutical ingredients (API) without changing pharmacological activity through non-covalent interactions with one or more co-formers. A “green method” has recently prompted many researchers to develop solvent-free techniques or minimize solvents for arranging the eco-friendlier process of co-crystallization. Researchers have also been looking for less-risk co-formers that produce the desired API’s physicochemical properties. This review purposed to collect the report studies of amino acids as the safe co-former and explored their advantages. Structurally, amino acids are promising co-former candidates as they have functional groups that can form hydrogen bonds and increase stability through zwitterionic moieties, which support strong interactions. The co-crystals and deep eutectic solvent yielded from this natural compound have been proven to improve pharmaceutical performance. For example, l-glutamine could reduce the side effects of mesalamine through an acid-base stabilizing effect in the gastrointestinal fluid. In addition, some amino acids, especially l-proline, enhances API’s solubility and absorption in its natural deep eutectic solvent and co-crystals systems. Moreover, some ionic co-crystals of amino acids have also been designed to increase chiral resolution. Therefore, amino acids are safe potential co-formers, which are suitable for improving the physicochemical properties of API and prospective to be developed further in the dosage formula and solid-state syntheses.

Objective: A new compound of salicylic acid derivative, namely 2-((3-(chloromethyl)benzoyl)oxy)benzoic acid (3CBB), was synthesized to find a compound exhibiting higher analgesic activity and smaller ulcer irritation than acetylsalicylic acid (ASA). Therefore, this study aimed to investigate the pharmacokinetics of this new compound in rats, following a single dose oral administration of 3CBB (45 mg/kg BW). Methods: Plasma samples of 9 healthy rats were collected before and up to 3 h after its oral administration, following an 18 h fasting period. Plasma concentrations of 3CBB were determined using a validated HPLC-DAD assay. Pharmacokinetic parameters were determined using the compartment model technique. All experiments were carried out in triplicate. Results: The pharmacokinetic parameters of 3CBB obtained were as follows: Tmax= 28.9±1.1 min, Cmax = 0.57±0.02 µg/ml, AUCtotal = 66.3±1.0 µg min/ml, Kel = 0.018±0.002 min-1, and T1/2el = 39.4±3.9 min. The long elimination half-life and low Cmax indicated that 3CBB was extensively distributed in the deep and very deep tissues. This confirmed the unique and special characteristics of a highly lipophilic compound like 3CBB (log P = 3.73). Conclusion: 3CBB demonstrated a slower onset of action and longer elimination time from the body compared to ASA. Thus this new compound is a potential candidate to be developed as a new drug.

Salah satu gangguan di permukaan kulit wajah yaitu jerawat yang disebabkan oleh Propionibacterium acnes. Perlakuan jerawat bisa secara oral atau topikal yang umumnya mengandung antibiotika yang lebih efektif mengatasi jerawat, sedangkan kelemahannya mudah terjadi resistensi bakteri terhadap antibiotik. Salah satunya yang potensial dikembangkan sebagai antijerawat dan anitoksidan yaitu limbah dari kulit buah jeruk purut (Citrus hystrix) memiliki kandungan sebagai antibakteri adalah alkaloid, flavonoid (naringenin dan hesperidin), tanin serta senyawa fenolik memiliki aktivitas antioksidan juga sebagai analgesik dan anti inflamasi. Metode ekstraksi secara maserasi dengan pelarut penyari 95% dengan bentuk ekstrak kental terstandar. Konsentrasi ekstrak kental jeruk purut yang digunakan dalam penelitian ini antara 10% - 20%. Dalam rangka penjaminan mutu ekstrak maka dilakukan proses standarisasi secara spesifik dan non spesifik selanjutnya dilakukan uji efektivitas yang terdiri dari aktivitas antioksidan dengan parameter IC50 menggunakan metode DPPH sedangkan antibakteri dilakukan dengan menggunakan parameter Daerah Hambat Pertumbuhan – DHP secara difusi. Tujuan dari penelitian ini untuk mengetahui pengaruh peningkatan konsentrasi sediaan gel ekstrak kental jeruk purut (10%, 15%, dan 20%) terhadap efektivitasnya serta korelasi antara peningkatan aktivitas antioksidannya dengan antijerawatnya (antibakterinya). Berdasarkan hasil percobaan ekstrak kulit buah jeruk purut terbukti memiliki daya antioksidan, dimana dengan peningkatan konsentrasi diikuti dengan penurunan nilai IC50 yaitu 2,49 mg/mL. Nilai DHP ekstrak kulit buah jeruk purut untuk masing-masing konsentrasi 10%, 15% dan 20% berurutan sebesar 15,58 ± 0,287 mm, 17,45 ± 0,319 mm, 18,27 ± 0,306 mm, dimana semakin meningkat konsentrasi ekstrak maka efek sebagai antijerawat juga meningkat. Berdasarkan hasil penelitian tersebut, maka disimpulkan ekstrak kulit jeruk purut berpotensi sebagai antioksidan dan antijerawat.