Pharmaceutical Assessment of Watermelon Rind Pectin as a Suspending Agent in Oral Liquid Dosage Forms.

Pectin is a high molecular weight polymer which is present in virtually all plants where it contributes to the cell structure. Pectin is a high valuable food ingredient widely used as a gelling agent and thickening agent with limited use in the pharmaceutical industry. The objective of this study is to evaluate the suspending properties of pectin from watermelon rind. Tragacanth was used as a standard suspending agent to which the suspending properties of pectin from watermelon rinds were compared with. The extracted pectin was subjected to phytochemical and physiochemical characterization for its safety and suitability to use as a suspending agent. Paracetamol suspensions were formulated using tragacanth concentrations of 0.5% w/v, 1% w/v, and 2% w/v and compared with paracetamol suspensions containing the same concentrations of watermelon pectin. The suspensions were all tested for their pH, sedimentation rate, sedimentation volume, flow rate, and ease of redispersibility over a period of 4 weeks. At the end of the 4-week period, all formulated suspensions had no changes in their pH values. Suspensions containing the extracted pectin had a lower rate of sedimentation and ease of redispersibility compared to that of tragacanth. In addition, their sedimentation volumes as well as flow rates were comparable to that of the tragacanth formulations. Ultimately, pectin from watermelon rind can serve as a suitable alternative to tragacanth in formulation of pharmaceutical suspensions.

Pharmaceutical Assessment of Melia azedarach Gum as a Binder and Disintegrant in Immediate-Release Tablets.

Excipients are components other than active ingredients that are added to pharmaceutical formulations. Naturally sourced excipients are gradually gaining preeminence over synthetically sourced excipients due to local availability and continuous supply. This study aimed to investigate the binding and disintegrating characteristics of gum extracted from the bark of Melia azedarach tree. The bark of Melia azedarach was harvested from Kwahu Asasraka in Ghana. The gum was extracted with ethanol (96%), and the percentage yield, phytochemical constituents, and flow characteristics were assessed. As a disintegrant, the gum was utilized to formulate granules at varying concentrations of 5% w/w and 10% w/w using starch as the standard. The gum was also utilized to prepare granules at varying concentrations of 10% w/v and 20% w/v as a binder, with tragacanth gum serving as the reference. Eight batches of tablets were produced from the granules. The formulated tablets from each batch were then subjected to quality control testing, which included uniformity of weight, friability, disintegration, hardness, drug content, and dissolution tests, respectively. Tannins, saponins, alkaloids, and glycosides were identified in the Melia azedarach gum. The gum had a percentage yield of 67.75% and also exhibited good flow properties. All tablets passed the uniformity of weight, friability, disintegration, hardness, dissolution, and drug content tests, respectively. According to the findings of the study, Melia azedarach gum can be utilized as an excipient in place of tragacanth and starch as a binder and disintegrant, respectively, in immediate-release tablets.

Potential and Comparative Tablet Disintegrant Properties of Pectin Obtained from Five Okra Genotypes in Ghana.

Okra pectin has been studied as a potential excipient in tablet formulations for pharmaceutical industries. Okra is widely grown and available in Ghana and other parts of the world. The prospective use of pectin from okra genotypes grown in Ghana as tablet disintegrants has not been reported. This study aims to determine the potential and comparative disintegrating properties of pectin from five okra genotypes (Abelmoschus esculentus L.) in Ghana using uncoated immediate release paracetamol tablet formulations. The yield of the pectin from the various genotypes ranged between 6.12 and 18.84% w/w. The extracted pectins had pH ranging from slightly acidic to almost neutral (6.39-6.92). Pectin from the various genotypes exhibited good swelling indexes (˃200%), varying solubility in different solvents, and low moisture content (˂20%). Elemental analysis of the extracted pectin from the various genotypes revealed very low levels of toxic metals and micronutrients. Pectin from the various genotypes was evaluated as disintegrants within concentrations of 5-10% w/w (F1-F18). Their disintegrating properties were compared to that of maize starch BP. All the formulated batches of uncoated immediate release paracetamol tablets (F1-F18) passed the following: uniformity of weight test, uniformity of dimensions, hardness, friability (˂1%), and drug content (95-105%). Significant differences (p ≤ 0.05) were observed between the hardness of the maize starch tablets and tablets formulated from pectin of the various genotypes. Pectin from all genotypes other than PC5 exhibited good disintegrating properties (D T ˂ 15 min) and subsequently passed the dissolution profile test (≥70% release in 45 minutes). Tablets formulated with PC5 as disintegrants at all concentrations (5% w/w (F5), 7.5% w/w (F11), and 10% w/w (F17)) failed the disintegration and dissolution tests. Ultimately, pectins extracted from PC1, PC2, PC3, and PC4 can be commercially exploited as disintegrants in immediate release tablets.

Pectin from Okra (Abelmoschus esculentus L.) Has Potential as a Drug Release Modifier in Matrix Tablets.

