PLANT BASED BIOAVAILABILITY ENHANCERS

Many of the synthetic as well as herbal drugs despite of their notable in vitro finding demonstrate insignificant in vivo activity majority of times due to poor bioavailability. As per Biopharmaceutical Classification System (BCS) one of the main concern is low solubility and/or permeation of drugs resulting in reduced absorption and poor bioavailability. To overcome these issues the various strategies have been adopted including use of permeation enhancers which are also known as bioenhancers. Bioenhancers are synthetic or natural compounds that increases the bioavailability of drugs and nutrients such as vitamins, amino acids, minerals, etc. into the systemic circulation and at the site of action for exhibiting improved therapeutic action. By improving bioavailability, bioenhancers can lead to reduction in drug dose, decrease in the treatment period and can circumvent the problem of drug resistance. Numerous studies have reported application of synthetic bioenhancers. On the other hand, owing to the natural origin, plant based bioenhancer can serve as better alternative. Literature review have revealed that the plant-based bioenhancers have been used in with a wide varieties of drugs including antibiotics, antiviral and anti-cancer. These can be categorized based on their sources and the mechanism of activity. This review will provide a systematic and detailed overview of the various plant based bioenhancers and applications.

Eutectic Formation of Naproxen with Some Dicarboxylic Acids

Eutectic formation with additives is one of the established methods to improve the dissolution behaviors of active pharmaceutic ingredients (APIs). The improvement is mainly due to the increase in the surface area for dissolution, which originates from the finely divided micro-domains generated through the phase separation of the miscible liquid components upon solidification. The present study is to identify eutectic-forming additives for naproxen (NPX), a class II API of the biopharmaceutical classification system. A particular aim was to develop a eutectic mixture with NPX at least over 20 wt%, a minimum to be practical for oral delivery. Screening based on the proximity of the solubility parameter values identified dicarboxylic acids (succinic acid, glutaric acid, and suberic acid) as desirable additives for NPX. Binary melting diagrams were constructed to confirm the eutectic compositions, and the eutectic mixture with suberic acid (NPX 55 wt%) was further investigated. The dissolution (at pH 5.0) of the melt crystallized eutectics was enhanced compared to the simple physical mixture of the same compositions and neat NPX, which was attributed to the microscopically observed lamellar structures. The current study should support the systematic investigations of API eutectic mixtures by selecting appropriate eutectic-forming additives.

Karakterisasi Karbamazepin Hasil Rekristalisasi Berbagai Pelarut Organik dengan Metode Slow Evaporation

Pendahuluan: Karbamazepin termasuk ke dalam golongan Biopharmaceutical Classification System (BCS) kelas II yang artinya bahwa karbamazepin memiliki permeabilitas membran tinggi dan kelarutan rendah. Rekristalisasi merupakan salah satu cara untuk memodifikasi kristal dalam upaya mengubah sifat fisikokimia dan laju disolusi obat. Tujuan: Penelitian ini bertujuan untuk mengevaluasi sifat fisikokimia karbamazepin melalui rekristalisasi berbagai pelarut. Metode: Pada penelitian ini dilakukan rekristalisasi dengan cara penguapan pelarut menggunakan pelarut etanol, tetrahidrofuran (THF), dan kloroform. Padatan kristal hasil rekristalisasi dikarakterisasi dengan menggunakan spektrofotometri FTIR, difraksi sinar-X (PXRD), dan analisis differential scanning calorimetry (DSC). Selanjutnya dilakukan evaluasi mikromeritik dan uji disolusi. Hasil: Berdasarkan hasil karakterisasi dengan FTIR dan PXRD menunjukan tidak terjadi perubahan struktur kimia dari karbamazepin, tetapi menyebabkan perubahan internal struktur dan perubahan bentuk (polimorfisme) kristal karbamazepin. Hasil evaluasi mikromeritik menunjukkan adanya perubahan sifat fungsional pada padatan kristal hasil rekristalisasi dibandingkan dengan karbamazepin murni, diketahui padatan kristal hasil rekristalisasi etanol menunjukkan sifat mikromeritik yang lebih baik dibandingkan bentuk murni. Uji disolusi menunjukkan bahwa terjadi peningkatan laju disolusi pada padatan kristal hasil rekristalisasi berbagai pelarut dibandingkan dengan karbamazepin murni. Pada padatan kristal hasil rekristalisasi THF memiliki laju disolusi paling tinggi dari pelarut yang lain, yaitu pada menit ke-60 jumlah terdisolusi sebesar 65,09%. Kesimpulan: Proses rekristalisasi karbamazepin dengan pelarut etanol, tetrahidrofuran dan kloroform menghasilkan polimorf baru sehingga sifat fisikokimia padatan hasil rekristalisasi berbeda dibandingkan karbamazepin murni. Berdasarkan hasil uji disolusi in vitro dapat diketahui bahwa karbamazepin hasil rekristalisasi dengan pelarut tetrahidrofuran memiliki laju disolusi yang paling tinggi.