Natural polymers have become attractive to pharmaceutical researchers and manufacturers as excipients because of the advantages they possess relative to their semisynthetic and synthetic counterparts. Although pectin from some natural sources has been investigated for use in the pharmaceutical industry as excipients, pectin from okra, which is readily available and used as food in many parts of the world, has not been extensively investigated as a potential control-releasing agent in tablets. This study thus seeks to determine the drug release modifying properties of okra pectin from 6 different genotypes of okra cultivated and available in Ghana. Pectin was extracted from different genotypes of okra, physicochemical properties were characterized, and control release matrix tablets of metformin (F1-F6) were formulated using the wet granulation method with the okra pectin as the drug release modifier, respectively. The drug content, in vitro drug release, and mathematical kinetic modeling of drug release from the matrix tablets were studied. Drug release profiles of formulated matrix tablets were compared to an existing (innovator) brand of metformin sustained-release tablet on the market using the similarity and difference factors, respectively. The extracted pectin had percentage yields ranging from 6 to 20% w/w with swelling indexes and water-holding capacities between 300-500% and 9-10 mL/g, respectively, and pH within 6.20-6.90. All the formulated batches passed the drug content test (90-105%) and produced the optimal release of metformin (>80%) after 24 hours. Different batches of formulated tablets exhibited different mechanisms of drug release with batches F1, F2, F5, and F6 being similar (ƒ2 values being >50 and ƒ1 values <15) to the innovator brand. Pectin from the 6 different genotypes of okra studied has the potential for use as drug release modifiers in pharmaceutical manufacturing of control release matrix tablets and production of more affordable medicines.

Scorpion Venom peptide, AGAP inhibits TRPV1 and potentiates the analgesic effect of lidocaine.

The current study was designed to test the hypothesis that BmK AGAP (AGAP) potentiates the analgesic effect of lidocaine. The chronic constrictive injury was performed on 72 rats to induce a rapid onset and long-lasting pain. The rats were randomly assigned to one of six groups; Group A (n = 12) received an intrathecal administration of saline, Group B (n = 12) received an intrathecal injection of lidocaine, Group C (n = 12) received an intrathecal administration of AGAP, Group D, E, and F (n = 12 each) received an intrathecal administration of lidocaine 0.005 mg/ml + AGAP 25, 50, 100 µg/kg respectively. The von Frey filaments were used to assess mechanical allodynia. Nav1.7 and TRPV1 currents were recorded by the whole-cell aspiration patch-clamp technique, and KCNQ2/3 currents were recorded by the whole-cell drilling patch-clamp technique. The whole-cell aspiration patch-clamp technique showed that AGAP inhibited TRPV1and KCNQ2/3 currents and increased the analgesic effect of lidocaine. AGAP may have a synergistic effect with lidocaine which demonstrates a potential therapeutic approach for optimizing post-operative analgesia.

The Challenges and Knowledge Gaps in Malaria Therapy: A Stakeholder Approach to Improving Oral Quinine Use in the Treatment of Childhood Malaria in Ghana.

BACKGROUND: The study was undertaken to elicit the knowledge, views, and perceptions of key stakeholders on malaria, its bioburden, and treatment options, in order to ascertain the knowledge gabs and challenges, especially in the use of oral quinine in childhood malaria. METHODS: A cross-sectional survey was conducted using a well-structured Likert Scale and self-administered questionnaire. The principal site of the study was a government-run children's hospital located in the Ashiedu Keteke Sub-Metro of Accra. The study population included health workers, parents, and guardians or care givers. The participants were 300, purposively selected, and consisted of both men (41%) and women (59%) who were twenty years and above, whether employed (42%), self-employed (37%), or unemployed (21%). RESULTS: Majority of the participants (78%) demonstrated above average knowledge of malaria. However, their awareness of the causes, modes of transmission, signs, and symptoms as well as preventive mechanisms of malaria did not result in low incidence of malaria. About 77% of the respondents agreed they would seek treatment within 24 hours once signs and symptoms are detected. Though close to 50% undertook home treatment of malaria, majority eventually sought treatment at hospital or clinic. Above 92% of respondents knew that quinine is used to treat malaria and agreed its bitter taste greatly affects compliance, especially in children. Consequently, 95% of the respondents would be glad if its bitter taste is masked. CONCLUSION: The study demonstrated the availability of substantial knowledge of the devastating effects of malaria, especially in children. Therefore, there is the need to ensure the availability and utilization of effective paediatric formulations in the fight against malaria. From this study, fast dissolving oral thin film with a good mouth feel, would be the formulation of choice for quinine.

Wound healing potential of methanol extract of Spathodea campanulata stem bark formulated into a topical preparation.

This study evaluated the wound healing potential of Spathodea campanulata stem bark in Sprague Dawley rats using the excision wound model. The methanol extract contained glycosides, flavonoids and tannins, and was relatively stable when stored at the room temperature for six (6) months. Solvent-free, semi-solid extract of S. campanulata was incorporated into an aqueous cream and applied (10 % w/w and 20 % w/w) on excision wounds of thirty two (32) rats. Cicatrin(®) cream was used as a standard wound healing agent. Prior to the remedial cream application, done later on twice daily, sixteen (16) rats had their wounds infected with Staphylococcus aureus, while in the remaining sixteen the wounds were kept clean. The surface area of the excision wounds was monitored planimetrically every four (4) days until a complete wound closure or healing took place. Excision wounds treated with 20 % w/w Spathodea cream and Cicatrin(®) cream showed a rapid and comparable decrease (p > 0.05) in wound size. In uninfected wounds, both 20 % w/w Spathodea cream and Cicatrin(®) cream application resulted in ∼ 95 %-wound closure seen on Day 20, and a complete closure seen on Day 24. In infected wounds, both 20 % w/w Spathodea cream and Cicatrin(®) cream administration led to ∼ 91 %-wound closure on Day 24 and a complete wound contraction on Day 28. The results of this study justify the folkloric use of S. campanulata stem bark to the effect of wound treatment.