Recent solubility and dissolution enhancement techniques for repaglinide a BCS class II drug: a review

Repaglinide is an oral blood-glucose-lowering drug used to manage type-2 diabetes mellitus by lowering post-prandial glucose by stimulating insulin secretion from pancreatic beta cells. According to the biopharmaceutical classification system, repaglinide falls under the class II category. For such drugs, limited solubility and poor dissolution rate are the major hurdles to overcome by formulation scientists, as they hinder drug absorption and lead to inadequate therapeutic effects. Therefore, this review aims to discuss in depth the various approaches investigated in the past five years to improve the solubility and dissolution of orally administered repaglinide: namely, solid dispersion, co-amorphous technology, cyclodextrin complexation, phospholipid complexes and polymeric micelles, nanocrystals, nanosuspensions and nanofibers.

COMPARATIVE PHARMACEUTICAL EVALUATION OF VARIABLE RETAIL PRICED MEDICINES CONTAINING BIOPHARMACEUTICAL CLASSIFICATION SYSTEM CLASS-II OR CLASS-IV DRUGS

The purpose of the present study is to highlight the discriminations if any, between the quality of low and high-cost medicines, which would help to select the right brand of medicine. In the present work, brands of medicines having high, medium, and low prices containing either of biopharmaceutical classification system class-II or class-IV drugs were comparatively evaluated for different pharmacopoeial standards as well as for biopharmaceutical classification system solubility and permeability. An ex vivo permeability test was carried out using a simple and non-invasive everted gut sac technique. Insignificant variation in pharmaceutical quality and permeability of the tested three types of brands was observed; however, the study could not consider the state of quality assurance facilities and parameters used while manufacturing these medicines. The study will help to make aware and assure medical and pharmacy practitioners and consumers for the selection of quality quality generic medicines.

Review: Solid Dispersion of Fenofibrate Using Poly Ethylene Glycol 6000

This review aimed to find information about the solubility of the fenofibrate solid dispersion system using PEG 6000. Fenofibrate is an antihyperlipidemic drug that belongs to the Biopharmaceutical Classification System Class II (BCS II) with low solubility. To find information was by conducting a literature search in national and international journals in the last ten years (2010-2020) through websites, namely Google Scholar, Science Direct, NCBI, ResearchGate, and other trusted journals. Several keywords were used as follows: fenofibrate, solid dispersion, PEG 6000, and dissolution rate. The results of several research journals showed that the solid dispersion of fenofibrate using PEG 6000 made by various methods causes a reduction in particle size to increase the solubility and dissolution rate of fenofibrate. The solid dispersions system was made using several methods, namely fusion (melting), solvent evaporation, dropping, and co-grinding, which is a technique used to increase the solubility of a drug. PEG 6000 was chosen as the carrier because it has high hydrophilicity, is non-toxic, inert, economical, has a low melting point, and is dense at melting temperature to withstand crystallization. Thus it can be concluded that the manufacture of solid dispersion of fenofibrate using PEG 6000 and several methods showed the same results, namely an increase in solubility and dissolution rate.

An Overview on Dietary Polyphenols and Their Biopharmaceutical Classification System (BCS)

Polyphenols are natural organic compounds produced by plants, acting as antioxidants by reacting with ROS. These compounds are widely consumed in daily diet and many studies report several benefits to human health thanks to their bioavailability in humans. However, the digestion process of phenolic compounds is still not completely clear. Moreover, bioavailability is dependent on the metabolic phase of these compounds. The LogP value can be managed as a simplified measure of the lipophilicity of a substance ingested within the human body, which affects resultant absorption. The biopharmaceutical classification system (BCS), a method used to classify drugs intended for gastrointestinal absorption, correlates the solubility and permeability of the drug with both the rate and extent of oral absorption. BCS may be helpful to measure the bioactive constituents of foods, such as polyphenols, in order to understand their nutraceutical potential. There are many literature studies that focus on permeability, absorption, and bioavailability of polyphenols and their resultant metabolic byproducts, but there is still confusion about their respective LogP values and BCS classification. This review will provide an overview of the information regarding 10 dietarypolyphenols (ferulic acid, chlorogenic acid, rutin, quercetin, apigenin, cirsimaritin, daidzein, resveratrol, ellagic acid, and curcumin) and their association with the BCS classification.

Comparative Study of Different Products of Carbamazepine Tablets Available in Iraqi Market

Carbamazepine (CBZ) is a widely used antiepileptic drug to control grand mal epilepsy, as well as for the treatment of peripheral neuralgia. According to the biopharmaceutical classification system (BCS), CBZ is considered a class II drug. CBZ is characterized by a slow and irregular gastrointestinal absorption, with irregular oral bioavailability; due to its low water solubility. Therefore, the release of the drug from the dosage form (tablets in this study) and the subsequent step of dissolution represent the most important parameters that decide whether a sufficient plasma concentration will be achieved or not. In the current study, the FTIR study for the pure API, CBZ, and the different commercially available brands of CBZ conventional tablets, available in the Iraqi drug market (Mosul city as an example), were examined. Subsequently, various quality control parameters such as the weight variation, content uniformity, friability, and hardness of the conventional CBZ tablets were conducted. Moreover, the disintegration and the dissolution tests of the different brands of CBZ available in the Iraqi drug market were performed. Keywords: Antiepileptic Drug, Bioequivalence; Epilepsy; Generic; Brand vs generic; IVIVC; QC